Natural indole butyrylcholinesterase inhibitors from Nauclea officinalis

Sook Yee Liew, Kooi Yeong Khaw, Vikneswaran Murugaiyah, Chung Yeng Looi, Yi Li Wong, Mohd Rais Mustafa, Marc Litaudon, Khalijah Awang

Research output: Contribution to journalArticleResearchpeer-review

28 Citations (Scopus)

Abstract

Nine monoterpenoid indole alkaloids; naucletine (1), angustidine (2), nauclefine (3), angustine (4), naucline (5), angustoline (6), harmane (7), 3,14-dihydroangustoline (8), strictosamide (9) and one quinoline alkaloid glycoside; pumiloside (10) from Nauclea officinalis were tested for cholinesterase inhibitory activity. All the alkaloids except for pumiloside (10) showed strong to weak BChE inhibitory effect with IC50 values ranging between 1.02-168.55 μM. Angustidine (2), nauclefine (3), angustine (4), angustoline (6) and harmane (7) showed higher BChE inhibiting potency compared to galanthamine. Angustidine (2) was the most potent inhibitor towards both AChE and BChE. Molecular docking (MD) studies showed that angustidine (2) docked deep into the bottom gorge of hBChE and formed hydrogen bonding with Ser 198 and His 438. Kinetic study of angustidine (2) on BChE suggested a mixed inhibition mode with an inhibition constant (Ki) of 6.12 μM.

Original languageEnglish
Pages (from-to)45-48
Number of pages4
JournalPhytomedicine
Volume22
Issue number1
DOIs
Publication statusPublished - 9 Aug 2015
Externally publishedYes

Keywords

  • Angustidine
  • Cholinesterase
  • Kinetic study
  • Molecular docking
  • Nauclea officinalis

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