Bourinbaiar A S, Lee-Huang S
Department of Biochemistry, New York University Medical Center, NY 10016, USA.
Contraception. 1995 May;51(5):319-22. doi: 10.1016/0010-7824(95)00094-q.
Serine proteases are involved in a wide variety of seemingly unrelated physiological functions including capacitation of the spermatozoa and potentiation of human immunodeficiency virus (HIV) infection. The experimental vaginal contraceptives derived from 4-guanidinobenzoic acid act through inhibition of acrosin--a serine protease from the sperm. The serial ten-fold dilutions of 4'-acetamidophenyl 4-guanidinobenzoate (AGB) were tested in vitro for the effect against HIV infection by assaying the suppression of de novo p24 synthesis in virus-inoculated MT-4 T lymphocytes. The results reveal that complete inhibition of HIV occurred at 100 micrograms/ml--a dose corresponding to previously reported concentrations responsible for preventing fertilization in rabbits. These findings suggest that serine protease inhibitors and in particular the guanidinobenzoates, reported to be up to 100-fold more potent and less irritating than nonoxynol-9, can be potentially operative against sexual transmission of HIV.
丝氨酸蛋白酶参与多种看似不相关的生理功能，包括精子获能和增强人类免疫缺陷病毒（HIV）感染。源自4-胍基苯甲酸的实验性阴道避孕药通过抑制顶体蛋白酶（一种来自精子的丝氨酸蛋白酶）发挥作用。通过测定接种病毒的MT-4 T淋巴细胞中从头合成p24的抑制情况，对4'-乙酰氨基苯基4-胍基苯甲酸酯（AGB）的系列十倍稀释液进行体外抗HIV感染作用测试。结果显示，在100微克/毫升时HIV被完全抑制，该剂量与先前报道的对兔避孕有效浓度相当。这些发现表明，丝氨酸蛋白酶抑制剂，特别是胍基苯甲酸酯，据报道比壬苯醇醚-9效力高100倍且刺激性小，可能对HIV的性传播有效。
