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一种合成强效抗菌三环类黄酮的环保方法。

An Eco-Friendly Method to Synthesize Potent Antimicrobial Tricyclic Flavonoids.

作者信息

Mantea Loredana-Elena, Moldovan Cristina-Veronica, Savu Mihaela, Sarbu Laura Gabriela, Stefan Marius, Birsa Mihail Lucian

机构信息

Department of Biology, Faculty of Biology, Alexandru Ioan Cuza University of Iasi, Bd. Carol I, No. 11, 700506 Iasi, Romania.

Department of Chemistry, Alexandru Ioan Cuza University of Iasi, No. 11 Carol I Blvd., 700506 Iasi, Romania.

出版信息

Antibiotics (Basel). 2024 Aug 24;13(9):798. doi: 10.3390/antibiotics13090798.

Abstract

The rapid emergence and spread of multidrug-resistant microorganisms is threatening our ability to treat common infections, with serious medical, social, and economic consequences. Despite substantial progress in the global fight against antibiotic resistance, the number of effective antibiotics is rapidly decreasing, underlying the urgent need to develop novel antimicrobials. In the present study, the green synthesis of novel iodine-substituted tricyclic flavonoids has been accomplished using an eco-friendly reagent, HPW-SiO, as a cyclization agent for the precursor 3-dithiocarmamic flavanones. In vitro antimicrobial activity of the new compounds was evaluated using minimum inhibitory concentration (MIC) and minimum bactericidal/fungicidal concentrations. All tested compounds displayed potent inhibitory activity against all tested microbial strains, with the lowest MIC values of 0.12 µg/mL and 0.48 µg/mL recorded for compound against Gram-positive bacteria and . Higher MIC values (7.81 µg/mL) were registered for several flavonoids against Gram-negative bacteria and . No inhibitory activity was evidenced against strain. The highest antifungal activity was displayed by flavonoid against (MIC = 3.9 µg/mL). The same compound also exhibited the most potent bactericidal and fungicidal activity against (0.9 µg/mL) and (1.97 µg/mL), and (7.81 µg/mL). Based on the reported results, we believe that the novel iodine-substituted tricyclic flavonoids have good potential to become new antimicrobial agents effective against bacterial and fungal strains, including WHO-priority pathogens.

摘要

多重耐药微生物的迅速出现和传播正威胁着我们治疗常见感染的能力,会带来严重的医学、社会和经济后果。尽管全球在抗击抗生素耐药性方面取得了重大进展,但有效抗生素的数量却在迅速减少,这凸显了开发新型抗菌药物的迫切需求。在本研究中,使用环保试剂HPW-SiO作为前体3-二硫代氨基甲酰黄烷酮的环化剂,完成了新型碘取代三环类黄酮的绿色合成。使用最低抑菌浓度(MIC)和最低杀菌/杀真菌浓度评估了新化合物的体外抗菌活性。所有测试化合物对所有测试微生物菌株均显示出强效抑制活性,化合物对革兰氏阳性菌和的最低MIC值分别为0.12 µg/mL和0.48 µg/mL。几种黄酮类化合物对革兰氏阴性菌和的MIC值较高(7.81 µg/mL)。对菌株未显示出抑制活性。黄酮类化合物对的抗真菌活性最高(MIC = 3.9 µg/mL)。同一化合物对(0.9 µg/mL)、(1.97 µg/mL)、和(7.81 µg/mL)也表现出最强的杀菌和杀真菌活性。基于报告结果,我们认为新型碘取代三环类黄酮有很大潜力成为对包括世界卫生组织重点病原体在内的细菌和真菌菌株有效的新型抗菌剂。

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