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Post# of 148179
https://pubmed.ncbi.nlm.nih.gov/24868872/
Isocorilagin, a Cholinesterase Inhibitor From Phyllanthus Niruri
Yee-Hui Koay, Alireza Basiri, Vikneswaran Murugaiyah, Kit-Lam Chan
PMID: 24868872
Abstract
Drugs that have dual inhibition of acetylcholinesterase (AChE) and butyrylcholinesterase (BChE) produce better clinical efficacy against Alzheimer's disease (AD) than those that selectively inhibit one enzyme. A dual cholinesterase inhibitory-guided fractionation of Phyllanthus niruri leaves afforded isocorilagin, a bioactive tannin possessing good inhibitory activities against AChE (IC50: 0.49 microM) and BChE (IC50: 4.20 microM). Interestingly, isocorilagin was relatively 2- to 3-fold more potent than galanthamine, the clinically used inhibitor. The kinetic analyses suggested that isocorilagin was a non-competitive inhibitor for AChE and an uncompetitive inhibitor for BChE, with calculated Ki values of 1.49 microM and 2.86 microM, respectively. In silico molecular docking revealed that isocorilagin effectively blocked the substrate entry by forming hydrogen bonding with residues at the entrance of the AChE active site. With BChE, the compound completely docked inside and occupied the active site of the enzyme. This study demonstrated for the first time the potent cholinesterase inhibitory activities of isocorilagin, a promising lead that is worthy of further investigation.
Chemical Components and Biological Activities of the Genus Phyllanthus: A Review of the Recent Literature
Medicinal plants have served humans since prehistoric times to treat various ailments. Both developed and underdeveloped countries rely on traditional systems of medication using natural sources from plants. Phyllanthus is one of the largest genus in the family Phyllanthaceae, comprising over 700 well known species cosmopolitan in distribution mainly in the tropics and subtropics. Phyllanthus species are being in constant used in traditional medications to cure an array of human diseases..and now are being used in practical clinical trials
https://www.ncbi.nlm.nih.gov/pmc/articles/PMC6222918/