排序酶A
金黄色葡萄球菌
糖苷
化学
多酚
毒力
最小抑制浓度
抗菌活性
微生物学
皂甙
耐甲氧西林金黄色葡萄球菌
生物化学
传统医学
细菌
体外
生物
抗氧化剂
立体化学
医学
基因
病理
替代医学
遗传学
作者
Wenhua Jing,Dandan Guo,Zunxi Ning,Ye Yang,Lei Zhu,Miao Wang,Huiyuan Gao
标识
DOI:10.1016/j.bioorg.2022.106193
摘要
Anti-virulence strategy represents an emerging alternative strategy in the war against increasing prevalence of methicillin-resistant Staphylococcus aureus (MRSA) due to its milder selection pressure on bacterial resistance. Sortase A (SrtA), as an important virulence factor, is a membrane-localized cysteine transpeptidase which anchors cell surface proteins to the cell wall. Natural products in medicinal plants are the source of targeting bacterial virulence factors. Here, we found polyphenolic glycosides (1-15), including thirteen new derivatives isolated from the stems of Caesalpinia cucullata, exhibited weak to moderate SrtA inhibitory activity without affecting the growth of MRSA, and compound 7 (53.7 % inhibition at 100 μM) was superior to the positive control curcumin. Meanwhile, compounds 2, 4 and 8 could effectively reduce the dose of ceftiofur in combination in vitro with fractional inhibitory concentration index (FICI) ranging from 0.188 to 0.375, which meant polyphenolic glycosides have got antibacterial activity with different ways. Here, we reported all new compounds structures determined by spectroscopy methods and their antibacterial activities, together, the relationship between structures with the inhibitory efficiency. The results indicated that polyphenolic glycosides could be used as promising therapeutic agents to prevent resistance development for S. aureus infections.
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