Dual inhibition of acetylcholinesterase and butyrylcholinesterase enzymes by allicin.

Abstract

OBJECTIVES:

The brain of mammals contains two major form of cholinesterase enzymes, acetylcholinesterase (AChE) and butyrylcholinesterase (BuChE). The dual inhibition of these enzymes is considered as a promising strategy for the treatment of neurological disorder such as Alzheimer's disease (AD), senile dementia, ataxia, and myasthenia gravis. The present study was undertaken to explore the anticholinesterase inhibition property of allicin.

MATERIALS AND METHODS:

An assessment of cholinesterase inhibition was carried out by Ellman's assay.

RESULTS:

The present study demonstrates allicin, a major ingredient of crushed garlic (Allium sativum L.) inhibited both AChE and BuChE enzymes in a concentration-dependent manner. For allicin, the IC₅₀ concentration was 0.01 mg/mL (61.62 μM) for AChE and 0.05 ± 0.018 mg/mL (308.12 μM) for BuChE enzymes.

CONCLUSIONS:

Allicin shows a potential to ameliorate the decline of cognitive function and memory loss associated with AD by inhibiting cholinesterase enzymes and upregulate the levels of acetylcholine (ACh) in the brain. It can be used as a new lead to target AChE and BuChE to upregulate the level of ACh which will be useful in alleviating the symptoms associated with AD.

• Authors: Suresh Kumar
• Journal: Indian journal of pharmacology (Indian J Pharmacol) 2015 Jul-Aug Vol. 47 Issue 4 Pg. 444-6 ISSN: 1998-3751 [Electronic] India
• PMID: 26288480 (Publication Type: Journal Article)

Chemical References

• Cholinesterase Inhibitors
• Disulfides
• Sulfinic Acids
• allicin
• Acetylcholinesterase
• Butyrylcholinesterase

Topics

• Acetylcholinesterase (drug effects)
• Animals
• Butyrylcholinesterase (drug effects)
• Cattle
• Cholinesterase Inhibitors (administration & dosage, pharmacology)
• Disulfides
• Dose-Response Relationship, Drug
• In Vitro Techniques
• Inhibitory Concentration 50
• Sulfinic Acids (administration & dosage, pharmacology)