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经雄性大鼠抗生育试验证明,无毒性剂量的雷公藤提取物可导致不育,停药后恢复;临床试用1/3~1/4常规量的雷公藤提取物可使男病人不育。进行了植化分离和动物筛选,获得了6个雄性抗生育有效环氧二萜类化合物:雷藤甲素、雷藤乙素、雷醇内酯、雷藤氯内酯醇,16-羟雷藤甲素以及T7/T19,均鉴定了结构。它们的结构和作用均类似,因而估计为某母物质的植物代谢产物。对雷藤氯内酯醇进行了较深入的研究,表明其作用部位为晚期精子细胞及附睾精子。几个化合物的不良反应主要是大剂量(5.5~11.5倍抗生育有效量)时有一定的免疫抑制作用。优选对免疫影响最小的化合物及寻找更佳的类似物,为今后研究的重点。
Anti-fertility test in male rats showed that non-toxic dose of Tripterygium wilfordii extract can cause infertility and recovery after discontinuation; clinical trials of 1/3 to 1/4 of the conventional amount of tripterygium extract can make male patients infertile. Phytochemical separation and animal screening were performed and 6 male antifertility effective epoxy diterpenoids were obtained: letothropoietin, rattanbine, ranolactone, phytolactone, 16-hydroxylamine Rattan A and T7/T19 all identified structures. Their structures and effects are similar, and they are estimated to be plant metabolites of a parent substance. A more in-depth study of levovatochlor-olactone showed that the site of action is late spermatids and epididymal sperm. The adverse reactions of several compounds are mainly immunosuppressive at high doses (5.5 to 11.5 times the effective antifertility dose). It is preferable that compounds that have minimal impact on immunity and find better analogs are the focus of future research.