Neyts J, Kristmundsdóttir T, De Clercq E, Thormar H
Rega Institute for Medical Research, Katholieke Universiteit Leuven, B-3000 Leuven, Belgium.
J Med Virol. 2000 May;61(1):107-10. doi: 10.1002/(sici)1096-9071(200005)61:1<107::aid-jmv17>3.0.co;2-w.
Hydrogel formulations containing the 1-monoglyceride of capric acid (monocaprin) possess potent in vitro microbicidal activity against HIV and HSV, Chlamydia trachomatis and Neisseria gonorrhoeae. These formulations were studied to determine whether they prevent intracutaneous and intravaginal infections of mice with HSV-2, a virus that is in vitro as sensitive to the virucidal action of the compound as is HIV. In mice intravaginal infection with HSV-2 and the associated mortality was prevented completely when the infection was carried out in the presence of a 20 mM monocaprin containing gel formulation. Similarly, virtually complete protection of lesion development and associated mortality was observed when mice were infected intracutaneously with HSV-2 in the presence of gels containing 10 or 20 mM monocaprin. No irritation or toxicity was observed following application of the gel to the skin or the vaginal mucosa. Hydrogel formulations of monocaprin could thus be pursued as vaginal microbicides for the prevention of sexual transmission of HSV, HIV and other infectious pathogens.
含有癸酸单甘油酯(单癸酸甘油酯)的水凝胶制剂对HIV、HSV、沙眼衣原体和淋病奈瑟菌具有强大的体外杀菌活性。对这些制剂进行了研究,以确定它们是否能预防小鼠的HSV-2皮内和阴道感染,HSV-2是一种在体外对该化合物的杀病毒作用与HIV一样敏感的病毒。在含有20 mM单癸酸甘油酯的凝胶制剂存在的情况下进行阴道感染时,小鼠的HSV-2阴道感染及相关死亡率被完全预防。同样,当在含有10或20 mM单癸酸甘油酯的凝胶存在的情况下给小鼠进行HSV-2皮内感染时,观察到对病变发展和相关死亡率几乎完全的保护作用。将凝胶应用于皮肤或阴道黏膜后未观察到刺激或毒性。因此,单癸酸甘油酯水凝胶制剂可作为阴道杀菌剂用于预防HSV、HIV和其他感染性病原体的性传播。