R.Ramasubramania raja and M.Likitha, M.Sekar, JPRR, 2018; 2:17
Review Article JPRR (2018) 2:17
Journal of Pharmaceutical Research and Reviews (ISSN:2576-8417)
Alkaloids – an overview
R.Ramasubramania raja, M.Likitha, M.Sekar
Department of pharmacognosy, narayana pharmacy college Nellore,A.P
ABSTRACT
Alkaloids are a chemically heterogenous group of natural *Correspondence to Author: substances and comprises more than 6000 basic nitrogen R.Ramasubramania raja containing organic compounds which occur in about 15 percent Department of pharmacognosy, of all vascular terrestrial plants and in more than 150 different narayana pharmacy college Nel- plants families. The alkaloids exhibit diversity of structures lore,A.P and also show an extraordinary spectrum of pharmacological activities. Because of these characters, they are important for chemical, physiological, taxonomic and biogenetic studies. How to cite this article: R.Ramasubramania raja, M.Likitha, Keywords: Alkaloids, organic, spectrum, taxonomic M.Sekar.Alkaloids – an overview. Journal of Pharmaceutical Re- search and Reviews, 2018; 2:17.
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JPRR: http://escipub.com/journal-of-pharmaceutical-research-and-reviews/ 0001 R.Ramasubramania raja and M.Likitha, M.Sekar, JPRR, 2018; 2:17 Introduction : With few exceptions, all the alkaloids are colourless, crystalline solids with a sharp In view of their chemical and physiological melting point or decomposition range. diversity, there is no comprehensive definition Some alkaloids are amorphous gums , of alkaloids . While others like coniine, sparteine, etc..,are The term is derived from the word alkali- like liquid and volatile in nature. and hence , they resemble some of the Some alkaloids are coloured in nature characters occurring complex amines. Eg .,betanidin is red, berberine is yellow and The term alkaloid also covers pseudo proto salts of sanguinarine are copper red in colour. alkaloids and peudoalkaloids. In general, the free bases of alkaloids are In view of all such variations , the only definition soluble in organic non-polar, immiseible that brings all such compounds under one title solvents. is as follows. The salts of alkaloids are soluble in water. These are the organic products of natural or In contrast, free bases are insoluble in water synthetic origin which are basic in natures and and their salts are very sparingly soluble contain one or more nitrogen atoms ,normally organic solvents. of heterocyclic nature, and posses specific The alkaloids containing quaternary bases are physiological actions on human or animal body, only water soluble. when used in small quantities . Some of the pseudoalkaloids and protoalkaloids show higher solubility in water. The true alkaloids are toxic in nature, contain For example, colchicine is soluble in alkaline heterocyclic nitrogen which is derived from water, acid or water and caffeine(free bases) is amino acids and always basic in nature. freely soluble in water. True alkaloids are normally present in plants as Quinine hydrochloride is highly soluble in water salts of organic acids . i.e 1 part of quinine hydro chloride is soluble in The proto alkaloids or amino alkaloids are less than 1 part of water,while only 1 part of simple amines in which the nitrogen is not in a quinine sulphate is soluble in 1000 parts of hetrocyclic ring. water. Some times, they are considered as biological The solubility of alkaloids and their salts is amines . useful in pharmaceutical industry for the They are basic in nature and prepared in plants extraction and formulation of final from amino acids. pharmaceutical preparations Some of the examples of these alkaloids are CHEMICAL PROPERTIES : mescaline, N, N – dimethyl tryptamine Most of the alkaloids are basic in reaction, due ,colchicne, ephedrine. to the avaliability of lone pair of electrons on The term pseudoalkaloids includes mainly nitrogen. steroidal and terpenoid alkaloids and purines. The basic character of the alkaloidalcompound is enhanced if the adjacent functional groups They are not derived from aminoacids . are electron withdrawing like amide group They do not show many of the typical which reduces the availability of the lone pair of characters of alkaloids, but give the standard electrons. qualitative tests for alkaloids. But, alkaloids exhibiting basic character are PROPERTIES: very much sensitive to decomposition and Physical Properties: cause a problem during their storage. Their salt formation with an inorganic acid prevents many a time decomposition. JPRR: http://escipub.com/journal-of-pharmaceutical-research-and-reviews/ 0002 R.Ramasubramania raja and M.Likitha, M.Sekar, JPRR, 2018; 2:17 The alkaloids may contain one or more number 1).Pharmacological classification : of nitrogen and it may exist in the form as Depending on the physiological response ,the primary ( R – NH 2) , e.g . mescaline ; alkaloids are classified under various secondary amine ( R2 - NH) ,e.g. ephedrine pharmacological categories,like central nervous ;tertiary amine (R3N) e.g. atropine ;and system stimulants are depressants quaternary ammonium compounds ( R4N+X) ,sympathomimetics ,analgesics,purgatives e.g. tubocurarinc chloride. ,etc.This method doesn’t take in to account In the last type,their properties vary from chemical nature of crude drugs .With in the alkaloids , owing to quaternary nature of same drug ,the individual alkaloid may exhibit nitrogen. different action e.g.morphine is narcotic In the natural form, the alkaloids exist either in analagesic , while codeine is mainly antitussive free state, as amine or as salt with acid or .In cinchona,quinine is anti malarial ,while alkaloid N-oxides. quindine is cardiac depressant. CHEMICAL TESTFOR ALKALOIDS: 2).Taxonomy classification: This method claassifes the vast number of -The qualitative chemical tests used for alkaloids based on their distribution in various detection of alkaloids are dependent on the plant families ,likesolanaceous or charecters of alkaloids to give precipitates as papillionaceous alkaloids . Preferably , They salts of organic acids or with compounds of are grouped as per the name of the genus in heavy metals ,like mercury ,gold, platinum,etc. which they occur e.g. ephedra, cinchona,etc. -The different reagents used are MAYERS From this classification, the chemotaxonomic REAGENT(potassium mercuric iodide classification has been further derived . solutions) givingcream coloured precipitate 3).Biosynthetic classification : ;DRAGENDORFFS REAGENTS ( potassium This is the most accepted way of classification bismuth iodide solution ) giving reddish brown of alkaloids . The main criterion for chemical precipitate ; and WAGNERS REAGENT (iodine classification is a type of fundamental (normally –potassium iodide solution ) yielding reddish hetero cyclic ) ring structure is present in brown precipitate .some alkaloids also yellow alkaloid . coloured precipitate with picric acid called as The alkaloid drugs are broadly charecterised in HAGERS REAGENT and picrolonic acid to two divisions . .Individual alkaloid gives colour or precipitate (a ) Hetero cyclic alkaloid (true alkaloids) are with certain specific reagent . divided in to tweleve groups according to nature -The chemical tests with heavy metals or not of their hetero cyclic ring . solely limited to alkaloids .Proteins ,coumarins (b) Non hetero cyclic alkaloids or proto and alpha –pyrones also gives precipitates with alkaloids or biological amines or pseudo these reagants.It may be also noted that some alkaloids. alkaloids do not give such tests ,like caffeine which is highly water soluble . ERGOT: -Hence ,the tests with heavy metals or in some Synonyms: cases false positive reactionsor false negative Ergot of Rye,Ergota. reactions .For this purpose ,the specific testsfor Biological Source: individual alkaloids are more important for qualitative evaluation of crude drugs.These Ergot is the dries sclerotium of a fungus, tests are covered under individual drugs. ClavicepspurpureaTulasne (Clavicipitaceae or CLASSIFICATION OF ALKALOIDS: Hypocreaceae)developed in ovaryof rye The various methods proposed for classification plant,Secale cereal Linne(Graminae).It contains of alkaloids are as follows not less than 0.19 per cent of the total alkaloids
JPRR: http://escipub.com/journal-of-pharmaceutical-research-and-reviews/ 0003 R.Ramasubramania raja and M.Likitha, M.Sekar, JPRR, 2018; 2:17 Name of Active S.No. drug and Constituents Uses synonym 1. Ergot A fungal sclerotium of Ergometrine, Oxytocic, (Ergot of Rye) Clavicepspurpurea in ovary ergotamine prevents postpartum of rye plant Secale cereal. haemorrhage Family of fungus- used in treatment of 2. Nuxvomica Clavicipitaceae; migraine (Crow Fig) Family of rye Graminae strychnine, CNS stimulant, Seeds of Strychnousnux brucine bitter 3. Vinca vomica, ,stomachic, (Catharanthus) Loganiaceae tonic
Entrie plant of vincristine, anticancer Catharanthusroseus, vinblastine (treatment Apocynaceae of Hodgkin`s disease and leukemia)
S.No. Name of drug Biological Active Uses and Source Constituents Synonym 4. Rauwolfia Roots and rhizomes of Rauwolfia reserpine, Hypotensive (Sarpagandha) serpentina, rescinnamine tranquilliser Apocyanaceae
5. Opium Dried latex from the capsules of narcotine, narcotic (Raw opium) Papaversomniferum, papaverine analgesic, Papaveraceae in diarrhoea
Belladonna Dried leaves and flowering tops of Atropa I-hyoscyamine, anti- 6. (Deadly night shade belladonna, atropine spasmodic, leaf) Solanaceae anti- cholinergic
Datura herb Dried leaves and flowering tops of scopolamine, anti- 7. (Angel`s trumpet) daturametel var. fastuosa, hyoscyamine, cholinergic, Solanaceae atropine in deodenal ulcers
8. Cinchona Dried root or stem bark of cinchona quinine, antimalarial, (Peruvian bark) calisaya,C.offi- quinidine, bittertonic. cinalis,C.ledgeriana,C.succirubra,Rubiace cinchonine, ae cinchonidine
9. Vasaka antitussive, (Adulsa) Leaves of Adhatoda expectorant vasica, vasicine and 10. Acanthaceae vasicinone
Coffee stimulant,to counter 11. Dried ripe seeds of Coffeaarabica, caffeine effect over dosage of Rubiaceae trigonelline CNS depressant. Ashwagandha Sedative and also as (Asgandh) anti- rheumatic Dried roots of Withaniasomnifera, 12. Solanaceae withanine, somniferine, C.N.S. stimulant Tea(Thea) withanolide(steroid) Leaves and leaf buds of Theasinensis, Caffeine, Theaceae Theoromine,
Theophylline JPRR: http://escipub.com/journal-of-pharmaceutical-research-and-reviews/ 0004 R.Ramasubramania raja and M.Likitha, M.Sekar, JPRR, 2018; 2:17 of ergot, calculated as ergotoxine,of which not conidiospores,which remain in a suspended less than 15 percent consists of water soluble form in honey-dew. alkaloids of ergot,calculated as ergometrine. Due to the sugary fluid i.e. honey-dew, the Geographical Source: insects and ants are attracted which further Switzerland,Yugoslavia,Hungary and help in the spread of the fungus to other host Czechoslovakia plants.This developmental stage is the sexual stage and called as spread of the fungus to Collection and Preparation of Ergot: other host plants.This developmental stage is -Presently,ergot is produced by natural way i.e. the sexual stage and called as SPHACELIAL cultivation of rye plants and subsequently STAGE. infecting with this fungus,as well as,by artificial The hyphae further invade into the deeper parts way i.e. saprophytic production. of ovary and slowly replace the entire tissue of -For the natural way of production, rye plant is ovary by a compact tissue called host and ergot is a parasite.It is known that pseudoparenchyma which is hard and dark more than 600 plants from different families of purple. It is called as Sclerotium stage and is wild and cultivated grasses act as hosts for considered as resting or dormant stage of the ergot fungus as a parasitic or pathogen. The fungus and contain maximum amount of ergot various other known species of this fungus are alkaloids.If this sclerotium is left uncollected, it C.microcephala,C.nigricans and eventually falls on the ground and in the C.paspali,which can produce ergot.Among all favourable season, i.e. spring gives out the hosts,rye is the better host for the large `stomata’which are in the elongated scale production of ergot by way of quality and form.Eachstromatumhasa globular head and a quantity. stalk.The head portion contains a large number -Among the various stages of development of of perithecia and every perithecium is like a this fungus,sclerotial stage or a dormant stage flask shaped structure which contains a number contains the maximum amount of drug.For a of sacs,each sac containing the ascospores systematic study, it is necessary to know the which are thread like in other development stages of fungus or more appearance.Ascospores are the sexual spores precisely the life history of ergot. capable of inducing fresh life cycle of fungus by Life Cycle of Ergot: infecting the ovary of rye plant. The ovary of the rye plant at its base,gets Selection of a correct strain of infected by ascospores of the fungus in spring fungus(Clavicepspurpurea),appropriate or summer season.The spread of ascospores containers for preparing large scale ergot to ovaries is influenced by wind and inoculum and an ideal nutrient medium are insects.Afterinfecting,theascospores germinate important requirements for commercial in the favourable conditions, like moisture and production of ergot. The various chemical races damp climate.The germination of ascospores of fungus can produce only specific ergot leads to formation of hyphal strands which go alkaloids like on invading the wall of ovary with the help of an ergotamine,ergometrineandergotoxin in enzyme.By this way,the hyphae form a soft, appreciable quantities from their white mass of tissue over the surface of the sclerotia.Theascospores of this species with the ovary which is called as mycelium.The specific chemical race are germinated on mycelium secrets a viscous and sugary fluid nutritive medium and by this way large bulk of called honey-dew.At the same time, the conidiospores are formed.The suspension of hyphalstrands produce asexualspores called this strain of fungus is sprayed on rye plants in large in large cultivated areas. JPRR: http://escipub.com/journal-of-pharmaceutical-research-and-reviews/ 0005 R.Ramasubramania raja and M.Likitha, M.Sekar, JPRR, 2018; 2:17 Apart from field cultivation,other method which Longitudinal furrows and transverse cracks are is much practised is saprophytic production of present on each surface. ergot.This process was initiated in japan by Microscopic Characters: Prof.Abe.Saprophytic production is convenient The outermost layer of the sclerotium is made in many ways as it eliminates the variation in up of few thin,flattened,polygonal cells of purple yield due to weather conditions and production to brown colour,while inner part is made up of can be achieved throughout the year.For this dense pseudo parenchymatous cells method,various strains of ergot are used composedofchitin.Themycelialcells(central depending on the type of ergot alkaloid to be region) are round or oval,thick and with high obtained,Clavicepspaspali gives clavines and refractive walls.They also contain cells with simple lysergic acid derivatives. fixed oil. Sclerotium does not contain It is much easier to manufacture clavines and starch,calcium oxalate or any of the lignified simple lysergic acid derivatives and then tissue. convert them to different peptide alkaloids,i.e. Chemical Constituents: ergot alkaloids.For nutrition of cultureof fungus,specific nutrients are used and Ergot contains large number of fermentation is carried out in temperature range potentindolealkaloids(0.1 to 0.25%),which are of 20-30 degree C and in a pH of 4.6-6.3.The derivatives of lysergic acid.Lysergic acid is fermentation process for these submerged present in its peptide derivative form and hence cultures in shaking flasks or fermenters or the alkaloids are also called as peptide synthesized alkaloidals is done by usual ways alkaloids. The six pairs of alkaloids are broadly applied for other alkaloids.The lysergic acid grouped into water soluble and water insoluble derivatives are converted to lysergic acid categories. Each pair contains laevo-form further partly synthesized into ergometrine and which is medicinally active,whiledextro forms is other peptide alkaloids. inert in action.The water soluble pair contains (- ) ergometrine and its dextro part as The saprophytic production is much practised ergometrinine.The water insoluble group is now-a-days,becausemycelial dry weight gives further divided into Ergotamine and ergotoxine even more than 20 percent of alkaloids,while group. natural sclerotia contain less than 1 percent of alkaloids.The process of fermentation is Besides the alkaloids,ergot also contain properly regulated or controlled for optimum pigments,ergosterol and bioproduction of useful metabolites. fungisterol,histamine,trymine,amino acids, acetyl choline,chitin,upto 30%fixed oil and 8% Macroscopic Characters: moisture. Colour-Externally, it is dark violet Chemical Tests: toblack.Internally,it is whitish or pinkish white. 1)Ergot powder gives a blue colour with p- Odour- Disagreeable and faint. dimethylaminobenzaldehyde(Van-Urk`s Taste- Unpleasant reagent). Size- The sclerotia are 1 to 3 cm in length and 2) Ergot is treated with solvent ether and 1to 5 mm in width. sulphuric acid the filtrate obtained shows red Shape- Sclerotia are fusiform,triangular and violet colour in its aqueous layer, when treated usually tapering on both the ends. with Saturated solution of sodium bicarbonate. Fracture- It is brittle with short fracture. 3) Ergometrine gives a blue fluorescence in EXTRA FEATURES: water. Uses:
JPRR: http://escipub.com/journal-of-pharmaceutical-research-and-reviews/ 0006 R.Ramasubramania raja and M.Likitha, M.Sekar, JPRR, 2018; 2:17 -Ergotamine tartarate is used as a specific -Each fruit contains about 4 to 5 seeds and analgesic in treatment of migraine. heavy bitter pulp.The ripened fruits are -Lysergic acid diethylamide is a semisynthetic collected and seeds are freed of the pulp. derivative,and possesses psychotomimetic -They are washed with water thoroughly. action and used in psychiatry. -Unripened seeds are separated by the floating Storage: test in water.The seeds are dried on mat and -It should be stored in well closed containers. packed in gunny bags for marketing. -Ergot alkaloids are sensitive to light and -The collection of the fruit and seeds is carried temperature. out from November to February. -The drug is stored at low temperature in cool -In India,about 15,000 tonnes of seeds are place away from light. collected annually. Seeds, pure and crude alkaloids of Nux-vomica are reguarly exported NUXVOMICA from India. Synonyms: -Exports of the alkaloids for 1988 – 89 and Crow-fig, Semen strychni,Nux vomica seed. 1989 – 90 are Rs. 407.7 lakhs and Rs. 429.5 Biological Source: lakhs respectively. Nux vomica consists of dried ripe seeds of Macroscopic Character : Strychnosnux vomica Linn., Family Colour: Greenish – brown Loganiaceae. Odour: None It should contain not less than 1.2 percent of Taste: Intensely bitter total alkaloids calculated as strychnine. Size: Seeds are 10 to 30 mm in diameter and 4 Geographical Source: to 6 mm in thickness. It is indigenous to East India and is largely Shape: The seeds are disc shaped, somewhat collected from forests in Sri Lanka,Northern flat or irregularly bent and concavo-convex. Australia and India. Margin of the seeds is rounded. It is found abundantly in South India i.e. in EXTRA FEACTURES- Tamil Nadu, Kerala and on Malabar coast. Surface of the seeds is silky due to the radially It also available in the forests of Bihar, arranged, densely covered, closely appressed Orissa,Konkan, Mysore and Gorakhpur. unicellular lignified covering trichomes.The Collection: presence of endosperm, embryo and -In India, the entire drug is collected from wild cotyledons can be confirmed in the L.S of the grown plants by the local tribal community. seed. -The nux vomica tree is found throughtout the Microscopic Charecters: tropical area,1300 m above the sea level. -The epidermis consists of strongly thickened, -The plants are about 10 to 12 metres in height pitted and lignified trichomes. Epidermis is with a crooked trunk and several branches. followed by a layer of collapsed cells. -The leaves are orange,oppositelyarranged,with -Endosperm is characterised by thick walled oval shape,entire margin and acute apex. polyhedral unlignified cells with plasmodesma, -The flowers are greenish-white and the bark is aleuronegrains and oil globules. greyish to yellow. -Calcium oxalate crystals and starch grains are -Fruits of the plants are orangreyellow,berries absent in drug. of normal size. Chemical Constituents:
JPRR: http://escipub.com/journal-of-pharmaceutical-research-and-reviews/ 0007 R.Ramasubramania raja and M.Likitha, M.Sekar, JPRR, 2018; 2:17 -Nux vomica seeds contain 1.5 to 5% of bitter Biological Source: indolealkaloids.Chief constituents of nux It is the dried whole plant of vomica are strychnine and Catharanthusroseus, belonging to family brucine,whilevomicine, alpha- Apocynaceae. It is aslo known as Vincarosea. colubrine,pseddostrychnine and strychnicine Geographical Source: are also present. It is probably indigenous to Madagascar.It is -Apart from seeds,other parts of the plant cultivated in south contain alkaloids.Seeds also contain 3.0% of Africa,India,U.S.A.,Europe,Australia and fat. Caribbean islands as an ornamental plant,as -Bark contains brucine and traces of strychnine. well as,for its medicinal properties. -Wood and root of the plant also contain Macroscopic Characters: strychininne. The leaves are green,roots are pale -The other minor, but,chemically related grey,flowers are violet pink-white or carmine- alkaloids are isostrychninne,N- red in colour.The odour is characteristic and oxystrychnine,protostrychnine,novacine. taste is bitter.Vivca is an -The nuxvomica also contains a glycoside viz. erect,pubescentherb,with branched tap- loganin,chlorogenic acid and fixed oil. root.Leaves are Chemical Tests: simple,petiolate,ovate,oroblong,unicostate,retic ulate,entire,brittle with acute apex and glossy The thin sections of nux vomica seed are appearance.Flowers are defatted and the following tests are performed. bractate,pedicellate,complete,hermaphrodite,no 1) Stain the transverse section of nux rmally 2 to 3 cm in cymoseasillaryclusters.Fruits vomica with ammonium vanadate and are follicles with several black seeds. sulphuric acid Manddin`sreagent.The Macroscopic Characters: endospermic cells because purple due to the presence of strychnine. Upper surface shows presence of single layer 2) Stain the transverse section of nux of rectangular celled epidermis with unicellular vomica with concentrated nitric covering trichomes.Palisade is made up of acid.Endospermic cells take yellow single layer beneath upper epidermis and colour due to the presence of brucine. contains compact elongated cells.Spongy 3) Srychnine with sulphuric acid and parenchyma is 5 to 8 layered with intercellular potassium dichromate gives violet spaces.Midrib shows presence of collenchyma colour which turns to red and finally below the upper epidermis and above the lower yellow. epidermis.Xylem and phloem are present in the centre.Cruciferous stomata are present more Uses: frequently on lower epidermis.Calcium oxalate -Due to its bitter taste, nux vomica is used as crystals are absent. bitter stomachic and tonic. Chemical Constituents: -It is astimulant to central nervous system. A large number of indole alkaloids are present -It increases the blood pressure and is in vinca.Out of them,about 20 dimericindole- recommended in certain forms of cardiac dihydroindole alkaloids failure. possesoncolyticactivity,andamomgthem,vincrist VINCA ine and vinblastine are most Synonyms: significant.Vinblastine contains indole alkaloid Catharanthus, periwinkle. part called catharanthine and dihydroindole alkaloid part called vindoline.The other JPRR: http://escipub.com/journal-of-pharmaceutical-research-and-reviews/ 0008 R.Ramasubramania raja and M.Likitha, M.Sekar, JPRR, 2018; 2:17 alkaloids present in vinca are Pradesh, Bihar, Orissa, Tamil Nadu, West ajmalicine,lochnerine,serpentine and Bengal, Karnataka, Maharashtra, and Gujarat. tetrahydroalstonine.It requires about 500 kg Cultivation and Collection: crude drug to extract out 1 g of vincristine, Under wide range of climate conditions, because of its extreme low content,viz.0.0002 rauwolfia grows luxuriantly. However, it per cent. This makes these alkaloids very flourishes in hot humid condition and grows costlier and hence,the efforts for their synthesis satisfactorily in shade.In wild state, it grows in are under attempts.From their structure, the variety of solis. But for cultivation, clay loamy five-ring dihydroindole system is present in few soil with large amount of humus and good other natural drugs. Therefore, the attempts drainage are supposed to be ideal. The pH of towards the synthesis of four-ring indole system the soil should be acidic and around 4. The are going on presently. Such two systems can temperature range for cultivation is 10 degree be further coupled. to 38 degree Centigrade.Rainfall should be in Uses: the range of 250- 500 cm. Soils containing -Vinca is used to extract vincristine,vinblastine large amount of sand make the plants more and ajmalicine. susceptible to diseases. -Vincristine sulphate is an antineoplastic agent In can be propagated by various methods, such which may act by arresting mitosis at the as by seeds, roots, cutting,root stumps, etc. metaphase. It is given intravenously in the The propagation from seeds is usually the treatment of acute-leukemia of children; some method of choice. The healthy seeds are sown childhood leukemias are also responded. into the nursery beds. The rate of germination -Vinca also exhibits hypotensive and anti- of seeds is very low, hence sufficient quantity of diabetic actions. the seeds are sown. Sowing is done in the month of May or at the break of monsoon. The Dose: seedlings are then transplanted in the month of 1)Vincristine sulphate:10 to 30 ug/kg of body August at a distance of 16 to 30 cm. The plants weight intravenously,but maximum upto 2 mg are provided with various chemical fertilizers 2)Vinblastine sulphate : 100 ug/kg body weight and manures. The chemical fertilizers include intravenously. ammonium sulphate, urea; while the manures SERPGANDHA include, generally, the bone-meal. The plants Synonyms: are kept free from weeds. When the plants are about 3 to 4 years old, they are uprooted. The Rauwolfia root, Serpentina root, Chhotachand roots are cut properly, washed so as to remove Biological Source: the earthy matter and dried in air. Rauwolfia consists of dried roots of the known It needs abot 5 kg of seeds to produce the as RauwolfiaserpentiaBenth, belonging to seedlings sufficient to cover the area of one family Apocynaceae.Serpgandha contains not hectare after transplantation.The average yield less than 0.15 % of reserpine and ajmalcine, of roots per hectare is 1200 kg. It may vary, calculated on dried basis. depending upon the soil, climatic conditions Geographical Source: and age of the plant. Several species of Rauwolfia are found Macroscopic Characters: distributed in the tropical regions of Asia, Colour – Root bark is greyish yellow to brown America and Africa.Commercially, it is and wood, pale yellow. produced in India, srilanka,Myanmar,Thailand Odour – Odourless and America. In India, it is cultivated in Uttar Taste – Bitter JPRR: http://escipub.com/journal-of-pharmaceutical-research-and-reviews/ 0009 R.Ramasubramania raja and M.Likitha, M.Sekar, JPRR, 2018; 2:17 Size – About 10 to 18 cm long and from 1 to 3 rescinnamine, reserpine, yohimbine, serpentine cm diameter. and reserpate and trimethoxybenzoic acid in Shape – Roots are sub-cylindrical, slightly reserpine and trimethoxycinnamic acid in case tapering, tortuous. of rescinnamine. Syrosingopine is methyl carbethoxysyringoylreserpate. Fracture is short and irregular. The transversely cut surface is white, dense with finely radiating Reserpine like alkaloids arecolorimetrically xylem. determined by reaction between acidic solution of alkaloids and sodium nitrite. Extra Features:
Roots are rough with longitudinal marking and slightly wrinkled surface. Rootlets are usually Chemical Tests: absent, but few small circular root scars with (1) A red coloration along the medullary tetrastichous arrangements are seen. rays is observed when the freshly Microscopic Characters: fractured surface is treated with concentrated nitric acid. The cork is made up of stratified cells followed (2) Reserpine shows violet red colour by phelloderm of few rows of parenchyma. when treated with solution of vanillin Phloem is narrow, parenchymatous with small in acetic acid. scattered sieve tissue. Parenchyma contains (3) Powdered ranwolfia when treated with starch grains and few latex cells, with brown sulphuric acid and p-dimeeghyl resinous matter.Secondary phloem contains amines benzaldehyde, develops violet calcium oxalate crystals. Xylem is about 4/5 th to red colour.(Test is for modle of the diameter of the root and consists of alkaloids). vessels, tracheids, wood parenchyma and wood fibres. Xylem vessels are elongated upto Uses: 350 u in length and 50 u in width and contain Rauwolfia is antihypertensive in activity. simple or bordered pits. Stone cells and phloem Among the various alkaloids of rauwolfia, fibres are absent. reserpine, rescinnamine and ajmalicine are Chemical Constitutents: clinically important. About 30 indole alkaloids have been reported in Rescinnamine is used as antihypertensive, but drug and total alkaloidal content of rauwolfia it causes mental depression in higher doses. roots ranges from 0.7 to 3%, depending upon Deserpidine is used as antihypertensive and the source. Alkaloids are concentrated mostly tranquilliser. It shows very less side effects. in the bark of the roots. The alkaloids of Ajmalicine, though less in quantity, has the rauwolfia are broadly classified into the uses in treatment of circulatory diseases,inrelief following types, of obstruction of normal cerebral blood flow. (1) Indole alkaloids, Syrosingopine shows peripheral effects similar (2) Indoline alkaloids, to reserpine. It has less sedative actions and it (3) Indolenine alkaloids, is used for the treatment of mild or moderate (4) Oxyindole alkaloids and hypertension. (5) Pseudo indoxyl alkaloids Dose: The important alkaloid of rauwolfia is resperine. Apart from the alkaloids, it also contains oleo- Rauwolfia : 100 to 150 mg ( oral twice daily) resin, phytosterol, fatty acids, alcohol and Reserpine : Initial dose 250 ug once a day sugars. The other alkaloids present in the drug (oral) are ajmaline, ajmaline, rauwolfinine,
JPRR: http://escipub.com/journal-of-pharmaceutical-research-and-reviews/ 0010 R.Ramasubramania raja and M.Likitha, M.Sekar, JPRR, 2018; 2:17 Rescinnamine : 500 ug oral twice a day ( initial Being a potent narcotic drug, the cultivation and dose); 250 ug oral daily maintenance dose. other aspects of opium are governed by OPIUM respective in different countries, including India. In India, all the activities about opium and its Synonym: derivatives are controlled under narcotic drugs Raw opium and psychotropic substances act, 1985. Biological Source: The genus Papaver has 50 different species, of It is the dried latex obtained by incision from the which six species are found in India, viz. unripe capsules of Papaversomniferum Linn., P.somniferum(Opium poppy), P. nudicaule dried or partly dried by heat or spontaneous (Iceland poppy), P.rhoeas(corn poppy), evaporation, and worked into somewhat P.orientale, P.argemone, and P.dubium. irregulary shaped masses ( natural opium) or Poppy is an erect plant attaining 60-120 cm moulded into masses of more uniform size and height. It is rarely branched. The leaves are shape (manipulated opium).Poppy plant linear, oblong or ovate oblong and have a belongs to family Papaveraceae. It contains not dentate or serrate margin. It bears bluish white, less than 10 percent of morphine, and not less purple or violet coloured large flowers. than 2.0% of codeine, both calculated as Accordingly, the varieties anhydrous morphine. P.somniferumvar.glabrum, P.somniferum var. Geographical Source: album, P.somniferumvar.nigrum are India, Pakistan, Afghanistan, Turkey, Russia, described.The second variety is cultivated in China, and Iran. india. Indian opium is considered as the only History: legal source of opium to many countries including united states of America and Britain. Opium has been known to mankind since centuries due to its narcotic properities. It was In India, about 54 thousand hectares of land is first cultivated in Mediterranean regions and under opium poppy cultivation.It is under probably brought by Alexander in 327 B.C. to government control, and cultivation of poppy is India. It is known that Dioscorides and restricted to Madhya Pradesh, Rajasthan and Theophrastus were aware of the medicinal Uttar Pradesh. properties of opium. The weather conditions affect,upto a large The earliest written record about opium is extent, the yield of opium. Although, temperate revealed from Historiaplantarum(some where in climate is the natural requirement of opium 300 B.C.) and De MateriaMedica (78 A.D.). poppy, it can be grown with success under Narcotine was the first alkaloid reported both subtropical climate in winter season, as there is from opium and among alkaloidal series, to be a favourable effect on yield by cold weather. isolated in 1803 by Derosne. But, extreme cold conditions, including frost, adversely affect the plant and ultimately yield of Segnin isolated morphine in 1804.Magendi and opium. In short, the best climatic conditions for Bally first introduced it in medical practise in opium poppy are cool weather freezing 1818.Gulland and Robinson elucidated the temperature and cloudiness, and sufficient structure of morphine in 1923.In 1833, Robiquet sunshine. isolated codeine from opium, and in 1881, Grimaux reported that codeine is o-methyl Opium poppy is grown from November to derivative of morphine.Merck company isolated March. Propagation is done by sowing the papaverine in 1848. seeds, for which 3-4 kg of seeds per hectare are necessary. The seeds admixed with about Cultivation, Collection and Preparation: 3-4 parts of sand are sown. Opium poppy
JPRR: http://escipub.com/journal-of-pharmaceutical-research-and-reviews/ 0011 R.Ramasubramania raja and M.Likitha, M.Sekar, JPRR, 2018; 2:17 requires, highly fertile, well drained loamy soil cover the industrial method for extraction of with fine sand.The soil should contain organic alkaloids of opium. matter, nitrogen and should have a PH around Macroscopic Characters: 7. Colour : strong characteristic The distance between two plants maintained is Taste:bitter usually 25 cm and the plant reaches maximum height of one metre. 1. Indian opium – Dark brown in colour. It is found in the form of cubical pieces weighing Periodically, the thinning of plants is done to get about 900 g for marketing purposes. I t is uniform growth and better development. The enclosed in tissue paper and is brittle and plants are kept totally free from weeds with the plastic in nature. Internally, it is homogenous use of suitable weedicides. The plant should be upon the requirement, the powdered form is protected from various insect pests like cut available in the pack of 5 to 10 kg. worms, leaf minor and poppy borer. The use of 2. Persian opium – Dark brown in colour, found manures and fertilizers markedly improve the in the form of brick shaped masses, quality and yield of opium poppy. Especially, weighing 450 g. It is hygroscopic in nature, nitrogen and phosphorus have remarkable granular or nearly smooth with brittle effects on growth of plant. fracture. After sowing, within 3-4 months, the plant bears 3. Natural Turkish or European opium – Brown flowers, which are converted to capsules within or dark brown in colour. It is found in conical few days and attain maturity after 15-20 days. or rounded and somewhat flattend masses, During the maturity period, the capsule exudes weighing 250 to 1000 g. On keeping, it maximum latex which shows a colour change becomes hard and brittle. from dark green to light green. Such capsules It is covered with poppy leaves. are incised vertically in the afternoon with the 4. Manipulated Turkish opium – It is chocolate help of specific needle like apparatus called brown or dark brown internally and covered ‘nushtur’. with broken poppy leaves externally. It penetrates maximum upto 2 mm into the The masses of this type are oval and capsule.Because of incisions, latex exudes out flattened on upper and lower surface and thickens due to cold weather in night which weighing about 2000 g. It is somewhat is eventually scrapped and collected next plastic or even brittle. morning by an iron scoop called Charpala. The 5. Manipulated European opium – It is dark incising process is repeated for about 4 times brown in colour internally and covered with on the same capsule with 2 days interval. The broken leaves. It is firm, plastic and with latex is collected in plastic containers.Then, brittle fracture. capsules are collected and dried in open areas Chemical Constituents – and further the seeds are separated by beating. The average yield of opium is about 25-26 kg The latex contains mainly the alkaloids derived per hectare and for seeds, it is from 4-5 quintals from amino acids phenylalanine and tyrosine. per hectare.Opium is exported traditionally from Chemically, they are placed under India.The exports for 95- 96 and 96-97 were benzylisoquinoline and phenanthrene types. Rs.2365.5 lakhs and 4102 lakhs respectively. Narcotine(also called noscapine), narceine and The opium collected by this way is either papaverine belong to the former, while exported or some of the part is further morphine, codeine and thebaine represent processed at government opium factory at latter category. Ghazipur. A generalised process is outlined to
JPRR: http://escipub.com/journal-of-pharmaceutical-research-and-reviews/ 0012 R.Ramasubramania raja and M.Likitha, M.Sekar, JPRR, 2018; 2:17 Fruits of poppy contain numerous off white is added by dissolved which deep coloured and minute seeds. These contain 30- reddish purple colour is obtained, 35 % drying fixed oil. Which is used which persists even on addition of commercially in oil plant industry, which is hydrochloric acid. colourless, tasteless and transparent. (2) Morphine when sprinkled on nitric OPIUM ALKALOIDS acid gives orange red colour. Codeine does not respond to this test. • Morphine is monoacidic, laevorotatory (3) The treatment of morphine solution phenolic alkaloid and also contains an with potassium ferricyanide and ferric alcoholic hydroxyl group at C(6) position. chloride solutions gives bluish green Due to presence of phenolic hydroxyl colour. Codeine does not respond to group, it is soluble in alkali hydroxides, this test. expect ammonium hydroxide. Morphine (4) Papaverine solution in hydrochloric is very less soluble in different solvents acid gives a lemon yellow colour with like ether(1 in 600), chloroform( 1 in potassium ferricyanide solution. 1200), alcohol( 1 in 200) and water( 1- 3000). Diacetylderivatie of morphine is Uses: heroin. Opium belongs to the category of hypnotic • Codeine(methyl morphine) is a strong sedative and analgesic in which the action is monoacidic base and laevorotatory. It is mainly due to morphine. soluble in water and organic solvents. Morphine is a potent analgesic. Due to its • Papaverine is a weak monoacidic base central narcotic effects, it causes addiction. and inactive optically.It is slightly soluble Hence, it is given only in severe pains and in in organic solvents, but insoluble in those cases, when patient does not show water. response to other analgesics. • The other important benzylisoquinoline Morphine has a biphasic action on central alkaloid narcotine is aslo a weak nervous system. monoacidic base and is laevorotatory, while its salts are dextrorotatory. It sedates the cerebrum and has a mixture of Narcotine is soluble in acetone, benzene, stimulation and sedation on the medulla. chloroform, but insoluble in water, alcohol In the medulla, it sedates the respiratory centre, and ether. emetic centre and the cough reflex. It also • The opium alkaloids are present as salts stimulates chemoreceptor trigger zone in the of meconic acid. medulla, which leads to nausea and vomiting • Protopine and hydrocotarnine are the and is considered as a side effect. minor alkaloids of opium. Opium also Morphine also produces respiratory depression contains sugar, wax, mucilage and salts and constipation. of calcium, potassium and magnesium. Codeine relieves local irritation in the bronchial Opium does not contain tannis, starch tract and as an antitussive used in various and calcium oxalate. cough medicines. Chemical Tests: It has mild analgesic effects,which are potent (1) The general test to detect opium is by than asprin, but only one tenth activity of that of testing presence of meconic acid. The morphine. Papaverine has relaxant effects on alkaloids are present as the salts of smooth muscles of the intestinal and bronchial meconic acid. Opium is dissolved in tract and the blood vessels. water and to the filtrate, ferric chloride
JPRR: http://escipub.com/journal-of-pharmaceutical-research-and-reviews/ 0013 R.Ramasubramania raja and M.Likitha, M.Sekar, JPRR, 2018; 2:17 Narcotine has a specific depressant action on (1) Powdered opium – It contains 10 per cough reflex and used in the preparation of cent anhydrous morphine with cough lintus. lactose, caramel and powderes cocoa Opium alkaloids are semisynthesized like other husks. medicinal agents.Diacetylmorphine(herion) has (2) Opium concentration – It contains more narcotic, analgesic property than different alkaloid hydrochlorides of morphine. opium in following proportions: Anhydrous morphine – 47.5 to 52.5% By losing one molecule of water, morphine Codeine – 2.5 to 5 % gives apomorphine which is emetic and used Narcotine – 16 to 22 % subcutaneously to treat poisoning cases. Papaverine – 2.5 to 7 % Hydromorphone is formed by replacing one of (3) Camphorated opium tincture – It the hydroxyl groups and also removal of contains alcoholic solution of opium, adjancent double bond. It is aslo a potent benzoic acid, camphor, anise oil and narcotic analgesic, but habit forming tendencies the formulation is prepared in alcohol. are less. It is used in treatment of diarrhoea as Dose: antiperistaltic. (1) Morphine sulphate: 10 mg, 6 times a Storage: day parenterally. Opium is preserved in a well closed container (2) Codenine sulphate/phosphate:10 – 20 to prevent loss of morphine. mg every 4-6 hours, orally. (3) Narcotine(noscapine):15 mg, 4 times BELLADONNA HERB a day, orally. Synonyms: (4) Papeverine hydrochloride: 150 mg Belladonna leaf; Belladonnae Folium; Deadly orally and 30 mg parenterally. night shade leaf(European belladonna). Commercial Varieties of opium: Biological Source: (1) Indian opium- It is dark brown in Belladonna herb consists of dried leaves or the colour and found in the form of cubical leaves and other aerial parts of Atropa pieces weighing 900g. It is brittle and belladonna Linn.(European belladonna) or plastic in nature. The powdered form Atropa acuminate Royle ex-Lindley(Indian is available as 5 to 10 kg packs. It belladonna) or mixture of both the species contains 10 % anhydrous morphine. collected when the planrs are in flowering (2) Persian opium- It is dark brown in condition. It belongs to family Solanaceae. It colour and brick shaped masses of contains not less than 0.3% of the alkaloids of 450 g. It is hygroscopic, granular or belladonna herb, calculated as I- hyoscyamine. smooth. Geographical Source: (3) Turkish opium- It is commonly called as druggists opium or soft opium. It is It is indigenous to and cultivated in England and brown or dark brown in colour and other European countries. In India. It is found in available as conical rounded or the western Himalayas from simla to Kashmir flattened masses. and adjoining areas of Himachal Pradesh.Its (4) Chinese opium- It comes in market in chief habitat is jammu and in forests of Sindh, the form of flat globular cakes and and chinab valley. contains 4-11% morphine. History: Different Forms of opium: Because of the hallucinogenic effect of this plant, it was used as craft in the middle ages.
JPRR: http://escipub.com/journal-of-pharmaceutical-research-and-reviews/ 0014 R.Ramasubramania raja and M.Likitha, M.Sekar, JPRR, 2018; 2:17 In ancient times, the juice of this plant was used Size – Leaves are 5 to 25 cm long and 2.5 to as a cosmetic, because of its dilatory effect on 12 cm wide. the pupil of the eye. This drug was first Flowers – Corolla 2.5 cm long and 1.5 introduced in the London Pharmacopoeia in cm wide. 1809. Fruits – About 10 cm in diameter. Cultivation and Collection: Shape – Leaves-Ovate, lanceolate to broadly Cultivation of belladonna at an altitude of 1400 ovate, with acuminate apex, decurrent lamina, m from sea level is found to be satisfactory, if entire margin, petiolate, brittle and transversely proper irrigation facilities are provided. It is broken. observed that the yield per hectare can be Flowers- Campanulate, 5, small reflexed lobes increased substantially by proper cultivation of corolla. technology. Fruits- Berries, sub-globular in shape with The experimental trails of applications of numerous flat seeds. several fungicides and insectides right from the treatment of the seeds upto the foliar sprays Extra Features: were very encouraging. Its cultivation in Jammu In general the entire drug is seen as crumpled and Kashmir is found to be successful. and twisted. The dropping flowers are Belladonna berries are crushed to get the associated with as many pairs of leaves. The seeds for cultivation.Proper processing like flowers are with 5 stamens, superior bilocular washing and sieving is performed.Only healthy ovary and numerous seeds. seeds are used are used for cultivation.Seeds Macroscopic Characters: are sown by broadcasting method in well Epidermal cells with slightly sinuous anticlinal prepared beds with the application of fungicide wall and striated cuticle,anisocytictrichomes like diathon.Sowing is done in May and July. which are uniseriate and with unicellular heads. Transplanting is done by keeping certain The palisade ratio is 5 to 7. distance between two plants and the seedlings Chemical Constituents: are irrigated carefully. The total alkaloidal content of drug is 4.4 to 1% Fertilizers like urea, potash and and varies in different parts of plant, superphosphate are given as per the needs. roots(o.6%), stems(0.05%), leaves(0.4%), Insecticidal sprays like sevin are also tried unripe berries(0.19- 0.21%) and seeds(0.33%). when the plant reaches maturity. The leaves, The main alkaloids are I- hyoscyamine and its as well as, the flowering tops are cut and racemic form atropine. The drug also contains sundried or dried in shade. During drying, care belladonine, scopoletin (I-methyl aescuetin), is taken to retain the green colour. While hyoscine, pyridine and N- methyl pyrroline. The grading and packing for market, woolly stems later two are the volatile bases. and foreign organic matter are rejected. The Standards: yield per hectare is found to be 200 to 600 kg. 1) Total ash – 14 per cent Macroscopic characters: 2) Acid-insoluble ash - 3 per cent Colour –Leaves are green to brownish-green 3) Foreign organic matter – not more than Flowers are purple to yellowish-brown 3 per cent Fruits are green to brown. It gives Vitali-Morin reaction – positive. Odour – Slight and characteristic Uses: Taste – Bitter and acrid It is the parasympatholytic drug with anticholinergic properities.It is used to reduce JPRR: http://escipub.com/journal-of-pharmaceutical-research-and-reviews/ 0015 R.Ramasubramania raja and M.Likitha, M.Sekar, JPRR, 2018; 2:17 the secretions such as sweat, saliva and gastric leaf has length of 9-18 cm and width of 8-13 juice and also to reduce spasm in cases of cm. Normally, the margin os of entire, but in intestinal gripping due to strong purgatives. It I some cases sinuated with rounded or acute 2-4 also used as an antidote in opium and chloral broad lobes. The leaf is covered with minute hydrate poisoning. hairs, lower surface is slightly pale in colour Dose: and the leaf has a thin texture. The leaf is unequal at the base with acute apex and 0.6 to 1 ml in the form of belladonna tincture – glabrouslamina.Each leaf has 3-4 coarse veins 4 times a day. on each side and 4-6 secondary veins on either DATURA side of the midrib. Synonyms: Flowers are reddish-purple on outer side and Datura herb, Angel`s trumpet. whitish on inner side.Corolla is thin, acuminate, Biological Source: triangular to circular in shape. Flowers are Datura consists of the dried leaves and funnel shaped with pedicel which is never erect. flowering tops of Daturametel and D.metel var. The stems, as well as, branches of drug are fastuosa Safford. It belongs to family purple coloured. Brown coloured seeds are Solanaceae. triangular and are found in the thorny capsule. It should contain not less than 0.20 per cent of Microscopic Characters: total alkaloids of datura, calculated as I- Through the transerve section, it shows its hyoscyamine. dorsiventral character. The epidermal cells of Geographical Source: both sides show anisocytic or cruciferous It is found in india, England and other tropical stomata. The cells are covered with thin cuticle and subtropical regions. and glandular and non-glandular simple trichomes. About 40% of the lamina is occupied Cultivation and Collection: by single layer of palisade cells. About 6-8 The drug is cultivated by sowing the seeds. The layers of spongy parenchymatous cells are germination is normally very slow. If the seeds present. The midrib shows vascular tissue with are soaked in water and kept overnight, the rate protoxylem and metaxylem. Trichomes are of germination increases. About 7-8 kg of seeds more on the midrib region. Stomatal index is per hectare are required for sowing purpose. 12.7 to 19.5 for upper surface and 21.2 to 24 The seeds require about 15-20 days for for lower surface. Palisade ratio is 3.5 to 6.5. germination. Weeding and thinning are The spongy parenchyma contains calcium necessary and performed when the plants oxalate crystals. reach 10-15 cm height. The distance kept in Chemical Constituents: between 2 plants is about 75-100 cm. The plants should be supplied with organic fertilizers Datura herb contains upto 0.5%of total and proper irrigation. The drug is collected after alkaloids, among which hyoscine(scopolamine) 4 months of its cultivation. The leaves and is the main alkaloid, while I- branches are removed, drug is dried in the sun hyoscyamine(scopoline) and atropine are and marketed by packing in gunny bags. present in very less quantities. Macroscopic Characters: Standards: The drug has a characteristic but unpleasant 1. Stems, flowers, fruits- not more than 20% odour and a bitter taste. The drug contains 2. Foreign organic matter- not more than entire, broken wrinkled, crushed leaves along 2% with stem fragments and floral parts.The entire 3. Acid-insoluble ash- not more than 4% Chemical Test: JPRR: http://escipub.com/journal-of-pharmaceutical-research-and-reviews/ 0016 R.Ramasubramania raja and M.Likitha, M.Sekar, JPRR, 2018; 2:17 1) The tropane alkaloid is treated with Cultivation, Collection and Preparation: fuming nitric acid, followed by Most of the cinchona species profusely grow in evaporation to dryness and addition of sub-tropical or tropical climates at a height of methanolic potassium hydroxide solution about 1000-3000 metres. The trees, growing to an acetone solution of nitrated residue. below this height are found to have less Violet coloration takes place due to percentage of quinine. The rainfall conditions tropan derivative. required are uniform (from 250-380 cm in a 2) On addiction of silver nitrate solution to year). The favourable growth is achieved solution of hyoscinehydrobromide, between an atmospheric temperature of 60 yellowish white precipitate is formed, degree – 75 degreeF. Cinchona requires light, which is insoluble in nitric acid, but well drained forest soil which is rich in organic soluble in dilute ammonia. matter. The acidic soil having a PH of 4.2 - 5.6 Uses: and a small amount of nitrogen are found to be Datura herb and its main alkaloid hyoscine are most favourable for growth. Cinchona needs parasympatholytic with anticholinergic and slopping situation, high humidity and protection central nervous system depressant effects. from wind. The drug is used in cerebral excitement. Along The propagation is done either seeds or with morphine, it is used as preoperative budding or layering. In West Bengal, only medication. budding is practised and in Tamil Nadu, the budding and layering methods are applied. The It is also used in treatment of asthma and seeds of cinchona are very small and light in cough. weight. About one gramme of cinchona seeds Hyoscinehydrobromide used in motion contain 3500 seeds. They are admixed with soil sickness, gastric or duodenal ulcers. during sowing. The maintenance of genetic CINCHONA purity causes a problem as high cross Synonyms: fertilization occurs in cinchona plants.. The Jesuit`s bark, Peruvian bark affects the yield, like in high alkaloid content giving species, such as C.ledgeriana, the Biological Source: average alkaloid content is reduced. The seeds It is the dried bark of the cultivated trees of should be immediately used for propagation as Cinchona calisaya Wedd.,C. ledgerianaMoens, on storage they lose their lose viability. The C.officinalis Linn., C.succirubraPav. Ex- germination takes place in 3-6 weeks. The klotzsch, or of hybrids of either of the last two seedlings with 2 pairs of leaves are species with either of the first two. Cinchona transplanted and space of 6-10 cm is belongs to family Rubiaceae. It contains not maintained in between two seedlings and 2 less than 6 per cent of total alkaloids of rows. The young seedlings are protected from cinchona. direct sunlight. In forest soil, they are Geographical Source: transplanted after 15 months of growth and preferably before heavy rainfall. A distance of 2 India, Bolivia, Columbia, Ecuador, Peru, metres is maintainedbetween two plants. As Tanzania, Guatemala, Indonesia and Sri Lanka cinchona consists of stem, as well as root bark, are the countries where cinchona is found. In the plants from 4 to 20 years old age are India, it is cultivated in selected for harvesting, but the maximum Annamalaihills(Coimbatore district) and Nilgiri alkaloidal content is found to 6 to 10 years old hills(Nilgiri district)in Tamil Nadu and in plants. The bark is collected by coppicing Darjeeling area of West Bengal. method. For this purpose, vertical incisions are
JPRR: http://escipub.com/journal-of-pharmaceutical-research-and-reviews/ 0017 R.Ramasubramania raja and M.Likitha, M.Sekar, JPRR, 2018; 2:17 made on branches, trunk of tree and these The fractures is short in external layers and incisions are connected by horizontal circles. fibrous in the inner portion. The bark is then stripped off and dried in sun ROOT BARK – light and further by artificial heat. The drying is It occurs in length of 2-7 cm. The bark is done below 175 degree F. During drying, the curved, twisted or irregulary channelled. bark loses upto 70 per cent of its weight. The care should be taken to avoid molding or The different commercial varieties have some fermentation during drying. The quills of drug special characters. C. succirubra is also called are packed in gunny bags and marketed. The red bark, while C.ledgeriana is referred to as root bark is collected by uprooting the trees and yellow bark. C. robusta is the hybrid between C. bark is separated manually. succirubra and C.officinalis. During the two world wars, Java and Indonesia The typical characters of 4 main species of lost their positions as potential as potential cinchona: producers of cinchona. After that, India has Charact C.calisya C.ledgeri C.officin c.succirub gained the prime position as producer and ers ana alis ra supplier of cinchona and quinine. By 1985 – 86, the production had reached upto 10 lakh kg of Size Diameter Diameter Diamete Diameter bark and about 26,000 kg of quinine salts. is from 12-25 r is upto is from 12-25 mm and 12 mm 20-40 mm India exported quinine and its salts of Rs. 299.0 mm and thickness and and lakhs during 1995 – 96. thickness varies thicknes thickness Extraction of Quinine: from 2-5 from 2-5 s is upto from 2-5 mm mm 1.5 mm mm. For extraction of quinine, the bark is powdered and extracted with benzene or toluene in presence of alkali. Further, the alkaloids are Other Broad Broad It shows Well extracted with dil.sulphuric acid. By bringing the feacture longitudu longitudu a marked s nal with nal number longitudun acid extract to neutrality, quinine sulphate transvers fissures of al separates, as it is sparingly soluble. e cracks. and transerv wrinkles, Macroscopic Characters: cracks e but less more in cracks. number of Cinchona bark has a slight and characteristic number, transvers odour, but somewhat astringent and intensely but less e bitter taste. In general, the bark is available in deep.So cracks.On the form of quills and curved pieces. me ly some pieces pieces STEM BARK- shoe shoe It is upto 30 cm in length and about 2 to 6 mm longitudu reddishwa in thickness. The outer surface shows dull nal rts. wrinkles brown grey or grey colour and many a time, and shows presence of mosses and lichens owing reddish to its growth in heavy rainfall areas. The bark is warts. rough and has transverse fissures. These Microscopic Characters: fissures are different in different species. It is Cinchona exhibits the typical histological furrowed or wrinkled longitudinally. The outer characters of the bark. The cork cells are thin bark in some varieties shows exfoliation. The walled, followed by phelloderm. The cortex inner surface is pale yellowish-brown to deep consists of several secretory channels and reddish-brown and the colour on the species. phloem fibres. Medullary rays with radially
JPRR: http://escipub.com/journal-of-pharmaceutical-research-and-reviews/ 0018 R.Ramasubramania raja and M.Likitha, M.Sekar, JPRR, 2018; 2:17 arranged cells are present.Idioblast of calcium Quinine sulphate is important from oxalate is the specific characteristic of cinchona pharmaceutical point of view. It has very less bark. Starch grains are present in the solubility in water(1 in 810), due to which, it is parenchymatous tissues. suitable for oral use. Stone cells are rarely present in the structure. A Quinidine is similar to quinine in its physical and few of the cork cells are lignified. Medullary chemical properties and has higher water rays are 2 to 3 cells wide. solubilty. The free base is soluble in water, Chemical Constituents: ethyl alcohol, methyl alcohol and chloroform. Cinchona bark contains about 25 alkaloids, Chemical Tests: which belong to quinolone group. The important (1) Heat the powdered drug in a dried test alkaloids are quinine, quinidine, cinchonine and tube with little glacial acetic acid, purple cinchonidine. The alkaloids of lesser vapours are produced at the upper part of importance are quinicine, test tube. cinchonicinehydroquinine, hydrocinchonidine (2) Thalleoquin test: The powdered drug and homocinchonidine. C. succirubra contains gives emerald green colour with bromine 5-7% of total alkaloids, of which 30% is quinine. water and dilute ammonia solution. C. ledgeriana yields from 6-10% and, in some (3) Quinidine solution gives a white cases, upto 14% of total alkaloids, with upto precipitate with sliver nitrate solution, 75% is quinine. C.salisaya has 6-8% total which is soluble in nitric acid. alkaloids (about 50% quinine). Standards: Quinine and Quinidine are stereoisomers of (1) Total ash – not more than 4 per cent each other. Quinidine is aslo obtained (2) Foreign organic matter – not more than 2 commercially from cuprea bark i.e. per cent RamijiapendunculataFluckiger belonging to The UV spectrophotometric method of family Rubiaceae, or by isomerization of estimation is carried out for quinine. quinine. Uses: Quinine and Quinindine from many salts, but medicinally their suilphates are more Quinine and its salts are used in the treatment significant. Cinchonine and cinchonidine are of malaria. also isomers of each other. Quinine is a protoplasmic poison, especially for Apart from alkaloids, cinchona also contains protozoa like Plasmodium vivax, P. falciparum, quinic acid and cinchotannic acid. In the plant, P.malarie and P. fatal, and hence, used as the alkaloids are present as salts of these powerful antimalarial drug. acids. Cinchotannic acid decomposes into Quinine has also been found to be highly active insoluble cinchona red, due to its phlobatannin in vitro against nature. Cinchona bark aslo contains a Trypanosomacruziepimastigotes. glycoside called quinovin, tannis and bitter Quinidine is primarily a cardiac depressant and essential oil. used to prevent certain arrhythmias and The alkaloid quinine occurs as bitter white tachycardia. Quinidine is valuable in prevention crystals and it darkens and it darkens when of atrial fibrillation. exposed to light and has fluorescence Dose: properties. It shows a strong blue fluorescence 1. Chinchona powder- 0.3 to 1 g in ultra-violet light. This fluorescence is 2. Quinine sulphate-1 g daily for 2 days and enchanced in presence of dilute sulphuric acid. then 600 mg daily for 5 days. Quinine forms salts with different acids. JPRR: http://escipub.com/journal-of-pharmaceutical-research-and-reviews/ 0019 R.Ramasubramania raja and M.Likitha, M.Sekar, JPRR, 2018; 2:17 3. Quinidine sulphate- 0.2 to 0.4 g every two Stomatal index is from 10.8 to 18.2 and to four to a total dose of 3 g daily in atrial palisade ratio from 5 to 8.5. fibrillation. Chemical Constituents: VASAKA Vasaka leaves contain quinazolinederivaties Synonyms: such as vasicine, vasicinone and 6- hydroxyl Adhatoda, Adulsa, Malabar nut. vasicine. Biochemically, vasicine is oxidised to its ketonic derivative vasicinone and the latter Biological Source: exerts main activity as bronchodilator. The drug It consists of dried, as well as, fresh leaves of aslo contains volatile oil, betain and Vasakin. It the plant AdhatodavasicaNees, belonging to is also reported that vasaka contains adhatodic family Acanthaceae, and contains not less than acid. 0.6% of vasicine on dried basis. Standards: Geographical Source: Foreign organic matter – not more than 2 per Vasaka is indigenous to India, where it is found cent. in sub- Himalayan track upto an altitude of 1000 Uses: m, and in Maharastra especially, in Konkan region. Besides India, it is found in Myanmar, Vasaka is used as expectorant and Sri Lanka and Malaysia. bronchodilator. The large doses are irritant and cause vomiting and diarrhoea. Cultivation and Collection: The pharmacological investigations have shows The uses of vasaka have been known since old oxytocic property similar to oxytocin and methyl times and it is included in different formulations ergometrine. of Ayurveda. Vasicine also shows abortificient action and The plant is not cultivated on commercial scale. both the actions are due to release of It is obtained from garden plants or wild prostaglandins. sources. It can be easily propagated by stem cuttings and by seed germination. The plant is COFFEE obtained in all seasons of the year. It reaches Synonyms: to an height of 2 to 3 meters. It is also observed Coffee bean,coffee seed. that the plant favourably grows in loamy soil. Biological Source: Macroscopic Characters: It is the dried ripe seed of Coffea Arabica Linne The drug contains stem leaf, fruit and seeds. or C. libericaHiern, and deprived of most the The leaves have 10 – 30 cm length is crenate seed coast. It belongs to family Rubiaceae. with acuminate apex. There are 8-10 pairs of Geographical Source: lateral veins. Taste is better and odour is characteristic. Ethiopia, Brazil, India, Vietnam, Mexico, Guatemala, Indonesia and Sri Lanka. MicroscopicCharacters: Coffee beverage is popular in different parts of The epidermis shows caryophyllaceous world. The amount of caffeine present is also stomata with sinous epidermal cells, and more than in tea. In middle east countries, it is covering and glandular trichomes. I t is a known by name ‘qahuah’. It is a strong dorsiventral leaf with palisade having 2 layers decoction of coffee seed powder. The word has of cells. 2 – 3 bicollateral vascular bundles are its origin in Turkish and Arabic languages. The seen in midrib. Mesophyll contains prismatic major suppliers of coffee, now-a-days, are and acicular crystals of calcium oxalate. Brazil and India. Karnataka, Kerala and Tamil
JPRR: http://escipub.com/journal-of-pharmaceutical-research-and-reviews/ 0020 R.Ramasubramania raja and M.Likitha, M.Sekar, JPRR, 2018; 2:17 Nadu grow large plantation of coffee. At present actions are due to caffeine. It is sometimes, it is cultivated in Maharashtra too ! used to combat the toxic effects due to CNS Habitat: depressant drugs. Coffee plant is an evergreen shrub which bears Other Preparations- type of fruit with an ellipsoidal or spheroidal Decaffeniated coffee – This product has been shape. Each fruit has 2 locules, containing one introduced in developed countries. It has been seed in each chamber. Each plant gives about specially designed, because of addiction effects 2 – 3 kg of coffee seeds. The fruits are dried to of coffee. separate the seeds. The seeds are separated It has all the agreeable odour of coffee beans, by wetting them and mechinacally separating, but contains a meagre amount(about 0.08%) of followed by drying in heaps, which causes caffeine. fermentation. ASHWAGANDHA The separated seeds or beans are green in Synonyms: coilour. They are roasted by which the colour and adour is effected. The seeds acquire dark Withania root, Asgandh, Winter cherry. brown colour and possess an agreeable odour Biological Source: and bitter taste. It consists of dried roots and stem bases of India produced 1.65 and 2.35 lakh tonnes of Withaniasomnifera (Linn.) Dunal, belonging to coffee during 1998-99 and 99-2000 family Solanaceae and should contain not less respectively. than 0.02% of total withanolide A and Chemical Constituents: withaferinA on dried basis. The main constituents of coffee bean are Geographical Source: caffeine, tannin, fixed oil and proteins. It This plant grows wildly in all dry parts and contains 2-3% caffeine, 3- subtropical India. It occurs in Madhya Pradesh, 5%tannins,13%proteins, 10-15% fixed oils, Uttar Pradesh, Punjab plains and North chlorogenic or caffeotannicacis and sugars in Western parts of India like Gujarat and the form of dextrin, glucose, etc. In the seeds, Rajasthan. It is also found in Congo, South caffeine is present as a salt of chlorogenic acid. Africa, Egypt, Morocco, Jordan, Pakistan and During roasting process, the agreeable smell of Afghanistan. coffeeis developed which is due to an oil called Cultivation, Collection and Preparation: caffeol composed of mainly furfural along with It is reported that the plants from different minor quantities of phenol, pyridine and sources vary in their morphological and valerianic acid. therapeutic properties. Now-a-days, the Extraction of caffeine: cultivation is mainly done in Madhya Caffeine is prepared either by synthesis or Pradesh(Manasa plantations), where, about extracted from from natural sources. 2000 hectares are under cultivation. The Coffee bean is one of the major sources for it. propagation is done by seeds, for which about 4-5 kg of seeds are required per hectare. The For the extraction, coffee roasters are used in seeds are sown in the soil which is unsuitable which caffeine sublimed during roasting is for other crops. The sowing is done towards recovered. It is the commercial method for June – July and during growth, no special extraction of caffeine. arrangements are made forirrigation. Even the Uses: nitrogenous fertilizers lead to formation of small It is used as a source of caffeine. The main roots, but large foliage. Towards December or effects of coffee i.e. stimulant and diuretic January, the plants bear flowers and fruits and JPRR: http://escipub.com/journal-of-pharmaceutical-research-and-reviews/ 0021 R.Ramasubramania raja and M.Likitha, M.Sekar, JPRR, 2018; 2:17 during January, harvesting is initiated which Another series of steroidal lactones viz. lasts upto March. The roots are collected by withanolide E to M have been obtained from uprooting the plant and either entire roots or the chmotype 111. pieces there of are dried immediately. The drug also contains two monohydric Macroscopic Characters: alcohols called somnitol and somnirol; withanic The roots show buff to grey to grey outer colour acid; a phytosterol and ipuranol; and a mixture with longitudinal wrinkles. They are unbranched of fatty acids containing cerotic acid; oleic acid, straight, conical and some of them bear a palmitic acid and stearic acid. crown. The root crown possesses a number of Standards: bud scars. Roots are bitter in taste andfresh 1) Foreign organic matter- not more than 2 roots smell similar to urine of horse(hence per cent ashwagandha).The fracture is smooth and 2) Total ash- not more than 7 per cent powdery. 3) Acid- insoluble ash- not more than 1.2 Microscopic Characters: per cent The transverse section of root shows exfoliated 4) Alcohol soluble matter- not less than 16 cork which is nonlignified with 2-4 layers of per cent. phellogen and about 15-20 rows of phelloderm. Uses: It prominently shows parts of vascular tissue Ashwagandha has sedative and hyptonic like cambium, constiting of 3-5 layers of effects. tangentially elongated cells, phloem region with It has hypotensive, respiratory, stimulant parenchyma, sieve tubes and companion cells. actions along with bradycardia. Secondary xylem is hard which forms a continuous vasculasr ring interrupted by It is an immune- modulatory agent. medullary rays. The transerve section of stem Sitoindosides have been shown to possess base shows pith, pericyclic fibres, xylem with anti-stress activity. tracheids, fibres, and starch grains. Traditionally, it has been used in treatment of Chemical Constituents: rheumatism, gout, hypertension, nervine and The main constituents of ashwagandha are skin diseases. alkaloids and steroidal lactones. Among the This drug prevents bony degenerative changes various alkaloids, withanine is the main in arthritic conditions. constituent. The other alkaloids are It has been widely used as sex stimulant and somniferine, somnine, somniferinine, rejuvenator and is considered as strength and withananine, isopelletierine, anaferine and vigour promoting drug especially in geriatric anahydrine. Two acyl sterylglucosides viz. cases. sitoindoside VII and sitoindoside VIII have been The leaf extract shows activity against isolated from roots. Staphylococcus aureus and Ranikhet virus. The leaves contain steroidial lactones, which TEA are commonly called as ‘Withanolides’. The Synonyms: withanolides have C28 steroidal nucleus with C9 side chain, having six membered lactone Camellia thea ring. Lavie et.al, have isolated such compounds Biological Source: from plants grown in Israel, India and S.Africa. It contains the prepared leaves and leaf buds of The various withanolidesresported are as Theasinenasis(Linne) O. Kuntze, belonging to follows. These compounds have been obtained family Theaceae (Ternstroemiaceae). from W.somniferachemotype 1. GeographicalSource: JPRR: http://escipub.com/journal-of-pharmaceutical-research-and-reviews/ 0022 R.Ramasubramania raja and M.Likitha, M.Sekar, JPRR, 2018; 2:17 Large areas of land are put under cultivation of It aslo contains theobromine and theophylline in tea in India, Sri Lanka, China, Indonesia, and minor quantities.The colour of tea leves is due Japan. It is available as black tea from India to gallotannicacid(15%). and Sri Lanka and green tea from China and The agreeable odour is due to presence of a Japan. yellow volatile oil. Black tea is obtained by fermenting the heap of Tea leaves also contain an enzymatic mixture fresh tea leaves and further drying with artificial called thease. heat. Green tea is obtained by putting tea Use: leaves in copper pans and then drying by artificial heat. CNS stimulant in the form of beverage and also as diuretic. Macroscopic Characters:
It is a small evergreen shrub when cultivated reaches to the height of 1.0 – 1.5 metres, while wild growing plants reach upto 6.0 metres. Plant is much branched and bears grey bark. Leaves- Dark green, lanceolate or elliptical, blunt at apex, base is tapering margin shortly serrate. Young leaves are hairy while matured leaves are glabrous. Flowers- are solitary or in groups of 2 to 3 in the leaf axils, and drooping. Odour- Characteristics Taste- Bitter Preparation of Green Tea: It is prepared by exposing the freshly collected leaves to the air until most of the moisture is removed. Then they are roasted and stirred continuously until leaves become moist and flaccid. Then they are passed to rolingtable and rolled into balls and subjected to a pressure which removes the moisture. Then the leaves are shaken out on the copper pans and roasted again till the leaves assume dull green colour. Then the leaves are winnowed, screened and graded into various varieties. Chemical Constituents: Tea leaves are considered as a rich source of caffeine(1 – 3%).
It is extracted from tea dust and tea leaf waste or sweepings.
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