MsrA Efflux Pump Inhibitory Activity of Piper cubeba L.f. and its Phytoconstituents against Staphylococcus aureus RN4220. Issue 8 (3rd July 2020)

• Record Type: Journal Article
• Authors: Ahirrao, Pallavi; Tambat, Rushikesh; Chandal, Nishtha; Mahey, Nisha; Kamboj, Anjoo; Jain, Upendra K.; Singh, Inder Pal; Jachak, Sanjay M.; Nandanwar, Hemraj S.
• Is Part Of: Chemistry & biodiversity. Volume 17:Issue 8(2020)
• Page Start: n/a
• Page End: n/a
• Publication Date: 2020-07-03
• Subjects: Piper cubeba -- methicillin-resistant Staphylococcus aureus (MRSA) -- MsrA efflux pump -- pellitorine -- sesamin -- phytoconstituents; Biochemistry -- Periodicals; Molecular biology -- Periodicals; Biodiversity -- Periodicals; 572
• DOI: 10.1002/cbdv.202000144
• Languages: English
• ISSNs: 1612-1872

Abstract

Abstract: MsrA, an efflux pump belonging to ATP‐binding cassette (ABC) transporter family that conferred resistance to macrolides, was detected in Staphylococcus aureus strains. Herein, we report the isolation of phytoconstituents from Piper cubeba fruit methanol extract and investigated their efflux pump inhibitory potential against S. aureus MsrA pump. Four isolated compounds, viz. pellitorine, sesamin, piperic acid and tetrahydropiperine 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. Abstract :