| Literature DB >> 25636869 |
Sook Yee Liew1, Kooi Yeong Khaw2, Vikneswaran Murugaiyah2, Chung Yeng Looi3, Yi Li Wong3, Mohd Rais Mustafa3, Marc Litaudon4, Khalijah Awang5.
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.Entities:
Keywords: Angustidine; Cholinesterase; Kinetic study; Molecular docking; Nauclea officinalis
Mesh：
Substances：
Year: 2014 PMID： 25636869 DOI： 10.1016/j.phymed.2014.11.003
Source DB: PubMed Journal: Phytomedicine ISSN： 0944-7113 Impact factor: 5.340