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本文采用体外杀精实验检查ＫＦ－９５０对大鼠精子活力的影响和明胶底物膜法测定 ＫＦ－９５０对精子顶体蛋白酶活性的抑制作用。结果表明，ＫＦ－９５０与大鼠精液作用 ２０ ｓｅｅ 及 １２０ ｓｅｅ，最低杀精浓度分别为 １． ５６±０． １３ ｍｇ／ｍｌ和 ０． ７３±０． ０７ ｍｇ／ｍｌ，其杀精能力 明显低于壬苯醇醚（Ｐ＜０．０１）；当ＫＦ－９５０浓度为１× １０－１２ｍｇ／ｍｌ时，平均晕轮阳性率 （％）及平均晕轮直径（μｍ）分别为８３．００±７．１０及１８．２７±１．９４（与对照组比较Ｐ＜ ０．０１），完全抑制浓度为 １×１０－３ｍｇ／ｍｌ。抑制平均晕轮阳性率和平均晕轮直径的半数有效 浓度ＥＤ５０分别为４．１５×１０－７ｍｇ／ｍｌ和２．３４×１０-7 ｍｇ／ｍｌ。本实验证明ＫＦ－９５０对精子顶 体蛋白酶具有高效抑制作用，而杀精子作用较弱，是一种新型的顶体蛋白酶抑制剂。
In this paper, the effect of KF-950 on the sperm motility of rats and the inhibitory effect of KF-950 on the acrosin activity of sperm were examined by in vitro spermicidal assay. The results showed that KF-950 and rat semen 20 see and 120 see, the minimum spermicidal concentrations were 1. 56 ± 0. 13 mg / ml and 0. 73 ± 0. 07 mg / ml, the spermicidal activity was significantly lower than nonoxynol (P <0.01); when the concentration of KF-950 was 1 × 10-12 mg / ml, the average halo positive rate (% The wheel diameters (μm) were 83.00 ± 7.10 and 18.27 ± 1.94, respectively (P <0.01 compared with the control group), and the complete inhibitory concentration was 1 × 10-3 mg / ml. The median effective inhibitory concentrations (ED50) of 4.15 × 10-7 mg / ml and 2.34 × 10-7 mg / ml, respectively, for inhibiting the average halo positive rate and the average halo diameter. The experiment shows that KF-950 has high inhibitory effect on sperm acrosin, while spermicidal effect is weak. It is a new type of acrosin protease inhibitor.