药理学评价从药蜀葵中提取的 Bakuchiol 对金黄色葡萄球菌的强效抗菌剂。

IF 2.5 3区 化学 Q3 BIOCHEMISTRY & MOLECULAR BIOLOGY Chemistry & Biodiversity Pub Date : 2024-11-25 DOI:10.1002/cbdv.202401272
Nancy Tripathi, Arnab Roy, Puja Kumari Agnivesh, Nivedita Bhardwaj, Sanju Kumari, Nitin Pal Kalia, Shreyans K. Jain
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引用次数: 0

摘要

由于金黄色葡萄球菌对多种药物产生抗药性,因此迫切需要找到新的替代品来有效对抗抗药性。Bakuchiol 是一种具有生物活性的前炔基酚类 Meroterpene,主要富含于 Psoralea corylifolia 的种子中。在本研究中,我们对从榛子中提取的巴克烯醇作为抗菌剂进行了生物学评估。金黄色葡萄球菌是一种重要的机会性病原体,因其生物膜的形成和对多种抗生素的耐受性而受到全球关注,并能逃脱抗生素的压力。将巴豆酚作为一种抗菌剂对金黄色葡萄球菌进行初步筛选后,发现它具有很强的杀菌潜力,其 MIC 和 MBC 分别为 2 μg/mL 和 8 μg/mL。重要的是,bakuchiol 对 HepG2 细胞的毒性也很低,选择性指数为 14.4。此外,Bakuchiol 对实验室产生的金黄色葡萄球菌环丙沙星耐药突变体也具有类似的活性(MIC = 2 μg/ mL)。Bakuchiol 能以剂量依赖的方式显著抑制金黄色葡萄球菌生物膜的形成,MBIC50 为 0.956 μg/mL。在 MIC 为 8 倍的浓度下,百草枯能有效抑制 DNA 回旋酶的超卷曲活性,从而确定了 DNA 回旋酶抑制是百草枯的作用机制。我们的研究结果表明,巴枯酚是金黄色葡萄球菌介导的鼻腔感染的潜在治疗药物。
本文章由计算机程序翻译,如有差异,请以英文原文为准。

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Pharmacological Evaluation of Bakuchiol From Psoralea corylifolia L. as Potent Antimicrobial Agent Against Staphylococcus aureus

The surge in multidrug resistance in Staphylococcus aureus is the pressing need to identify novel alternatives to combat antimicrobial resistance effectively. Bakuchiol is a bioactive prenylated phenolic meroterpene largely abundant in the seeds of Psoralea corylifolia. In this study, we present the biological assessment of bakuchiol derived from P. corylifolia as an antimicrobial agent. S. aureus, a significant opportunistic pathogen, attracts global concern for its biofilm formation and resilience against numerous antibiotics, escaping antibiotic pressure. The primary screening of bakuchiol as an antimicrobial agent against S. aureus delineated its potential as a strong bactericidal agent with a minimum inhibitory concentration (MIC) and minimum bactericidal concentration (MBC) of 2 and 8 µg/mL, respectively. Importantly, bakuchiol also exhibited low toxicity against HepG2 cells, showing a favorable selectivity index (SI) of 14.4. Furthermore, bakuchiol demonstrated comparable activity (MIC = 2 µg/mL) against a laboratory-generated ciprofloxacin-resistant mutant of S. aureus. Bakuchiol could significantly inhibit the biofilm formation of S. aureus in a dose-dependent manner with minimum biofilm inhibitory concentration (MBIC)50 of 0.956 µg/mL. Bakuchiol effectively inhibited DNA gyrase supercoiling activity at a concentration eight times the MIC, establishing DNA gyrase inhibition as the mechanism of action for bakuchiol. Our findings suggest bakuchiol as a potential therapeutic agent for S. aureus-mediated nosocomial infections.

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来源期刊
Chemistry & Biodiversity
Chemistry & Biodiversity 环境科学-化学综合
CiteScore
3.40
自引率
10.30%
发文量
475
审稿时长
2.6 months
期刊介绍: Chemistry & Biodiversity serves as a high-quality publishing forum covering a wide range of biorelevant topics for a truly international audience. This journal publishes both field-specific and interdisciplinary contributions on all aspects of biologically relevant chemistry research in the form of full-length original papers, short communications, invited reviews, and commentaries. It covers all research fields straddling the border between the chemical and biological sciences, with the ultimate goal of broadening our understanding of how nature works at a molecular level. Since 2017, Chemistry & Biodiversity is published in an online-only format.
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