Likhitwitayawuid K, Angerhofer C K, Chai H, Pezzuto J M, Cordell G A, Ruangrungsi N
Department of Medicinal Chemistry and Pharmacognosy, College of Pharmacy, University of Illinois at Chicago 60612.
J Nat Prod. 1993 Sep;56(9):1468-78. doi: 10.1021/np50099a005.
Biological evaluation of extracts prepared from the tubers of Stephania pierrei revealed cytotoxic and antimalarial activity. During the course of separation, two new aporphine alkaloids, (-)-asimilobine-2-O-beta-D-glucoside [2] and (-)-nordicentrine [8], in addition to twenty-one known isoquinoline alkaloids, were isolated. Each isolate was assessed for cytotoxic and antimalarial activities. It was found that the cytotoxicity of S. pierrei was mainly due to the presence of the aporphine alkaloids containing the 1,2-methylenedioxy group 3-10, whereas the antimalarial activity was attributed to the nonquaternary aporphine alkaloids 1, 3-10 and the tetrahydroprotoberberines possessing a phenolic functionality, 13-15, 18. None of the isolates showed a degree of selectivity comparable to that of antimalarial drugs such as chloroquine, quinine, mefloquine, and artemisinin. Comparison of the alkaloid content of S. pierrei and Stephania erecta strongly suggested separate identities for the two plants.
从粉防己块茎中制备的提取物的生物学评价显示出细胞毒性和抗疟活性。在分离过程中，除了21种已知的异喹啉生物碱外，还分离出两种新的阿朴啡生物碱，(-)-去甲乌药碱-2-O-β-D-葡萄糖苷[2]和(-)-去甲华千金藤碱[8]。对每种分离物进行了细胞毒性和抗疟活性评估。结果发现，粉防己的细胞毒性主要归因于含有1,2-亚甲二氧基的阿朴啡生物碱3-10，而抗疟活性则归因于非季铵型阿朴啡生物碱1、3-10以及具有酚官能团的四氢原小檗碱13-15、18。没有一种分离物表现出与氯喹、奎宁、甲氟喹和青蒿素等抗疟药物相当程度的选择性。粉防己和直立千金藤生物碱含量的比较强烈表明这两种植物具有不同的特性。
