Introduction to Alkaloides

 Extremely difficult to define because these do

not represent homogeneous compounds either
from, Chemical, biochemical or physiologic view
point. Except the fact, all Alkaloids are, Organic
Nitrogenous compounds and are of basic nature
and have some definite pharmacological activity.
 “Basic Nitrogenous compounds of natural origin
having some definite pharmacological/
physiological activity.”
 They are alkali like compounds therefore they
are called Alkaloids.
 Distribution of Alkaloids:
 Angiosperms
  Leguminosae
  Papaveraceae
  Ranunculaceae
  Rubiaceae
  Solanaceae
  Berbaridaceae
  Plant families Labiatae and Rosaceae are almost free of

Alkaloids

 Gymnosperms
  Rarely contain Alkaloids like Taxaceae family
 Occurrence of Alkaloids:
 Alkaloids occur in,
  Seeds  Physostigma, Areca
  Fruits  Conium
  Leaves  Belladonna, Coca
  Underground stem  Sangunaria
  Roots  Belldonna
  Roots and rhizomes  Ipecac, Hydrastis
  Barks  cinchonna
  Fungi  Ergot
 Taxonomy of Alkaloids:
 They can be named on basis of,
  Genus name of plant  Hydrastine, Atropine

  Species name of plant  Cocaine, belladonine

  Common name of plant  Ergotamine
  Pharmacological activity  Emetine, Morphine
  Ocassionally on the name of discoverer 

Ajmaline, Pelletiernine
 Properties of Alkaloids:
 Alkaloids usually contain 1 Nitrogen atom.

Some may contain up to 5 nitrogen atoms.

Nitrogen may exist as;
 1. Primary amine R – NH2
 2. Secondary amine R2 – NH
 3. Tertiary amine R3 – N
 4. Quaternary amine R4 – N+X-
 Physical properties:
 The various physical properties are;
  Alkaloids are usually bitter in taste
  Alkaloids are insoluble or sparingly soluble in water.,
but alkaloidal salts are freely soluble in water
  Free Alkaloids are usually soluble in ether, chloroform
and other relatively non polar solvents.
  Most of the alkaloids are crystalline solids, few
Alkaloids are amorphous
  Some are liquids (usually which lack oxygen) like
Nicotine, Conine and sarpenteine.
  Alkaloidal salts are also crystalline in nature
 Role of Alkaloids in Plants:
 In plants alkaloids performs various functions given

below;
  Poisonous agents protecting plants against insect

and herbivores attack

  End products of detoxification reactions, so are

metabolic locking-up of compounds harmful to plants

  Regulatory factors

  Reserve substances for supplying Nitrogen and

other elements to plants

  Like many other secondary metabolic products
 Pharmacological activities of Alkaloids
 Alkaloids are capable of extensive pharmacological activity

and display variety of pharmacological actions like Alkaloids

are,
 1. Analgesics and Norcotics  Morphine, Codeine
 2. Central NS Stimulants  Strychnine, Brucine
 3. Mydriatics  Atropine
 4. Myotics  Physostigmine, Pilocarpine
 5. Hypertenssives  Ephedrine
 6. Antihypertenssives  Reserpine
 7. Anti malarials  Quinine
 8. Antiarrhythmic  Quinidine
 9. Oxytocic agent  Methyl Ergonovine
 Classification of Alkaloids
 Alkaloids are generally classified by;
 Their molecular precursors, based on the biological

pathway used to construct the molecule. From

Structural point of view, alkaloids are divided
according to their shape and origins.
 Alkaloids are classified in three main types,
 1. True Alkaloids  Derived from Amino acids
 2. Proto Alkaloids  Derived from Amino acids
 3. Pseudo Alkaloids  Not derived from Amino

acids
 1. True Alkaloids:
 These are derived from Amino acids. They share
heterocyclic ring with Nitrogen. They are highly reactive
substances with biological activity at low doses. Most of the
alkaloids belongs to this group. They occur in plants,
 1. In Free State
 2. As salts
 3. As N-oxides

 Primary precursors of these Alkaloids are amino acids, like

L-ornithin, L-Lysine, L-Phenylalanine, L-Tyrosine, L-
Tryptophan, and L-Histidine
 Proto alkaloids:
 They are derived from Amino acids. The N-

atom derived from an amino acid is not a part

of the heterocyclic ring. They are structurally
simple alkaloids. The minority of the
alkaloids belongs to this group.
 These are derived from L-tyrosine and L-

tryptophan
 Pseudo alkaloids:
 These are basic carbon skeletons of which are not derived
from amino acids. There synthesis is connected with
amino acid pathways. They are derived from the Pre-
cursors or post-cursors of amino acids and are
synthesised from amination or tans-amination reactions
of thesis pre and post cursors.
 These can also be derived from non-amino acid
precursors. The N-atom can also be donated by amino
acids source across a tans amination reaction, if there is a
suitable aldehyde or ketone group.
 N-atom is inserted into the molecule at a relatively late
stage for example steroidal or triterpenoid skeleton.
Chemical classification of alkaloids

 1. Pyridine-piperidine alkaloids

 Drugs: Areca nut, Lobelia, Tobacco

 2. Tropane Alkaloids

 Drugs: Belladonna, Hyoscyamus, Stramonium, Cocaine

 3. Quinoline Alkaloids

 Drugs: Cinchona
 4. Isoquinoline Alkaloids

 Drugs: Ipecacuanha, Opium

 5. Indole Alkaloids

 Drugs: Rauwolfia, Catharanthus, Nux-vomica, Physostigma, Ergot

 6. Imidazole Alkaloids

 Drugs: Pilocarpus
 7. Steroidal Alkaloids

 Drugs: Veratrum
 8. Alkaloidal Amines

 Drugs: Ephedra, colchicum

 9. Purine bases
 Drugs: Tae, Coffee
Extraction of alkaloids
 Extraction of alkaloids can be carried out in
either of the two bases;
  Basic character
  Solubility profile

 Generally alkaloids are extracted mainly using

two methods;
  Method A: (for alkaloidal salts)
 The powdered material that contains alkaloidal salts is
moistened with alkaline substances like sodium
bicarbonate, ammonia, calcium hydroxide etc. which
combines with acids, tannins, and other phenolic
substances and sets free the alkaloidal bases.
 Extraction is then carried out with organic solvent such as
ether or petroleum spirit. The concentrated organic liquid
is then shaken with aqueous acid and allowed to
separate. Alkaloid salts will be present in aqueous liquid,
while many impurities remain behind in the organic
liquid.
  Method B: (for alkaloidal base)
 The collected powdered material is extracted with water or
aqueous alcohol containing dilute acid. Chloroform or other
organic solvents are added and shaken to remove the
pigments and other unwanted materials.
 The free alkaloids are the precipitated by the addition of
excess alkalis like sodium bicarbonates, or ammonia and
separated by filtration or by extraction with organic solvents.
 Volatile liquid alkaloids (nicotine & coniine) are isolated by
distillation. The powdered material that contains alkaloids is
extracted with water and the aqueous extract is made alkaline
with sodium carbonate or ammonia and alkaloidal base is
distilled off in steam this could be collected and purified.
1. Pyridine-piperidine alkaloids:

 The class include tobacco, areca nuts, and lobelia.

 (i) Tobacco

 Botanical origin: Nicotiana tobaccum

 Family: Solanaceae
 Part used: Dried Cured leaves
 Habit: Perennial herb
 Habitat:
 It is cultivated in many countries, majorly found in
India, USA, China, Brazil, Russia, Italy and Turkey.
 Constituents:
 It contains Pyridine-piperidine alkaloids, major

is nicotine, nicotianine, nicotinine and nicoteine.

Nicotine is primarily synthesize in roots, by
demethylation takes place in leaves.
 Tobacco smoking is not as much dangerous as

for the smoker as its smoke for the others

people. Because tobacco alkaloids especially
nicotine decompose to furfural, collidine,
carbon monoxide and HCN. As, all are toxic so
are dangerous for health.
 Structure and Medicinal uses:
 - It is used as sedative.
 - It is used as Diuretic.
 - It is used as expectorant.
 - It is used as Antiseptic.
 - It is used as insecticide.
 - It is used as stimulant of heart and nervous

system.
(ii) Areca nuts

 Botanical origin: Areca catechu

 Family: Palmae
 Part used: Areca nut (Seeds) obtained from fruit.
 Habit: Tree
 Habitat:
 It is found in East Indies, India, Southern Eastern Asia,
and some parts of East Africa and Sri-Lanka. India is
the major producer of the plants and also a huge
consumer of the drug. Major world supplies come from
Sri Lanka. India also import it from Sri Lanka.
 Constituents:
 It contains alkaloids and tannins. The taenifuge properties

were discovered in 1863. Chemically contains different

alkaloids which are derivative of pyridine, major are;
aracoline, arecaidene, guavacine, guavacoline.
 Medicinal uses:
 - It is used as anthelmintic especially as wormicide and

taenifuge. As anthelmintic areca nuts are used in sheep,

dogs, and horses.
 - In veterinary medicine first betel nuts are used for

chewing purposes and dried betel nuts are used in

medicine.
 - Its usual dose is 2g to 4g in dogs and 4g to 8g in horses.
(iii) Lobelia

 Botanical origin: Lobelia inflata

 Family: Lobeliaceae

 Part used: Dried leaves and Aerial tops

 Habit: Annual herb

 Habitat:

 It is found in Eastern and Central America. Major

supplies are from Virginia, Carolina, and Tennessee.

 Constituents:

 It mainly contain alkaloids. 14 different alkaloids have

been identified. The active constituent of drug is L

 Medicinal uses:
 - It is used in the treatment of the

combination therapy of peptic ulcer,

functional digestive disorders including
spastic, mucus & ulcerative colitis.
 - Due to anticholinergic properties, it is used

to control excess motor activity of GIT and

spasm of urinary track.
 - It is used as anticholinergic i.e. anodyne,

diuretic & as mydriatic agent.

 2. Tropane alkaloids:
 The tropane nucleus is made up of pyrrole

and pyridine nucleus. The class include

Belladonna, Hyoscyamus, Stramonium, and
Cocain.
(i) Belladonna

 Common name: Deadly nightshade

 Botanical origin: Atropa belladonna
 Family: Solanaceae
 Part used: Dried leaves and flowering tops
 Habit: Perennial herb
 Habitat:
 Indigenous to southern and Central Europe &
Asia. Cultivated in England Germany and USA.
 Constituents:
 It mainly contains Tropane alkaloids. The
prominent alkaloidal base is L-Hyoscyamine.
Among the others there is Atropine,
Apotropine, Belladonine.
 Among the volatile bases there is Homatropine,
Rutin, N-oxide and N-methyl pyrroline.
 Medicinal uses:
 - It is used in the treatment of the

combination therapy of peptic ulcer,

functional digestive disorders including
spastic, mucus & ulcerative colitis.
 - Due to anticholinergic properties, it is used

to control excess motor activity of GIT and

spasm of urinary track.
 - It is used as anticholinergic i.e. anodyne,

diuretic & as mydriatic agent.

(ii) Hyocyamus

 Common Name: Henbane

 Botanical origin: Hyocyamus niger
 Family: Solanaceae
 Part used: Dried leaves and flowering tops
 Habit: Biennial herb
 Habitat:
 Indigenous to Europe, Asia & Africa. Cultivated
in England, Germany and Belgium.
 Constituents:
 It mainly contains Tropane alkaloids. The main
alkaloid is Hyoscyamine together with small
quantities of Atropine & hyocine (scopolamine).
 Among the other constituents, there is
mucilage, albumin and calcium oxalate crystals.
 Medicinal uses:
 - It is used as Antispasmodic.
 - It is used as mild Diuretic.
 - It is used as Hypnotic.
(iii) Stramonium

 Common Name: Commonly called Jimson

Weed and Devil’s apple
 Botanical origin: Datura stramonium
 Family: Solanaceae
 Part used: Dried leaves and flowering tops
 Habit: Biennial herb
 Habitat:
 Indigenous to Europe, Asia & Africa. Cultivated in England
Germany and Belgium.
 Constituents:
 It mainly contains Tropane alkaloids. The main alkaloids
are Hyoscyamine, Atropine, Hyocine (scopolamine). All
three are tropane alkaloids. L & D hyoscyamine both are
present in the hyocyamus. The racemic of these both two
is Atropine or when extracted these both two are
converted into Atropine.
 Among the other constituents there is proteins i.e.
albumin, 6-hydroxy Hyoscyamine, acetyl derivatives of
caffeic acid, feurlic acid and para coumaric acid.
 Medicinal uses:
 - It is used as antispasmodic.
 - It is used as anodyne.
 - It is used as narcotic.
 - It is used to treat the spasm of bronchioles

in asthma.
 - It is used to treat Parkinsonism, boils, sores

and fish bite.

(iv) Cocaine

 Botanical origin: Erthroxylum coca

 Family: Erthroxylaceae
 Part used: Dried leaves
 Habit: Perennial tree
 Habitat:
 It is found in Europe, USA, Russia and

sovereign union.
 Constituents:
 Erthro means ‘Red,’ Xylum means ‘wood,’ while’
coca is means ‘tree.’ It mainly contains Tropane
alkaloids. The major alkaloid is cocaine.
 Medicinal uses:
 - 1% solution of cocaine is used as local
anesthetic.
 - Cocaine hydrochloride is also used as local
anesthetic in 2 to 4 % concentration.
 - It is a component of brompton's cocktail (pain
killer).
3. Quinoline Alkaloids:

 Cinchona
 Common name: Cinchona bark, Countess

Bark, Peruvian bark

 Botanical origin: Cinchona succirubra,

Cinchona ledgeriana, Cinchona calisaya,

Cinchona officinalis
 Family: Rubiaceae
 Part used: Dried bark of stem and roots
 Habit: Tree
 Habitat: Indigenous to Central and Southern

America. Before World War 2 major supplies

were from Java (Indonesia).
 Constituents:
 Over 30 different alkaloids have been isolated

from plant. All are quinolone derivative. Major

alkaloids are cinchonidine, cinchonine (both
are isomer), and quinine, quinidine (both are
isomer).
 6-methoxy cinchonine is Quinine. While, 6-

methoxy cinchonidine is Quinidine.

 Medicinal uses:
 - It is used to treat malarial fever.
 - These alkaloids works against plasmodium and

its different species.

 - It is used as analgesic.
 - Quinine is mainly used as antimalarial drug.

Some alkaloids are used as cardiac depressants.

 - Quinidine is employed as antiarrhythmic drug,

in ventricular fibrillation. For this purpose 800mg

dose is given with a maintainace dose of 600mg.
4. Isoquinoline Alkaloids:

 The class include ipecac and opium.

 (i) Ipecac
 Botanical origin: Cephaelis ipecacuanha, Cephaelis
acuminata
 Family: Rubiaceae
 Part used: Dried Roots and Rhizomes
 Habitat:
 It is mainly cultivated in Brazil. Brazil is also a major
exporter of the drug. Some cultivation is also carried
out in Malaysia and India.
 Constituents:
 It contain isoquinoline alkaloids. The major

alkaloids are emetine, cepheline and

psychotrine.
 Medicinal uses:
 - It is used as emetic. Ipecac syrup is

available in market which is used for this

purpose.
Opium

 Common name: Post, Afim

 Botanical origin: Papaver somniferum
 Family: Papveraceae
 Part used:
 Dried milky latex obtained by the incision of

fully grown but unripe capsules.

 Habit: Annual herb
 Habitat:
 The drug is cultivated in India, Persia,

Macedonia, Turkey, China, Afghanistan and

Pakistan.
Cultivation and Collection:

 It is cultivated in October with selective seeds. After growth

of about 2cm to 3cm plant out, winter season starts at that
time growth retarded. In spring season, it grows little. When
seedlings are of 12cm to 14cm, thinning of seeds are done.
Flowers occur in June and July. Purple white or yellow flower
and poppy start growing on each plant.
 When capsule start maturing from purple to yellow the
constituents are at its peak. Cuts are applied so that
endocarp don’t get damage. Latex oozes out, initially it is
white but on exposure to sun and it turns brown.
 Latex is converted into kneaded into small box and packed
in opium leaves and is shade dried and these balls are crude
opium.
 Constituents:
 Over 30 different alkaloids have been derived
from opium. Major alkaloids are morphine 4% -
21%, thebaine, noscapine, codeine, codinone 0.8%
- 2.5%, papaverine and protopine.
 There are three varieties of opium which are
commercially available;
  Indian opium, previously it was considered
good but not now available in markets.
  Chinese opium, it is of best quality.
  Turkish opium
 Medicinal uses:
 - It acts on CNS initially a stimulant action

but then a depressant action of them.

 - These are potent analgesics.
 - Especially they are used in Cancer induced

pains.
 - One of the major back draw of these drugs

is addiction.
 - They are used to treat cough especially

codeine, an ingredient of cough syrups.

5. Indol Alkaloids:

 A number of theraputic drugs belongs to this

class. The drugs of this class are;
 1. Nux-vomica (strychnine, brucine)
 2. Rauwolfia (serpentine, ajmaline)
 3. Catharanthus (vincristine, vinblastine)
 4. Ergot (ergotine, ergotamine)
 5. Physostigma (physistigmine)
(i) Rauwolfia

 Common name: Snake root

 Botanical origin: Rauwolifia serpentina
 Family: Apocynaceae
 Part used: Dried roots but sometimes rhizomes and
stem cuttings are also used.
 Habit: It is 1 meter tall erect shrub with wiry roots
 Habitat:
 It is found in India, Burma, Sri-Lanka, Vietnam,
Malaysia, Indonesia, and Philippines. It is also present
in the hot climates of the world. Major supplies are
form India and Thiland.
 Constituents:
 Over 50 different alkaloids have been isolated,

major are reserpine, serpentine, resepinine,

ajmaline, and isoajmaline.
 Medicinal uses:
 - It is used as hypotensive sedative agent.

Especially, reserpine is antihypertensive agent. It

slows down the pulse rate and produce euphoria.
 - It is used to treat cardiac arrhythmia.
 - It is used as hypnotic agent.
 - It is used to treat neuro-psychotic disorders.
(ii) Catharanthus

 Botanical origin: Vinca rosea, Catharanthus

roseus
 Family: Apocynaceae
 Part used: Dried whole plant parts
 Habitat: It is native to Madagascar but it is

cultivated as ornamental plant cell over the

world in tropical areas.
 Constituents: It contain indol-indolene alkaloids in it.
The major alkaloids are vinblastine, vincristine,
venerosine and extra. Vincristine and vinblastine are
unstable and need refrigeration 0oC – 8oC.
 Medicinal uses:
 - It is used to treat various cancers.
 - Vinblastine sulphate used to treat ovarian cancer, it is
resistant to other therapies.
 - Vinblastine is also used to treat Hodgkin’s disease.
 - Vincristine sulphate is used in combination with
anticancer agents to treat Hodgkin’s disease.
 - Vincristine is also used to treat leukemia.
 (iii) Nux-vomica
 Botanical origin: Strychnos nuxvomica
 Family: Loganiaceae
 Part used: Dried ripe seeds
 Habitat It is found in Africa and Sri Lanka.
 Constituents:
 It contain different alkaloids. The major

alkaloids are brucine, loganine, Strychnine.

The total alkaloidal content is about 3% to 5%.
Strychnine constitute 1/3rd of total alkaloids.
 Strychnine is major alkaloid and is more

pharmacologically active. It is present in the

thick walled endospermic cells present in the
center of the cell. While, brucine is present in
the outer part of the seeds.
 Medicinal uses:
 - They are not currently employed in the

medicine but are used in neuroanatomical

research.
 - These are CNS stimulants.
 - It is used as Pesticides specially to kill rodents.
 - Strychnine is more toxic than brucine it is used

for alcohol denaturing.

 - It is used as tonic for sexual impotence.
 - It is used to produce paralysis of intestine.
(iv) Physostigma

 Botanical origin: Physostigma venenosum

 Family: Leguminosae
 Part used: Dried Ripe seeds
 Habitat:
 It is found in West Africa and in the vicinity of

gulf of Guinea. Plant contains poisnous

alkaloides.
 Constituents:
 It contain contain alkaloids. The total

alkaloidal content is 0.15%. The major

alkaloids are physostigmine (serine),
physovenine, esramine, and genesine.
 Medicinal uses:
 - They are used as a reversible inhibitors of

choline esterase.
 - 0.25% ointment of physostigmine is used

topically on conjunctiva 3 to 4 times a day.

 - Physostigmine potentiated the effects of

Acetyl choline.
 - It is used as antidote for anticholinergic

inhibitors.
(v) Ergot

 Botanical origin: Secale cereale

 Family: Graminae
 Part used: Dried sclerotium developed on rye

plant
 Habitat: It is found in Yugoslavia, Switzerland,

Hungary, and Czechoslovakia.

 Collection: The ergot is formed by the fungus

Cleviceps purourea (Clavicipitaceae or

Hypocreaceae).
 Asexual stage:
 In spring season one of the fungal spore come in contact with

rye plant. It resides over the ovary. Hyphal strands are

produced which penetrate into the ovary for nutrition. Fungus
is parasitic in nature. Hyphal strands will eventually from a
soft white mass called mycelium. Some of the hyphal strands
in mycelium will produce asexual spore called conidiospores.
These conidiospores will be suspended in honey dew (a
secretary secretion of mycelium). Insects will be attracted to
honey dew. Conidiospore than will be carried to another host
plant through the insect to repeat the cycle. This stage of
development is called asexual or Sphacelial stage.
 Sexual stage:
 In this stage of development the mycelium grown in

size and eventually replace entire ovary to form soft

white color mass which over the time will become
hard and purple in color to form Seclerotia. These
seclerotia will fall down on ground over the winter
season.
 In the start of spring season sexual spores will be

produced in seclerotium and will repeat the entire

cycle. This stage of development is called sexual or
Ascigerous cycle.
 Constituents:
 It contain indole alkaloids more specifically

ergot alkaloids are derivatives of Lysergic

acid LSD. The total alkaloidal content is
0.15%. The major alkaloids are ergotmine and
its isomer ergotaminine, ergonovine,
erginine, methyl ergonovine.
 Medicinal uses:
 - It is used as oxytocic agent (increase

uterine muscle contractions), these include

strong uterine muscle contraction.
 - It is used in labour room to facilitate the

baby birth.
 - It also help to prevent post-partum

haemorrhage.
 - It is used to treat migraine. They produce

vasodilation and decrease blood pressure.

6. Imidazole Alkaloids:

 These alkaloids contain imidazole ring in their

chemical structure. The class includes Pilocarpus.
 (i) Pilocarpus

 Common name: Jaborandi

 Botanical origin: Pilocarpus jaborandi
 Family: Rutaceae
 Part used: Dried leaflets
 Habit: Shrub
 Habitat: It is indigenous to Brazil.
 Constituents:
 It contain imidazole alkaloids the major alkaloids are
pilocarpine, iso-pilocarpine, pilocarpidine, psilocine. Bur,
pilocarpine is more therapeutically active.
 Pilocarpine is a hygroscopic compound. It is a liquid alkaloid at
room temperature but its salts are crystallized in nature.
Pilocarpine hydrochloride and pilocrpine nitrate are
therapeutically used.
 Medicinal uses:
 - Pilocarpine hydrochloride and pilocrpine nitrate are used as
cholinergic agonist.
 - Topically applied to conjunctiva to treat glaucoma.
 - It is also used orally or simultaneously at dose of 5mg in
patients using ganglion blocking agents.
7. Steroidal Alkaloids:

 These alkaloids contain steroidal ring in their structure. The

class includes Veratrum.
 (i) Veratrum
 Common name:
  American hellebore
  European hellebore

 Botanical origin:
  Veratrum viridi
  Veratrum album

 Family: Liliaceae
 Part used:
  Dried rhizomes and roots
  Dried rhizome

 Habit: Shrub
 Constituents:
 These alkaloids have cholesterol like structure. Basic ring is present
in such alkaloids is perhydrocyclopentano phenantherine ring.
 There different types of alkaloids are present in Veratrum viridi are;
  Group 1: esters of alkamine with organic acids. For example;
Cevadine, Germidine, Germitrine, Neogermitrine, Protoveratrine A
and Veratrine.
  Group 2: glucoalkaloids or glucoalkamines. For example;
pseudojervine and veratrosine.
  Group 3: alkamines. For example; Germine, rubijervine and
jervine.

 While, Veratrum album contains Protoveratrine A & B.

 Medicinal uses:
 - It is used as hypotensive agent.
 - It is used as depressant of cardiac and

respiratory system. Therefore, their used in

USA discontinued but at dose of 100mg
veratrum alkaloids precisely lowers the blood
pressure without effecting heart rate.
8. Alkaloidal amines:

 These alkaloids do not possess nitrogen

containing heterocyclic ring. The nitrogen atom
is present outside the ring. They do not possess
alkaloidal properties but they gives positives
tests with basic reagents i.e. Hager’s reagent,
Wagner’s reagent etc.
 The class includes Ephedra and colchicum.

These are simple amines or their derivatives.

They are biosynthesized by the phenyl alanine
and tyrosine.
 (i) Colchicum
 Botanical origin: Colchicum luteum,

colchicum autmnale
 Family: Liliaceae
 Part used: Dried ripe seeds and corms
 Habit: Herb (maximum height 60 – 90 cm)
 Habitat: It is indigenous and cultivated in

England, USA, and Africa. In USa it is

cultivated as ornamental plant.
 Constituents:
 Colchicum seeds and corms are collected for alkaloids. Major alkaloid
is colchicine, it is present about 0.5% in seeds and 0.6% in corms.
 Colchicine is a compound which lack pronounced basicity and
alkaloidal properties i.e. it doesn’t form alkaloidal salts but it
conventionally placed in alkaloids because it gives positive basic
tests for alkaloids.
 Uses:
 - It is used as gout suppressant. For this purpose 500μg – 650μg are
administered at the rate 1 – 3 times a day orally. The IV dose is
500μg – 1mg daily.
 - It is used as a mitotic poison therefore employed in agriculture for
polyploidy agent.
 - It is used in treating different tumours owing to their ability to stop
mitosis.
 (ii) Ephedra
 Botanical origin:
  Ephedra sinica
  Ephedra equisetina
  Ephedra distachya

 Family: Gnetaceae
 Part used: Whole herb
 Habitat:
 It is indigenous to the China, also found in India,

Pakistan, Indonesia, and Spain. Plants usually grows

in sandy clay soil. It has been used in medicine since
5000 years especially in Chinese medicine system.
 Constituents:
 It contain Ephedrine, which is alkaloidal amine and is

biosynthesized from phenyl alanine amino acid.

Ephedrine is therapeutically active compound.
Pseudoephedrine is also present in plant to a lesser
extent.
 Uses:
 Ephedrine HCl and Ephedrine SO4 used therapeutically. Both
these drugs are soluble in water and in hot alcohol but are
soluble in ether.
 - Ephedrine HCl is sympathomimetic drug. It increases the
blood pressure.
 - It is a CNS stimulant.
 - Ephedrine SO4 is used as vasoconstrictor and bronchodilator.
 - Both these salts are used to treat asthma and hay fever.
 - Ephedrine and pseudoephedrine are used in cough syrup as
antitussive agent.
 - Ephedrine is a cardio stimulant drug.
 - It is a potent vasoconstrictor.
9. Purine bases:

 They are also known as purine lakloids.

Purine ring is formed of two rings.
  Pyrimidine ring
  Imidazole ring
 The class includes only two drugs;
  Coffee
  Tea
 (i) Coffee
 Botanical origin: Coffea arabica
 Family: Rubiaceae
 Part used: Dried roasted seeds/ beans
 Habit: Shrub
 Habitat:
 Coffee is from Turkish word or Arabic word ‘quveh’ or ‘quhah’.
Arabica shows the habitat. It is indigenous to Ethiopia and
Eastern Africa. It is also cultivated world over in Tropical
countries mainly in Indonesia, Sri Lanka, Central & Southern
America and Brazil. Brazil is the major producer. It produces
600,000 tons of coffee. The yield of coffee is 0.5kg – 5kg per
plant.
 Constituents:
 Tea contain xanthine derivatives. Caffeine (1,

3, 7-trimethyl xanthine), theophylline (1, 3-

dimethyl xanthine), tannins (gallotannic acid),
Theobromine (1, 7-dimethyl xanthine),
proteins and volatile oils. Aroma is due to
volatile oil.
 Uses:
 The usual cup of tea contain 60mg of caffeine in it.

 - Caffeine is CNS stimulant.

 - Caffeine is used as stimulent of cardiac and respiratory center.

 - Caffeine also acts in smooth muscles and kidneys.

 - Tea is astringent due to tannins.

 - Theophylline is smooth muscle relaxant.

 - Theophylline is used as bronchodilator in asthma.

 - Theophylline is used as diuretic in cardiac patients.

 - Theobromine is also used as smooth muscle relaxant and

diuretic but it is ppreferred over theophylline because it doesn’t

act of CNS system as theophylline.
 - It is preferred in patients having Chronic heart failure of angina.