Chan Ben C L, Han X Q, Lui Sau Lai, Wong C W, Wang Tina B Y, Cheung David W S, Cheng Sau Wan, Ip Margaret, Han Simon Q B, Yang Xiao-Sheng, Jolivalt Claude, Lau Clara B S, Leung Ping Chung, Fung Kwok Pui
Institute of Chinese Medicine, The Chinese University of Hong Kong, Hong Kong, China; State Key Laboratory of Phytochemistry & Plant Resources in West China (CUHK), The Chinese University of Hong Kong, Hong Kong, China.
J Pharm Pharmacol. 2015 Jan;67(1):107-16. doi: 10.1111/jphp.12315. Epub 2014 Sep 11.
The aims of this study were to identify the active ingredients from Portulaca oleracea L. (PO) that could provide synergism with antibiotics against methicillin-resistant Staphylococcus aureus (MRSA) and their possible mechanisms of resistance inhibition.
High-speed counter-current chromatography (HSCCC) coupled with gas chromatography-mass spectrometry and a panel of laboratory MRSA strains were used for checkerboard and efflux inhibitory assays.
Linoleic and oleic acids were identified from HSCCC fraction 18 of PO with synergistic antibacterial activity when combined with erythromycin against RN4220/pUL5054. Ethidium bromide efflux inhibitory studies revealed that linoleic and oleic acids may interfere the activity of MsrA pump. By comparing among a panel of linoleic and oleic acids analogues, unsaturated fatty acids in salt form with cis configuration and an increase in number of double bonds were found to further increase the antibacterial activity when used alone or in combination with antibiotics.
This study reported for the first time that two active ingredients, namely linoleic and oleic acids, were identified from PO with synergistic antibacterial activity when combined with erythromycin against MRSA RN4220/pUL5054 and possibly act by inhibiting the efflux pumps of the bacteria cells.
本研究旨在从马齿苋中鉴定出可与抗生素协同作用对抗耐甲氧西林金黄色葡萄球菌(MRSA)的活性成分及其可能的耐药抑制机制。
采用高速逆流色谱(HSCCC)结合气相色谱 - 质谱联用技术以及一组实验室MRSA菌株进行棋盘法和外排抑制试验。
从马齿苋的HSCCC第18部分中鉴定出亚油酸和油酸,它们与红霉素联合使用时对RN4220/pUL5054具有协同抗菌活性。溴化乙锭外排抑制研究表明,亚油酸和油酸可能干扰MsrA泵的活性。通过比较一组亚油酸和油酸类似物,发现盐形式的具有顺式构型且双键数量增加的不饱和脂肪酸在单独使用或与抗生素联合使用时可进一步增强抗菌活性。
本研究首次报道从马齿苋中鉴定出两种活性成分,即亚油酸和油酸,它们与红霉素联合使用时对MRSA RN4220/pUL5054具有协同抗菌活性,可能通过抑制细菌细胞的外排泵发挥作用。