Department of Pharmaceutical Analysis and Drug Metabolism, College of Pharmaceutical Sciences, Zhejiang University, Hangzhou 310058, Zhejiang, China.
Molecules. 2012 Oct 1;17(10):11712-20. doi: 10.3390/molecules171011712.
Isoliensinine, a natural phenolic bisbenzyltetrahydroisoquinoline alkaloid, has received considerable attention for its potential biological effects such as antioxidant and anti-HIV activities. From the dog hepatic microsomes of isoliensinine, three new N-demethylated and O-demethylated metabolites, 2-N-desmethyl-isoliensinine (M1), 2'-N-desmethylisoliensinine (M2), and 2'-N-6-O-didesmethylisoliensinine (M3), were identified by high-performance liquid chromatography and data-dependent electrospray ionization tandem mass spectrometry. Possible metabolic pathways for isoliensinine have been proposed. The result should prove very helpful for evaluation of the drug-like properties of isoliensinine and other bisbenzylisoquinoline alkaloids.
异莲心碱是一种天然酚类双苄基四氢异喹啉生物碱，由于其具有抗氧化和抗 HIV 等潜在的生物活性，受到了广泛关注。从犬肝微粒体中鉴定出异莲心碱的三种新的 N-去甲基化和 O-去甲基化代谢物，分别为 2-N-去甲异莲心碱（M1）、2'-N-去甲异莲心碱（M2）和 2'-N-6-O-去甲二甲基异莲心碱（M3），采用高效液相色谱和数据依赖电喷雾串联质谱法进行鉴定。提出了异莲心碱的可能代谢途径。该结果对于评价异莲心碱和其他双苄基异喹啉生物碱的类药性具有重要意义。
