BIOTRANSFORMATION OF ANTIBIOTICS, STEROIDS

AND THEIR APPLICATIONS.

Biotransformation of steroids and antibiotics

-Suraj Begoor

What is Biotransformation?

Biotransformation is the chemical modification (or modifications) made by an organism on a chemical compound.

If this modification ends in mineral compounds like CO2, NH4

+, or H2O, the biotransformation is called mineralisation.

Biotransformation means chemical alteration of chemicals such as nutrients, amino acids, toxins, and drugs in the body.

Biochemical event in which a drug molecule is converted from a non polar molecule to a polar molecule through a series of reactions mainly involving enzymes is called as Biotransformaion.

PHASE I Converts non polar molecules into

relatively polar molecule . Exposing or adding a polar or

reactive group. Reactions such as , 1. oxidation 2.Reduction 3 .Dehalogenation. 4. Desulfuration. etc

ENZYMES Monooxygenases Oxidases . Reductases. Nitroreductases. Hydrolases. Azoreductase . Esterases , etc

Microsomal oxidation Salicyclic acid

Non microsomal oxidation

Ethyl alcohol carbon dioxide

and water.

CH3OH formic acid and

formaldehyde

Gentisic acid

Hydrolysis Pethidine procaine

(analgesic).

Digitalis ( leaf drug)

( only life saving cardiovascular drug)

esterases

Digoxin

PHASE II Attach small polar ionisable

endogenous compounds such as glucoronic acid, glycine and other amino acids to functional group.

Enzymes such as , acetyltransferase, methytransferase, acyltransferase etc

FACTORS that affect Biotransformation

Diet. Hormonal status. Age. Disease . Liver function. Chemicals . Enzymes .

Types of Transformation.

Inactivation Activation Intoxication Change of activity.

INACTIVATION

Phenobarbital p- hydroxy phenobarbital

glucoronide

ACTIVATION

INTOXICATION

p- phenatidine

deacetylation

Change of Activity

iproniazide isoniazide

Biotransformation of steroids.

Progesterone

pregnadiol

Plant Biotransformation. CHOLESTEROL

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DIOSOGENIN

BIOTRANSFORMATION OF ANTIBIOTICS

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