Lawung Ratana, Cherdtrakulkiat Rungrot, Nabu Sunanta, Prachayasittikul Supaluk, Isarankura-Na-Ayudhya Chartchalerm, Prachayasittikul Virapong
Department of Clinical Microbiology and Applied Technology, Faculty of Medical Technology, Mahidol University, Bangkok 10700, Thailand.
Center of Data Mining and Biomedical Informatics, Faculty of Medical Technology, Mahidol University, Bangkok 10700, Thailand.
EXCLI J. 2018 Aug 23;17:840-846. doi: 10.17179/excli2018-1602. eCollection 2018.
The multidrug resistance of becomes a public health problem worldwide, especially the strain H041 that showed the decrease susceptibility to ceftriaxone which is the last resort for gonorrhea treatment. Therefore, the simultaneous discovery and development of a new compound to fight this pathogen is urgently required. In this study, 8-hydroxyquinoline (8HQ) and derivatives were evaluated for their antimicrobial activities against the gonococcal pathogen using spectinomycin as the reference drug. The results showed that 8HQ derivatives gave an excellent antimicrobial potency. Particularly, the dihalogenated 8HQ (iodoquinol, clioquinol and 5,7-diCl-8HQ) exerted the high activity with MIC range of 0.08-0.15 μM, 0.10-0.20 μM and 0.28-0.56 µM, respectively, compared with the reference drug (MIC = 16 μg/mL or 48.14 μM). Moreover, these compounds were also shown to be non-cytotoxic/very high safety index. The findings reveal that these three compounds could be further developed as a new antimicrobial agent for fighting the gonorrheal disease.
淋病奈瑟菌的多重耐药性已成为全球公共卫生问题，尤其是H041菌株，它对头孢曲松（淋病治疗的最后手段）的敏感性降低。因此，迫切需要同时发现和开发一种新的化合物来对抗这种病原体。在本研究中，以壮观霉素作为参考药物，评估了8-羟基喹啉（8HQ）及其衍生物对淋病菌原体的抗菌活性。结果表明，8HQ衍生物具有优异的抗菌效力。特别是，二卤代8HQ（碘喹啉、氯碘喹啉和5,7-二氯-8HQ）表现出高活性，其MIC范围分别为0.08 - 0.15 μM、0.10 - 0.20 μM和0.28 - 0.56 μM，而参考药物的MIC为16 μg/mL或48.14 μM。此外，这些化合物还显示出无细胞毒性/非常高的安全指数。研究结果表明，这三种化合物可进一步开发成为对抗淋病的新型抗菌剂。
