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In Vitro Activity of Quaternary Ammonium Surfactants against Streptococcal Chlamydial and Gonococcal Infective Agents

机译:季铵表面活性剂对链球菌衣原体和淋球菌感染剂的体外活性。

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摘要

Quaternary ammonium compounds (QAC) are widely used, cheap, and chemically stable disinfectants and topical antiseptics with wide-spectrum antimicrobial activities. Within this group of compounds, we recently showed that there are significant differences between the pharmacodynamics of n-alkyl quaternary ammonium surfactants (QAS) with a short (C12) alkyl chain when in vitro toxicities toward bacterial and mammalian epithelial cells are compared. These differences result in an attractive therapeutic window that justifies studying short-chain QAS as prophylactics for sexually transmitted infections (STI) and perinatal vertically transmitted urogenital infections (UGI). We have evaluated the antimicrobial activities of short-chain (C12) n-alkyl QAS against several STI and UGI pathogens as well as against commensal Lactobacillus species. Inhibition of infection of HeLa cells by Neisseria gonorrhoeae and Chlamydia trachomatis was studied at concentrations that were not toxic to the HeLa cells. We show that the pathogenic bacteria are much more susceptible to QAS toxic effects than the commensal vaginal flora and that QAS significantly attenuate the infectivity of N. gonorrhoeae and C. trachomatis without affecting the viability of epithelial cells of the vaginal mucosa. N-Dodecylpyridinium bromide (C12PB) was found to be the most effective QAS. Our results strongly suggest that short-chain (C12) n-alkyl pyridinium bromides and structurally similar compounds are promising microbicide candidates for topical application in the prophylaxis of STI and perinatal vertical transmission of UGI.
机译:季铵化合物(QAC)被广泛使用,廉价,化学稳定的消毒剂和具有广谱抗菌活性的局部防腐剂。在这组化合物中,我们最近显示,当比较对细菌和哺乳动物上皮细胞的体外毒性时,具有短(C12)烷基链的正烷基季铵盐表面活性剂(QAS)的药效学之间存在显着差异。这些差异导致了一个有吸引力的治疗窗口,该窗口证明了对短链QAS作为性传播感染(STI)和围产期垂直传播的泌尿生殖道感染(UGI)的预防措施进行研究的合理性。我们已经评估了短链(C12)正烷基QAS对几种STI和UGI病原体以及共生乳酸杆菌的抗微生物活性。淋病奈瑟菌和沙眼衣原体对HeLa细胞的感染抑制作用在对HeLa细胞无毒的浓度下进行了研究。我们表明,病原细菌比普通阴道菌群对QAS毒性作用更敏感,并且QAS显着减弱了淋病奈瑟氏球菌和沙眼衣原体的感染力,而没有影响阴道黏膜上皮细胞的活力。 N-十二烷基溴化吡啶鎓(C12PB)被发现是最有效的QAS。我们的研究结果强烈表明,短链(C12)正烷基溴化吡啶鎓和结构相似的化合物有望用于局部预防STI和围产期UGI垂直传播的杀菌剂。

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