Selective dual cholinesterase inhibitors from Aconitum laeve

Journal of Asian Natural Products Research
2018.0

Abstract

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 mu M, 4.53 mu M) and BChE (IC50=12.23 mu M, 9.94 mu M), respectively. Compounds 5 and 6 showed promising noncompetitive type of inhibitory profile against AChE (IC50=2.51 and 6.13 mu M) only. Compounds 3 and 4 showed weak inhibitory profile against both AChE and BChE.[GRAPHICS].

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