Octenidine/carbenicillin GUMBOS as potential treatment for oropharyngeal gonorrhoea
Octenidine/carbenicillin GUMBOS as potential treatment for oropharyngeal gonorrhoea
复制标题
奥替尼啶/羧苄西林 GUMBOS 作为口咽部淋病的潜在治疗方法
DOI：
10.1093/jac/dkaa346
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发表时间：
2020
影响因子：
5.2
通讯作者：
Warner, Isiah M
中科院分区：
文献类型：
--
作者：
Lopez, Kelsey M;Hobden, Jeffrey A;Warner, Isiah M
背景减少口咽部的淋病奈瑟菌菌落是最大程度地减少这种细菌在个体之间传播的可行解决方案。目的一种涉及常见防腐剂和已停用抗生素（即奥替尼啶和羧苄青霉素）之间静电相互作用的策略被评估为淋病的潜在治疗方法。奥替尼啶/羧苄西林是一组基于有机盐 (GUMBOS) 的新型均一材料，具有固有的体外抗菌活性，分别来自其母体防腐剂和抗菌离子奥替尼啶和羧苄西林。方法 奥替尼啶二盐酸盐、羧苄西林二钠、奥替尼啶/羧苄西林和化学计量相当的 1:1 奥替尼啶二盐酸盐的抗菌活性使用 Kirby-Bauer 纸片扩散测定法对 N 进行评估。淋球菌 (ATCC 49226) 和三种临床分离株。还评估了使用平行人工膜渗透性测定的预测渗透性和对 HeLa 细胞的细胞毒性。结果针对 N.N. 的附加体外抗菌活性。这项研究中观察到淋病菌，这表明奥替尼啶/羧苄青霉素可能是减少 N 的有用药物。淋病传播并最大限度地减少淋病感染。奥替尼啶/羧苄西林还表现出与目前处方的两种抗生素阿奇霉素和多西环素的生物等效性。同样，与奥替尼啶二盐酸盐相比，奥替尼啶/羧苄西林具有改善的预测渗透性。结论本研究中合成的抗菌GUMBOS可用作当前口咽部淋病感染控制和预防药物治疗的辅助治疗方法。
BackgroundReducingNeisseria gonorrhoeaecolonies in the oropharynx is a viable solution to minimize the transmission of this bacterium amongst individuals.ObjectivesA strategy involving the electrostatic interaction between a common antiseptic and a discontinued antibiotic (i.e. octenidine and carbenicillin) was evaluated as a potential treatment for gonorrhoea. Octenidine/carbenicillin is a novel group of uniform materials based on organic salts (GUMBOS) with inherentin vitroantibacterial activity that comes from its parent antiseptic and antibacterial ions, octenidine and carbenicillin, respectively.MethodsAntibacterial activities for octenidine dihydrochloride, disodium carbenicillin, octenidine/carbenicillin and stoichiometrically equivalent 1:1 octenidine dihydrochloride to disodium carbenicillin were assessed using the Kirby–Bauer disc diffusion assay forN. gonorrhoeae(ATCC 49226) and three clinical isolates. Predictive permeability using the Parallel Artificial Membrane Permeability Assay and cytotoxicity against HeLa cells was also evaluated.ResultsAdditivein vitroantibacterial activities againstN. gonorrhoeaewere observed in this study, which suggests octenidine/carbenicillin could be a useful agent in reducingN. gonorrhoeaetransmission and minimizing gonorrhoea infections. Octenidine/carbenicillin also exhibited bioequivalence to azithromycin and doxycycline, two currently prescribed antibiotics. Likewise, octenidine/carbenicillin had improved predicted permeability compared with octenidine dihydrochloride.ConclusionsAntimicrobial GUMBOS synthesized in this study could be used as an adjunctive treatment approach to current drug therapies for oropharyngeal gonorrhoea infection control and prevention.