没食子酸及其衍生物对耐多药细菌的抗菌评估

IF 1.9 4区 医学 Q3 CHEMISTRY, MEDICINAL
Mohamed Abdella, Chandrajit Lahiri, Iskandar Abdullah, Ayaz Anwar
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引用次数: 0

摘要

背景:传染病是全球第二大死因。病原菌对抗生素产生了巨大的抗药性,这给医疗系统带来了额外的负担。没食子酸属于天然酚类化合物,具有广泛的抗菌活性:在这项研究中,我们合成了十三种没食子酸衍生物,并在体外评估了它们对七种多重耐药细菌的抗菌潜力以及对人类胚胎肾细胞系的细胞毒性作用。方法:成功合成了 13 种化合物,并对其进行了评估。利用核磁共振光谱、质谱和傅立叶变换红外光谱对合成的衍生物进行了表征。抗菌活性采用微量稀释法测定,细胞毒性采用 MTT 法评估:抗菌试验结果表明,13 种化合物中有 7 种具有抗菌效果,其中化合物 6 和 13 对金黄色葡萄球菌(MIC 为 56 μg/mL)和肠炎沙门氏菌(MIC 为 475 μg/mL)的抗菌效果最强。另一方面,大多数化合物对人类胚胎肾细胞(HEK 293)的细胞毒性较低,IC50 值在 700 μg/mL 以上:值得注意的是,化合物 13 在浓度高达 5000 μg/mL 时也无毒性。这些发现表明,目前的没食子酸合成衍生物具有进一步研究开发强效抗菌剂的潜力。
本文章由计算机程序翻译,如有差异,请以英文原文为准。
Antibacterial Evaluation of Gallic Acid and its Derivatives against a Panel of Multi-drug Resistant Bacteria.

Background: Infectious diseases are the second leading cause of deaths worldwide. Pathogenic bacteria have been developing tremendous resistance against antibiotics which has placed an additional burden on healthcare systems. Gallic acid belongs to a naturally occurring phenolic class of compounds and is known to possess a wide spectrum of antimicrobial activities.

Aims & objectives: In this study, we synthesized thirteen derivatives of gallic acid and evaluated their antibacterial potential against seven multi-drug resistant bacteria, as well as cytotoxic effects against human embryonic kidney cell line in vitro. Methods: 13 compounds were successfully synthesized with moderate to good yield and evaluated. Synthesized derivatives were characterized by using nuclear magnetic resonance spectroscopy, mass spectrometry, and Fourier transformation infrared spectroscopy. Antibacterial activity was determined using microdilution while cytotoxicyt was assessed using MTT assay.

Results: The results of antibacterial assay showed that seven out of thirteen compounds exhibited antibacterial effects with compound 6 and 13 being most potent against Staphylococcus aureus (MIC 56 μg/mL) and Salmonella enterica (MIC 475 μg/mL) respectively. On the other hand, most of these compounds showed lower cytotoxicity against human embryonic kidney cells (HEK 293), with IC50 values ranging from over 700 μg/mL.

Conclusion: Notably, compound 13 was found to be non-toxic at concentrations as high as 5000 μg/mL. These findings suggest that the present synthetic derivatives of gallic acid hold potential for further studies in the development of potent antibacterial agents.

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来源期刊
Medicinal Chemistry
Medicinal Chemistry 医学-医药化学
CiteScore
4.30
自引率
4.30%
发文量
109
审稿时长
12 months
期刊介绍: Aims & Scope Medicinal Chemistry a peer-reviewed journal, aims to cover all the latest outstanding developments in medicinal chemistry and rational drug design. The journal publishes original research, mini-review articles and guest edited thematic issues covering recent research and developments in the field. Articles are published rapidly by taking full advantage of Internet technology for both the submission and peer review of manuscripts. Medicinal Chemistry is an essential journal for all involved in drug design and discovery.
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