Department of Biological Engineering, College of Engineering, Konkuk University, Seoul 05029, Republic of Korea.
College of Pharmacy and Graduate School of Pharmaceutical Sciences, Ewha Womans University, Seoul 03760, Republic of Korea.
J Microbiol Biotechnol. 2022 Jun 28;32(6):730-739. doi: 10.4014/jmb.2203.03054. Epub 2022 May 6.
Methicillin-resistant (MRSA) causes severe infections and poses a global healthcare challenge. The utilization of novel molecules which confer synergistical effects to existing MRSA-directed antibiotics is one of the well-accepted strategies in lieu of development of new antibiotics. Thymol is a key component of the essential oil of plants in the and . Despite the absence of antimicrobial potency, thymol is known to inhibit MRSA biofilm formation. However, the anti-MRSA activity of thymol analogs is not well characterized. Here, we assessed the antimicrobial activity of several thymol derivatives and found that 4-chloro-2-isopropyl-5-methylphenol (chlorothymol) has antimicrobial activity against MRSA and in addition it also prevents biofilm formation. Chlorothymol inhibited staphyloxanthin production, slowed MRSA motility, and altered bacterial cell density and size. This compound also showed a synergistic antimicrobial activity with oxacillin against highly resistant clinical isolates and biofilms associated with these isolates. Our results demonstrate that chlorinated thymol derivatives should be considered as a new lead compound in anti-MRSA therapeutics.
耐甲氧西林金黄色葡萄球菌（MRSA）可引起严重感染，是全球医疗保健面临的一个挑战。利用能与现有针对 MRSA 的抗生素产生协同作用的新型分子，是替代开发新型抗生素的一种公认策略。百里酚是和科植物精油的主要成分之一。尽管百里酚没有抗菌效力，但已知它可以抑制 MRSA 生物膜的形成。然而，百里酚类似物的抗 MRSA 活性尚未得到很好的描述。在这里，我们评估了几种百里酚衍生物的抗菌活性，发现 4-氯-2-异丙基-5-甲基苯酚（氯百里酚）对 MRSA 具有抗菌活性，此外，它还可以防止生物膜形成。氯百里酚抑制了金黄色素的产生，减缓了 MRSA 的运动能力，并改变了细菌的细胞密度和大小。该化合物还与苯唑西林对高度耐药的临床分离株和与这些分离株相关的生物膜表现出协同抗菌活性。我们的结果表明，氯化百里酚衍生物应被视为抗 MRSA 治疗的新先导化合物。
