雷公藤单体(T_4)与棉酚抗生育机理及毒性作用的比较

Comparative Studies on Antifertility Mechanism and Toxicology of Tripterygium wilfordii Monomer T4 and Gossypol

喂服雷公藤单体(T_4)0.05mg/kg/d6周后,大鼠生精作用及晚期精子细胞碱性核蛋白转换与替代受到抑制程度均较喂服棉酚组明显。实验组附睾上皮腔缘部γ-GT,ALP出现成簇的阳性沉淀。附睾尾部精子头尾断裂,断端卷曲,尾部纵行粗纤维脱位,线粒体LDH,LDH-X,MDH受到抑制。T_4对肾脏、肝脏各种酶虽有轻度影响但没有引起酶活性明显的变化。T_4对内脏的影响较棉酚轻,但致雄性不育的效果比较明显。本研究提示T_4是一种有发展前途的男性抗生育药物。

Inhibition of spermatogenesis and turnover of basic nuclear protein in late elongated spermatids of ray testis by Tripterygium wilfordii monomer T4 was more obvious than that by gossypol. Clustered positive deposits of γ-GT, ALP reaction were found in the inner edges of epididymal epithelium. Head and tail separation, mid-piece coiling and axial fiber dislocation of epididymal spermatozoa in T4 treated rats were more obvious than those of gossypol-treated rats. Mitochondrial LDH, LDH-X and MDH were also found to be inhibited by T4. T4 did not significantly affect enzyme activities in kidney and liver, though it did cause slight changes. Effects of T4 on the chief rat organs were milder than those of gossypol, except for a more obvious antifertility effect. The authors suggest that T4 may be developed into an ideal male contraceptive.