摘要
雷藤氯内酯醇（Ｔｒｉｐｃｈｌｏｒｏｌｉｄｅ，Ｔ４）由雷公藤中分离的单体，除有增强抗炎、免疫抑制作用外，还增强雄性抗生育活性。Ｔ４经大鼠口服，可致附睾尾精子活率和密度明显下降而不育。精子活力主要受Ｃａ２＋等调控，为了探讨Ｔ４抑制精子活力的作用机制，我们观察了Ｔ４对人射出精子Ｃａ２＋内流的作用和对离体大鼠胸主动脉及输精管收缩的影响。结果指出，Ｔ４Ｉ抑制人射出精子对Ｃａ２＋摄取，但不影响由去甲肾上腺素和高Ｋ＋依赖Ｃａ２＋支持而诱发的大鼠胸主动脉和输精管的自发收缩。提示，Ｔ４抑制人射出精子Ｃａ２＋内流，导致精子膜内外Ｃａ２＋梯度浓度失去动态平衡，可能是Ｔ４抑制精子活力的重要机理之一。但Ｔ４不影响离体大鼠胸主动脉和输精管的收缩，可能有选择性的作用在附睾部位。
Tripchlorolide (T4), an active monomer isolated from Chinese herb Tripterygium wilfordii, could enhance not only antiinflammatory and immunsuppressive action but antifertility effect in male rats. It could significantly reduce the motility and density of the epididymal spermatozoa of rats after oral administration. It is well known that calcium plays an important role in regulating the sperm motility. In order to explore the mechanism by which T4 inhibits sperm motility, the effects of T4 on Ca2+ influx of human ejaculated sperm and contraction action of rat aorta and vas deferens were observed. The results indicated that T4 inhibited Ca2+ influx of human ejaculated sperm, but had not effects on NE and high K+ induced spontaneous contractions of rat aorta and vas deferens which were dependent on Ca2+ support. These findings suggest that T4 inhibits sperm Ca2+ influx and breaks the dynamic equilibrium of internal and external Ca2+ gradient concentrations of sperm membrane, it may be one of Mimportant mechanism by which T4 inhibits sperm motility. T4 does not result in contraction reaction of rat aorta and vas deferens, it may selectively affect on epidipymides.
出处
《中国药理学通报》
CSCD
北大核心
1996年第5期441-444,共4页
Chinese Pharmacological Bulletin
关键词
雷藤氯内酯醇
精子
胸主动脉
输精管
钙离子
tripchlorolide (T_4)
spermatozoa
Ca￣(2+)
rat aorta
vas deferens
