Perumal Shanmugapriya, Mahmud Roziahanim, Ismail Sabariah
Pharmaceutical Chemistry, School of Pharmaceutical Sciences, Universiti Sains Malaysia, Malaysia.
Centre for Herbal Standardization, Penang, Malaysia.
Pharmacogn Mag. 2017 Jul;13(Suppl 2):S311-S315. doi: 10.4103/pm.pm_309_15. Epub 2017 Jul 11.
The escalating dominance of resistant strains as infectious pathogen had urged the researchers to look for alternative and complementary drugs.
The objective of this study is to address the biological targets and probable mechanisms of action underlying the potent antibacterial effect of the isolated compounds from (L.) against .
The action mechanisms of caffeic acid (CA) and epicatechin 3-gallate (ECG) on cells were investigated by several bacterial physiological manifestations involving outer membrane permeabilization, intracellular potassium ion efflux, and nucleotide leakage.
The findings revealed that ECG and CA targeted both cell wall and cytoplasmic membrane of . The cellular membrane destruction and ensuing membrane permeability perturbation of had led to the ascending access of hydrophobic antibiotics, release of potassium ions, and leakages of nucleotides.
The overall study concludes that ECG and CA isolated from possess remarkable anti-infective potentials which can be exploited as drug template for the development of new antibacterial agent against resistant pathogen.
Epicatechin 3-gallate (ECG) and caffeic acid (CA) exhibited remarkable bactericidal abilities by increasing the outer membrane and plasma membrane permeability of pathogenECG and CA had facilitated the entry of hydrophobic antibiotics into by disintegrating the lipopolysaccharides layer of the outer membraneECG-induced potassium efflux with efficiency close to that obtained with cefepime suggesting mode of action through membrane disruptionBoth ECG and CA had caused consistent leakage of intracellular nucleotide content with the increase in time. ECG: Epicatechin 3-gallate; CA: Caffeic acid; : Euphoria hirta.
耐药菌株作为感染病原体的优势不断升级，促使研究人员寻找替代和补充药物。
本研究的目的是探讨从（L.）中分离出的化合物对的强效抗菌作用的生物学靶点和可能的作用机制。
通过几种细菌生理表现，包括外膜通透性、细胞内钾离子外流和核苷酸泄漏，研究了咖啡酸（CA）和表儿茶素3-没食子酸酯（ECG）对细胞的作用机制。
研究结果表明，ECG和CA靶向的细胞壁和细胞质膜。细胞膜的破坏以及随之而来的膜通透性扰动导致疏水性抗生素的进入增加、钾离子的释放和核苷酸的泄漏。
总体研究得出结论，从分离出的ECG和CA具有显著的抗感染潜力，可作为开发针对耐药病原体的新型抗菌剂的药物模板。
表儿茶素3-没食子酸酯（ECG）和咖啡酸（CA）通过增加病原体的外膜和质膜通透性表现出显著的杀菌能力ECG和CA通过分解外膜的脂多糖层促进疏水性抗生素进入ECG诱导的钾外流效率接近头孢吡肟，表明其作用方式是通过膜破坏随着时间的增加，ECG和CA均导致细胞内核苷酸含量持续泄漏。ECG：表儿茶素3-没食子酸酯；CA：咖啡酸；：地锦草。
