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对耐甲氧西林金黄色葡萄球菌具有活性的植物化学物质。

Phytochemicals with activity against methicillin-resistant Staphylococcus aureus.

作者信息

Liang Miaomiao, Ge Xueliang, Xua Hui, Ma Kaifeng, Zhang Wei, Zan Yibo, Efferth Thomas, Xue Zheyong, Hua Xin

机构信息

Key Laboratory of Saline-alkali Vegetation Ecology Restoration (Northeast Forestry University), Ministry of Education, Harbin, China.

Department of Cell and Molecular Biology, Biomedical Center, Uppsala University, Uppsala SE-75124, Sweden.

出版信息

Phytomedicine. 2022 Jun;100:154073. doi: 10.1016/j.phymed.2022.154073. Epub 2022 Apr 1.

Abstract

BACKGROUND

The evolution of resistance to antimicrobials is a ubiquitous phenomenon. The evolution of antibiotic resistance in Staphylococcus aureus suggests that there is no remedy with sustaining effectiveness against this pathogen. The limited number of antibacterial drug classes and the common occurrence of cross-resistant bacteria reinforce the urgent need to discover new compounds targeting novel cellular functions. Natural products are a potential source of novel antibacterial agents. Anti-MRSA (methicillin-resistant S. aureus) bioactive compounds from Streptomyces and the anti-MRSA activity of a series of plant extracts have been reviewed respectively. However, there has been no detailed review of the precise bioactive components from plants.

PURPOSE

The present review aimed to summarize the phytochemicals that have been reported with anti-MRSA activities, analyze their structure-activity relationship and novel anti-MRSA mechanisms.

METHODS

Data contained in this review article are compiled from the authoritative databases PubMed, Web of Science, Google Scholar, and so on.

RESULTS

This review summarizes 100 phytochemicals (27 flavonoids, 23 alkaloids, 17 terpenes and 33 others) that have been tested for their anti-MRSA activity. Among these phytochemicals, 39 compounds showed remarkable anti-MRSA activity with MIC values less than 10 μg/ml, 14 compounds with MIC ranges including values < 10 μg/ml, 5 compounds with MIC values less than 5 μM; 11 phytochemicals show synergism anti-MRSA effects in combination with antibiotics. Phytochemicals exerted anti-MRSA activities mainly by destroying the membrane structure and inhibiting the efflux pump.

CONCLUSIONS

The 58 compounds with excellent anti-MRSA activity the 11 compounds with synergistic anti-MRSA effect, especially cannabinoids, xanthones and fatty acids should be further studied in vitro. Novel targets, such as cell membrane and efflux pump could be promising alternatives to develop antibacterial drugs in the future in order to prevent drug resistance.

摘要

背景

抗菌药物耐药性的演变是一种普遍现象。金黄色葡萄球菌抗生素耐药性的演变表明,没有对该病原体持续有效的补救措施。抗菌药物种类有限以及交叉耐药细菌的普遍存在,凸显了发现针对新型细胞功能的新化合物的迫切需求。天然产物是新型抗菌剂的潜在来源。分别综述了链霉菌产生的抗耐甲氧西林金黄色葡萄球菌(MRSA)生物活性化合物以及一系列植物提取物的抗MRSA活性。然而,尚未对植物中确切的生物活性成分进行详细综述。

目的

本综述旨在总结已报道具有抗MRSA活性的植物化学物质,分析其构效关系和新型抗MRSA机制。

方法

本综述文章中的数据来自权威数据库PubMed、Web of Science、谷歌学术等。

结果

本综述总结了100种已测试其抗MRSA活性的植物化学物质(27种黄酮类、23种生物碱、17种萜类和33种其他物质)。在这些植物化学物质中,39种化合物表现出显著的抗MRSA活性,其最低抑菌浓度(MIC)值小于10μg/ml,14种化合物的MIC范围包括小于10μg/ml的值,5种化合物的MIC值小于5μM;11种植物化学物质与抗生素联合显示出协同抗MRSA作用。植物化学物质主要通过破坏膜结构和抑制外排泵发挥抗MRSA活性。

结论

58种具有优异抗MRSA活性的化合物和11种具有协同抗MRSA作用的化合物,尤其是大麻素、呫吨酮和脂肪酸,应在体外进一步研究。细胞膜和外排泵等新靶点可能是未来开发抗菌药物以预防耐药性的有前景的替代方案。

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