Back D J, Glover T D, Shenton J C, Boyd G P
J Reprod Fertil. 1975 Oct;45(1):117-28. doi: 10.1530/jrf.0.0450117.
The relationship between the antifertility effect of alpha-chlorohydrin and changes in composition of luminal plasma from the cauda epididymidis of rats and rabbits has been investigated. At each dose regimen studied, the fertilizing capacity of rats treated with alpha-chlorohydrin was reduced to zero. The levels of sodium, potassium, glycerylphosphorylcholine (GPC), acid phosphatase and alkaline phosphatase in epididymal plasma were not markedly affected by drug treatment. The most noticeable change was a considerable increase in the concentration of lactic dehydrogenase (LDH) at all dose levels and of glutamic-oxaloacetic transaminase (GOT) after 7 days of treatment with 8 and 16 mg/kg. The effect of cold shock on the composition of epididymal plasma showed that LDH and GOT are, at least in part, derived from spermatozoa. In contrast, alpha-chlorohydrin did not have an antifertility action in the rabbit, and the only notable change in the compositon of epididymal plasma was an increase in the level of GPC. These results provide evidence that, in the rat, alpha-chlorohydrin or a metabolite primarily exerts its antifertility effect by a direct action on the spermatozoa, whilst in the rabbit a barrier may exist to the entrance of the drug into the lumen of the epididymal duct.
已对α-氯醇的抗生育作用与大鼠和家兔附睾尾部管腔血浆成分变化之间的关系进行了研究。在所研究的每种剂量方案下,用α-氯醇处理的大鼠的受精能力均降至零。附睾血浆中钠、钾、甘油磷酸胆碱(GPC)、酸性磷酸酶和碱性磷酸酶的水平未受到药物处理的明显影响。最显著的变化是在所有剂量水平下乳酸脱氢酶(LDH)的浓度显著增加,以及在以8毫克/千克和16毫克/千克剂量处理7天后谷草转氨酶(GOT)的浓度显著增加。冷休克对附睾血浆成分的影响表明,LDH和GOT至少部分源自精子。相比之下,α-氯醇在家兔中没有抗生育作用,附睾血浆成分中唯一显著的变化是GPC水平的升高。这些结果提供了证据,表明在大鼠中,α-氯醇或其代谢产物主要通过对精子的直接作用发挥其抗生育作用,而在家兔中可能存在药物进入附睾管腔的屏障。