Garcinexanthone G, a selective butyrylcholinesterase inhibitor from the stem bark of garcinia atroviridis

Kooi Yeong Khaw, Vikneswaran Murugaiyah, Melati Khairuddean, Wen Nee Tan

Research output: Contribution to journalArticleResearchpeer-review

3 Citations (Scopus)

Abstract

The present study was undertaken to investigate the isolated compounds from the stem bark of Garcinia atroviridis as potential cholinesterase inhibitors and the ligand-enzyme interactions of selected bioactive compounds in silico. The in vitro cholinesterase results showed that quercetin (3) was the most active AChE inhibitor (12.65 ± 1.57 μg/ml) while garcinexanthone G (6) was the most active BChE inhibitor (18.86 ± 2.41 μg/ml). It is noteworthy to note that compound 6 was a selective inhibitor with the selectivity index of 11.82. Molecular insight from docking interaction further substantiate that orientation of compound 6 in the catalytic site which enhanced its binding affinity as compared to other xanthones. The nature of protein-ligand interactions of compound 6 is mainly hydrogen bonding, and the hydroxyl group of compound 6 at C-10 is vital in BChE inhibition activity. Therefore, compound 6 is a notable lead for further drug design and development of BChE selective inhibitor.

Original languageEnglish
Pages (from-to)88-92
Number of pages5
JournalNatural Product Sciences
Volume24
Issue number2
DOIs
Publication statusPublished - 2018
Externally publishedYes

Keywords

  • Butyrylcholinesterase
  • Garcinexanthone G
  • Garcinia atroviridis
  • Molecular docking

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