Selective dual cholinesterase inhibitors from Aconitum laeve

New lycoctonine-type dual cholinesterase inhibitor, swatinine-C (1), along with three known norditerpenoid alkaloids, hohenackerine (2), aconorine (5) and lappaconitine (6) and two synthetically known but phytochemically new benzene derivatives, methyl 2-acetamidobenzoate (3) and methyl 4-[2-(methox...

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Bibliographic Details
Published in:Journal of Asian Natural Products Research
Main Author: Ahmad H.; Ahmad S.; Shah S.A.A.; Khan H.U.; Khan F.A.; Ali M.; Latif A.; Shaheen F.; Ahmad M.
Format: Note
Language:English
Published: Taylor and Francis Ltd. 2018
Online Access:https://www.scopus.com/inward/record.uri?eid=2-s2.0-85018407862&doi=10.1080%2f10286020.2017.1319820&partnerID=40&md5=94928c13a9ddf72f387d434de1ff49e1
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Summary:New lycoctonine-type dual cholinesterase inhibitor, swatinine-C (1), along with three known norditerpenoid alkaloids, hohenackerine (2), aconorine (5) and lappaconitine (6) and two synthetically known but phytochemically new benzene derivatives, methyl 2-acetamidobenzoate (3) and methyl 4-[2-(methoxycarbonyl)anilino]-4-oxobutanoate (4), was isolated from the roots of A. laeve. Structures of new and known compounds (1–6) were established on the basis of latest spectroscopic techniques and by close comparison with the data available in literature. In vitro, compounds (1–6) were tested against AChE and BChE inhibitory activities. Compounds 1 and 2 showed competitive inhibition against AChE (IC50= 3.7 μM, 4.53 μM) and BChE (IC50= 12.23 μM, 9.94 μM), respectively. Compounds 5 and 6 showed promising noncompetitive type of inhibitory profile against AChE (IC50= 2.51 and 6.13 μM) only. Compounds 3 and 4 showed weak inhibitory profile against both AChE and BChE. © 2017 Informa UK Limited, trading as Taylor & Francis Group.
ISSN:10286020
DOI:10.1080/10286020.2017.1319820