14-O-[(4,6-Diamino-pyrimidine-2-yl) thioacetyl] mutilin inhibits alpha-hemolysin and protects Raw264.7 cells from injury induced by methicillin-resistant S. aureus

文献类型： 外文期刊

第一作者： Fu, Yunxing

作者： Fu, Yunxing;Yang, Zhen;Zhang, Hongjuan;Liu, Yu;Hao, Baocheng;Shang, Ruofeng;Fu, Yunxing

作者机构：

关键词： DPTM; MRSA; alpha-Hemolysin; Raw264; 7 cells; Inflammation

期刊名称：MICROBIAL PATHOGENESIS （ 影响因子：3.738； 五年影响因子：3.664 ）

ISSN： 0882-4010

年卷期： 2021 年 161 卷

页码：

收录情况： SCI

摘要： A new pleuromutilin derivative, 14-O-[(4,6-Diaminopyrimidine-2-yl) thioacetyl] mutilin (DPTM), has been synthesized and proven to be a potent agent against Gram-positive pathogens, especially for Staphylococcus aureus (S. aureus). However, its pharmacological activities against alpha-hemolysin (Hla), a major virulence factor produced by S. aureus, and inflammations related to S. aureus are still unknown. In the present study, we investigated the DPTM inhibition activities against methicillin-resistant S. aureus (MRSA) Hla and protective efficacy of Raw264.7 cells from injury induced by MRSA. The results showed that DPTM with sub-inhibitory concentrations significantly inhibited Hla on the hemolysis of rabbit erythrocytes and down-regulated the gene expressions of Hla and agrA with a dose-dependent fashion. In Raw264.7 cells infected with MRSA, DPTM efficiently attenuated the productions of lactate dehydrogenase (LDH), nitric oxide (NO) and pro-inflammatory cytokines, as well as the express levels of nuclear factor-kappaB (NF-kappa B), nitric oxide synthase (iNOS) and cyclooxygenase-2 (COX-2). Furthermore, DPTM inhibited the translocation of p-65 to nucleus in RAW264.7 cells infected by MRSA.

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