Oleanolic acid derivatives against drug-resistant bacteria and fungi by multi-targets to avoid drug resistance

doi:10.1016/j.ejmech.2024.116940

KIB OpenIR

	Oleanolic acid derivatives against drug-resistant bacteria and fungi by multi-targets to avoid drug resistance
	Wei, Mei-Zhen; Wang, Zhao-Jie; Zhu, Yan-Yan; Zu, Wen-Biao; Zhao, Yun-Li; Luo, Xiao-Dong
	2024
发表期刊	EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
ISSN	0223-5234
卷号	280 页码:116940
摘要	Mixed infections caused by drug-resistant bacteria and fungi pose a severe threat to human health, and multitarget drugs may provide an effective approach to combat drug-resistant pathogens. Therefore, this study aimed to investigate the efficacies of some oleanolic acid (OA) derivatives against multidrug-resistant (MDR) bacteria and fungi using in vitro and in vivo experiments. Novel amphiphilic OA derivatives were designed and optimised, in which compounds G1 and J1 exhibited effective antimicrobial activity (MICs = 1-2 mu g/mL), high selectivity against MDR strains, rapid bactericidal activity, and good predictive pharmacokinetics. Mechanistically, both compounds prevented drug resistance by disrupting the bacterial cell membrane, inserting into the DNA, and binding to DNA gyrase. Additionally, J1 reduced microbial count in a mouse MRSA skin infection model and accelerated wound healing much better than vancomycin. Conclusively, this study presents a new class of potential drugs for resistant bacteria and fungi.
DOI	10.1016/j.ejmech.2024.116940
WOS记录号	WOS:001336083600001
引用统计
文献类型	期刊论文
条目标识符	http://ir.kib.ac.cn/handle/151853/76103
专题	中国科学院昆明植物研究所
推荐引用方式 GB/T 7714	Wei, Mei-Zhen,Wang, Zhao-Jie,Zhu, Yan-Yan,et al. Oleanolic acid derivatives against drug-resistant bacteria and fungi by multi-targets to avoid drug resistance[J]. EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY,2024,280:116940.
APA	Wei, Mei-Zhen,Wang, Zhao-Jie,Zhu, Yan-Yan,Zu, Wen-Biao,Zhao, Yun-Li,&Luo, Xiao-Dong.(2024).Oleanolic acid derivatives against drug-resistant bacteria and fungi by multi-targets to avoid drug resistance.EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY,280,116940.
MLA	Wei, Mei-Zhen,et al."Oleanolic acid derivatives against drug-resistant bacteria and fungi by multi-targets to avoid drug resistance".EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY 280(2024):116940.

条目包含的文件		下载所有文件
文件名称/大小	文献类型	版本类型	开放类型	使用许可
10.1016_j.ejmech.202（7454KB）	期刊论文	出版稿	开放获取	CC BY-NC-SA	浏览下载