期刊
BIOORGANIC & MEDICINAL CHEMISTRY
卷 23, 期 13, 页码 3126-3134出版社
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmc.2015.04.080
关键词
Lycopodiella cernua; Serratene-type triterpenoids; Hydroxy unsaturated fatty acid; Cholinesterase; beta-Secretase
资金
- National Research Foundation of Korea (NRF) - Ministry of Education, Science and Technology [KRF-2012R1A2A2A06046921]
- National Research Council of Science & Technology (NST), Republic of Korea [KGM4311541] Funding Source: Korea Institute of Science & Technology Information (KISTI), National Science & Technology Information Service (NTIS)
Three new serratene-type triterpenoids (1-3) and a new hydroxy unsaturated fatty acid (13) together with nine known compounds (4-12) were isolated from Lycopodiella cernua. The chemical structures were established using NMR, MS, and Mosher's method. Compound 13 showed the most potent inhibitory activity against acetylcholinesterase (AChE) with an IC50 value of 0.22 mu M. For butyrylcholinesterase (BChE) inhibitory activity, 5 showed the most potent activity with an IC50 value of 0.42 mu M. Compound 2 showed the most potent activity with an IC50 of 0.23 mu M for BACE-1 inhibitory activity. The kinetic activities were investigated to determine the type of enzyme inhibition involved. The types of AChE inhibition shown by compounds 4, 5, and 13 were mixed; BChE inhibition by 5 was competitive, while 2 and 6 showed mixed-types. In addition, molecular docking studies were performed to investigate the interaction of these compounds with the pocket sites of AChE. The docking results revealed that the tested inhibitors 3, 4, and 13 were stably present in several pocket domains of the AChE residue. (C) 2015 Elsevier Ltd. All rights reserved.
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