Hughes Louise M, Griffith Renate, Aitken R J
Discipline of Biological Sciences School of Environmental and Life Sciences, University of Newcastle, Callaghan NSW 2308, Australia.
Curr Med Chem. 2007;14(7):775-86. doi: 10.2174/092986707780090972.
There is an urgent clinical need to research novel methods of fertility control that are also protective against sexually transmitted diseases (STDs) such as the human immunodeficiency virus (HIV) or Chlamydia. The most obvious way to generate such a dual-purpose contraceptive method would be to develop safe, effective spermicides that were also active against a wide range of pathogenic organisms. The currently available formulations such as nonoxynol-9, gramicidin and benzalkonium chloride are effective spermicides but are toxic to the vaginal epithelium and do not provide protection against STDs. Over 60 agents are in clinical trials as potentially safer topical spermicides and/or microbicides. Compounds that have reached this stage of development include acid buffers, detergents, dendrimers, non-nucleoside reverse transcriptase inhibitors and anionic polymers. In addition, a number of potential spermicides/microbicides are the subject of preclinical investigation, including beta-cyclodextrin, cyanovirin, porphyrins, cyclotriazadisulfonamides, dermaseptins, short-interfering RNA (siRNA) and HIV antibodies. The chemical principles underlying these disparate approaches and potential avenues for future investigation are discussed.
临床迫切需要研究新型生育控制方法，这些方法还能预防诸如人类免疫缺陷病毒（HIV）或衣原体等性传播疾病（STD）。研发这种两用避孕方法最显而易见的途径是开发安全、有效的杀精剂，这些杀精剂还能对多种致病生物起作用。目前可用的制剂，如壬苯醇醚 - 9、短杆菌肽和苯扎氯铵，是有效的杀精剂，但对阴道上皮有毒性，且不能预防STD。超过60种制剂正处于临床试验阶段，作为潜在更安全的局部杀精剂和/或杀菌剂。已进入该开发阶段的化合物包括酸缓冲剂、洗涤剂、树枝状大分子、非核苷逆转录酶抑制剂和阴离子聚合物。此外，一些潜在的杀精剂/杀菌剂正处于临床前研究阶段，包括β - 环糊精、氰基胍、卟啉、环三氮二磺酰胺、皮肤抗菌肽、短干扰RNA（siRNA）和HIV抗体。本文讨论了这些不同方法背后的化学原理以及未来研究的潜在途径。
