Herold B C, Bourne N, Marcellino D, Kirkpatrick R, Strauss D M, Zaneveld L J, Waller D P, Anderson R A, Chany C J, Barham B J, Stanberry L R, Cooper M D
Pediatric Infectious Diseases, Mount Sinai School of Medicine, New York, NY 10029, USA.
J Infect Dis. 2000 Feb;181(2):770-3. doi: 10.1086/315228.
Presently marketed vaginal barrier agents are cytotoxic and damage the vaginal epithelium and natural vaginal flora with frequent use. Novel noncytotoxic agents are needed to protect women from sexually transmitted diseases. One candidate compound is a high-molecular-mass form of soluble poly(sodium 4-styrene sulfonate) (T-PSS). The antimicrobial activity of T-PSS was evaluated in primary culture systems and in a genital herpes murine model. Results obtained indicate that T-PSS is highly effective against herpes simplex viruses, Neisseria gonorrhoeae, and Chlamydia trachomatis in vitro. A 5% T-PSS gel protected 15 of 16 mice from vaginal herpes, compared with 2 of 16 mice treated with a placebo gel. Moreover, T-PSS exhibited little or no cytotoxicity and has an excellent selectivity index. T-PSS is an excellent candidate topical antimicrobial that blocks adherence of herpes simplex virus at low concentrations, inactivates virus at higher concentrations, and exhibits a broad spectrum of antimicrobial activity.
目前市面上销售的阴道屏障剂具有细胞毒性,频繁使用会损害阴道上皮和天然阴道菌群。需要新型无细胞毒性的制剂来保护女性免受性传播疾病的侵害。一种候选化合物是高分子量形式的可溶性聚(4-苯乙烯磺酸钠)(T-PSS)。在原代培养系统和生殖器疱疹小鼠模型中评估了T-PSS的抗菌活性。所得结果表明,T-PSS在体外对单纯疱疹病毒、淋病奈瑟菌和沙眼衣原体具有高效性。与用安慰剂凝胶治疗的16只小鼠中的2只相比,5%的T-PSS凝胶保护了16只小鼠中的15只免受阴道疱疹感染。此外,T-PSS几乎没有细胞毒性,具有出色的选择性指数。T-PSS是一种出色的局部抗菌候选药物,在低浓度下可阻止单纯疱疹病毒的粘附,在高浓度下可使病毒失活,并具有广谱抗菌活性。