Wijesundara Niluni M, Lee Song F, Cheng Zhenyu, Davidson Ross, Langelaan David N, Rupasinghe H P Vasantha
Department of Biology, Faculty of Science, Dalhousie University, Halifax, NS B3H 3E2, Canada.
Department of Plant, Food, and Environmental Sciences, Faculty of Agriculture, Dalhousie University, Truro, NS B2N 5E3, Canada.
Pharmaceutics. 2022 Sep 21;14(10):1992. doi: 10.3390/pharmaceutics14101992.
Carvacrol, a mono-terpenoid phenol found in herbs, such as oregano and thyme, has excellent antibacterial properties against . However, its mechanism of bactericidal activity on has not been elucidated.
This study investigated the bactericidal mechanism of carvacrol using three strains of .
Flow cytometry (FCM) experiments were conducted to determine carvacrol's membrane permeabilization and cytoplasmic membrane depolarization activities. Protoplasts of were used to investigate carvacrol's effects on the membrane, followed by gel electrophoresis. The carvacrol-treated protoplasts were examined by transmission electron microscopy (TEM) to observe ultrastructural morphological changes. The fluidity of the cell membrane was measured by steady-state fluorescence anisotropy. Thin-layer chromatographic (TLC) profiling was conducted to study the affinity of carvacrol for membrane phospholipids.
Increased membrane permeability and decreased membrane potential from FCM and electron microscopy observations revealed that carvacrol killed the bacteria primarily by disrupting membrane integrity, leading to whole-cell lysis. Ultra-structural morphological changes in the membrane induced by carvacrol over a short period were confirmed using the protoplast and membrane isolate models in vitro. In addition, changes in the other biophysical properties of the bacterial membrane, including concentration- and time-dependent increased fluidity, were observed. TLC experiments showed that carvacrol preferentially interacts with membrane phosphatidylglycerol (P.G.), phosphatidylethanolamine (P.E.), and cardiolipins (CL).
Carvacrol exhibited rapid bactericidal action against by disrupting the bacterial membrane and increasing permeability, possibly due to affinity with specific membrane phospholipids, such as P.E., P.G., and CL. Therefore, the bactericidal concentration of carvacrol (250 µg/mL) could be used to develop safe and efficacious natural health products for managing streptococcal pharyngitis or therapeutic applications.
香芹酚是一种单萜类酚,存在于牛至和百里香等草药中,对……具有优异的抗菌性能。然而,其对……的杀菌活性机制尚未阐明。
本研究使用三株……研究香芹酚的杀菌机制。
进行流式细胞术(FCM)实验以确定香芹酚的膜通透性和细胞质膜去极化活性。使用……的原生质体研究香芹酚对膜的影响,随后进行凝胶电泳。通过透射电子显微镜(TEM)检查经香芹酚处理的原生质体,以观察超微结构形态变化。通过稳态荧光各向异性测量细胞膜的流动性。进行薄层色谱(TLC)分析以研究香芹酚对膜磷脂的亲和力。
FCM和电子显微镜观察结果显示膜通透性增加和膜电位降低,表明香芹酚主要通过破坏膜完整性杀死细菌,导致全细胞裂解。使用体外的……原生质体和膜分离模型证实了香芹酚在短时间内诱导的膜超微结构形态变化。此外,还观察到细菌膜其他生物物理性质的变化,包括浓度和时间依赖性的流动性增加。TLC实验表明,香芹酚优先与膜磷脂酰甘油(P.G.)、磷脂酰乙醇胺(P.E.)和心磷脂(CL)相互作用。
香芹酚通过破坏细菌膜并增加通透性,对……表现出快速杀菌作用,这可能是由于与特定膜磷脂如P.E.、P.G.和CL的亲和力所致。因此,香芹酚的杀菌浓度(250μg/mL)可用于开发安全有效的天然健康产品,用于治疗链球菌性咽炎或用于治疗应用。