Natural Product Sciences

The Korean Society of Pharmacognosy (한국생약학회)
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Garcinexanthone G, a Selective Butyrylcholinesterase Inhibitor from the Stem Bark of Garcinia atroviridis

  • Khaw, Kooi-Yeong (Discipline of Pharmacology, School of Pharmaceutical Sciences, Universiti Sains Malaysia) ;
  • Murugaiyah, Vikneswaran (Discipline of Pharmacology, School of Pharmaceutical Sciences, Universiti Sains Malaysia) ;
  • Khairuddean, Melati (School of Chemical Sciences, Universiti Sains Malaysia) ;
  • Tan, Wen-Nee (School of Distance Education, Universiti Sains Malaysia)
  • Received : 2017.10.31
  • Accepted : 2018.01.15
  • Published : 2018.06.30
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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 ($12.65{\pm}1.57{\mu}g/ml$) while garcinexanthone G (6) was the most active BChE inhibitor ($18.86{\pm}2.41{\mu}g/ml$). 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.

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References

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