Ahmad Hanif, Ahmad Shujaat, Shah Syed Adnan Ali, Khan Hidayat Ullah, Khan Farman Ali, Ali Mumtaz, Latif Abdul, Shaheen Farzana, Ahmad Manzoor
a Department of Chemistry , University of Malakand , Dir (Lower) 18550 , Pakistan.
b Department of Pharmacy , Shaheed Benazir Bhutto University Sheringal , Dir (Upper) 18000 , Pakistan.
J Asian Nat Prod Res. 2018 Feb;20(2):172-181. doi: 10.1080/10286020.2017.1319820. Epub 2017 May 2.
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 (IC= 3.7 μM, 4.53 μM) and BChE (IC= 12.23 μM, 9.94 μM), respectively. Compounds 5 and 6 showed promising noncompetitive type of inhibitory profile against AChE (IC= 2.51 and 6.13 μM) only. Compounds 3 and 4 showed weak inhibitory profile against both AChE and BChE.
从光滑乌头的根中分离出新型牛扁碱型双胆碱酯酶抑制剂斯瓦廷宁 - C（1），以及三种已知的降二萜生物碱霍内卡林（2）、阿替新碱（5）和拉帕乌头碱（6），还有两种合成已知但植物化学上为新的苯衍生物，2 - 乙酰氨基苯甲酸甲酯（3）和4 - [2 - （甲氧基羰基）苯胺基] - 4 - 氧代丁酸甲酯（4）。基于最新的光谱技术并与文献中的现有数据进行仔细比较，确定了新化合物和已知化合物（1 - 6）的结构。在体外，测试了化合物（1 - 6）对乙酰胆碱酯酶（AChE）和丁酰胆碱酯酶（BChE）的抑制活性。化合物1和2分别对AChE（IC = 3.7 μM，4.53 μM）和BChE（IC = 12.23 μM，9.94 μM）表现出竞争性抑制。化合物5和6仅对AChE表现出有前景的非竞争性抑制模式（IC = 2.51和6.13 μM）。化合物3和4对AChE和BChE均表现出较弱的抑制作用。
