Namyniuk M A, Chaturvedi A K
Department of Pharmaceutical Sciences, North Dakota State University College of Pharmacy, Fargo 58105.
Arch Int Pharmacodyn Ther. 1988 Mar-Apr;292:286-304.
In the motility of sperm, which resembles the automaticity of smooth muscle in some features, calcium plays an important role. Chlorpromazine (CPZ), an inhibitor of calmodulin (CaM), decreases contractile responses of smooth muscle to agonists, alters microsomal calcium movements and inhibits human sperm motility. The involvement of CaM in the contraction of smooth muscle and in sperm motility and its presence in sperm cells have also been established. Therefore, the effects of CPZ on boar sperm motility and microsomal calcium uptake were studied. CPZ (0.05-0.5 mM) was found to depress the motility index of boar sperm. At 60 min time point, an inhibition of the motility index ranging from 28 to 85% was observed (p less than 0.05). The spermatozoa microsomal calcium uptake (5.2 nmol/mg protein/hr) was Mg++- and ATP-dependent and azide insensitive. Ionophore A23187 (1 microM) and EDTA (10 mM) inhibited the uptake (67-94%). The calcium uptake was inhibited (40-60%) by CPZ (0.25 and 0.5 mM). The CPZ-induced inhibition of the motility index or calcium uptake was overcome by additional CaCl2. The observations suggested that the CPZ-caused changes were calcium-mediated and possibly involved CaM.
在精子的运动中,钙起着重要作用,精子运动在某些特征上类似于平滑肌的自动性。氯丙嗪(CPZ)是钙调蛋白(CaM)的抑制剂,它能降低平滑肌对激动剂的收缩反应,改变微粒体钙的运动,并抑制人类精子的运动。CaM参与平滑肌收缩和精子运动以及它在精子细胞中的存在也已得到证实。因此,研究了CPZ对公猪精子运动和微粒体钙摄取的影响。发现CPZ(0.05 - 0.5 mM)能降低公猪精子的运动指数。在60分钟时间点,观察到运动指数的抑制范围为28%至85%(p小于0.05)。精子微粒体钙摄取(5.2 nmol/mg蛋白质/小时)依赖于Mg++和ATP,对叠氮化物不敏感。离子载体A23187(1 microM)和EDTA(10 mM)抑制摄取(67 - 94%)。CPZ(0.25和0.5 mM)抑制钙摄取(40 - 60%)。额外添加CaCl2可克服CPZ诱导的运动指数或钙摄取抑制。这些观察结果表明,CPZ引起的变化是钙介导的,可能涉及CaM。