阿切
胆碱酯酶
化学
IC50型
立体化学
丁酰胆碱酯酶
乙酰胆碱酯酶
体外
非竞争性抑制
抑制性突触后电位
酶
生物碱
乌头
生物化学
药理学
生物
神经科学
作者
Hanif Ahmad,Shujaat Ahmad,Syed Adnan Alı Shah,Hidayat Ullah Khan,Farman Ali Khan,Mumtaz Ali,Abdul Latif,Farzana Shaheen,Manzoor Ahmad
标识
DOI:10.1080/10286020.2017.1319820
摘要
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.
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