Origin, History, Introduction
the term “alkaloid” (alkali-like) is commonly used
to designate basic heterocyclic nitrogenous
compounds of plant origin that are physiologically
The term alkaloid ot Pflanzenlkalien was coined by
Meissner, a German pharmacist, in 1819.
The mankind has been using alkaloid for various
purposes like poisons, medicines, poultices, teas
The French chemist, Derosne in 1803, isolated
Effects of alkaloids on humans
High biological activity
Produce varying degrees of physiological and
psychological responses - largely by interfering
others interfere with membrane transport,
protein synthesis or other processes
In large doses - highly toxic - fatal
In small doses, many have therapeutic value
muscle relaxants, tranquilizers, pain killers, mind
altering drugs, chemotherapy
Although only a small percent are psychoactive, these
get much focus
Affect the central nervous system - often by
Categories of psychoactive cmpds
May also be narcotic (addictive)
Most alkaloids are synthesized from a few
common amino acids (tyrosine, tryptophan,
ornithine or argenine, aspartic acid, & lysine)
Nicotinic acid precursor for part of nicotine
Purine precursor for caffeine
Some alkaloids synthesized from terpenes - along
mevalonic acid pathway
Generally classified by the predominant ring
structure and/or carbon skeleton
True (Typical) alkaloids that are derived
from amino acids and have nitrogen in a
Protoalkaloids that are derived from
amino acids and do not have nitrogen in a
Pseudo alkaloids that are not derived
from amino acids but have nitrogen in a
False alkaloids are non alkaloids give false
positive reaction with alkaloidal reagents.
Function in Plants
They may act as protective against insects and
herbivores due to their bitterness and toxicity.
They are, in certain cases, the final products
of detoxification (waste products).
Source of nitrogen in case of nitrogen
They, sometimes, act as growth regulators in
certain metabolic systems.
They may be utilized as a source of energy in
case of deficiency in carbon dioxide
Trivial names should end by "ine". These names may
The genus of the plant, such as Atropine from Atropa
The plant species, such as Cocaine from Erythroxylon
The common name of the drug, such as Ergotamine
The name of the discoverer, such as Pelletierine that
was discovered by Pelletier.
The physiological action, such as Emetine that acts as
emetic, Morphine acts as narcotic.
A prominent physical character, such as Hygrine that
Prefixes and suffixes:
"Apo-" designates dehydration e.g. apomorphine.
"Iso-, pseudo-, neo-, and epi-" indicate different
types of isomers.
"-dine" designates isomerism as quinidine and
"-ine" indicates, in case of ergot alkaloids, a lower
pharmacological activity e.g. ergotaminine is less potent
test: (I2/kI):Reddish brown
Mayer’s: (HgCl2) Creamy precipitate with True
Hagger's test: (Picric acid) Yellow precipitate
with True alkaloid.
Dragendorff: (Potassium Bismuth Iodide)
Reddish Brown precipitate .
Tannic acid solution: different alkaloid colored
Most alkaloids are crystalline solids.
Few alkaloids are amorphous solids e.g. emetine.
Some are liquids that are either:
Volatile e.g. nicotine and coniine, or
Non-volatile e.g. pilocarpine and hyoscine.
The majority of alkaloids are colorless but some are
Colchicine and berberine are yellow.
Canadine is orange.
The salts of sanguinarine are copper-red.
Both alkaloidal bases and their salts are soluble in alcohol.
Generally, the bases are soluble in organic solvents and
insoluble in water
Bases soluble in water: caffeine, ephedrine, codeine, colchicine,
pilocarpine and quaternary ammonium bases.
Bases insoluble or sparingly soluble in certain organic
solvents: morphine in ether, theobromine and theophylline in
Salts are usually soluble in water and, insoluble or sparingly
soluble in organic solvents.
Salts insoluble in water: quinine monosulphate.
Salts soluble in organic solvents: lobeline and apoatropine
hydrochlorides are soluble in chloroform.
Optically active isomers may show different
l-ephedrine is 3.5 times more active than d-ephedrine.
l-ergotamine is 3-4 times more active than dergotamine.
d- Tubocurarine is more active than the
corresponding l- form.
Quinine (l-form) is antimalarial and its d- isomer
quinidine is antiarrythmic.
The racemic (optically inactive) dl-atropine is
Quaternary ammonium salts R4-N e.g
R2-NH > R-NH2 > R3-N
Saturated hexacyclic amines is more basic than aromatic
Class of Alkaloid
Amino or Proto Alkaloid
Amino or Proto Alkaloid
DERIVED FROM PHENYL ALANINE
Do not contain heterocyclic nitrogen atoms
Mostly are simple derivatives of phenylethylamine
Synonym: Ma-Huang “ma”=astringent,
Biological Source: Dried young stems of Ephedra
gerardiana (wall.) Stapf. And E. nebrodensis
Contain not less than 1 % of total alkaloids,
calculated as ephedrine.
Varities: Indian: E. gerardiana, E. intermedia
Chinese: E. sinica and E. equisetina.
Geographical Source: China, Pakistan, North-west part of India,
Australia, Kenya, Spain and Yugoslavia.
Altitude: 2500-3000m, Annual rainfall should not exceed 50cm,
Propagated by seeds or by layers or divisions of the root stock.
Seeds are sown early in the spring at a distance of 5 cm, distance of
one meter between two rows. Requires proper irrigation and
weeding. The alkaloidal content varies from season to season and
found to be maximum in autumn when plants and twigs are dark in
Collection: After attaining 4 yrs plants are collected for the extraction of
alkaloid. Twigs are generally dried in sun or even by artificial ways. After
drying stored in dry and well closed containers, away from light.
Gymnospermous plant, thin woody stems, cylindrical and grey to
greenish in color (5mm diameter). Internodes at a about 3-3.5 cm,
bears scaly leaves from the nodes in a whorl of 2.
i. Unicellular epidermis made up of quadrangular cells along with
thick walled cuticle.
ii. Non-lignified , hypodermal fibers
iii. Chlorenchymatus cortex
iv. Lignified pericyclic fibers.
v. Parenchymatous dark brown colored pith
Contains amino alkaloids
Ephedrine, nor-ephedrine, n-methyl ephedrine, pseudoephedrine, etc.
Ephedrine (C10H15NO) is 1-phenyl-1-hydroxy-2-methyl
aminopropane, soluble in water, alcohol, organic solvents and
Chemical test: Ephedrine+ water and HCL and then treated
with CUSO4 and NaOH, the solution gives violet color and
when shaken with solvent ether the organic layer shows purple
and aq. Layer shows blue color.
Bronchodilator in Asthma, colds, flu and Hay fever medications
Allopathic: Sinumed (dries a runny nose)
Used as an anti-inflammatory.
Weight loss (increases metabolism, decreases appetite – CNS
stimulant – acts on adrenergic receptors)
Also used to correct low B.P. conditions.
Ephedradines have hypotensive effects
Above ground parts are normally used, although the roots are
better to use (less alkaloids)
DIHYDROXY PHENYL ALANINE
Meadow saffron seeds,
Biological source: Dried ripe seeds of
Colchicum luteum Baker and Colchicum
Colchicum corm is also used medicinally.
Geographical Source :Various parts of
Europe, like England, Holland,
Czechslovakia, Poland and Yugoslavia. Also
cultivated in India.
Chemical Constituents: 0.2-1% of amino alkaloids,
colchicine is the main constituent, seeds contain upto
0.8% of colchicine and in corms upto 0.6%, also contains
demecolcine. Both contain tropolane or cycloheptatrienol-one ring structure.
Constituent in colchicum seeds and corm.
Amorphous, yellow-white alkaloid (darkens on exposure
Gives a strong yellow coloration with strong mineral
Dissolves readily in water, alcohol and chloroform, but
only slightly in ether or petroleum spirit.
Gives yellow color with 70% sulphuric acid.
Alcoholic solution when treated with FeCl3 gives red color.
Uses: Antitumor activity.
Relieve gout (used with caution – professional supervision)and
Also used in biological experiments to produce polyploidy
(multiplication of the chromosomes in a cell nucleus), hence
used in horticulture and cultivation of medicinal plants
Syn: Cocoa bean
Source: seeds of Theobroma cocoa
GS: South America, Central America & West indies
Constituents: Theobromine & cocoa butter (Theobrom),
Use: Nutritive, stimulant, diuretic.
(Theorbrominediuretic), oil is widely used as
suppository base & chocolates
Prepared leaves & leaf buds of Thea sinesis
GS: India, Srilanka, China, Indonesia, Japan
Small shrub height 1-1.5 m, much branched and bears
Leaves: dark green,lanceolate or elliptical, blunt at apex,
Flowers: solitary and in groups
Odor: characterisitc & Bitter taste
Preparation of Green tea:
1. freshly collected leaves, exposed to air until moisture is
2. roasted and stirred continuously until leaves become moist &
3. passed to rolling table and rolled into balls and subjected to
pressure which removes moisture.
4.leaves are shaken out to the copper pans and roasted again till
the leaves assume dull green color.
5. leaves are winnowed, screened and graded into various
CC: caffeine, theobromine, theophylline
Odor: volatile oil
Use: CNS stimulant, beverages, diuretic
Syn: coffee beans
Source: dried ripe fruits of Coffee arabica & C. liberica
GS: Brazil, India
Constituents: Caffeine, tannin, fixed oil, protein,
During roasting process, the agreeable smell of coffee is
developed due to oil called caffeol composed of mainly
furfural along with minor quantities of phenol, pyridine &
Use: source of caffeine, CNS stimulant & diuretic
Syn: bissy or gooroo seeds
Source: cotyledons of Cola nitida
GS: West africa, south america, South-East asia
Constituents: caffeine, theobromine, kolacatechin:tannin
Use: preparation of aerated beverages and as stimulant
7. Lobelia - pyridine alkaloid
Indian tobaccoa, asthama weed
Source: dried aerial parts of the Lobelia nicotianafolia
GS: western ghats of Maharashtra
Constituents: Lobeline, lobelidine, lobelanine and lobelanidine
1. solution of lobeline in H2SO4 red color with HCHO
2. Lobeline solution on boiling produces acetophenone
Use: treatment of asthma, respiratory stimulant, chronic
8. Black Pepper
Local name: Mari, Miri
Source: dried unripe fruits of Piper nigrum
GS: India, Malaysia, South america, West indies
Constituents: volatile oil, piperine, piperettine
Use: gonorrhoea, chronic bronchitis, condiment
8A. Long pepper
Source: dried unripe fruit of Piper longum,
GS: Indonesia, India, Philippines
Fusion od pyrrolidine & piperidine ring with common
Methylated nitrogen nuclues containing drugs are
chemotaxonomic characters of family solanaceae.
Hyoscyamine as main constituent: Datura stramonium,
Atropa belladonna, A.acuminata, Dubosia
Hyoscine as main constituent: D.metel, Dubosia
Hyoscyamine & Hyoscine (both in low quantity):
Local name: Tambakhu
Source: dried leaves of Nicotiana tobacum, Turkish-N.rustica
GS: indigenous to tropical america, China, US, India
Constituents: varies Nicotine up to 1-10%, narcotine,
Use: pesticidal, insecticidal.
Nicotine: stomach, contact, fumigant poison
Could be used for plants & comparatively safer,
Syn: deadly night shade
Source: dried leaves and other aerial parts of
European: Atropa belladonna, Indian: Atropa acuminata-contains NLT
0.3% of l-hyoscyamine
GS: Europe-England, India
Constituents: roots-0.6%, stem-0.5%, leaves-0.4%, unripe-ripe
Main: l-hyoscyamine, belladonin, pyridine and N-methyl pyrroline
Use: parasympatholytic drug, anticholinergic, reduce the secretions
such as sweat, saliva and gastric juice and also reduce spasm in case
of intestinal gripping due to strong purgative.
As an antitode in opium and chloral hydrate poisoning.
11. Datura stramonium
Syn: Thornapple leaves, Jimson or Jamestown weed
Source: dried leaves and flowering tops of Datura
stramonium (NLT 0.25% Hyoscyamine)
GS: US, South america, France, Germany, Hungary
Cultivation: seed propogation
Seeds sown by keeping a distance of 1 meter between two
plants and 60 meter between 2 rows.
Calcarious soil, flowers in september
Collection: twice, once before flowering and another
during the flowering
Constituents: 0.2-0.5% alkaloid, l-hyoscyamine &
hyoscine, small quantity of atropine
CT: vitali morin test positive
Tropane alkaloid + Fuming HNO3 evaporation to dryness
addition of methanolic KOH to an acetone solution
of nitrated residue purple color due to tropane alkaloids.
Hyoscine hydrobromide + AgNO3 yellowish white ppt,
soluble in ammonia.
Use: in Asthma, control salivation, muscular rigidity,
tremors in parkinsonism, motion sickness,
Substitute & Adulternat:
Solanum nigrum: resemble stramonium small leaf but not
contains calcium oxalate crystals.
Source: dried leaves and flowering tops of Hyoscyamus
GS: Western Asia, North africa, Europe, India.
Constituents: 75% hyoscyamine, atropine, hyoscyamine in
Use: counteract gripping effect, relieves spasms of urinary
tracts, sedative, expectorant, anti-asthmatic.
Source: dried leaves of (bolivia-Erythroxylon coca),
(Peruvian-E. truxillense), E. novogranatense
GS: South america-peru, bolivia, now a days cultivated in
Constituents: 0.7-1.5% total alkaloid, lesser alkaloids,
higher cocaine, cinnamyl cocaine, alpha-truxilline,
tropocaine, benzoyl tropine, dihydroxytropine,
Java coca has higher alkaloid & lesser cocaine.
Commercial price is determined by ecognine content because
it is synthetically converted to cocaine.
Cinnamyl cocaine cocaine + methyl alcohol + cinnamic
Cocaine ecgonine + methyl alcohol + benzoic acid
Alpha-truxilline ecgonine + methyl alcohol + alpha-truxillic
CT: cocaine powder + H2SO4 heated water
characteristic smell of methyl benzoate.
Use: local anaesthetic, stimulant, restorative, in colvulsion,
First local anaesthetic from which various other synthetic substitute
with similar activity have been prepared.
Owing to hallucinogenic and addictive effects of cocaine, drug of
abuse & limited to ophthalmic& ENT surgery
Synonym: Jesuit’s bark, Peruvian bark
Biological source: It is the dried bark
of the cultivated trees of Cinchona
Varities: C. succirubra, C. calisaya,
C. ledgeriana, C. officinalis
GS: India, Bolivia, Colombia Equador,
Peru, Tanzania, Guatemala, Indonesia,
and Sri lanka. In India Annamalai hills
and Nilgiri hills, Tamilnadu and in
sub-tropical/tropical climates, height of about 1000-3000 m.
If growing below this height, found to have less % of quinine.
Rainfall: Uniform, 250-380 cm in a year. Atmospheric temp.: 16-24 degree C
Soil: drained forest soil and rich in organic matter, acidic soil having pH of 4.25.6, small amount of N favorable for growth.
Specification: Needs slopping situation, high humidity and protection from
Propagation: either seeds or budding or layering, in WB only budding is used
and in TN budding or layering methods are applied.
Seeds are very small and light in weight, about 1 gm seeds contain 3500 seeds
so that seeds are admixed with soil during sowing
Seeds immediately used for propagation , on storage they lose their viability
Germination take place in 3-6 weeks.
Seedlings with 2 pairs of leaves are transplanted and space of 6-10 cm is
maintained in between 2 seedlings and 2 rows.
Young seedlings are protected from direct sunlight.
In forest soil, transplanted after 15 months of growth and before heavy rainfall.
Distance of 2X2m is maintained between 2 plants.
4-20 yrs of age, plants, selected for
but the maximum alkaloid content is found in
6-10 yrs old plants.
Bark is collected by coppicing method,
vertical incisions are made on branches ,
trunk of tree and incisions are connected by
horizontal circles, the bark is then stripped
Dried in sun light and further by artificial heat,
drying is done below 80 degree C.
During drying loses 70% of its wt.
Avoid molding and fermentation during
Odor: slight and characteristic odor
Taste: astringent and bitter
Form : quills and curved pieces.
1. Length about 30 cm
2. Thickness about 2-6 cm
Length about 2-7 cm
3. Outer surface is dull brown grey or Inner and outer surfaces are similar in
inner surface is pale yellowish-brown
to deep reddish in color.
4. Presence of mosses and lichens
no mosses and lichens
Bark is rough and has transverse
Bark is scaly and shows depression.
Typical characters of 4 main species of Cinchona
Character C. calisaya
varies from 25 mm
cracks more in
numbers but less
less no. of
Quinoline Alkaloids: about 25 types
Imp: quinine, quinidine, cinchonine and cinchonidine.
Alkaloids of lesser importance are quinicine, cinchonocine
hydroquinine, hydrocinchonidine and homocinchonidine.
C.succirubra: 5-7% 0f total alkaloid of which 30% is quinine.
C. ledgeriana: 6-10 % and in some cases upto 14% of which upto
75% is quinine.
C. calisaya: 6-8% total alkaloids about 50% is quinine.
Quinine and Quinidine are sterioisomers .
Quinine and Quinidine form many salts but medicinally their
sulphates are more significant.
Cinchonine and cinchonidine are isomers.
Also contains quinic and cinchotannic acid, also contains
glycosides such as quinovin, tannins and bitter essential oil.
Quinovin on Hydrolysis quinovic acid +quinovose
cinchona is slightly moistened with glacial acetic acid &
heated in an ignition tube, purple vapours are produced at the upper
part of tube.
2.Thalleoquin test: Powdered drug gives emrald green color with
bromine water and dil. Ammonia solution.
3.Quinidine solution gives a white ppt. with silver nitrate solution,
which is soluble in nitric acid ,
Anti malarial, Skeletal muscles relaxant, night muscles
spasm and abortifacient .
Quinidine : Indicated for treatment of arrhythmia and cardiac
depressant, atrial fibrillation
Cinchonine : Has mild anti malarial activity.
Cinchona extract and tincture: bitter stomachics and antipyretic.
oSource: Opium (Raw Opium) is the dried
latex obtained by incision from the unripe
capsules of Papaver somniferum
oIt is dried partially by spontaneous
evaporation and partly by artificial heat.
oGS: India, Pakistan, Afganistan, Turkey,
Russia, China and Iran.
subtropical climate in winter season.
Cold weather gives a favorable effect on yield, but extreme cold conditions,
including frost adversely affect the plant and yield of opium.
Cool weather without freezing temperature , cloudiness and sufficient sunshine
are the best climatic conditions for opium poppy.
Grown from November to March.
Propagation is done by sowing the seeds and 3-4 kg seeds per hectare are
required and admixed with about 3-4 parts of sand are sown.
Soil: highly fertile, well drained loamy soil with fine sand, should contain organic
matter, N containing, pH around 7.
Distance between two plants 25 cm and reaches maximum height of 1 m.
Periodically, the thinning of plants is done for uniform and better development.
Plants are kept free from weeds with the use of weedicides.
Protected from various insect pests like cut worms, leaf minor and poppy borer.
Nitrogen and phosphorus have remarkable effects on growth of plant.
Collection and Preparation:
Plant bears flowers within 3-4 months, converted to capsules and
attain maturity after 15-20 days.
During maturity period , the capsules exudes maximum latex shows
color change from dark green to light green.
Such capsules are incised vertically in the afternoon with the help of
specific needle like apparatus called ‘nushtur’.
It penetrates maximum into the capsule.
Latex exudes out and thickens in night.
Scrapped and collected next morning by an
iron scoop called ‘Charpala’.
Process is repeated for about 4 times on the same
capsule with 2 days interval
To maintain the external exudation of latex superficial incisions are
Latex is collected in plastic containers.
Capsules are collected and dried and further the seeds are separated
Odor: Strong characteristics & Taste: bitter
1. Indian Opium: Color- dark brown, Cubical pieces, Weight- 900
gm, enclosed in tissue paper and is brittle and plastic in nature,
internally homogenous, powdered form is available in 5-10 kg pack.
2. Persian Opium: Color- dark brown, brick shaped, weight- 450 gm,
hygroscopic in nature, granular or nearly smooth with brittle
3. Natural Turkish or European opium: color-brown or dark brown,
conical or rounded and flattened, Weight- 250-1000 gm, become
hard and brittle, covered with poppy leaves.
4. Manipulated Turkish opium: color- chocolate brown or dark
brown internally, oval and flattened, weight- 2000 kg, plastic or even
brittle, covered with poppy leaves.
5. Manipulated European opium: color- dark brown, elongated
masses with rounded ends, weight- 150-500 gm, firm, plastic, and
with brittle fracure, covered with poppy leaves.
More than 40 alkaloids usually combined with a specific acid
(Meconic acid) or with other acids e.g. sulfuric and acetic
from phenylalanine and tyrosine and are placed under
benzylisoquinoline and phenanthrene types
Opium alkaloids can be subclassified into 3 main groups with
different basic nuclei:
Phenanthrene alkaloids e.g. morphine and codeine.
Benzylisoquinoline alkaloids e.g. papaverine and noscapine
Phenylethylamine alkaloids e.g. narceine
Opium alkaloids are present as salts of
•insoluble in water
in ethanol (1:250) and
•practically insoluble in ether
•It contains 2 OH groups, one
is a phenolic at C-3 (gives a
soluble phenate with alkali) and
the other is a 2ry alcoholic at
R= H Morphine
R= CH3 Codeine
As opium alkaloids are salts of meconic acid.. To check …
1. Test for meconic acid: opium is dissolved in water, filer it,
to the filtrate add FeCl3 deep reddish purple color, which
persists even after addition of HCl
2. Test for Morphine: Morphine powder, when sprinkled on
HNO3 orange red color (codeine won’t give)
3. Test for Morphine: Morphine solution + potassium
ferricyanide + FeCl3 bluish green color (codeine won’t)
4. Test for Papaverine: Papaverine solution in HCl lemon
yellow color with potassium ferricyanide solution.
Opium: Sedative-Hypnotic Class, Action is due to Morphine
Morphine: potent analgesic, due to central narcotic effects,
causes addiction. Severe pain or when patient does not show
response to other narcotic
Sedates cerebrum and medulla respiration, emetic & cough
Triggers Chemo receptor trigger zone nausea, vomiting
Respiratory depression ad constipation
Codeine: relieves local irritation in bronchial tract, antitussive
Papaverine: smooth muscle relaxant of bronchial, intestinal
and blood vessels
Narcotine: cough reflex depressant, cough linctuses
Heroin: diacetyl morphine: more narcotic, analgesic property
Apomorphine: emetic & in poison
Hydromorphine: narcotic analgesic habit forming tendency is
Synthetic morphine compounds are called Opioids: non habit
(Tetra hydroxy-Iso-quinoline mono terpenoid)
Brief: derived from condensation of
dopamine with secologanin (a C10
monoterpene) to give two series of
Source: dried roots & rhizomes of
Cephalis ipecacuanha, C. acuminata
Specfication: should contain NLT
0.2% alkaloids, in that atleast 50%
GS: Brazil, India, Myanmar, Malaysia
[C.acuminata from panama]
Propagation: seed, season: mid January to mid February
Germination improvement: treatment with lime water or
2 month old seedling, transplanted at a spacing 10 X 10
cm, temp range: 23-28 degree C, rainfall: 300 cm
Atmosphere: humid, facilitates plant growth
Fertilizers: Nitrogenous, effect in increasing the quantity
Collection & Preparation:
After 3 years of vegetative growth.
Method: using pointed stick, levers
Drying: roots are dried in the sun or by fires and
transported down river to ports such as Rio de Janeiro
Roots & Rhizome
Color: dark brick red to brown
Size: up to 150 mm in length &
6 mm in thickness; rhizome 2
mm in diameter
Shape: tortuous pieces for
roots, cylindrical for rhizome
Pith is present in rhizome not
Color: reddish brown to
Size: up to 9 mm in
Isoquinoline alkaloid of phenolic & non phenolic group.
Alkaloid: Rio- up to 2% while Panama- about 2.2%
Imp: emetine, cephaeline, psychotrione, o-methyl
psychotrine and emetamine
Proportion of emetine: cephaeline (4:1-rio, 1:1-panama,
Cephaeline emetine by methylation of phenolic C(6)
phenolic: cephaeline, psychotrine
Non-phenolic: emetine,o-methyl psychotrine
Misc: ipecacuanhic acid, starch, Cal Ox, glycoside:
Powdered drug + HCl + water shake & filter
filtrate Potassium chlorate presence of yellow
color gradually changes to red, after standing due to
Emetine + Frohde’s reagent (H2SO4 + sodium
molybdate) bright green color
Expectorant in small doses, emetic in higher doses
Cephaeline is more emetic less expectorant than emetine
Emetine HCl antiprotozoal
Syn: south american arrrow root poison
Specification: some of the plants found in amazon region
like brazil and peru, contain highly poisonous substances.
The extract of all such plants is called curare.
The plants belonging to Loganiaceae & Menispermaceae.
Imp plants: Chondrodendron tomentosum, Strychnos
castelnaea, S.toxifera (Loganiaceae)
(Menispermaceae): Stephania, Menispermum, Cyclea,
GS: Brazil, peru, columbia, Guiana, Venezuela
Description: black or brown, resinous material having a
bitter taste,,soluble in cold water & dilute alcohol.
(+) tubocurarine –bisbenzyl iso quinoline moiety & most
potent, curine, curarine, isochondrodendrin, cycleanine,
Tubocurarine chloride quaternary base, insoluble in
organic solvent & soluble in water.
1. saturated solution of (+)tubocurarin green color
(+) tubocurarine solution + HgNO3 wild cherry red
(+) tubocurarine chloride
Surgical operations, to
muscles due to which
lower and safer dose of
general anesthesia is
Occasionally used to
aid myasthenia gravis.
Arise by inclusion of a basic nitrogen at some point in the
C27 compounds having cyclopenteno phenanthrene
Could act as a precursor for synthesis of various other
Syn: winter cherry, withania root
Source: dried roots and stem bases
of Withania somnifera
Specification: should contain NLT
0.02% of withanolide A & B
GS: all dry and subtropical region.
India: MP, UP, PB, GJ,RJ
Constituents: steroidal lactone
Main: withanine, pseudo withanine,
tropine, pseudo tropinem anaferine,
Leaves: steroidal lactone: withanolides, C28 steroid
nuclues with C9 side chain.
Two monohydric alcohol, somnitol, withanic acid,
sedative, hypnotic, hypotensive, respiratory, stimulant
actions along with bradycardia, immuno-modulatory,
anti-stress, mood stabilizer revives mind & body.
Traditionally: rheumatism, gout, hypertension, nervine
and skin disease, sex stimulant, rejuvenator
Source: dried stem bark of Holarrhena
Specification: should contain NLT 2% of total
GS: thorough out India-OS,AS,UP,MH
Plants which are 8-10 years old are selected;
LS, TS are made on the trunks from July to
After detachment, the bark is separated from
the wood and dried.
The recurved pieces of the bark are marked.
Color: buff to pale brown on
outer surface, slightly brown
in inner surface
Outer surface: longitudinally
wrinked and bears horizontal
Pieces are recurved with
varying size and thickness.
The drug shows a short and
Taste: bitter & acrid
Contains total 25 alkaloids
C21 group steroidal alkaloids.
Antiprotozoal and used to treat
Conessine is highly active against
Rauwolfia root, Serpentina root,
Source: Dried roots of Rauwolfia serpentina
It contains NLT 0.15% of reserpine and
GS: Tropical regions of Asia, America and
Africa. Commercially, In India, Sri lanka,
Myanmar, Thailand and America. In India UP,
Bihar, Orissa, Tamil Nadu, West Bengal,
Karnataka, Maharashtra and Gujarat.
Climate: wide range of, best suited humid, shade
Soil: wide range of with large amount of sand makes plants more
susceptible for disease
Clay: loamy soil, pH: acidic up to 4
Temperature: 10-38 degree C, Rainfall: 250-500 cm
Propagation: seeds, roots, cutting, root stumps
Initially seeds are sown into the nursery beds.
Sowing period: May or breakdown of monsoon
Implanting seedling: August, at a distance of 16-30 cm
Various fertilizer, manures: ammonium sulphate, urea, bone meal.
when plants are 3-4 year old.
Uprooting, roots are cut properly, washed as to remove earthy
matter & dried in air.
About 30 indole alkaloids; range from 0.7-3% on GS
Mostly in bark, root
Indole, Indoline, Indolenine ,Oxyindole, Pseudo indoxyl
Oleo-resin, phytosterol, fatty acid, alcohol, sugar
Ajmalicine, ajmaline, rauwolfinine, rescinnamine,
reserpinine, yohimbine, serpentine, serpentinine
Reserpine: ester of trimethoxy benzoic acid
Rescinnamine: ester of trimethoxycinnamic acid
With conc. HNO3 red coloration of medullary rays
Reserpine: with vanillin in acetic acid violet red color
Modle alkaloids: powdered rauwolfia + H2SO4 + p-dimethyl amino
benzaldehyde violet-red color
Reserpine: lowers BP by depleting store of catecholamine at nerve
ending, prevent re-uptake of nor-epinephrine at storage sites, allowing
enzymatic destruction of neuronal transmitter.
Rescinnamine: anti hypertensive but Higher dose depression
Dereserpine: anti hypertensive & tranquiliser
Ajmalicine: treatment of circulatory diseases, relief of obstruction of
normal cerebral blood flow.
Syrosingopine: same as above but milder
Source: dried whole plant of
Catharanthus roseus or Vinca rosea
GS: Indigenous to Madagascar.
Cultivated in South Africa, India,
U.S.A., Europe, Australia and
20 dimeric indole-dihydroindole (indoline) alkaloids possess
Vincristine and Vinblastine are most significant.
Indole: Vinblastine termed as Catharanthine
Dihydroindole alkaloid: Vindoline
Other: ajmalIcine, lochnerine, serpentine and tetrahydroalstonine.
Vincristine sulphate: antineoplastic: arrest mitosis at the
metaphase, IV: acute acute leukemia for children, Hodgkin’s disease,
reticulum cell sarcoma, lymphosarcoma, myosarcoma
Vinblastine sulphate: either above mechanism or by interfering
with amino acid metabolism, suppress immune response
Hypotensive & Antidiabetic
Syn Crow fig, Semen Strychni
Source: Dried ripe seeds of Strychnous
Contain NLT 1.2 % of total alkaloids
calculated as strychinine.
GS: East India, Sri lanka, Northern
Australia, and India. Abundantly in South
India i.e. Tamil nadu, Kerala and on Malabar
coast. Also available in Bihar, Orrisa,
Konkan, Mysore and Gorakhpur.
Collection & Preparation
-Found throughout the tropical area, 1300 m above sea level.
-Plant height: 10-12 m, crooked trunk, several branches.
-Leaves are orange, oppositely arrange, oval shape, entire margin and
-Flowers are greenish white and the bark is greyish to yellow.
-Fruit are orange yellow, consists a berry about the size of a small
-When ripe it has a hard orange-yellow pericarp and a white, pulpy
interior – containing 4-5 seeds & Seeds are washed to remove pulp
-Unripen seeds are separated by the floating test in water.
-Seeds are dried on mat and packed in gunny bags for marketing.
-Collection of fruit and seeds is carried out from NovemberFebruary.
-Exported in small sacks known as pockets.
Hilum, ridge on testa and micropyle
Color: greenish brown
Lignified Trichomes, layer of collapsed cells and endosperm
1.5-5% bitter Indole alkaloids, Strychnine and Brucine
-Vomicine, α-colubrine, pseudostrychnine,
Isostrychnine, N-oxystrychnine, protostrychnine, β-colubrine and
Glycosides: loganin, chlorogenic acid and fixed oil
Allied specids: Strychnos nuxblanda, S. potatorum
Brucine is the dimethoxy derivative of Strychnine.
Both alkaloids contains 2 Nitrogen atoms.
Hemitoxiferine is a degradation product of strychnine.
Dimerization of hemitoxiferine produces a valuable skeletal
muscle relaxant Toxiferine
R= OCH3 Brucine
Thin sections of nux vomica seeds are defatted and following test are
1. Stain the TS of nux vomica with conc. HNO3 endospermic cells
take yellow color due to presence of brucine.
2. Stain the TS of nux vomica with ammoium vandate & H2SO4
Manddin’s reagent -- endospermic cells become purple due to
3. Strychnine + H2SO4 + Potassium dichromate violet color
red finally yellow
-Bitter stomachic, tonic, CNS stimulant, increases BP, certain
forms of cardiac failure, stimulant for respiratory & CVS
-Brucine: very less physiological action, 1/6 th potency as
compared to strychine, 4 times bitter than strychine.
Brucine: denaturinng alcohol, inedible fats, dog poison.
Syn: Ergot of rye, Ergot.
Source: It is the dried sclerotium of a
fungus, Claviceps purpurea
(Clavicipitaceae or Hypocreaceae)
developed in ovary of rye plant,
Secale cereale Linne (Graminae). It
contains not less than 0.19 % of the
total alkaloids of ergot, calculated as
GS: Switzerland, Yugoslavia, Hungary
History and Source
Origin: french word, Argot, which means fur and indicates
the shape & attachment of the sclerotia to the infected rye
spikes, like the fur which is attached to the body of birds.
Even in old days, ergot fungus was known to be a pathogen,
infecting the rye fields in European countries and Russia.
It is known that the toxic effects were observed owing to
its contamination of ergot with rye grains.
The toxic symptoms were gangrene in the extremities and
In the middle ages, such symptoms were reported and
called St. Antony’s fire.
After knowing the cause, it was called as ergotism which
had severly occurred in 16th century in Germany.
Further it was discovered that the ergot has specific uses in
obstestrics and came into wide use from 19 th century
In 1836, it was introduced in London Pharmacopoeia.
Collection and Preparation:
Two ways : Natural and Artificial i.e. saprophytic production
Ergot is produced by natural way i.e. cultivation of rye plants
and subsequently infecting with this fungus.
For natural way of production, rye plant is host and ergot is
More than 600 plants from different families of wild and
cultivated grasses are act as hosts
other fungus are C. microcephala, C. nigricans and C. paspali
Rye is the better host for the large scale production of ergot
by way of quality and quantity.
Among the various stages of development of this fungus,
sclerotial stage or a dormant stage contains the maximum
amount of drug.
The ovary of the rye plant at its base, gets infected by ascopores to
ovaries is influenced by wind and insects.
After infecting, the ascopores germinate in the favorable conditions
like moisture and damp climate.
The germination of ascopores leads to formation of hyphal strands
which go on invading the wall of ovary with the help of an enzyme.
By this way, the hyphe from soft, white mass of tissue over the
surface of the ovary which is called as mycelium.
The mycelium secrets a viscous and sugary fluid called honey-dew.
At this time, the hyphal strands produces asexual spores called
conidiospores, which remain in a suspended form in honey-dew.
Due to the sugary fluid i.e. honey-dew, the insects and ants are
attracted which further help in the spread of the fungus to other
The development stage is the sexual stage and called as Sphacelia
The hyphae further invade into the deeper parts of ovary and
slowly replace the entire tissue of ovary by a compact tissue called
pseudoparenchyma which is hard and dark purple.
It is called as sclerotium stage and is considered as resting or
dormant stage of the fungus and contain maximum amount of ergot
If this sclerotium is left uncollected, it eventually falls on the ground
and in the favourable season, i.e. spring gives out stromata which
are in the elongated form.
Each stromatum has globular head and stalk.
The head portion contains a large number of perithecia and every
perithecium is like a flask shaped structure which contains a
number of sacs, each sac containing the ascopores which are
thread like in appearance.
Ascopores are the sexual spores capable of inducing fresh life cycle
of fungus by infecting the ovary of rye plant.
Selection of correct strain of fungus (Claviceps purpurea),
appropriate containers for preparing large scale ergot
inoculum and an idea nutrient medium are important
requirements for commercial production of ergot.
The various chemical races of fungus can produce only
specific ergot alkaloids like ergotamine, ergometrine and
ergotoxin in appreciable quantity from their sclerotia.
The ascopores of this species with the specific chemical
race are germinated on nutritive medium and by this way
large bulk of conidiospores are formed.
The suspension of this strain of fungus is sprayed on rye
plants in large cultivated areas.
Saprophytic production is much practised now-a-days, because mycelial
dry weight gives even more than 20% of alkaloids, while natural
sclerotia contains less than 1% of alkaloids. The process of fermentation
is properly regulated or controlled for optiumum bioproduction of useful
This process was initiated in Japan by prof. abe
It is convenient in many ways as it eliminates the variation in yield due to
weather conditions and production can be achieved throughout the year.
Various strain of ergot are used depending on the type of ergot alkaloid to
Claviceps paspali gives clavines and simple lysergic acid derivatives.
It is much easier to manufacture clavines and simple lysergic acid derivative
and the convert them to different peptide alkaloids, i.e. ergot alkaloids.
For nutrition of cultures of fungus, specific nutrients are used and
fermentation is carried out in temperature range of 20-30 degree C and in
a pH of 4.6-6.3.
The fermentation process for this submerged cultures in shaking flasks of
fermenters taken from 7-21 days.
The isolation, separation and purification of simple lysergic acid derivative
of synthesized alkaloids us done by ways applied for other alkaloids.
The lysergic acid derivative are converted to lysergic acid and further
partly synthesized into ergometrine and other peptide alkaloids.
Color: externally dark violet,
internally whitish or pinkish
Odor: disagreeable or faint
Size: sclerotia 1-3 cm in length &
1-5 cm in width
Shape: sclerotium is fusiform,
triangular and usually tapering on
Fracture: brittle with short
1.Few thin, flattened,
polygonal cells of purple to
dark brown color
2.Inner part made up of dense
pseudo parenchymatous cells
composed of chitin
3.Mycelial cells-central region
are round or oval, thick and
with high refractive walls.
4.Contain cells with fixed oil
5.Sclerotium does not contain
starch, calcium oxalate or any
of lignified tissue.
Indole alkaloids (1-0.25%)
Derivatives of lysergic acid
Lysergic acid: peptide derivative form, peptide alkaloids
Water soluble and insoluble categories.
Laevo form medicinally active and dextro form inert in
Water soluble: laevo-ergometrine, dextro-ergometrinine
Water insoluble: ergotamine, ergosine, & ergotoxin
Pigment, ergosterol, fungisterol, histamine, tyramine,
amino acids, acetyl choline, chitin, up to 30% fixed oil, 8%
Tests for identification:
1. Van-Urk's Reagent (p-dimethyl aminobenzaldehyde
(PDAB) in 15% H2SO4, containing traces of FeCl3) +
Alkaloid → Deep blue color.
2. Ergot + solvent ether + H2SO4 filter filtrate
red-violet color in aqueous layer, when treated with
saturated solution of NaHCO3.
3. Little quantity of ergotamine is dissolved in glacial acetic
acid and ethyl acetate small portion of this is treated
with H2SO4 shaken well by which blue color with red
tinge appears, by addition of FeCl3, blue color deepens,
while red tinge becomes faint.
4. Ergometrine gives a blue fluorescence in water.
Ergonovine: oxytocic, sometimes used to enhance labor
pain in delivery cases, prevent post partum heamprrhage.
Ergotamine tartarate: analgesic, migraine treatment, given
along with caffeine
Ergotoxin methanesulphonates (mesylates): geriatric
Lysergic acid derivative LSD: psychomimetic (controlled
Syn: Adhatoda, Adulsa, Malabar nut
Source: dried as well as fresh leaves of
the plant Adhatoda vasica
Specification: should contain NLT 0.6%
of vasicine of dried basis.
GS: sub himalaya track up to an
altitude of 1000m , Konkan region,
Myanmar, Srilanka, Malaya
Propagation: stem cutting & Seed
Soil: loamy soil
Quinazoline alkaloids: Vasicine up to 2-2.5%, vasicinone,
Vasicine oxidized to ketonic derivative
Volatile oil, betain, vasakin, adhatodic acid
Large dose: irritant & cause vomiting, diarrhoea
Vasicine oxytocic, abortificient (due to release of
Bromhexine HCl synthetic derivative of vasicine which
changes the structure of bronchial asthama & reduces
viscosity of sputum, does not cause drowsiness &
Source: leaves of closely related
plants of the genus Pilocarpus spp
Genus: P. jaborandi, P. pennatifolius, P.
P.microphyllus Maranham jaborandi
is the main source of the drug.
GS: South america: Brazil, Venezuela,
Carribean island, Central america
Imidazole alkaloid: pilocarpine
Isopilocarpine, pilocarpidine, pilosine, pseudopilocarpine and
Pilocarpine solution + dil. H2SO4 + H2O2 + benzene +
Potassium chromate on shaking organic layer bluish
violet color , aq. Layer yellow color
In the form of pilocarpine hydrochloride
Physiological antagonist of Atropine
Acts directly on ANS by post-ganlionic cholinergic nerves.
Contraction of pupil of the eye, Increase sweating & salivation.
Use in ophthalmology in Glaucoma.
Syn: Bachnag, Monkshood
Source: dried root of Aconitum napellus
Should contain NLT 0.6% of alkaloid of
aconite, of which 30% should be aconitine.
GS: Hungary, Germany, Spain, Switzerland,
Wild : A. chasmanthum, A. ferox
Constituents: diterpene alkaloid: aconitine,
hypoaconitine,neopelline, napelline, neoline
and traces of sparteine and ephedrine
Aconitine most important and ether soluble & poisonous
Aconitic acid, succinic acid and starch
Aconitine hydrolysis benzoyl aconine + acetic acid
Benzoyl aconine hydrolysis aconine + benzoic acid
Hydrolysis products are less active.
Highly poisonous drugs, externally in the form of liniment for
neuralgia, sciatica, rheumatism, inflammation, analgesic, cardiac