Structure optimizing of flavonoids against both MRSA and VRE

doi:10.1016/j.ejmech.2024.116401

KIB OpenIR

	Structure optimizing of flavonoids against both MRSA and VRE
	Wei, Mei-Zhen; Zhu, Yan-Yan; Zu, Wen-Biao; Wang, Huan; Bai, Li -Yu; Zhou, Zhong-Shun; Zhao, Yun-Li; Wang, Zhao-Jie; Luo, Xiao-Dong
	2024
发表期刊	EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
ISSN	0223-5234
卷号	271 页码:116401
摘要	Methicillin-resistant Staphylococcus aureus (MRSA) and vancomycin-resistant Enterococci (VRE) cause more than 100,000 deaths each year, which need efficient and non-resistant antibacterial agents. SAR analysis of 162 flavonoids from the plant in this paper suggested that lipophilic group at C-3 was crucial, and then 63 novel flavonoid derivatives were designed and total synthesized. Among them, the most promising K15 displayed potent bactericidal activity against clinically isolated MRSA and VRE (MICs = 0.25 -1.00 mu g/mL) with low toxicity and high membrane selectivity. Moreover, mechanism insights revealed that K15 avoided resistance by disrupting biofilm and targeting the membrane, while vancomycin caused 256 times resistance against MRSA, and ampicillin caused 16 times resistance against VRE by the same 20 generations inducing. K15 eliminated residual bacteria in mice skin MRSA-infected model ( >99 %) and abdominal VRE-infected model ( >92 %), which was superior to vancomycin and ampicillin.
DOI	10.1016/j.ejmech.2024.116401
WOS记录号	WOS:001232155100001
引用统计
文献类型	期刊论文
条目标识符	http://ir.kib.ac.cn/handle/151853/76320
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,Zhu, Yan-Yan,Zu, Wen-Biao,et al. Structure optimizing of flavonoids against both MRSA and VRE[J]. EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY,2024,271:116401.
APA	Wei, Mei-Zhen.,Zhu, Yan-Yan.,Zu, Wen-Biao.,Wang, Huan.,Bai, Li -Yu.,...&Luo, Xiao-Dong.(2024).Structure optimizing of flavonoids against both MRSA and VRE.EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY,271,116401.
MLA	Wei, Mei-Zhen,et al."Structure optimizing of flavonoids against both MRSA and VRE".EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY 271(2024):116401.

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