棉酚衍生物中的酚醛类和其它化合物的体外杀精作用

用金黄仓鼠附睾尾部精液，比较了４０个棉酚衍生物中酚醛类化合物的体外杀精作用，发现２５个化合物对精子有杀灭作用，其中１４个化合物的杀精作用强于棉酚。该结果提示酚基或酚醛基是这类化合物具有体外杀精作用的重要活性基团。对杀精作用较强的６个化合物，用不同种属动物及人精液进行比较；表明ＮＣ－００９与ＮＣ－０１０的体外杀精作用最强，它们对人精子的杀精作用（６．１×１０－５Ｍ）约为棉酚（９．６×１０－３Ｍ）的１００倍，略强于ＮＰ－９（１．９×１０－４Ｍ）。不同种动物的精子敏感性存在种属差异，且亦随化合物而异。大鼠、狗和人的精子对ＮＣ－００９与ＮＣ－０１０较为敏感（其杀精强度分别为；９．５×１０－５、６．１×１０－５与６．１×１０－５Ｍ）；小鼠、金色仓鼠和兔精子则相对不敏感。

Spermicidal Effect of Gossypol Derivatives and Its Phenol Aldehyde Compounds in Vitro

Spermicidal effects of 40 compounds were screened by hamster in vitro.Among them,25compounds(9 phenol compounds, 15 phenol aldehyde compounds and 1 compound without phenol group)possessed the activity of immobilizing spermatozoa within 20s at a concentration of 5mg/ml or less.Out of these 25 compounds,there were 14 with a spermicidal potency higher than that of gossypol.Results suggested that the Phenol and phenol aldehyde groups were the important active groups of these compounds for spermicidal effects in vitro.The Spermicidal activity of 5 phenol aldehydes compounds and one quinone in vitro was compared in various species including rats,mice,rabbits,hamsters,dogs and human.The results showed that rats seemed to be the most sensitive one to all the testing compounds.The compounds named NC-010 and NC-009 presented higher potency of spermicidal effect to the spermatozos of rats,dogs and human,the lowest effective concentration of NC-010 and NC - 009was 6.1×10-5,9.5×10-5and 6.1×10-5 in dogs,rats and human respectively.In human the spermicidal potency of those two compounds was 100 times higher than that of gossypol, and the effective concentration of NC-010 or NC-009 might be promising to be developed as a spermicidal agent.