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MsrA efflux pump inhibitory activity of Piper cubeba L.f. and its phytoconstituents against Staphylococcus aureus RN4220
Chemistry & Biodiversity ( IF 2.9 ) Pub Date : 2020-07-03 , DOI: 10.1002/cbdv.202000144
Pallavi Ahirrao 1, 2 , Rushikesh Tambat 3 , Nishtha Chandal 3 , Nisha Mahey 3 , Anjoo Kamboj 1 , Upendra K Jain 1 , Inder Pal Singh 4 , Sanjay M Jachak 4 , Hemraj S Nandanwar 3
Affiliation  

Methionine sulfoxide reductase A (MsrA), an efflux pump belonging to ATP-binding cassette (ABC) transporter family that conferred resistance to macrolides, was detected in Methicillin-Resistant Staphylococcus aureus (MRSA) RN4220 strain. Herein we report isolation of phytoconstituents from Piper cubeba fruit methanol extract and investigated their efflux pump inhibitory potential against MsrA pump. Four isolated compounds viz. pellitorine, sesamin, piperic acid and tetrahydropiperine when studied in combination with erythromycin in S. aureus RN4220, exhibited 2-8 fold reduction in Minimum inhibitory concentration (MIC) of erythromycin. Pellitorine and sesamin decreased MIC of erythromycin by 8-fold. The real-time fluorometry-based efflux and accumulation studies of ethidium bromide (EtBr) on S. aureus RN4220 in the presence of these compounds showed reduced efflux and enhanced uptake, thus indicating inhibition of the efflux pump. Pellitorine showed significant post-antibiotic effect of erythromycin. The results revealed that the primary mechanism of action of these compounds involves steady ATP production impairment.

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中文翻译:

MsrA 外排泵抑制作用 小蒺藜 Lf 及其植物成分对金黄色葡萄球菌 RN4220 的抑制作用

甲硫氨酸亚砜还原酶 A (MsrA),属于 ATP 结合盒的外排泵(ABC)转运蛋白家族,为大环内酯类赋予的抗性,在耐甲氧西林检测金黄色葡萄球菌MRSA) RN4220 菌株。在这里我们报告从phytoconstituents的分离派山苍子果实甲醇提取物,并研究对MSRA泵的外排泵抑制的潜力。四个孤立的化合物即。当在金黄色葡萄球菌RN4220 中与红霉素联合研究时,胡椒碱、芝麻素、胡椒酸和四氢胡椒碱显示红霉素的最低抑菌浓度 (MIC) 降低了 2-8 倍。Pellitorine 和芝麻素使红霉素的 MIC 降低了 8 倍。基于实时荧光测定法的溴化乙锭 (EtBr) 对金黄色葡萄球菌的外排和积累研究RN4220 在这些化合物的存在下表现出减少的外排和增强的吸收,因此表明外排泵受到抑制。Pellitorine 显示出显着的红霉素后抗生素作用。结果表明,这些化合物的主要作用机制涉及稳定的 ATP 生产障碍。

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更新日期:2020-07-03
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