Lecture No. 3.

Sources and Nature of Drugs

LECTURE NO. 3

Sources and nature of drugs:

Sources of drugs:

The drugs are obtained from four main sources.

I. Natural
II. Synthetic
III. Semisynthetic
IV. Biosynthetic
I. Natural source
It is very important source and provided many important drugs. Drugs are economical
and easily available. Various types of natural sources are:
1. Plants/vegetable source
2. Animal
3. Microorganisms
4. Minerals
1. Plants/Vegetable source
* One of the most important and oldest sources of drugs. The traditional Indian system of
medicines, viz. Ayurveda, Sidha and Unani system are based on use of plants and other
natural substances.
* The pure substances extracted from the vegetable sources which is responsible for the main
biological activity is known as active principle.
* The active principle may act as drug or source of some chemical intermediates needed for
the production of a no. of drugs.
* The active principle may be concentrated in a particular part of plant. The biological
activity of a plant or parts of plant depends upon the presence of these chemicals
constituents.
* These active ingredients are generally purified by various techniques to be used as a drug.

1
Lecture No. 3. Sources and Nature of Drugs
Examples
Plant Part Active Principle Use
1. Cinchona Bark Quinine Antimalarial
2. Urginea or Squill Bulbs Scilliroside Emetic/rodenticide
3. Colchicum Corns Colchicine Antigout
4. Clove Flower/ Flowering Buds Eugenol Local anaesthetic
5. Anise Fruits Anethole Carminative
6. Digitalis Leaves Digitoxin Cardiac Stimulant
7. Rauwolfia Roots Reserpine Antihypertensive
8. Nux vomica Seeds Strychnine Rodenticide

2. Animals Source:
Animal sources provide relatively few but important drugs. Synthesis of these drugs is
very cumbersome and expensive. Some of the important products obtained from animals are.
i) Antisera - Antitetanus serum, canine distemper serum, Haemorrhagic septicaemia
serum
ii) Hormones: Posterior pituitary hormone, insulin, equine chorionic gonadotrophin,
thyroxine.
iii) Enzymes: Trypsin, chymotrypsin, pancreatin, pepsin, fibrinolysin.
iv) Vitamins: Cod-liver oil, halibut liver oil
v) Blood and blood components: Whole blood, plasma, packed red cells, platelets.
vi) Ointment bases: Wool fat, lanolin
vii) Animal extracts and organs: Liver extract, bile, bile acids.

3. Microorganism sources:
Microorganisms are important source of many drugs like antibiotics, vaccines and
vitamins.
i) Antibiotics: Bacitracin, penicillins, cephalosporins, streptomycin.
ii) Vaccines: Anti-rabies vaccines, canine distemper vaccine, anthrax spore
vaccine.
2
Lecture No. 3. Sources and Nature of Drugs
iii) Vitamins: B-complex vitamins (from yeast)

4. Mineral Sources:
Some of the minerals of medicinal value are – Iron, calcium, magnesium, sodium,
potassium, sulphur, zinc etc.
e.g. Bismuth subnitrate – antiseptic
Calcium carbonate – Antacid
Copper sulphate – Emetic
Ferrous sulphate – haematinic
Ferric chloride – styptic

II. Synthetic Source

Synthetic drugs are prepared in laboratory from chemical substances. Most drugs in
use today are synthetic in origin. These drugs are chemically pure and can be manufactured
in bulk to maintain a supply line.
e.g. Diethyl ether, halothane, sulphonamides, aspirin.

III. Semisynthetic Source

These are synthesized from naturally occurring complex chemical. These are neither
pure natural chemicals nor pure synthetic sybstances.
Examples
i) Plant steroid sapogenin are important raw material for the synthesis of steroidal
hormones.
ii) Morphine is used to produce semisynthetic opioid analgesics, viz., oxymorphone and
hydromorphone
iii) Natural penicillin  Semisynthetic penicillins, e.g. ampicillin, cloxacillin.
IV. Biosynthetic Source
Various drugs particularly the polypeptide drugs are synthesized for large scale
production by using recombinant DNA technology.

3
Lecture No. 3. Sources and Nature of Drugs
Such drugs are difficult to obtain in pure form from natural animal sources and are also
difficult to be synthesized in laboratory.
e.g.
i) Biosynthetic human insulin has been prepared by introducing coded DNA into
E. coli.
ii) Recombinant human erythropoietin (rhEPO)
iii) Recombinant bovine somatotrophin
iv) Recombinant feline rabies virus vaccine.

NATURE OF DRUGS

Drugs can be classified in various classes depending upon the physico-chemical

properties of the drugs.
Alkaloids, glycosides and saponins, oils and fats, resins, gums, tannins, waxes, organic
acids
1. Alkaloids
- Alkaloids are complex organic nitrogenous bases, occurring mainly in plants and animals.
- They are alkali-like organic compounds and exhibit basic properties.
- Besides containing carbon, hydrogen and nitrogen, molecules of alkaloids may contain
sulfur and rarely chlorine, bromine or phosphorus. These may or may not contain oxygen.
Oxygen containing alkaloids are solid in nature.
- The first individual alkaloid, morphine, was isolated in 1804 from poppy (Papaver
somniferum).
e.g. Atropine  Atropa belladonna
Strychnine  Strychnos nux-vomica
Quinine  Cinchona plant
Morphine  Papaver somniferum
Cocaine  Erythroxylon coca
Alkaloids free from oxygen are liquid in nature.
Nicotine  Nicotiana tabacum

4
Lecture No. 3. Sources and Nature of Drugs
Lobeline  Lobelia inflata
- All alkaloids as organic bases are insoluble in water (little soluble in alcohol) but soluble
in chloroform and ether.
- They form salts with acids without production of water. These salts are freely soluble
in water but insoluble in chloroform and ether e.g. morphine sulphate, quinine sulphate,
atropine sulphate, strychnine HCl.
- Most alkaloids are incompatible with tannic acid, salt of heavy metals and iodine
solutions. These are oxidized by potassium permanganate.
- Most alkaloids have bitter in taste and produce marked pharmacological actions.
- Their names end with the suffix –‘ine’
2. Glycosides and saponins
- Glycosides are ether like combinations of sugars with some other organic compounds.
These are large compounds and may or may not contain nitrogen & sulphur.
- Their essential elements are carbon, hydrogen and oxygen.
- They are neutral in reaction.
- They donot react with acids to form salts.
- Soluble in water and alcohol and insoluble in ether.
- On acid hydrolysis, the sugar component splits off leaving the residual structure called
genin/ aglycone. The genin may be an alkaloid, tannin, or saponin or a compound of
unknown structure. When sugar present in glycoside is glucose, then called as glucoside,
if it is fructose, then the molecule is a fructoside; if it is glucuronic acid, then the
molecule is a glucuronide; etc. In the body, toxic substances are often bonded to
glucuronic acid to increase their water solubility; the resulting glucuronides are then
excreted.
- Pharmacological properties are inherent in the gennin. The sugar component only
modifies the penetration, persistence and reactivity of the glycosides.
e.g. Digitoxin
Gitoxin Digitalis purpurea
Digoxin
Ouabain – Strophanthus gratus.

5
Lecture No. 3. Sources and Nature of Drugs
The first glycoside ever identified was amygdalin, by the French chemists Pierre
Robiquet and Antoine Boutron-Charlard, in 1830.
Difference in spelling – Like alkaloids their name do not end with ‘e’.

Digitoxin

Classification

Glycosides can be classified by the glycone, by the type of glycosidic bond, and by the
aglycone.

A. By glycone/presence of sugar

If the glycone group of a glycoside is glucose, then the molecule is a glucoside; if it is

fructose, then the molecule is a fructoside; if it is glucuronic acid, then the molecule is a
glucuronide; etc. In the body, toxic substances are often bonded to glucuronic acid to
increase their water solubility; the resulting glucuronides are then excreted.

B. By type of glycosidic bond

Depending on whether the glycosidic bond lies "below" or "above" the plane of the cyclic
sugar molecule, glycosides are classified as α-glycosides or β-glycosides. Some enzymes
such as α-amylase can only hydrolyze α-linkages; others, such as emulsin, can only affect β-
linkages.

There are four types of linkages present between glycone and aglycone:

 C-linkage/glycosidic bond, "nonhydrolysable by acids or enzymes"

 O-linkage/glycosidic bond.

6
Lecture No. 3. Sources and Nature of Drugs
 N-linkage/glycosidic bond
 S-linkage/glycosidic bond

C. By aglycone

Glycosides are also classified according to the chemical nature of the aglycone. For purposes
of biochemistry and pharmacology, this is the most useful classification.

Alcoholic glycosides

An example of an alcoholic glycoside is salicin, which is found in the genus salix. Salicin is
converted in the body into salicylic acid, which is closely related to aspirin and has
analgesic, antipyretic, and antiinflammatory effects.

Anthraquinone glycosides

These glycosides contain an aglycone group that is a derivative of anthraquinone. They have
a laxative effect. They are present in senna, rhubarb and Aloe species.

Coumarin glycosides

Here the aglycone is coumarin or a derivative. An example is apterin which is reported to

dilate the coronary arteries as well as block calcium channels.

Chromone glycosides

In this case, the aglycone is benzo-gamma-pyrone.

Cyanogenic glycosides e.g. Amygdalin from almonds, Dhurrin, linamarin, lotaustralin, and
prunasin. They can also be found in the fruits (and wilting leaves) of the rose family
(including cherries, apples, plums, almonds, peaches, apricots, raspberries, and crabapples).

In this case, the aglycone contains a cyanide group. All of these plants have these glycosides
stored in the vacuole, but, if the plant is attacked, they are released and become activated by
enzymes in the cytoplasm.

7
Lecture No. 3. Sources and Nature of Drugs
Flavonoid glycosides

Here the aglycone is a flavonoid. Examples of this large group of glycosides include:

 Hesperidin (aglycone: Hesperetin, glycone: Rutinose)

 Naringin (aglycone: Naringenin, glycone: Rutinose)
 Rutin (aglycone: Quercetin, glycone: Rutinose)
 Quercitrin (aglycone: Quercetin, glycone: Rhamnose)

Among the important effects of flavonoids are their antioxidant effect. They are also known
to decrease capillary fragility.

Phenolic glycosides (simple)

Here the aglycone is a simple phenolic structure. An example is arbutin found in the
Common Bearberry Arctostaphylos uva-ursi. It has a urinary antiseptic effect.

SAPONINS: These are generally plant glycosides having distinctive property of frothing.
These produce foam when shaken in a solution of water.
- These produce stable emulsion on shaking with oils and fats.
- In terms of structure, by their composition of one or more hydrophilic glycoside moieties
combined with a lipophilic triterpene derivative.
- Saponins are now classed as subgroups of glycosides e.g. digitonin, senegin and
glycerrhizin.
3. OILS AND FATS:
OILS: Oils are diverse substances obtained from plant, animal and mineral sources.
Broadly they are of three types.
i) Fixed oils ii) Volatile oils iii) Mineral oils
Fixed oils (Glycerides):
- These are esters of higher fatty acids and glycerol, which are liquid at room temperature.
F.As can be oleic, palmitic & stearic acid.
- These are insoluble in water but soluble in organic solvents like ether, chloroform etc.
- These have lubricant properties and thus leave permanent greasy spot on the paper.
8
Lecture No. 3. Sources and Nature of Drugs
- They saponify with alkalies to form soaps and glycerol.
- Most of the vegetable fixed oils are bland oils (Non-irritant) and are used as emollient and
vehicle for some other drugs.
- When given internally some of the fixed oils cause irritation in G.I.T. after forming soaps
and thus these may be used as purgatives e.g. castor oil and linseed oil.
- Various examples of fixed oils are castor oil, olive oil, linseed oil, groundnut oil, mustard
oil, cod liver oil and shark liver oil.
- They are chiefly obtained from the seeds of plants. Within the cells, remain present in
droplets or crystal forms.
- These are non-volatile and as such cannot be distilled without decomposition. These are
obtained by the process of expression.
Volatile Oils:
Synthetic essential oils, ethereal oils, aromatic or flavouring oils.
These are diverse chemical compounds obtained from plants and are volatilized by heat
and are extracted by distillation.
Chemically, these are mixtures of alcohols, aldehydes, ketones, esters, phenols, ethers and
terpenes.
The basic building block of many essential oils is a five-carbon molecule called an
isoprene. Most essential oils are built from isoprene. This is the building block that makes
up the terpenoids. When two isoprene units link together, they create a monoterpene;
when three join, they create a sesquiterpene; and so forth. Triterpenoids are some of the
largest molecules found in essential oils. They consist of 30 carbon atoms or six isoprene
units linked together.
- These are secreted in particular secretory cells in the plants which are in abundance in
flowers, leaves and fruits.
- They are colourless liquids or crystalline or amorphous solids.
- Evaporation at ordinary temperature occurs without leaving any greasy spot on paper.
- These are nonlubricating in nature.
- They are soluble in water and miscible in fixed oils and organic solvents.
- Do not form soap with alkalies.

9
Lecture No. 3. Sources and Nature of Drugs
- On cooling these usually separate into liquids (oleoptene) and solids (stearoptene), e.g.
camphor, thymol, menthol.
- Unlike fixed oils, the volatile oils possess diverse pharmacological actions.
o e.g. Oil of peppermint and oil of terpentine are used as carminative and
antizymotics.
o Oil of clove – as local anodyne (analgesic).
o Oil of eucalyptus, T.T. oil, camphor, thymol  counter irritant and expectorant.
- On exposure to light and air, these tend to oxidize and turn rancid.
Examples: Liquid volatile oils –Eucalyptus oil, clove oil, peppermint oil.
Solid volatile oils – camphor, menthol, thymol.
Note: Some volatile oils are not present in living plants but are products of destructive
distillation e.g. creosote and oil of tar.
Now-a-days, they are part of aromatherapy.
Mineral oils:
- Mineral oils are obtained from petroleum by fractional distillation.
- These are mixture of hydrocarbon of methane and related aliphatic series.
- They do not form soap with alkalies.
- Depending upon the size of molecule these are present in different consistencies and have
diverse uses.
- e.g. hard paraffin, soft paraffin, liquid paraffin.
FATS:
- Fats are fixed oils which remain solid or semisolid at ordinary temperature.
- These contain more palmitin and stearin and mostly obtained from animal sources.
- Hydrogenation of vegetable oils can also lead to solidification of oils at room
temperarure.
4. RESINS:
These are brittle amorphous ill-defined solid substances found in plants usually
produced by oxidation and polymerization of volatile oils. These are secreted through
resin ducts.
- They are insoluble in water but soluble in organic solvents and oils.
10
Lecture No. 3. Sources and Nature of Drugs
- These get dissolved in water in presence of some alkali and form non-detergent resin
soaps.
- Resins are usually irritant to mucous membrane and many of them are used as purgatives
e.g. Podophyllum, Jalap and Scamony.
Various types of resins are:
i) Oleoresins: are semisolid mixtures of resins with volatile oils. They are natural
secretions of plants and may vary in composition. e.g. Crude turpentine.
ii) Gum-resins: mixture of resins with gums. e.g. Asafoetida
iii) Balsams: Balsams are oleoresins, which contain benzoic acid or cinnamic acid or
both e.g. Benzoin, Balsam of Peru, Balsam of Tolu.
5. GUMS:
- are excretory products of plants. Chemically these are composed of various
polysaccharides which on hydrolysis yield simple sugars.
- These are colloidal exudates from plants which on drying become transparent and
amorphous solids.
- Pharmacologically, they are inert. Mostly used as suspending agents for insoluble
substances and emulsifying agents for oils.
- Internal administration through oral route may cause laxation. e.g. Gum acacia, gum
tragacanth.
6. TANNINS:
Tannins are complex non-nitrogenous phenolic compounds, which have an astringent
action on mucous membranes.
- They are soluble in water and alcohols but insoluble in ether and chloroform.
- They precipitate with metallic salts, alkaloids and proteins.
- Due to their property to precipitate proteins of m.m. these are used as intestinal astringent
in controlling diarrhoea.
- They are irritant and bitter in taste.
Tannins are of two types.
i) Pyrogallol tannins: - derived from trihydric benzene pyrogallol. Occur in oak galls,
clove, chestnut etc. e.g. Tannic acid obtained from oak gall.

11
Lecture No. 3. Sources and Nature of Drugs
ii) Pyrocatechol tannins: - derived from dihydric benzene catechol. These occur in
catechu, cinnamon and cinchona.
7. WAXES:
- They are esters of higher alcohols (e.g. Acetyl alcohols) with higher fatty acids.
- They are firm in consistency and have high melting points.
- They are insoluble in water but are soluble in many organic solvents.
- They can be saponified by alcoholic alkali e.g. yellow bee’s wax & white bee’s wax.
8. ORGANIC ACIDS:
Several organic acids, viz. citric acid, tartaric acid, benzoic acid and salicylic acid are
present in plants.
- These may be present in free form or as salts of potassium, calcium or magnesium.

*************************

12