Effects of demethylzeylasteral and celastrol on spermatogenic cell Ca2+ channels and progesterone-induced sperm acrosome reaction
Effects of demethylzeylasteral and celastrol on spermatogenic cell Ca2+ channels and progesterone-induced sperm acrosome reaction
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DOI：
10.1016/s0014-2999(03)01351-7
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发表时间：
2003-03-07
影响因子：
5
通讯作者：
Shi, QX
中科院分区：
文献类型：
--
作者：
Bai, JP;Shi, YL;Shi, QX
雷公藤氯仿提取物的雄性抗生育作用。F. (GTW)并且从GTW分离的几种单体引起了全世界的兴趣。本研究采用全细胞膜片钳技术和金霉素染色法，分别研究了雷公藤多甙的两个单体去甲基泽拉木醛和雷公藤红素对小鼠生精细胞钙通道和精子顶体反应的影响。结果表明，去甲泽拉木醛浓度依赖性地和以部分可逆的方式抑制生精细胞的Ca ~（2+）电流，IC_（50）为8.8 μ g/ml。南蛇藤酚呈时间依赖性地和不可逆地降低细胞内Ca ~（2+）电流。应用这两种化合物后的钙电流的激活和失活时间常数的变化也进行了检查。去甲基泽拉木醛增加钙电流的激活和失活的时间常数，雷公藤红素没有显着的效果。这两种化合物对孕酮诱导的精子顶体反应也有明显的抑制作用。这些数据表明，钙电流的抑制可能是负责这些化合物的抗生育活性。(C)2003 Elsevier Science B. V.保留所有权利。
The male antifertility effect of a water-chloroform extract of Tripterygium wilfordii Hook. f. (GTW) and several monomers isolated from GTW has attracted worldwide interest. In the present study, the effects of two isolated monomers from GTW, demethylzeylasteral and celastrol, on the Ca2+ channels in mouse spermatogenic cells and on the sperm acrosome reaction were investigated by whole-cell patch-clamp recording and chlortetracycline staining methods, respectively. The results showed that demethylzeylasteral concentration-dependently and in a partially reversible manner inhibited the Ca2+ current in spermatogenic cells with an IC50 of 8.8 mug/ml. Celastrol decreased the Ca2+ current in the cells time-dependently and irreversibly. The changes in the activation and inactivation time constants of Ca2+ currents after application of these two compounds were also examined. Demethylzeylasteral increased both activation and inactivation time constants of Ca2+ currents, and celastrol had no significant effect on them. The two compounds also inhibited significantly the sperm acrosome reaction initiated by progesterone. These data suggest that inhibition of Ca2+ currents could be responsible for the antifertility activity of these compounds. (C) 2003 Elsevier Science B.V. All rights reserved.