Zhong C L, Ge R S, Shi Q X
Family Planning Research Institute, Zhejiang Academy of Medicine, Hangzhou, China.
Zhongguo Yao Li Xue Bao. 1990 Mar;11(2):169-72.
dl-Propranolol (Pro), known to have spermicidal effect, was evaluated for its ability to influence capacitation, the acrosome reaction (AR) and fertilization of guinea pig spermatozoa at non-spermicidal dose levels. A concentration-dependent decrease in AR and the whiplashed motility occurred in Pro as low as 0.05 mmol/L. Pro 1.0 mmol/L completely abolished AR, followed by the loss of sperm capacity to penetrate into zona-free hamster egg. Pro exerted its inhibitory effect of AR primarily by restraining the capacitation stage of sperm but at Pro 0.5 mmol/L by blocking both capacitation and AR stages. % of AR of sperm preincubated with ionophore A-23187 0.2 mumol/L was significantly higher than that of the control, but markedly lower at Pro greater than or equal to mmol/L, implying that Pro prevented sperm Ca2+ influx. Prenylamine was also found to inhibit AR potentially and enhance the action of Pro against ionophore A-23187. Furthermore, Pro inhibition of the fertilizing ability of preincubated spermatozoa was antagonized by cAMP. Pro 0.5 mmol/L even caused the egg vesiculation. The reversibility of the action depends on the dose and time of sperm exposure to Pro. These findings suggest that the inhibitory effects of Pro on guinea pig sperm capacitation, the acrosome reaction and fertilization may be the mechanisms for its antifertility action.
已知具有杀精作用的消旋普萘洛尔(Pro),在非杀精剂量水平下,对豚鼠精子的获能、顶体反应(AR)和受精能力的影响进行了评估。低至0.05 mmol/L的Pro就会使AR和鞭打运动呈浓度依赖性降低。1.0 mmol/L的Pro完全消除了AR,随后精子穿透去透明带仓鼠卵的能力丧失。Pro对AR的抑制作用主要是通过抑制精子的获能阶段,但在0.5 mmol/L的Pro时则通过阻断获能和AR阶段。与0.2 μmol/L离子载体A - 23187预孵育的精子的AR百分比显著高于对照组,但在Pro大于或等于mmol/L时明显较低,这意味着Pro阻止了精子Ca2+内流。还发现普尼拉明也可能抑制AR,并增强Pro对离子载体A - 23187的作用。此外,cAMP拮抗Pro对预孵育精子受精能力的抑制作用。0.5 mmol/L的Pro甚至导致卵泡化。作用的可逆性取决于精子暴露于Pro的剂量和时间。这些发现表明,Pro对豚鼠精子获能、顶体反应和受精的抑制作用可能是其抗生育作用的机制。