Dong Jian-Wei, Cai Le, Fang Yun-Shan, Xiao Huai, Li Zhen-Jie, Ding Zhong-Tao
Key Laboratory of Medicinal Chemistry for Nature Resource, Ministry of Education, School of Chemical Science and Technology, Yunnan University, Kunming 650091, PR China.
Key Laboratory of Medicinal Chemistry for Nature Resource, Ministry of Education, School of Chemical Science and Technology, Yunnan University, Kunming 650091, PR China; School of Pharmaceutical Sciences and Chemistry, Dali University, Dali 671000, PR China.
Fitoterapia. 2015 Jul;104:102-7. doi: 10.1016/j.fitote.2015.05.019. Epub 2015 May 29.
An unusual proaporphine alkaloid bearing an isopropanenitrile group at isoquinoline nitrogen, named epiganine A (1) and a new aporphine alkaloid, epiganine B (2), together with eight known alkaloids, pronuciferine (3), dehydrodicentrine (4), romerine (5), romeline (6), N-methylcalycinine (7), phanostenine (8), dicentrine (9), and N-methyllaurotetanine (10), were isolated from the roots of Stephania epigaea. The absolute configuration of 1 was determined by calculating electronic circular dichroism (ECD) and comparing with experimental data. Compounds 2 and 4 showed strong acetylcholinesterase (AChE) inhibitory effects with the IC50 values of 4.36 and 2.98μM, respectively. Compounds 5-9 also exhibited potent AChE inhibitory activities.
从地不容的根中分离出一种不寻常的原阿朴菲生物碱，其异喹啉氮上带有异丙腈基，命名为表千金藤宁A（1）和一种新的阿朴菲生物碱表千金藤宁B（2），以及8种已知生物碱，即前荷叶碱（3）、去氢双苄基异喹啉（4）、轮环藤酚碱（5）、罗默碱（6）、N-甲基卡利西宁（7）、番荔枝宁（8）、双苄基异喹啉（9）和N-甲基劳罗替丁（10）。通过计算电子圆二色性（ECD）并与实验数据比较确定了1的绝对构型。化合物2和4表现出较强的乙酰胆碱酯酶（AChE）抑制作用，IC50值分别为4.36和2.98μM。化合物5 - 9也表现出较强的AChE抑制活性。
