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Drugs Containing Glycosides

Chapter 16

Drugs Containing Glycosides

Drugs Containing Glycosides

INTRODUCTION

  • A glycoside is any molecule in which a sugar group is bonded through its anomeric carbon to another group via glycosidic bond. A glycosidic bond is a certain type of chemical bond that joins a sugar molecule to another molecule. Specifically, a glycosidic bond is formed between the hemiacetal group of a saccharide (or a molecule derived from a saccharide) and the hydroxyl group of an alcohol. A substance containing a glycosidic bond is a glycoside. The glycone and aglycone portions can be chemically separated by hydrolysis in the presence of acid. There are also numerous enzymes that can form and break glycosidic bonds.
  • The sugar group is known as the glycone and the nonsugar group as the aglycone or genin part of the glycoside. The glycone can consist of a single sugar group (monosaccharide) or several sugar groups (oligosaccharide). The sugars found in glycosides may be glucose and rhamnose (monosaccharides) or, more rarely, deoxysugars such as the cymarose found in cardiac glycosides.
  • In plants glycosides are both synthesized and hydrolysed under the influence of more or less specific enzymes. They are crystalline or amorphous substances that are soluble in water or alcohols and insoluble in organic solvents like benzene and ether. The aglycone part is soluble in organic solvents like benzene or ether. They are hydrolysed by water, enzymes and mineral acids. They are optically active. While glycosides do not themselves reduce Fehling’s solution, the simple sugars which they produce on hydrolysis will do so with precipitation of red cuprous oxide. The sugars present in glycoside are of two isomeric forms, that is, α form and β form, but all the natural glycosides contain β-type of sugar.
  • The term ‘glycoside’ is a very general one which embraces all the many and varied combinations of sugars and aglycones. 

CLASSIFICATION

  • The glycosides can be classified by the glycone, by the type of glycosidal linkage, and by the aglycone.

On the Basis of Glycone

  • If the glycone group of a glycoside is glucose, then the molecule is a glucoside; if it is fructose, then the molecule is a fructoside; if it is glucuronic acid, then the molecule is a glucuronide, etc.

On the Basis of Glycosidic Linkage

  • O-glycosides: Sugar molecule is combined with phenol or –OH group of aglycon, for example, Amygdaline, Indesine, Arbutin, Salicin, cardiac glycosides, anthraxquinone glycosides like sennosides etc. 
  • N-glycosides: Sugar molecule is combined with N of the –NH (amino group) of aglycon, for example, nucleosides.
  • S-glycosides: Sugar molecule is combined with the S or SH (thiol group) of aglycon, for example, Sinigrin.
  • C-glycosides: Sugar molecule is directly attached with C—atom of aglycon, for example, Anthraquinone glycosides like Aloin, Barbaloin, Cascaroside and Flavan glycosides, etc.

On the Basis of Aglycone

  • The various classes according to aglycone moiety are given below:

DISTRIBUTION OF GLYCOSIDES

  • Glycosides are the class of compounds abundant in nature. Some plant families containing important glycosides are listed bellow:
  • Scrophulareaceae (Digitalis purpurea and Digitalis lanata, Picrorhiza kurroa).
  • Apocyanaceae (Nerium oliander and Thevetia peruviana). 
  • Liliacea (Urgenea indica and U. maritima, Aloe vera) 
  • Leguminocae (Cassia acutefolia and C. angustefolia, Glycyrrhiza glabra, Psoralea corylifolia) 
  • Dioscoreaceae (Dioscorea floribunda)
  • Rosaceae (Prunus amygdalus, Carategus oxycantha) 
  • Cruciferae (Brassica sp.)
  • Gentianaceae (Gentian and Chirata)
  • Acanthaceae (Kalmegh) 
  • Simarubaceae (Quassia)
  • Umbelliferae (Ammi majus, Ammi visnaga) 
  • Rutaceae: Citrus sp. (Ruta graveolens) 
  • Polygonaceae (Fagopyrum sp.) 
  • Myrtaceae (Eucalyptus sp.) 

CHEMICAL TESTS OF GLYCOSIDES

  • Glycosides are the compounds with organic molecules having attached glucose or any mono-oligo sacchrid unit. Usually, these are crystalline or amorphous solids; optically active, soluble in water and alcohol but insoluble in organic solvents like ether, chloroform and benzene etc. Generally, aqueous or alcoholic extracts of crude drugs are tested with specific reagents for presence of various types of glycosides.

Chemical Tests for Anthraquinone Glycosides

Borntrager’s test
  • To 1 gm of drug add 5–10 ml of dilute HCl boil on water bath for 10 min and filter. Filtrate was extracted with CCl4 / benzene and add equal amount of ammonia solution to fil trate and shake. Formation of pink or red colour in ammonical layer due to presence of anthraquinone moiety.
Modified borntrager’s test
  • To 1 gm of drug, add 5 ml dilute HCl followed by 5 ml ferric Chloride (5% w/v). Boil for 10 min on water bath, cool and filter, filtrate was extracted with carbon tetrachloride or benzene and add equal volume of ammonia solution, formation of pink to red colour due to presence of anthraquinone moiety. This is used C-type of anthraquinone glycosides.  

Chemical Tests for Saponin Glycosides 

Haemolysis test
  • A drop blood on slide was mixed with few drops of aq. Saponin solution, RBC’s becomes ruptured in presence of saponins.
Foam test
  • To 1 gm of drug add 10–20 ml of water, shake for few minutes, formation frothing which persists for 60–120 s in presence of saponins.

Chemical Tests for Steroid and Triterpenoid Glycosides 

Libermann burchard test 
  • Alcoholic extract of drug was evaporated to dryness and extracted with CHCl3 , add few drops of acetic anhydride followed by conc. H2 SO4 from side wall of test tube to the CHCl3 extract. Formation of violet to blue coloured ring at the junction of two liquid, indicate the presence of steroid moiety.
Salkowaski test
  • Alcoholic extract of drug was evaporated to dryness and extracted with CHCl3 , add conc. H2 SO4 from sidewall of test tube to the CHCl3 extract. Formation of yellow coloured ring at the junction of two liquid, which turns red after 2 min, indicate the presence of steroid moiety. 
Antimony trichloride test 
  • Alcoholic extract of drug was evaporated to dryness and extracted with CHCl3 , add saturated solution of SbCl3 in CHCl3 containing 20% acetic anhydride. Formation of pink colour on heating indicates presence of steroids and triterpenoids.
Trichloro acetic acid test
  • Triterpenes on addition of saturated solution of trichloro acetic acid forms coloured precipitate. 
Tetranitro methane test
  • It forms yellow colour with unsaturated steroids and triterpenes.
Zimmermann test 
  • Meta dinitrobenzene solution was added to the alcoholic solution of drug containing alkali, on heating it forms violet colour in presence of keto steroid. 

Chemical Tests for Cardiac Glycosides

Keller-kiliani test 
  • To the alcoholic extract of drug equal volume of water and 0.5 ml of strong lead acetate solution was added, shaked and filtered. Filtrate was extracted with equal volume of chloroform. Chloroform extract was evaporated to dryness and residue was dissolved in 3 ml of glacial acetic acid followed by addition of few drops of FeCl3 solution. The resultant solution was transferred to a test tube containing 2 ml of conc. H2 SO4 . Reddish brown layer is formed, which turns bluish green after standing due to presence of digitoxose. 
Legal test 
  • To the alcoholic extract of drug equal volume of water and 0.5 ml of strong lead acetate solution was added, shaked and filtered. Filtrate was extracted with equal volume of chloroform and the chloroform extract was evaporated to dryness. The residue was dissolved in 2 ml of pyridine and sodium nitropruside 2 ml was added followed by addition of NaOH solution to make alkaline. Formation of pink colour in presence of glycosides or aglycon moiety.
Baljet test 
  • Thick section of leaf of digitalis or the part of drug containing cardiac glycoside, when dipped in sodium picrate solution, it forms yellow to orange colour in presence of aglycones or glycosides.
3,5-dinitro benzoic acid test
  • To the alcoholic solution of drug few drops of NaOH followed by 2% solution of 3,5-dinitro benzoic acid was added. Formation of pink colour indicates presence of cardiac glycosides.  

Chemical Tests for Coumarin Glycosides

FeCl3 test
  • To the concentrated alcoholic extract of drug few drops of alcoholic FeCl3 solution was added. Formation of deep green colour, which turned yellow on addition of conc. HNO3 , indicates presence of coumarins.
Fluorescence test 
  • The alcoholic extract of drug was mixed with 1N NaOH solution (one ml each). Development of blue-green fluorescence indicates presence of coumarins.  

Chemical Tests for Cynophoric Glycoside

Sodium picrate test 
  • Powdered drug was moistened with water in a conical flask and few drops of conc. Sulphuric acid was added. Filter paper impregnated with sodium picrate solution followed by sodium carbonate solution was trapped on the neck of flask using cork. Formation of brick red colour due to volatile HCN in presence of cynophoric glycosides takes place. 

Chemical Tests for Flavonoid Glycosides

Ammonia test
  • Filter paper dipped in alcoholic solution of drug was exposed to ammonia vapor. Formation of yellow spot on filter paper.
Shinoda test 
  • To the alcoholic extract of drug magnesium turning and dil. HCl was added, formation of red colour indicates the presence of flavonoids. To the alcoholic extract of drug zinc turning and dil. HCl was added, formation of deep red to magenta colour indicates the presence of dihydro flavonoids.
Vanillin HCl test 
  • Vanillin HCl was added to the alcoholic solution of drug, formation of pink colour due to presence of flavonoids.

ISOLATION

Stas-Otto Method

  • The general method of extraction of glycosides is outlined here. The drug containing glycoside is finely powdered and the powder is extracted by continuous hot percolation using soxhlet apparatus with alcohol as solvent. During this process, various enzymes present in plant parts are also deactivated due to heating. The thermolabile glycosides, however, should be extracted at temperature preferably below 45°C. The extract is treated with lead acetate to precipitate tannins and thus eliminate nonglycosidal impurities. The excess of lead acetate is precipitated as lead sulphide by passing hydrogen sulphide gas through solution. The extract is filtered, concentrated to get crude glycosides. From the crude extract, the glycosides are obtained in pure form by making use of processes like fractional solubility, fractional crystallization and chromatographic techniques such as preparative thin layer and column chromatography. The characterization of isolated purified compounds is done by IR, UV, visible, NMR and mass spectrometry and elemental analysis.

ANTHRACENE GLYCOSIDES

  • Anthracene glycosides are chiefly found in dicot plants but to some extent it is also found in monocot and lower plants. It consists of glycosides formed from aglycone moieties like anthraquinones, anthranols, anthrones or dimers of anthrones or their derivatives. Anthrones are insoluble in alkali and do not show strong fluorescence with them, while anthronols which are soluble in alkali show strong fluorescence. The reduced anthraquinones are biologically more active. Anthroquinones that are present in fresh drugs are in reduced form, which on long storage get oxidized and hydrolysed, Glycosides of reduced derivatives are more active than oxidized aglycones. This is due to the fact that sugars take the glycosides to the site of action and thus are more active.
  • Anthraquinone is an aromatic organic compound and a derivative of anthracene. It has the appearance of yellow or light grey to grey-green solid crystalline powder. Its chemical formula is C14H8 O2 . It melts at 286°C, boils at 379.8°C. It is insoluble in water or alcohol, but dissolves in nitrobenzene and aniline. It is chemically fairly stable under normal conditions.
  • Anthraquinone naturally occurs in some plants (e.g. aloe, senna, rhubarb and cascara), fungi, lichens and insects, where it serves as a basic skeleton for their pigments. Natural anthraquinone derivates tend to have laxative effects. These glycosides are characterized by a chemical test, known as Borntrager test and show the property of microsublimation. Most of the glycosides are O-glycosides and S-glycosides, by their hydrolysis derivatives of 1,8-dihydroxy anthraquinone, anthranol, anthrone, or dianthrone are obtained. The common aglycones are aloe-emodin, emodin, rhein, chrysophanol and physcion which may exist as anthraquinones, anthranols or anthrones. The sugars presents are usually arabinose, rhamnose and glucose. In the drug originally glycosides of reduced derivatives or their dimers are present. During drying and storage by hydrolysis and oxidation free anthraquinones are produced.

SENNA LEAF

Synonyms
  • Alexandrian senna, Tinnevelly senna, Folia senna.
Biological Source 
  • Senna leaf consists of the dried leaflets of Cassia acutifolia Delile (C. senna L.) known as Alexandrian senna and of C. angustifolia Vahl., which is commercially known as Tinnevelly senna. It belong family Leguminosae.
Geographical Source 
  • Alexandrian senna is indigenous to South Africa. It widely grows and sometimes is cultivated in Egypt and in the middle upper territories of Nile river. It is also cultivated in Kordofan and Sennar regions of Sudan. Indian or Tinnevelly senna is indigenous to southern Arabia and cultivated largely in Tinnevelly and Ramnathpuram districts of Tamilnadu. It also grows in Somaliland, Sindh and Punjab region.

Cultivation and Collection

  • Senna plant is a small shrub of 1–1.5 m height with paripinnate compound leaves. Tinnevelly senna is mostly cultivated in well-ploughed, levelled, rich clayed semiirrigated land sometimes after paddy crop in South India. Propagation is done by seeds which are rubbed with coarse sand and sown thinly by broadcasting or in rows 30 cm apart, first during February–March and second after rain in July. Seeds germinate on the third day. The crop becomes ready for harvesting after about 2 months but first plucking of leaflets is done after 3 months of sowing when the leaves appears mature, thick and bluish in colour. Second plucking is followed after a month and subsequent pluckings after 4–6 weeks. The plant can survive for two to three years, but it is grown as an annual. After third plucking the plants are uprooted. Plant shows great tolerance for salinity. It sometimes shows die-back symptoms in which the branches or shoots die from the tip inward, which is caused by parasites or environmental conditions. Leaflets of Tinnevelly senna are collected by careful plucking from luxuriantly grown plants and compressed into bales.

Characteristics

  • Senna leaflets are 3–5 cm long, 2 cm wide and about 0.5 mm thick. It shows acute apex, entire margin and asymmetric base. Outline is lanceolate to ovate lanceolate. Pubescent lamina is found on both the surfaces. Leaves show greyish green colour for Alexandrian senna and yellowish green for Tinnevelly senna. Leaves of Tinnevelly senna are somewhat larger, less broken and firmer in texture than that of Alexandrian senna. Odour of leaves is slight but characteristic and the taste is bitter, mucilagenous. Both the types of leaflets show impression or transverse markings due to the pressing of midrib. Distingushing characters of Alexandrian and Indian senna are given in Table 16.1.

Microscopy

  • Being isobilateral leaf, senna shows more or less similar features at both the surfaces of leaf with few differences. Transverse section of leaf shows upper and lower epidermis with straight wall cells, few of which contain mucilage. Paracytic stomata and nonlignified unicellular trichomes are found on both the surfaces. A single layer of palisade parenchyma is observed at both the sides but it is discontinued in the midrib region of lower epidermis due to the zone of collenchymatous tissues. Palisade is followed by spongy mesophyll which contains cluster crystals of calcium oxalate and vascular strands. Midrib shows the vascular bundle containing xylem and phloem, almost surrounded by lignified pericyclic fibres and a sheath of parenchyma which contains prismatic crystals of calcium oxalate.

Chemical Constituents

  • Senna contains sennosides A and B (2.5%) based on the aglycones sennidin A and B, sennosides C and D which are glycosides of heterodianthrones of aloe-emodin and rhein are present. Others include palmidin A, rhein anthrone and aloe-emodin glycosides. Senna also contains free chryso
  • phanol, emodin and their glycosides and free aloe-emodin, rhein, their monoanthrones, dianthrones and their glycosides. Mucilage is present in the epidermis of the leaf and gives red colour with ruthenium red.

ALOE

Biological Source

  • Aloe is the dried juice collected by incision, from the bases of the leaves of various species of Aloe. Aloe perryi Baker, Aloe vera Linn or Aloe barbadensis Mil and Aloe ferox Miller., belonging to family Liliaceae. Aloe perryi Baker is found in Socotra and Zanzibar islands and in their neighbouring areas and so the aloes obtained from this species is known as Socotrine or Zanzibar aloe. Aloe vera Linn is also known as Aloe vulgairis Lamarek, or Aloe barbadensis Mil. or Aloe officinalis Forskal. It was formerly produced on the island of Barbados, where it was largely cultivated, having been introduced at the beginning of the sixteenth century. It is now almost entirely made on the Dutch islands of Curacoa, Aruba and Bonaire. The aloes obtained from this species is known as Curacao or Barbados aloe. Aloe ferox Miller and hybrids of this species with Aloe africana and Aloe spicata, A. platylepia and other species of Aloe grows in Cape Colony and so is known as Cape aloe.

Geographical Source
  • Aloes are indigenous to East and South Africa, but have been introduced into the West Indies and into tropical countries, and will even flourish in the countries bordering on the Mediterranean.
Cultivation and Collection
  • It is an evergreen perennial growing to 0.8 m by 1 m at a slow rate. The plant prefers light (sandy) and medium (loamy) soils, requires well-drained soil and can grow in nutritionally poor soil. The plant prefers acid, neutral and basic (alkaline) soils. It cannot grow in the shade. It requires dry or moist soil and can tolerate drought. They are xerophytic plant. It can be propagated by seeds. Seeds are sown in the spring in a warm green house. The seed usually germinates in 1–6 months at 16°C. The seedlings are transferred to the pots containing well-drained soil. They are allowed to grow in sunny part for at least their first two winters. The offsets will be available, usually in spring. The plants produce offsets quite freely and they can be divided at any time of the year as long as it is warm enough to encourage fresh root growth to allow reestablishment of the plants. Young offsets are planted in the soil after the rainy season in rows situated at a distance of 60 cm. In the second year leaves are collected by the natives by protecting their hands because of the spiny nature of leaves. The leaves are cut near the base, kept inside of kerosene tins and taken them to a central place for the preparation of aloe. Juice of aloe is present in parenchymatous cells of pericycle that are mucilage cells. In a single incision mucilage cells exert pressure on pericycle cells and the entire juice from the leaves is drained out.

Preparation of Aloe

Curacao or barbados aloe
  • In West Indies the cut leaves are arranged with their cut surface on the inner side, on the sides of V shaped vessel of about 1–2 m long and the flowing juice is collected in a tin vessel that is placed below the V-shaped vessel This juice thus collected is concentrated either by spontaneous evaporation, or more generally by boiling until it becomes of the consistency of thick honey. These conditions favours the crystallization of barbaloin and this aloe contains crystals of barbaloin because of the presence of which it becomes opaque and so also known as hepatic or livery aloe. On cooling, it is then poured into gourds, boxes, or other convenient receptacles and solidifies.
Socotrine aloe 
  • When it is prepared, it is commonly poured into goat skins, and spontaneous evaporation is allowed for about a month when it becomes viscous pasty mass which are then packed into cases. In European countries it is dried in wooden pans with hot air till moisture is about 10%
Zanzibar aloe 
  • This aloe is prepared similar to Socotrine aloe. It is packed in skins, of carnivorous animals. This aloe is also known as monkey skin aloe.
Cape aloe 
  • The leaves of the plants from which Cape aloe is obtained are cut off near the stem and arranged around a hole in the ground, in which a sheep skin is spread, with smooth side upwards. When a sufficient quantity of juice has drained from the leaves it is concentrated by heat in iron cauldrons and subsequently poured into boxes or skins in which it solidifies on cooling. Large quantities of the drug are .exported from Cape Town and Mossel Bay.

Characteristics

Curacao aloe 
  • It is usually opaque and varies in colour from bright yellowish or rich reddish brown to black. Sometimes it is vitreous and small fragments are then of a deep garnet-red colour and transparent. It is then known as ‘Capey Barbados’ and is less valuable, but may become opaque and more valuable by keeping. Curacoa Aloes possesses the nauseous and bitter taste that is characteristic of all Aloes and a disagreeable, penetrating odour. It is almost entirely soluble in 60% alcohol and contains not more than 30% of substances insoluble in water and 12% of moisture. It should not yield more than 3% of ash. The fracture is waxy.
Cape aloes 
  • It forms dark coloured masses which break with a clean glassy fracture and exhibit in their splinters a yellowish, reddish-brown or greenish tinge. Its translucent and glossy appearance are very characteristic and red-currant like odour sufficiently distinguish it from all other varieties of Aloes.

Chemical Constituents

  • The most important constituents of Aloes are the three isomers of Aloins, Barbaloin, β-barboloin and Isobarbaloin, which constitute the so-called ‘crystalline’ Aloin, present in the drug at from 10 to 30%. Other constituents are amorphous Aloin, resin, emodin and Aloe-emodin. Barbaloin is present in all the varieties; it is slightly yellow coloured, bitter, water soluble, crystalline glycoside. Isobarbaloin is a crystalline substance, present in Curacao aloe and in trace amount in Cape aloe and absent in Socotrine and Zanzibar aloe. The chief constituents of Socotrine and Zanzibar aloe are Barbaloin and β-Barbaloin.

Marketed Products

  • It is one of the ingredients of the preparations known as Diabecon, Evecare (Himalaya Drug Company), Mensonorm (Chirayu Pharma) and Kumari Asava (Baidyanath).

RHUBARB

Biological Source 
  • Rhubarb consists of the peeled dried rhizomes and roots of Rheum palmatum Linn., belonging to family Polygonaceae.
Geographical Source
  • It is mainly found in E. Asia, N.W. China in Yunnan, W. Sichuan, E. Xizang and Gansu, Thibet and India.
Cultivation and Collection

  • The plant is perennial growing to 3 m by 2 m. The plant prefers medium (loamy) and heavy (clay) soils, requires well-drained soil and can grow in heavy clay soil. The plant prefers acid, neutral and basic soils. Drug is collected from wild plants but is also cultivated to some extent. The plant grows at an altitude of 2,500–4,000 m. It can grow in semishade or no shade. It requires moist soil. Plants can be grown in quite coarse grass, which can be cut annually in the autumn. Seeds are sown in autumn in a shaded cold frame. The seed can also be sown in spring in a cold frame. When large enough to handle, seedlings are pricked out and transferred into individual pots and allowed to grow them on in the green house or cold frame for their first winter, then they are transplanted out in the spring. The rootstocks are divided in early spring with a sharp knife, making sure that there is at least one growth bud on each division and the required amount of drugs is collected and the remaining are planted.

Characteristics
  • The leaves of the Turkey Rhubarb are palmate and somewhat rough. The root is thick, of an oval shape, sending off long, tapering branches; externally it is brown, internally a deep yellow colour. The stem is erect, round, hollow, jointed, branched towards the top, from 6 to 10 feet high. This species is distinguished from other Rhubarbs by its much larger size, the shape of its leaves, with their oblong, sharpish segments, and the graceful looseness of its little panicles of greenish-white flowers. The first buds which appear in spring are yellow, not red. Chinese or Turkey Rhubarb occurs in commerce in brownish-yellow pieces of various sizes, usually perforated, the holes often containing a portion of the cord used to hang the sections of the root on during drying. The outer surface is generally powdery (the bark having been removed) and shows a network of white lines. The taste is astringent and nauseous, and there is a characteristic odour. 
Chemical Constituents
  • Rhubarb contains free anthraquinones, their glycosides, reduced derivatives, anthrones, or dianthrone and heterodianthrones. The anthraquinones of rhubarb are chrysophanol, aloe-emodin, emodin, physcion and rhein. Anthrones or dianthrones are of chrysophanol, emodin and aloe-emodin. Heterodianthrones contain two different molecules of anthrones and they are from above anthrones. It also contains tannoid constituents, starch and calcium oxalate. There are also several resinous matters, one of which, Phaoretin, is purgative, and mineral compounds are also present. The astringency of Rhubarb is due to a peculiar tannic acid (Rheotannic), which is soluble in water and alcohol.

CASCARA BARK

Synonyms 
  • Californian Buckthorn, Cascara Buckthorn, Cascara Sagrada, Kaskara Sakrada, Kasukarasakurada, Pursh’s Buckthorn, Sacred Bark, Chittem Bark.
Biological Source
  • Cascara is the dried bark of Rhamnus purshiana DC., belonging to family Rhamnaceae. It is collected at least one year before use.
Geographical Source
  • It is indigenous to North America, British Columbia, Canada and Kenya.
Cultivation and 
  • Collection It is an evergreen tree growing to 6–12 m in height. The plant prefers sandy, loamy and clay soils. The plant prefers acid, neutral and basic soils. It can grow in semishade or no shade. It requires moist soil. It is cultivated using different techniques like sowing seeds, cuttings and layering. Seeds are sown in the autumn in a cold frame. Stored seed will require 1–2 months cold stratification at about 5°C and should be sown as early in the year as possible in a cold frame or outdoor seed bed. Seedlings are transferred to the pots and then they are transplanted in late spring or early summer of the following year. Cuttings are carried out using half-ripe wood, July/August. Layering can be done in early spring.
Characteristics
  • The drug mostly occurs in quilled, channelled or incurved of varying lengths and sizes, usually 20 cm long and 1–4 mm thick, smooth or nearly so externally, covered with a greyish-white layer, which is usually easily removed, and frequently marked with spots or patches of adherent lichens. Beneath the surface it is violet-brown, reddish-brown or brownish, and internally a pale yellowish-brown and nearly smooth. Fracture is short and granular in the outer part and fibrous in the phloem. It has no marked odour, but a nauseous, bitter taste. It is frequently also imported in flattened packets, consisting of small pieces of the bark compressed into a more or less compact mass.

Microscopy

  • The cork consists of numerous layers of small, thin walled flattened, polygonal prisms, arranged in radial rows and having yellowish brown contents. Next to cork few layers of collenchyma cells are present. Groups of irregular thick walled lignified stone cells are in the cortex and 1–5 celled wide phloem rays and tangentially elongated lignified fibres in the phloem. The fibres are crystal fibres and surrounded by parenchyma containing calcium oxalate prisms. Crystal fibres are of diagnostic importance in identification of the powdered drug.

Chemical Constituents

  • Cascara bark contains 80–90% of C-glycosides and 10–20% O-glycosides. The C-glycosides present in cascara are aloin or barbaloin and 11-deoxyaloin or chrysaloin. Cascarosides A and B are the primary glycosides of aloin and cascarosides C and D are primary glycosides of chrysaloin. Cascara also contains chrysaloin and barbaloins, dianthrones of emodin, aloe-emodin, chrysophanol; heterodianthrones like Palmidins A, B and C, free emodin, aloe-emodin and a bitter lactone. Apart from glycosides it also contains fat, starch, glucose, volatile odorous oil, malic and tannic acids. Fresh cascara bark contains anthranol derivatives which have griping; and emetic properties and after storage for one year, anthranol derivatives are oxidized to anthraquinone derivatives and bark loses irritant properties.

Substitutes
  • These include R. alnifolia, which is too rare to be a likely substitute; R. crocea, whose bark bears little resemblance to the official drug. R. californica is very closely related to R. purshiana. It has a more uniform coat of lichens and wider medullary rays than the official species, but resembles the latter in having sclerenchymatous cells. The bark of R.fallax has been recorded as a cascara substitute.
Marketed Products 
  • It is one of the ingredients of the preparations known as Herbal Laxative (Trophic Canada Ltd.).

STEROL OR CARDIAC GLYCOSIDES

  • The cardiac glycosides are an important class of naturally occurring drugs whose actions include both beneficial and toxic effects on the heart. Plants containing cardiac steroids have been used as poisons and heart drugs at least since 1500 B.C. Throughout history these plants or their extracts have been variously used as arrow poisons, emetics, diuretics and heart tonics. Cardiac steroids are widely used in the modern treatment of congestive heart failure and for treatment of atrial fibrillation and flutter. Yet their toxicity remains a serious problem. These drugs all act by affecting the availability of intracellular Ca+2 for myocardial contraction or increasing the sensitivity of myocardial contractile proteins.
  • Cardiac glycosides are composed of two structural features: the sugar (glycone) and the nonsugar (aglycone– steroid) moieties.
  • The steroid nucleus has a unique set of fused ring system that makes the aglycone moiety structurally distinct from the other more common steroid ring systems. The steroid nucleus has hydroxyls at 3- and 14-positions of which the sugar attachment uses the 3-OH group. 14-OH is normally unsubstituted. Many genins have OH groups at 12- and 16-positions. These additional hydroxyl groups influence the partitioning of the cardiac glycosides into the aqueous media and greatly affect the duration of action. The lactone moiety at C-17 position is an important structural feature. The size and degree of unsaturation varies with the source of the glycoside. Normally plant sources provide a fivemembered unsaturated lactone while animal sources give a six-membered unsaturated lactone.
  • One to four sugars are found to be present in most cardiac glycosides attached to the 3β-OH group. The sugars most commonly used include L-rhamnose, D-glucose, D-digitoxose, D-digitalose, D-digginose, D-sarmentose, L-vallarose and D-fructose. These sugars predominantly exist in the cardiac glycosides in the β-conformation. The presence of acetyl group on the sugar affects the lipophilic character and the kinetics of the entire glycoside. Two classes have been observed in nature—the cardenolides and the bufadienolides.

DIGITALIS LEAVES

Cultivation and Collection

  • Digitalis is a biennial herb growing wild but good quality of the drug is obtained especially from cultivated plant. The plant will flourish best in well drained loose soil, preferably of siliceous origin, with some slight shade. The plants growing in sunny situations possess the active qualities of the herb in a much greater degree than those shaded by trees, and it has been proved that those grown on a hot, sunny bank, protected by a wood, give the best results. It grows best when allowed to seed itself, if it is desired to raise it by sown seed, 2 lb of seed to the acre are required. For cultivation special strains of the seeds are selected which would produce disease-resistant plants with maximum activity. Attention is specially paid to the structure of the soil in seed beds. As the seeds are so small and light, they should be mixed with fine sand in order to ensure even distribution. Before sowing soil is sterilized. They should be thinly covered with soil. The seeds are uncertain in germination, but the seedlings may be readily and safely transplanted in damp weather, and should be pricked out to 6–9 inches apart. Sown in spring, the plant will not blossom till the following year. Seeds must be gathered as soon as ripe. In dry season sufficient water is supplied to the plant. In the first year, a long stalk with rosette of leaves is produced. The flowers of the true medicinal type must be pure, dull pink or magenta, not pale-coloured, white or spotted externally.

Morphology


 Microscopy

  • Digitalis has dorsiventral leaf structure. It has plenty of simple covering and glandular trichomes on both the surfaces. The covering trichomes are uniseriate, usually three to four cells long, having collapsed cells, acute apex and finely warty cuticle. The glandular trichomes have a short, unicellular stalk and bicellular or rarely unicellular head. It has anomocytic or ranunculaceous type of stomata. Trichomes and stomata are more in lower surface. The pericycle is parenchymatous above and collenchymatous below. Calcium oxalate crystals are absent.

Chemical Constituents

  • Digitalis leaves contains 0.2–0.45% of both primary and secondary glycosides. Purpurea glycosides A and B and glucogitoloxin are primary glycosides. Because of greater stability of secondary glycosides, and lesser absorption of primary glycosides a higher content of primary glycosides are not considered ideal and secondary glycosides are used. Purpurea glycosides A and B are present in fresh leaves and by their hydrolysis digitoxin and glucose or gitoxin and glucose are obtained respectively. Hydrolysis of purpurea glycosides can take place by digipuridase (enzyme) present in the leaves. Digitoxin yields on hydrolysis digitoxigenin and three digitoxose. By hydrolysis of verodoxin, gitaloxigenin and digitalose are obtained. Digitalis leaves also contains glycosides like odoroside-H, gitaloxin, verodoxin and glucoverodoxin. Verodoxin was found to potentiate the activity of digitoxin by synergism. Digitoxose and digitalose are desoxy sugars found only in cardiac glycosides and answers Keller– Killiani test. The important saponins include digitonin, tigonin and gitonin, and luteolin, a flavone responsible for the colour of the drug are also present in the leaves.

DIGITALIS LANATA

Biological Source

It consists of the dried leaves of Digitalis lanata J. F. Ehrh., belonging to family Scrophulariaceae.

Geographical Source

  •  It is mainly found in Central and Southern Europe, England, California and India.

Cultivation and Collection

  • It is an evergreen biennial/Perennial growing to 0.6 m by 0.3 m. The plant prefers light (sandy), medium (loamy) and heavy (clay) soils. The plant prefers acid, neutral and alkaline soils. It can grow in semishade or no shade. It requires dry or moist soil. It grows well even in ordinary garden soil, especially if it is rich in organic matter. It is propagated by seeds. Seed are sown on early spring in a cold frame. The seed usually germinates in 2–4 weeks at 20°C. When they are large enough to handle, seedlings are transplanted into individual pots and planted them out in the summer.

Characteristics

  • The leaves are sessile, linear-lanceolate, about 30 cm long and 4 cm broad with entire margin and apex is acuminate. The veins leave the midrib at an acute-angle. The epidermal cells are beaded with anticlinal walls, has 10–14 celled nonglandular trichomes, and the glandular one.

Chemical Constituents

  • Digitalis lanata contains cardiac glycosides like lanatoside A, B, C and E. Lanatosides A and B are acetyl derivatives of purpurea glycosides A and B respectively. Hydrolysis of Lanatoside C yields digoxin, a crystalline active glycoside.

Uses

  • It has gained much importance in recent years because of the less cumulative effect and three to four times greater activity than D. purpurea. They have the same actions as that of the D. purpurea. It is the commercial source of digoxin. Employed in the treatment of auricular fibrillation and congestive heart failure. Their use should always be supervised by a qualified practitioner since in excess they cause nausea, vomiting, slow pulse, visual disturbance, anorexia and fainting.

THEVETIA

Synonyms 

  • Yellow oleander, Lucky nut tree, Trumphet flower.

Biological Source

  • It is the dried seeds of Thevetia nerifolia Juss, Syn. Thevetia peruviana Merrill., belonging to family Apocynaceae.

Geographical Source 

  • It is a large, evergreen shrub 450–600 cm tall with scented bright yellow flowers in terminal cymes bears triangular fleshy drupes, containing two to four seeds. Leaves are about 10–15 cm in length, linear acute. It is mainly found in the United States, India and West Indies.

Morphology


Chemical Constituents

  • Thevetia kernels mainly contain cardioactive glycosides, Thevetin A, Thevetin B (cerebroside), peruvoside, Nerrifolin, thevenenin (ruvoside) peruvosidic acid (Perusitin), etc. The sugar units are L-thevetose, and D-glucose.

SQUILL

Cultivation and Collection

  • The plant prefers light (sandy) and medium (loamy) soils and requires well-drained soil. The plant prefers acid, neutral and basic (alkaline) soils. It cannot grow in the shade. It requires dry or moist soil. The plant can tolerate strong winds but not maritime exposure. Seeds are sown as soon as it is ripe in a greenhouse. The seeds were sown thinly so that the seedlings can be left in the pot for their first growing season. Fertilizers are to be used regularly. Once the plant becomes dormant the young bulbs are divided, placing two to three bulbs in each pot. After an year they are transplanted to the field. Division of offsets is done in late summer when the bulb is dormant. Larger bulbs can be replanted immediately into their permanent positions. It is probably best to pot up smaller bulbs and grow them on in a greenhouse for a year before planting them out when they are dormant in late summer. The bulb is large and 18–20 cm high with 12 cm to 15 cm in diameter. Bulbs are dug out from the soil in the end of August and external scaly leaves and central portion are removed. The slices are dried completely in the sunlight or by heat of the stove. The drug is stored in airtight and especially in moisture proof containers.

Characteristics

  • It is a perennial plant with fibrous roots proceeding from the base of a large, tunicated, nearly globular bulb, 4–6 inches long, the outer scales of which are thin and papery, red or orange-brown in colour. The bulb, which is usually only half immersed in the sand, sends forth several long, lanceolate, pointed, somewhat undulated, shining, darkgreen leaves, when fully grown, feet long. From the middle of the leaves, a round, smooth, succulent flower-stem rises, from 1 to 2 feet high, terminating in a long, close spike of whitish flowers, which stand on purplish peduncles, at the base of each, is a narrow, twisted, deciduous floral leaf or bract. 

Chemical Constituents

  • Squill contains cardiac glycosides of bufadienolides types, scillaren A and B and enzyme scillatenase. The other constituents present are glucoscillaren A (cardiac glycoside), proscillaridin A, flavonoid, mucilage, volatile substances and sinistrin. The cardiac glycoside (glucoscillaren A) on hydrolysis gives three glucose molecules, 2 molecules of glucose and a molecule of rhamnose along with scillarenin. Scillaren A is crystalline and responsible for the activity of the drug. Scillaren B is amorphous and its exact chemical structure is not known. Scillaren-A on hydrolysis with enzyme yields proscillaridin A and glucose. Proscillaridin A on further acid hydrolysis yields the aglycone scillarenin

INDIAN SQUILL

Geographical Source

  • It is found throughout India (Western Himalaya, Konkan, Coramandal coast, Bihar, etc.).

Cultivation and Collection

  • Though it is not been cultivated, it grows well at a temperature of 15–20°C and in sandy soil. The bulbs grow to full size within 5 years. The bulbs are collected after flowering, cut in to small slices and dried under sun.

Morphology

Microscopy

  • A thin transverse section when observed under the microscope shows the following characters. Single layer of polygonal elongated epidermis is present which is covered with the cuticle. Mesophyll region consists of acicular calcium oxalate crystals, mucilage sheath, small round starch grains and vascular bundle (annular and spiral xylem vessels).

STROPHANTHUS

Cultivation and Collection

  • The plants are large, woody climbers, climbing on the large trees in the forests of Africa. Fruit consists of two divergent follicles which are dehiscent and many seeded. Each follicle is 30 cm long, 2.5 cm broad, tapering both at the apex and base. Mature and ripe fruits are collected in the month of June–July. After collection epicarp and fleshy mesocarp are removed and seeds separated from yellow-brown leathery endocarp and awns. Seeds are washed and dried. The seeds are derived from anatropous ovules.

Characteristics

  • The name Strophanthus is derived from the Greek strophos (a twisted cord or rope) and anthos (a flower), thus expressing the chief peculiarity of its appearance, the limb of the corolla being divided into five, long, tail-like segments. The official description of the seeds is lance-ovoid, flattened and obtusely edged; from 7 to 20 mm in length, about 4 mm in breadth and about 2 mm in thickness; externally of a light fawn colour with a distinct greenish tinge, silky lustrous form, a dense coating of flat-lying hairs (S. Kombe) bearing on one side a ridge running from about the centre to the summit; fracture short and somewhat soft, the fractured surface whitish and oily; odour heavy when the seeds are crushed and moistened; taste very bitter.

Microscopy

  • Epidermis consists of elongated, polygonal, tabular cells and lignified covering trichomes. Next to epidermis collapsed layer of parenchyma cells are present that contain calcium oxalate crystals. Thin walled endosperm contains aleurone grains and fixed oil.

Chemical Constituents

  • The drug contains 8–10% cardiac glycosides known as k-strophanthin. k-strophanthin is a mixture of three glycosides, cymarin, k-strophanthin P and k-strophanthoside, which differ only through attached sugars and on hydrolysis yields same aglycone strophanthidin. It contains a sugar cymarose that is methoxy digitoxose which gives positive reaction for Keller–Killiani test. The drug also contains mucilage, resin, fixed oil, choline, trigonelline, and kombic acid—an acid saponin.

OLEANDER

Microscopy

  • Lamina shows an isobilateral structure, 3–4 layered palisade parenchyma cells below upper and above lower epidermis in the mesophyll, single layer of epidermis covered externally by thick cuticle, epidermal cells elongate to form unicellular, nonlignified and nonglandular hairs; four to seven layers of collenchymatous cells and a wide zone of parenchyma follows the epidermis; parenchymatous cells thin walled, more or less isodiametric with intercellular spaces, some cells contain rosette crystals of calcium oxalate; petiole receives three vascular bundles from stem, central one large and crescent shaped while other two much smaller and somewhat circular present on each side of central vascular bundle. The leaves contain anomocytic type of stomata.

Chemical Constituents

  • Cardiac glycosides oleandrine, gitoxigenin, neridiginoside, adynerigenin, etc., also it contains terpenoids, sterols, tannins, essential oils.

SAPONIN GLYCOSIDES

  • Saponins are glycoside compounds often referred to as a ‘natural detergent’ because of their foamy texture. They get their name from the soap wort plant (Saponaria), the root of which was used historically as a soap (Latin sapo— soap). Foremost among this is the strong tendency to froth formation when shaken with water. The other properties are hemolytic activity, sneezing effect, toxicity, complex formation with cholesterol and antibiotic properties. Saponins have long been known to have strong biological activity. When studying the effect that saponins have on plants, it has been discovered that saponins are the plants active immune system. They are found in many plants, they consist of a polycyclic aglycone that is either a choline steroid or tritetpenoid attached via C3 and an ether bond to a sugar side chain. The aglycone is referred to as the sapogenin and steroid saponins are called sarsaponins. The ability of a saponin to foam is caused by the combination of the nonpolar sapogenin and the water soluble side chain. Saponins are bitter and reduce the palatability of livestock feeds. However if they have a triterpenoid aglycone they may instead have a licorice taste as glucuronic acid replaces sugar in triterpenoids. Some saponins reduce the feed intake and growth rate of nonruminant animals while others are not very harmful. For example, the saponins found in oats and spinach increase and accelerate the body’s ability to absorb calcium and silicon, thus assisting in digestion. As mentioned earlier they are composed of a steroid (C-27) or triterpenoid (C-30) saponin nucleus with one or more carbohydrate branches.

Steroid Saponins

  • Steroid saponins are similar to the sapogenins and related to the cardiac glycosides. They have ability to interact medically and beneficially with the cardiac glycosides, sex hormones, Vitamin D and other factors, render these phytochemicals components of great medical significance. Diosgenin is the important steroid sapogenin. Recently from these saponins steroid hormones like progesterone, cortisone etc. are obtained by partial synthesis and thus their importance has increased considerably. Some of the families with steroidal saponins are Solanaceae, Apocynaceae, Liliaceae, Leguminosae, etc.

Triterpenenoid Saponins

  • Triterpenoid saponins, or sapogenins, are plant glycosides which lather in water and are used in detergents, or as foaming agents or emulsifiers, and have enormous medical implications due to their antifungal, antimicrobial, and adaptogenic properties. Triterpene saponins are usually β-amyrine derivatives and some are also α-amyrine and lupeol derivatives. It has a pentacyclic triterpenoid nucleus which is linked with either sugar or uronic acid. Glycyrrhizin, from licorice root, is an example of a saponin used for antiinflammatory purposes in place of cortisone. They are commonly available in dicot plants belonging to the family Rubiaceae, Compositae, Rutaceae, Umbelliferae, etc.

  • Saponins are extremely toxic to fishes but do not render them inedible, as saponins are not poisonous to man when taken orally. Very dilute solution of saponins hemolyses red blood corpuscles. The hemolysis take place due to the formation of complex with the cholesterol of erythrocyte membrane causing its destruction, this is a chief property of saponin, very rarely shown by any other plants product. Saponins accelerate the germination and growth of the seeds. Saponins show fungicidal, bactericidal activity, antiviralactivity, antibiotic property, inflammation inhibition activity, spermicidal, antifertility, molluscicidal, etc. Saponins have been reported to possess blood purifying and abortion causing properties, anthelmintic effect, sedative property and antispasmodic effects.

DIOSCOREA

Cultivation and Collection

  • It is a perennial climber growing to 3 m. The plant prefers sandy, loamy and clay soils and requires well-drained soil. The plant prefers acid, neutral and basic (alkaline) soils. It can grow in semishade or no shade. It requires moist soil. It can be cultivated in three methods, by sowing seeds or stem cuttings or by tubercles. Seeds are sown in the month of March to April in a sunny position in a warm green house and only just covered. It germinates in one to three weeks at 20°C. The seedlings are taken out as soon as they are large enough to handle and grown on in a green house for their first year. Transplanted in late spring as the plant comes into new growth. Basal stem cuttings are done in the summer. Division is done in the dormant season, never when in growth. The plant will often produce a number of shoots, the top 5–10 cm of the root below each shoot can be potted up to form a new plant whilst the lower part of the root can possibly be eaten. Tubercles (baby tubers) are formed in the leaf axils. These are harvested in late summer and early autumn when about the size of a pea and coming away easily from the plant. They should be potted up immediately in individual pots in a greenhouse or cold frame and transplanted out in early summer when in active growth.

Chemical Constituents

  • The roots contain diosgenin (4–6%) a steroidal sapogenin and its glycoside smilagenin, epismilagenin and beta isomer yammogenin. It also contains sapogenase (enzyme), phenolic compounds and starch (75%).

LIQUORICE

Cultivation and Collection

  • Liquorice is often cultivated for its edible root which is widely used in medicine and as flavouring. The plant requires a deep well cultivated fertile moisture-retentive soil for good root production. Prefers a sandy soil with abundant moisture and does not flourish in clay. Slightly alkaline conditions produce the best plants. The plant thrives in a maritime climate. It is propagated using seeds and roots. The seeds are presoaked for 24 h in warm water and then sown in spring or autumn in a greenhouse. The seedlings are individually potted when they are large enough to handle, and grown them for their first winter in a green house. They are transplanted in late spring or early summer when in active growth. Plants are rather slow to grow from seed. The plant parts are procured from old plantations, being waste from the harvesting process, consisting of those side roots or runners which have eyes or buds, cut into sections about 6 inches long. They are dibbled in rows 3 or 4 feet apart, about 4 inches underneath the surface and about 18 inches apart in the rows. In the autumn, the ground is dressed with farmyard manure, about 40 tons to the acre. Plants are slow to settle in and do not produce much growth in their first two years after being moved. The young growth is also very susceptible to damage by slugs and so the plant will require some protection for its first few years. This species has a symbiotic relationship with certain soil bacteria; these bacteria form nodules on the roots and fix atmospheric nitrogen. Some of this nitrogen is utilized by the growing plant but some can also be used by other plants growing nearby.

Characteristics

  • Liquorice root is in long, straight, nearly cylindrical, unpeeled pieces, several feet in length, varying in thickness from 1/4 inch to about 1 inch, longitudinally wrinkled, externally greyish brown to dark brown, warty; internally tawny yellow; pliable, tough; texture coarsely fibrous; bark rather thick; wood porous, but dense, in narrow wedges; taste sweet, very slightly acrid. The underground stem which is often present has a similar appearance, but contains thin pith. When peeled, the pieces of root (including runners) are shorter, a pale yellow, slightly fibrous externally, and exhibit no trace of the small dark buds seen on the unpeeled runners here and there. Otherwise it resembles the unpeeled.

Microscopy

  • Cork consists of several rows of radially arranged thin walled tubular cells. Phelloderm is composed of parenchymatous and sometimes collenchymatous cells. Starch grains and calcium oxalate crystals are seen in phelloderm. Pericyclic fibres are found in groups. Phloem consists of sieve tissue alternating with thick walled, lignified fibres surrounded by a sheath of parenchymatous cells containing prisms of calcium oxalate. Xylem vessels and xylem parenchyma are present. Medullary rays are radially elongated. Pith is present in rhizomes and absent in root.


Characteristics 

  • The leaves are like pine-needles, small and uniform. The inflorescence has tiny white flowers, in small spikes. The roots are finger-like and clustered. The roots are cylindrical, fleshy raberous, straight or slightly curved, tapering towards the base and swollen in the middle; white to colour, 5–15 cm in length and 1–2 cm diameter, irregular fracture, longitudinal furrows and minute transverse wrinkles on upper surface and is bitter in taste.

BRAHMI

Geographical Source 

  • The plant is found in swampy areas of India, commonly found as a weed in crop fields and other waste places throughout India up to an altitude of 600 m and also in Pakistan, Sri Lanka and Madagascar.

Characteristics

  • It is a slender, herbaceous creeper. Stems are long, prostate, filiform, often reddish and with long internodes, rooting at nodes. Leaves are long-petioled, 1.3–6.3 cm in diameter, several from rootstock and 1–3 cm from each node of stem. They are orbicular, reniform, rather broader than long, glabrous on both sides and with numerous slender nerves from a deeply cordate base. Fruit 8 mm long, ovoid, hard with a thick pericarp.

Microscopy

  • Root: Outer cork consisting of three- to five-layered, exfoliated rectangular cells, followed by cortex region consisting three or four layers of parenchyma cells containing oval to round, simple, starch grains and micro-sphenoidal crystals of calcium oxalate; secondary cortex composed of thin walled, oval to polygonal parenchymatous cells. Secretory cells are also present. Stem: Single layered epidermis composed of round to cubical cells covered by striated cuticle. Two or three layers of collenchymatous cells are found below the epidermis, collenchymatous cells are followed by six to eight layers of thin walled, isodiametric, parenchymatous cells with intercellular space present; vascular bundles collateral, open, arranged in a ring, capped, by patches of sclerenchyma and traversed by wide medullary rays. Resin ducts are also present in parenchymatous cells of cortex; pith consists of isodiametric parenchyma cells with intercellular spaces. Leaf: Single layered epidermis covered by a thick cuticle, two- or three-layered collenchyma in the midrib region on both surfaces, central zone occupied by vascular bundles, mesophyll consists of two or three layers of palisade cells, five to seven layers of loosely arranged, more or less isodiametric spongy parenchyma cells. Rosette type crystals of calcium oxalate and anisocytic stomata are also present. Few anomocytic stomata are also seen.

Chemical Constituents

  • The drug contains triterpenoid saponin glycosides, indocentelloside, brahmoside, brahminoside, asiaticosides, thankuniside and isothankuniside. The corresponding trirerpene acids obtained on hydrolysis of the glycosides are indocentoic, brahmic, asiatic, thankunic and isothankunic acids. These acids, except the last two, are also present in free form in the plant from isobrahmic and betulic acids. The presence of mesoinositol, a new oligosaccharide, centellose, kaempferol, quercetin and stigmasterol, have also been reported.

Characteristics

  • The root, varying in colour from light yellowish grey to brownish grey, and in size from the thickness of a straw to that of the little finger, has as its distinguishing mark a projecting line, along its concave side. It is usually twisted, sometimes almost spiral, and has at its upper end a thick, irregular, knotty crown, showing traces of numerous, wiry stems. It breaks with a short fracture, the wood often showing an abnormal appearance, since one or two wedgeshaped portions may be replaced by parenchymatous tissue, as if a segment of wood had been cut out. The keels are due to the development of the bast, and not to any abnormality in the wood. It taste sweet first and then turns to acrid and have characteristic odour.

Uses

  • The root promotes the clearing of phlegm from the bronchial tubes. It is antidote, cathartic, diaphoretic, diuretic, emetic, expectorant, sialagogue and stimulant. It was used by the North American Indians in the treatment of snake bites and has been found used in the treatment of various respiratory problems including pleurisy and pneumonia.

Allied Drugs

  • Polygala senega var. latifolia. (Northern senega), collected in the northwestern States, is considerably larger than the usual variety (Western senega), and darker in colour; it shows the keel less distinctly, but it has a very acrid taste.

QUILLAIA

Synonyms

Quillaia; Soap bark, Quillary bark, Panama bark; China bark, Murillo bark, Panama wood; Cortex quillaiae.

Biological Source

  • Quillaia bark is the inner dried bark of Quillaia saponaria Molina and other species of Quillaia, belonging to family Rosaceae.

Geographical Source

  • Q. saponaria is about 18 m high evergreen, graceful tree found in Peru, Chile, Bolivia, South America and California.

Characteristics

  • Quillaia bark occurs in flat pieces, about 1 m long, 20 cm wide, and 3–10 cm thick. Outer surface is brownish-white, smooth and contains reddish- or blackish-brown patches of rhytidome adhere to the outer surface. The rhytidome is made of dead secondary phloem. The inner surface is yellowish-white and smooth. Fracture is splintery. Large crystals of calcium oxalate are present. Odour is sternutatory and taste is acidic and astringent.

Microscopy

  • A transverse section of quillaia bark shows alter nating bands of lignified and nonlignified phloem. The medullary rays are usually two to four cells wide. The phloem fibres are tortuous and often accompanied by small groups of rectangular sclereids. The parenchyma contains numerous starch grains and calcium oxalate prism.

Chemical Constituents

  • Quillaia bark contains saponins (10%), quillaic acid, calcium oxalate, starch, sucrose and tannin. Quillaia saponin on hydrolysis forms pentacyclic triterpenoid, quillaic acid (Quillaia sapogenin), a sugar glucuronic acid and gypsogenin.

Chemical Tests

  • Powdered drug on shaking with water produces soap like froth which persists for some time.

  • On addition of a small portion of drug or its alcoholic extract in a drop of blood on a microscopic slide, a haemolytic zone surrounding the drug is formed.

Uses

  • Quillaia bark is used as an emulsifying agent, for coal tar emulsion, cleaning industrial equip ments, washing delicate fabrics, to prepare tooth powders, tooth pastes, hair shampoos, hair tonics, tar solutions and metal polishes. It is added in topical preparations for skin disorders, and as a protective agent for cracks, bruises, frostbite and insect bites. The drug is highly irritating and causes nausea and is expectorant on internal consumption. It is diuretic and a cutaneous stimulant.

GOKHRU

Synonym

  • Caltrops fruit.

Biological Source

  • In Ayurveda two types of Gokhru are used, that is, Bada and Chota Gokhru. The smaller or Chhota Gokhru is the dried ripe seeds of Tribulus terrestris Linn., belonging to family Zygophyllaceae.

Geographical Source

  • The plant is an annual, prostrate herb growing throughout India upto 3,500 m in Kashmir.

Characteristics

  • The fruits are yellowish in colour, globose, 1.2 cm in diameter containing five woody, densely hairy, spiny cocci. Large pointed spines are present in each coccus. Two smaller and shorter spines are directed downwards. Several seeds are present in each coccus.

Microscopy

  • Fruit section shows small rectangular epidermal cells of each coccus. Unicellular trichomes are found on the surface;

  •  6–10 layers of large parenchymatous cells forms mesocarp, next to mesocarp three to four compact layers of small cells are present which contains rosette of calcium oxalate crystals.

Chemical Constituents

  • The dried fruits of T. terstris consist of steroidal saponins as the major constituents. It includes terestrosins A, B, C, D and E, desgalactotigonin, F-gitonin, desglucolanatigonin and gitonin. The hydrolysed extract consists of sapogenins such as diosgenin, chlorogenin, hecogenin and neotigogenin. Certain other steroidal such as terestroside F, tribulosin, trillin, gracillin, dioscin have also been isolated from the aerial parts of the herb. The flavonoid derivatives reported from the fruits includes tribuloside and number of other glycosides of quercetin, kaempferol and isorhamnetin. It also consists of common phytosterols, such as, β-sitosterol, stigmasterol and cinnamic amide derivative, terestiamide.

Uses

  • The fruit has cooling, antiinflammatory, antiarthritic, diuretic, tonic, aphrodisiac properties. It is used in building immune system, in painful micturition, calculus affections and impotency. Improves and prolongs the duration of erection. It exerts a stimulating effect on reproductary organs.

Marketed Products

  • It is one of the ingredients of the preparations known as Bonnisan, Confido, Himplasia, Renalka (Himalaya), Dhatupoushtik churna (Baidyanath), Semento (Aimil) and Body plus capsule (Jay Pranav Ayurvedic Pharmaceuticals).

SARSAPARILLA

Synonyms

  • Smilax Medica, Red-bearded Sarsaparilla, Radix sarsae, Radix sarsaparillea, Jamaica sarsaparilla.

Biological Source

It consists of dried roots of Smilax ornata Hooker., belonging to family Liliaceae.

Characteristics

  • This plant derived its name from being exported to Europe through Jamaica. The word Sarsaparilla comes from the Spanish Sana, meaning a bramble, and parilla, a vine, in allusion to the thorny stems of the plant.

  • It is a large perennial climber, the drugs are found bundles in the market, each bundles consists of numerous long slender roots 3 mm in thickness. They are dark red to brown in colour. They are shrunken and furrowed longitudinally and bear numerous root lets. They are tough and flexible difficult to break. It is odourless and slight bitter in taste.

Chemical Constituents

  • The main constituent is a saponin glycoside, sarsaponin which on hydrolysis yields sarsasapogenin and dextrose. It also contains a small proportion of starch, sarsapic acid, and fatty acids, palmitic, stearic, behenic, oleic and linolic.

Other Species

  • Smilax officinalis (Native Jamaica Sarsaparilla) is obtained from the same place and it could be distinguished by colour, size and other characters. It has a twining stem, angular and prickly; young shoots unarmed; leaves ovate, oblong, acute, cordate, smooth, 1 foot long; petioles 1 inch long, having tendrils above the base. It consists of very long roots, with a thick bark, grey or brown colour. The roots bear scattered, stout rootlets. It is odourless and has mucilaginous taste.

Marketed Products

  • It is one of the ingredients of the preparation known as Purodil Capsules and Syrup (Aimil Pharmaceuticals).

 CYANOGENIC GLYCOSIDES

  • These are the glycosides which on hydrolysis yields hydrocynic acid (HCN), benzaldehyde and sugars. The medicinal activity of cyanogenetic glycosides is due to presence of hydrocyanic acid and these are the characteristics of family rosaceae. For examples Amygdalin obtained from bitter almond (Prunus amygdalus), Prunasin obtained from wild cherry bark.

Identification Tests

  • A strip of white filter paper is dipped in 10% aqueous solution of picric acid, drain it and dip in a 10% sodium carbonate solution and drain again. Moisten the powdered drug with water and put into a conical flask. Trap the sodium picrate paper on the neck of flask with cork. Because of volatile hydrocyanic acid, the paper will become brick red colour.

  • When drug treated with 3% aqueous solution of mercurous nitrate reduction to metallic mercury takes place.

ALMOND

Biological Source

  • Almond oil is a fixed oil obtained by expression from the seeds of Prunus amygdalus (Rosaceae) var. dulcis (sweet almonds), or P. amygdalus var. amara (bitter almonds).

Geographical Source

  • The oil is mainly produced from almonds grown in the countries bordering the Mediterranean (Italy, France, Syria, Spain and North Africa) and Iran.

Characteristics

  • Almond trees are about 5 m in height. The young fruits have a soft, felt-like pericarp, the inner part of which gradu ally becomes sclerenchymatous as the fruit ripens to form a pitted endocarp or shell. The shells, consisting mainly of sclerenchymatous cells, are sometimes ground and used to adulterate powdered drugs.

Chemical Constituents

  • Both varieties of almond contain 40–55% of fixed oil, about 20% of proteins, mucilage and emulsin. The bitter almonds contain in addition 2.5–4.0% of the colourless, crystalline, cyanogenelic glycoside amygdalin. Almond oil is obtained by grinding the seeds and expressing, them in canvas bags between slightly heated iron plates. The oil is clarified by subsidence and filtration. It is a pale yellow liquid with a slight odour and bland nutty taste. It contains olein, with smaller quantities of the glycosides of linoleic and other acids. Bitter almonds, after maceration on hydrolysis of amygdalin yield a volatile oil that is used as a flavoring agent. Sweet almonds are extensively used as a food, but bitter almonds are not suitable for this purpose.

Uses

  • Expressed almond oil is an emollient and an ingredient in cosmetics. Almond oil is used as a laxative, emollient, in the preparation of toilet articles and as a vehicle for oily injections. The volatile almond oils are used as flavouring agents.

Marketed Products

  • It is one of the ingredients of the preparations known as Baidyanath lal tail (Baidyanath Company), Himcolin gel, Mentat, Tentex Royal (Himalaya Drug Company) and Sage badam roghan (Sage Herbals).

WILD CHERRY BARK

Synonyms

  • Virginian Prune, Black Cherry, Virginian Bark, Cortex Pruni.

Biological Source

  • Wild cherry bark is the dried bark of Prunus serotina Ehrhart., belonging to family Rosaceae.

Geographical Source

  • North America generally, especially in Northern and Central States.

Cultivation and Collection

  • This tree grows from 50 to 80 feet high, and 2–4 feet in diameter. The bark is collected in autumn from young branches and stem. In some cases cork and cortex are removed after collection, by peeling. If the bark is peeled it is called rossed bark and if not peeled, it is unrossed barks. It is carefully dried and preserved in airtight containers.

Characteristics

  • The bark is black and rough and separates naturally from the trunk. Leaves deciduous, 3–5 inches long, about 2 inches wide, petioles have two pairs of reddish glands, they are obovate, acuminate, with incurved short teeth, thickish and smooth and glossy on upper surface; flowers bloom in May, and are white, in erect long terminal racemes, with occasional solitary flowers in the axils of the leaves.

Uses

  • Astringent tonic, pectoral, sedative and expectorant. It has been used in the treatment of bronchitis of various types. It is valuable in catarrah, whooping cough, and dyspepsia.

ISOTHIOCYNATE GLYCOSIDES

  • These are sulphur-containing compounds rich in family cruciferae, also known as glucosinolates and on hydrolysis yields isothiocyanate (-NCS) group. These glycosides are generally irritant and hence used externally as counter irritant, for example, Sinigrin from black mustard, sinalbin from white mustard and gluconapin from rapeseed.

MUSTARD

Description

  • It is yellow coloured liquid of strong acrid odour until refined, sp. gr. 0.914–0.923, saponification value 173–184, iodine value 96–194 and unsaponifiable matter 0.9–1.0%.

Uses

  • Fixed oil is used as edible oil after refining, but medicinal properties are due to allyl isothiocynate, which is a local irritant and emetic. If applied externally, it is rubefacient and vasicant. It is also used as condiment and in manufacture of soap. Refined mustard oil is used in vegetable ghee.

Marketed Products

  • Dabur Mustard oil is the one of the purest mustard oil that has a variety of uses. It is also one of the ingredients of the preparation known as Saaf Organic Eraser Body Oil.

FLAVONE GLYCOSIDES

  • These are complex organic compounds containing phenylbenzopyrone ring system. Flavones are present in plants in a free state or in glycosidal state (O-glycoside or C-glycoside) with its different derivatives like flavane, flavonol, flavonone, isoflavone and chalcones, for example, Rutin, quercitrin, hyperoside, diosmin (buchu leaf), hesperidin (lemon and orange peel) and vitexin (Carategus).

GINKGO

Biological Source

  • The leaves of Ginkgo are obtained from the dioeceous tree Ginkgo biloba, belonging to family Ginkgoaceae.

Geographical Source

  • It is a native to China and Japan and cultivated ornamentally in many temperate regions.

Characteristics

  • The leaves are bilobed, each lobe being triangular in outline with a fine radiating, fan-like venation. The leaf is glabrous, petiolate and has an entire margin.

Chemical Constituents

  • The diterpene lactones and flavonoids possess therapeutic activity. Five diterpene lactones (ginkgolides A, B, C, J, M) have been characterized; these have a cage structure involving a tertiary butyl group and six 5-membered rings including a spirononane system; a tetrahydrofuran moiety and three lactonic groups. These compounds are plateletactivating factor (PAF) antagonists and as they do not react with any other known receptor, their effect is very specific. A tertiary butyl group is present in the sesquiterpene bilobalide; no PAF-antagonist activity has been demonstrated for this compound.

  • About 40 flavonoids have now been isolated from the leaves including glycosides of kaempferol, quercetin and isorhamnetin derivatives. The tree also synthesizes a number of biflavonoids based on amentoflavone.

Uses

  • Ginkgo is used as an antiasthmatic and bronchodilator. Extracts of the leaf containing selected constituents are used for improving peripheral and cerebral circulation in those elderly with symptoms of loss of short-term memory hearing and concentration; it is also claimed that vertigo, headaches, anxiety and apathy are cured.

COUMARIN AND FURANOCOUMARIN GLYCOSIDE

  • In these type of glycosides the aglycone is coumarin. Coumarin is a chemical compound found in many plants, notably in high concentration in the tonka bean, woodruff, and sweet grass. They are benzopyrone derivative have aromatic smell and their alcoholic solutions when made alkaline show blue or green fluorescence. The biosynthesis of coumarin in plants is via hydroxylation, glycolysis and cyclization of cinnamic acid.
  • It has clinical value as the precursor for several anticoagulants, notably warfarin. Some naturally occuring coumarin derivatives include umbelliferone (7-hydroxycoumarin), herniarin (7-methoxy-coumarin), psoralen and imperatorin. Coumarins have flavouring property but they cause damage to liver. Coumarin drugs also cause drug interactions with many other drugs. Medicinally, coumarin glycosides have been shown to have hemorrhagic, antifungicidal and antitumor activities.
  • It has clinical value as the precursor for several anticoagulants, notably warfarin. Some naturally occuring coumarin derivatives include umbelliferone (7-hydroxycoumarin), herniarin (7-methoxy-coumarin), psoralen and imperatorin. Coumarins have flavouring property but they cause damage to liver. Coumarin drugs also cause drug interactions with many other drugs. Medicinally, coumarin glycosides have been shown to have hemorrhagic, antifungicidal and antitumor activities.

Characteristics

  • Fruits are 22.5 mm long and 0.5–1.7 mm broad. Ammi majus fruits can be distinguished by the presence of four prominent secondary ridges and by the absence of lacuane outside the vascular bundles, seen in the transverse section of Ammi visnaga. Odour, slightly aromatic, terbenthinate; taste, strongly pungent and slightly bitter.

PSORALEA

Characteristics

  • The plant is an annual herb attending to a height of 60 cm to 1 m. The plant contains prominent grooves of glands and white hairs on the stem and branches. Fruits are very small 3–4.5 mm long and 2–3 mm broad. Fruits are dark chocolate to black in colour with pericarp attached to seeds. Fruits are ovate, oblong or bean shaped, compressed, glabrous rounded or mucronate and pitted. Seed is produced from campylotropous ovule and are kidneyshaped, 2–4 mm long, 2–3 mm broad, smooth, exalbuminous with straw coloured hard testa. Fruit has no smell, taste is bitter, acrid and unpleasant.

ALDEHYDE GLYCOSIDES

VANILLA 

Cultivation and Collection

  • The plant is usually propagated by means of cuttings and, after two or three years, reaches the flowering stage. The cuttings attach to trees (e.g. Casuarina equisetifolia) where they strike roots on the bark; it continues to bear fruit for 30 or 40 years. The flowers, approximately 30 on each plant, are hand pollinated, thus producing larger and better fruits. The fruits are collected as they ripen to a yellow colour, 6–10 months after pollination, and are cured by dipping in warm water and repeated sweating between woolen blankets in the sun during the day and packing in wool-covered boxes at night. The characteristic colour and odour of the commercial drug are only developed as a result of enzyme action during the curing. Curing consists of slow drying in sheds with carefully regulated temperatures. This requires about 2 months, during which the pods lose from 70 to 80% of their original weight and take on the characteristic colour and odour of the commercial drug. The pods are then graded, tied into bundles of about 50–75, and sealed in tin containers for shipment.

PHENOL GLYCOSIDES

BEARBERRY

Characteristics

  • Leaves are spatula like, 2–2.5 cm in size tapering towards base, with short stalk or petiole. Fruits are scarlet red with calyx at base. The leaves are collected in April to June and dried under sun. They show olive green upper surface and pale colour on lower surface. They are small coriaceous, shining leaves. They have .astringent and bitter taste, without any specific odour.

Use

  • The leaves have diuretic and astringent properties. As an infusion, it is used in urethritis and cystitis.

STEROIDAL GLYCOSIDES

SOLANUM

Cultivation and Collection

  • In view of its solasodine content, it has commercial significance. Solasodine, a steroidal glycoalkaloid, has similar applications as that of diosgenin. The cultivation of this plant is scientifically studied and the observations of those trials are given here in brief. The seeds are used for propagation, either through nursery beds or by direct broadcasting. In February, the seeds are sown in nursery beds. The seed beds are covered with sand or farmyard manures and weeding is done periodically. When the seedlings show sufficient growth, they are transplanted into open fields. The raising in nurseries is preferred to direct broadcasting. The plant grows in various climatic and agricultural conditions. The well drained soil and sunny atmosphere are preferred. The seedlings are transplanted in moist soil at 50 x 50 cm distance. Urea, potash and superphosphate are given as fertilizers. In the initial period, irrigation is done once in a week and then in later stages as per requirement. After 6 months, the plants are harvested for collection of berries. They are immediately dried in shade or artificially at low temperature to reduce the large content of moisture.

Characteristics

  • It bears yellowish to greenish berries which are globose and 2.5 cm in diameter with compressed smooth brown seeds.

Chemical Constituents

  • The berries contain about 3% of steroidal glycoalkaloid called solasodine. A new glycoalkaloid solakhasianin having rhamnose and galactose as sugar components have been isolated. Mucilage surrounding part of the seeds contain highest amount of alkaloid. Immatured and over-ripe fruits contain negligible content of alkaloid, while it is maximum when fruits change colour from green to yellow. Colour change of fruits takes place about two months after setting the fruits to the plants. The berries also contain 8–10% of greenish-yellow fixed oil.

Uses

  • Solasodine is used as a precursor for steroidal synthesis. Like diosgenin, it is first converted to 16-dehydro-pregnenelone acetate. The latter is a precursor for steroids, like corticosteroids, pregnane and androstanes. All of these are useful as sex hormones, oral contraceptives, etc. 

BITTER AND MISCELLANEOUS GLYCOSIDES

  • Bitter glycosides are a class of compounds that plays an important role in the digestive process. Bitter drugs and bitter constituents are used since a very early period as stomachics, febrifuges, and bitter tonics and in digestive disturbances.
  • The bitterness of food on the tongue plays a very important role as the taste of bitter foods stimulates the appetite and triggers the secretion of digestive juices in the stomach, which in turn improves the break down of food. Bitters begin by stimulating the taste buds. This triggers off a reflex nerve action which increases the flow of saliva and stomach enzymes. At the same time, the hormone gastrin is secreted by the walls of the stomach. This improves the digestive process, by improving the passage of food from the stomach to the intestines. The sum total of this is an improvement in the digestive function of the stomach and small intestines. Bitters can also be very useful to improve immune disorders resulting from food intolerance or dietary antigen leakage, protect gut tissue (by increasing the tone of the gastro-esophageal sphincter thereby preventing reflux of corrosive stomach contents into the esophagus in ‘heart burn’, hiatus hernia, or esophageal inflammation), promote bile flow (thereby providing for increased ability of the liver to remove a toxic load from incomplete digestion and also provide for better digestion in the duodenum and small intestine), and enhance pancreatic function (normalizing hormone secretions to moderate excessive swings in blood–sugar levels).


PHENOL GLYCOSIDES

BEARBERRY

Characteristics

  • Leaves are spatula like, 2–2.5 cm in size tapering towards base, with short stalk or petiole. Fruits are scarlet red with calyx at base. The leaves are collected in April to June and dried under sun. They show olive green upper surface and pale colour on lower surface. They are small coriaceous, shining leaves. They have .astringent and bitter taste, without any specific odour.

Chemical Constituents

  • The leaves contain a glycoside called arbutin which contains phenolic aglycone. The leaves also contain methyl arbutin, quercetin, ursone, iriodoids, quinones, tannins (6–10%), gallic acid ursolic acid, α-amyrin, β-amyrin and terpenoids.

Uses

  • The leaves have diuretic and astringent properties. As an infusion, it is used in urethritis and cystitis.

STEROIDAL GLYCOSIDES

SOLANUM

Cultivation and Collection

  • In view of its solasodine content, it has commercial significance. Solasodine, a steroidal glycoalkaloid, has similar applications as that of diosgenin. The cultivation of this plant is scientifically studied and the observations of those trials are given here in brief. The seeds are used for propagation, either through nursery beds or by direct broadcasting. In February, the seeds are sown in nursery beds. The seed beds are covered with sand or farmyard manures and weeding is done periodically. When the seedlings show sufficient growth, they are transplanted into open fields. The raising in nurseries is preferred to direct broadcasting. The plant grows in various climatic and agricultural conditions. The well drained soil and sunny atmosphere are preferred. The seedlings are transplanted in moist soil at 50 x 50 cm distance. Urea, potash and superphosphate are given as fertilizers. In the initial period, irrigation is done once in a week and then in later stages as per requirement. After 6 months, the plants are harvested for collection of berries. They are immediately dried in shade or artificially at low temperature to reduce the large content of moisture.

Characteristics

  • It bears yellowish to greenish berries which are globose and 2.5 cm in diameter with compressed smooth brown seeds.

Chemical Constituents

  • The berries contain about 3% of steroidal glycoalkaloid called solasodine. A new glycoalkaloid solakhasianin having rhamnose and galactose as sugar components have been isolated. Mucilage surrounding part of the seeds contain highest amount of alkaloid. Immatured and over-ripe fruits contain negligible content of alkaloid, while it is maximum when fruits change colour from green to yellow. Colour change of fruits takes place about two months after setting the fruits to the plants. The berries also contain 8–10% of greenish-yellow fixed oil.

Uses

Solasodine is used as a precursor for steroidal synthesis. Like diosgenin, it is first converted to 16-dehydro-pregnenelone acetate. The latter is a precursor for steroids, like corticosteroids, pregnane and androstanes. All of these are useful as sex hormones, oral contraceptives, etc. 

 BITTER AND MISCELLANEOUS GLYCOSIDES

  • Bitter glycosides are a class of compounds that plays an important role in the digestive process. Bitter drugs and bitter constituents are used since a very early period as stomachics, febrifuges, and bitter tonics and in digestive disturbances. The bitterness of food on the tongue plays a very important role as the taste of bitter foods stimulates the appetite and triggers the secretion of digestive juices in the stomach, which in turn improves the break down of food. Bitters begin by stimulating the taste buds. This triggers off a reflex nerve action which increases the flow of saliva and stomach enzymes. At the same time, the hormone gastrin is secreted by the walls of the stomach. This improves the digestive process, by improving the passage of food from the stomach to the intestines. The sum total of this is an improvement in the digestive function of the stomach and small intestines. Bitters can also be very useful to improve immune disorders resulting from food intolerance or dietary antigen leakage, protect gut tissue (by increasing the tone of the gastro-esophageal sphincter thereby preventing reflux of corrosive stomach contents into the esophagus in ‘heart burn’, hiatus hernia, or esophageal inflammation), promote bile flow (thereby providing for increased ability of the liver to remove a toxic load from incomplete digestion and also provide for better digestion in the duodenum and small intestine), and enhance pancreatic function (normalizing hormone secretions to moderate excessive swings in blood–sugar levels).

Characteristics

  • When fresh, they are yellowish-white externally, but gradually become darker by slow drying. Slow drying is employed to prevent deterioration in colour and to improve the aroma. Occasionally the roots are longitudinally sliced and quickly dried; the drug being then pale in colour and unusually bitter in taste, but this variety is not official.

  • The dried root as it occurs in commerce is brown and cylindrical, 1 foot or more in length, or broken up into shorter pieces, usually 1/2 inch to 1 inch in diameter, rather soft and spongy, with a thick reddish bark, tough and flexible, and of an orange-brown colour internally. The upper portion is marked with numerous rings, the lower longitudinally wrinkled. The root has a strong, disagreeable odour, and the taste is slightly sweet at first, but afterwards very bitter.

Chemical Constituents

  • Gentian contains bitter glycosides. The dried gentian root contains Gentinin and Gentiamarin, bitter glucosides, together with Gentianic acid (gentisin), the latter being physiologically inactive. Gentiopicrin, another bitter glucoside, a pale yellow crystalline substance, occurs in the fresh root, and may be isolated from it by treatment with boiling alcohol. Gentinin, crystalline glycoside is not a pure chemical substance, but a mixture of gentiopicrin and a colouring substance gentisin (gentianine) or gentlanic acid. Gentian contains a bitter trisaccharide, gentianose which on hydrolysis yields two molecules of glucose and one molecule of fructose. The saccharine constituents of gentian are dextrose, laevulose, sucrose and gentianose, a crystallizable, fermentable sugar. It is free from starch and yields from 3 to 4% ash.

PICRORHIZA

Geographical Source

  • The plant is common on the alpine Himalayas from Kashmir to Sikkim between 3,000 and 5,000 m.

Characteristics

  • It is a low, hairy herb with a perennial woody bitter rhizome, 15–25 cm long, covered with dry leaf-bases It occurs as pieces, 2–4 cm long and 0.3–1.0 cm in diameter. Scales at distant intervals are present; frequently small protuberances, which probably represent accessary buds, are observed both at the rhizomes and the stolones. The drug consists of small pieces. Colour is greyishbrown, light, cylindrical, straight or slightly curved, often with remains of aerial stem which is very dark brown and wrinkled longitudinally, upper and lower surfaces bear a few small root scars, numerous scale leaves and thin scars; odour slightly unpleasant; taste very bitter.

Microscopy

  • Transverse section of the rhizome shows cork composed of several layers of uniformly arranged, tightly packed, thinwalled cells. Cork surrounds a broad cortex, composed of thin-walled; mostly irregularly rounded-oval parenchymatous cells and some of them merge into the secondary phloem tissue, which consists of sieve tubes, companion cells and parenchyma. Cambium is narrow and wavy consisting of several layers of compressed cells. The secondary xylem is composed of thick-walled vessels with annular, spiral or reticulate thickening, tracheids and fibres. Pith is composed of thin-walled parenchymatous cells.

CHIRATA

Characteristics

  • It is an annual, about 3 feet high; branching stem, Upper part of the stem is yellow to brown, thinner and 2 mm broad. The lower part is purplish or brown to dark brown; 6 mm broad cylindrical and exfoliated at some places showing dull wood. Leaves are smooth entire, opposite, very acute, lanceolate dark brown upto 8 cm long, 1.5–2 cm broad. Flowers numerous; peduncles yellow; one-celled capsule. Rhizome is angular to 5 cm long, pale yellow to brown in colour and covered with dense scale leaves. Root is primary, 5–10 cm long, light brown, oblique somewhat twisted, tapering, longitudinally wrinkled and with transverse ridges. Drug has no odour but taste is very bitter.

QUASSIA

Characteristics

  • It is in the form of chips or raspings, Chips are poanoconvex, has no smell but an intense bitter taste. They have false annual rings breaking easily longitudinally. Colour is white, but changes to yellow on contact with the air. Cork easily detaches from phloem. Sometimes black markings are present because of mould.

Microscopy

  • Wood consists of medullary rays, parenchyma and vessels. The whole drug is stained red with phloroglucinol and hydrochloric acid due to the presence of lignin in the cell wall. Medullary rays are one to five seriate but usually triseriate. Cells of medullary rays are radially elongated and their cell walls are pitted. Vessels are thick walled and are border pitted. Fibres are also present in the wood; they are long; tapering, thick walled with oblique shaped pits. Prismatic type of calcium oxalate is present in cells of medullary rays and parenchyma.

Chemical Constituents

  • Quassia contains bitter amaroid compounds like quassin, isoquassin (picrasmin), neoquassin and 18-hydroxy quassin. Volatile oil, gummy extractive pectin, woody fibre, tartrate and sulphate of lime, chlorides of calcium and sodium, various salts such as oxalate and ammoniacal salt, nitrate of potash and sulphate of soda are also present.

KALMEGH

Geographical source

  • It grows abundantly in southeastern Asia: India (and Sri Lanka), Pakistan and Indonesia but it is cultivated extensively in China and Thailand, the East and West Indies, and Mauritius.

Cultivation and Collection

  • It is normally grown from seeds ubiquitously in its native areas where it grows in pine, evergreen and deciduous forest areas, and along roads and in villages. In India, it is cultivated during rainy phase of summer season (Kharif) crop. Any soil having fair amount of organic matter is suitable for commercial cultivation of this crop. About 400 g seed are sufficient for one hectare. The spacing is maintained 30 × 15cm. No major insect and disease infestation has been reported. The plants at flowering stage (90–120 days after sowing) are cut at the base leaving 10–15cm stem for plant regeneration. About 50–60 days after first harvest, final harvest is performed. In Indian condition, the yield varies between 2,000–2,500 kg dry herb/hectare. 

Characteristics

  • The stem is erect, greenish brown, woody, 30–100 cm in height, and quadrangular particularly in the upper regions with four bulges arising on the four corners. The leaves are dark green, lanceolate, with a small winged petiole, 7 cm long, 2–5 cm broad; margin is entire, lamina glabrous, apex acuminate, slightly waxy and base tapering. The midrib varies in outline at different regions of the leaf. Stem branching is profuse which bears small arid solitary flowers. The dried drug is odourless and taste is extremely bitter.

Chemical Constituents

  • The plant possesses kalmeghin, a bitter crystalline diterpene lactone, such as, andrographolide flavonoids and phenols. The lactones isolated from Kalmegh are andrographolide, 14-deoxy-ll-oxo-andrographolide, 14-deoxy-11, 12-didehydroandrographolide, 14-deoxyandrographolide and neoandrographolide. 
  • The leaves contain β-sitosterol glucoside, caffeic, chlorogenic and dicaffeoyl-quinic acids, carvacrol, eugenol, myristic acid, hentriacontane, tritriacontane, oroxylin A, wogonin, andrograpanin, 14-deoxy-12-methoxyandrographolide, andrographidines A-F and stigmasterol.

Uses

  • Kalmegh has febrifuge, tonic, alterative, anthelmintic, astringent, anodyne, alexipharmic and cholagogue properties. It is useful in debility, cholera, diabetes, swelling, itches, consumption, influenza, piles, gonorrhoea, bronchitis, dysentery, dyspepsia, fever and in weakness. A decoction of the plant is used as a blood purifier and as a cure for torphid and jaundice. The pills prepared from macerated leaves and certain spices (e.g. Cardamom, Clove and Cinnamon) are given for stomach ailments of infants.

Marketed Products

  • It is one of the ingredients of the preparations known as Purim, Acene-n-pimple cream (Himalaya Drug Company), Herbohep (Lupin Herbal Laboratory), Sage Liverex (Sage Herbals) and Puridil syrup (Aimil Pharma).
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