Enzymes and modern medicine

Enzymes are biological polymers that catalyse biochemical reactions. The majority of enzymes

are protein with catalytic capabilities. Enzymes are found in all tissues and fluids of the body.

Each enzyme is highly specific to its substrate , determined by it’s three dimensional structure

and the active site’s configuration. Enzyme possesses regulatory functions in cellular and

biochemical processes. Their specificity, efficacy and biocompatibility have made them ideal for

various application in medicine. Immobilised enzymes are used in the manufacture of many

drugs and antibiotics. They are also used as therapeutic agents and in diagnosis of disease .

In recent years, enzymes have risen as promising therapeutic tools for different pathologies, from

metabolic deficiencies, such as fibrosis conditions, ocular pathologies or joint problems, to

cancer or cardiovascular diseases .

Application of enzyme in modern medicines

Enzyme in diagnosis of disease :

Normal serum level of an enzyme indicates the balance between its synthesis and release in the

routine cell turnover. The raised enzyme levels could be due to cellular damage, increased rate of

cell turnover, proliferation of cells, increased synthesis of enzymes etc. Serum enzymes are

conveniently used as markers to detect the cellular damage which ultimately helps in the
diagnosis of diseases. Elevated enzyme levels in blood sample can indicate tissue damage or

metabolic disorder .

Important enzymes in diagnosis of disease :

Serum enzyme (elevated ) Disease

Amylase Acute pancreatitis

Serum glutamate pyruvate Liver disease ( hepatitis)

transaminase

Serum glutamate oxaloacetate Heart attacks ( myocardial

transaminase infarction)

Alkaline phosphate Rickets, obstructive jaundice

Acid phosphatase Cancer of prostate gland

L dehydrogenase Heart attack , liver disease

Aldolase Muscular dystrophy

Therapeutic application

Therapeutic enzymes have been in use for quite a long time and are often considered under

replacement therapies for different diseases. They serve as better therapeutic agents due to their

affinity and high specificity towards target substrates. The most commonly used therapeutic

enzymes are pepsin, β-amylase and lipase used in various combinations to treat common

digestive disorders. Instead of providing intravenous injection, oral administration of enzyme

formulations is used to treat several diseases . Enzymes can be administered individually or

along with other drugs and treatments. Enzyme supplements are used for enzyme deficiencies .
• prolactazyme treats lactose intolerance

• collagenase treats skin ulcer

• Asparaginase is used to treat leukaemia

• Streptokinase is administered to patients immediately after heart attack

Some FDA approved enzyme drugs for various diseases :

Enzyme Disease Mode of delivery

Activase Clot bluster heart attack Intravenous

Ceredase Gaucher disease Intravenous

Phenylase Phenyl ketonuria Subcutaneous

Asparaginase Leukemia Intramuscular/ intravenous

Acid alpha glucosidase Pompe disease Intravenous

Hyaluronidase Adjuvant for absorption Intramuscular

injected drugs

PEGylated arginine Invasive malignant melanoma Intravenous

deaminase

PEGylated urate oxidase Gout Intravenous

Enzymes are used to test potential drug molecules interactions and improving the identification

of therapeutic compound. Prodrugs are activated through enzyme , such as the anticancer drug

capecitabine is activated by thymidine phosphorylase , cyclophosphamide is activated by

aldehyde dehydrogenase for chemotherapy.

body to modulate their activity. Enzyme dysregulation can lead to various diseases . Here are

some drug ( enzyme inhibitors ) that act on body’s own enzyme to maintain normal physiological

process :

Drug Target enzyme Field of therapy

Aspirin Cyclooxygenase Anti-inflammatory

Captoril and enalapril Angiotensin converting Antihypertension

enzyme ( ACE )

Phenelzine Monoamine oxidase Antidepressant

Selegiline Monoamine oxidase -B Parkinson’s disease

5- fluorouracil Thymidylate synthase Anticancer

Allopurinol Xanthine oxidase Treatment of Gout

Pentostatin Adenosine deaminase Antileukaemia

Zileutin 5-lipoxygenase Anti asthmatic

Physostigmine , donepezil , Acetylcholinesterase Glaucoma, Alzheimer’s

tacrine disease

● Overacting of Cyclooxygenase ( COX 1 & 2 ) enzyme leads to excessive prostaglandin

production by converting arachidonic acid into prostaglandin that mediate inflammation, pain

and fever .
Paracetamol reduces fever and pain by primarily acting on COX enzyme . Paracetamol’s main

action occurs in CNS , where it inhibits COX-2 activity more effectively, the inhibition of COX-

2 reduces the production of PGE-2 in hypothalamus , lowering the fever .

● ACE Converts angiotensin I to angiotensin II , which increases blood pressure by constricting

blood vessels . Hypertension and heart failure may occur .

Captoril is an ACE inhibitors that binds to the active site of ACE preventing the conversion of

angiotensin I to angiotensin II . Lower level of Angiotensin II lead to reduced vasoconstriction

causing blood vessels to relax (vasodilation) and manages hypertension .

● Monoamine oxidase breaks down neurotransmitters like dopamine , serotonin and

norepinephrine. The dysregulation may lead to depression and Parkinson disease .

Phenelzine is a MOA inhibitor that irreversibly inhibit both MOA-A & MOA-B , leading to the

decreased breakdown of these neurotransmitters. This medicine corrects the imbalances and

improve mood.

● Xanthine oxidase breaks down purines into uric acid . Over activity leads to uric acid

accumulation, causing joint pain . This condition can lead to Gout.

Allopurinol is a Xanthine oxidase inhibitor . It is structurally similar to hypoxanthine. It acts as a

competitive inhibitor binding to xanthine oxidase and preventing it from converting

hypoxanthine and xanthine into uric acid . By lowering uric acid level , allopurinol prevents the

deposition of monosodium urate crystals in joints and tissues which trigger Gout attacks.
● Acetylcholinesterase’s over activity reduces Acetylcholine levels , impairing memory and

cognition. It can lead to Alzheimer’s disease .

By inhibiting acetylcholinesterase , Physostigmine increases Acetylcholine levels , temporarily

improves memory , attention and improving communication between neurons .

Thus ,various drug acts on enzyme to maintain physiological balance.

Enzymes have profoundly impacted modern medicine , offering solutions to diagnose , treat and

prevent diseases . Despite their vast potential, the use of enzyme in medicine is also challenging.

As research continues, enzyme will play greater role in medicine sector .

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