Gupta Gopal
Division of Endocrinology, Central Drug Research Institute, Lucknow, India.
Eur J Contracept Reprod Health Care. 2005 Dec;10(4):212-8. doi: 10.1080/13625180500280753.
Vaginal contraception, the oldest method of fertility regulation that remained virtually forgotten for a few decades has recently come under focal review due to an increase in STDs and HIV infections worldwide. Today it is being considered very strongly that a conceptual microbicidal spermicide can tender protection against pregnancy as well as STDs (including AIDS), simultaneously. However the two activities (spermicidal and microbicidal) need to be integrated in vaginal preparations, as many women across the world may be concerned more about the unwanted pregnancy rather than the STI during a coital act. A strong detergent like nonoxynol-9 (N-9) has been used as a spermicide in many local contraceptive preparations and studies have shown that it also exhibits significant microbicidal activity in vitro. However, recent clinical trials have shown that detergent spermicides do not provide any protection against STDs and AIDS but may in fact even promote their transmission. This anomaly has largely been attributed to their surfactant nature that irritates the vagina and kills the normal vaginal flora making it more susceptible to STD infections. An urgent need for a suitable non-detergent spermicide has thus emerged to replace N-9 in local contraceptive preparations. Anticipating the potential of spermicide-based vaginal contraceptives in the reproductive health of women, a large number of synthetic, non-detergent molecules were designed and evaluated at this Institute over recent years. Simultaneously, a number of natural products from terrestrial plants and marine flora/fauna were also evaluated for spermicidal activity. A local contraceptive preparation incorporating the active ingredient from the fruit pericarp of Sapindus mukorossi has successfully completed Phase III clinical trials in India and is ready for marketing. Recent studies have indicated that in comparison to N-9, this ingredient is much less toxic to Lactobacillus spp. and effectively inhibits the growth of Trichomonas vaginalis in vitro. Other candidate spermicides/microbicides under development worldwide have been reviewed briefly.
阴道避孕是最古老的生育调节方法，在几十年间几乎被遗忘，近来由于全球性传播疾病和艾滋病毒感染增多而受到重点审视。如今，人们强烈认为，一种概念性的杀微生物杀精剂能够同时预防怀孕和性传播疾病（包括艾滋病）。然而，这两种活性（杀精和杀微生物）需要整合到阴道制剂中，因为世界各地许多女性在性交过程中可能更担心意外怀孕而非性传播感染。一种强效洗涤剂壬苯醇醚 -9（N -9）在许多局部避孕制剂中被用作杀精剂，研究表明它在体外也具有显著的杀微生物活性。然而，最近的临床试验表明，洗涤剂类杀精剂并不能预防性病和艾滋病，实际上甚至可能促进其传播。这种异常情况很大程度上归因于它们的表面活性剂性质，这种性质会刺激阴道并杀死正常的阴道菌群，使其更容易受到性传播疾病感染。因此，迫切需要一种合适的非洗涤剂类杀精剂来取代局部避孕制剂中的N -9。鉴于基于杀精剂的阴道避孕药对女性生殖健康的潜在作用，近年来本研究所设计并评估了大量合成的、非洗涤剂类分子。同时，还对许多来自陆生植物和海洋动植物的天然产物进行了杀精活性评估。一种含有无患子果实果皮活性成分的局部避孕制剂已在印度成功完成三期临床试验，准备上市。最近的研究表明，与N -9相比，该成分对乳酸杆菌属的毒性要小得多，并且在体外能有效抑制阴道毛滴虫的生长。本文还简要综述了全球正在研发的其他候选杀精剂/杀微生物剂。
