Abstract

BackgroundMethicillin-resistant Staphylococcus aureus (MRSA) causes serious infections in hospitals. Penthorum chinense Pursh (PCP), employed by the Miao ethnic minority in China, presents antibacterial activities. In this study, the anti-Staphylococcus aureus activities in the pinocembrin-7-O residue-rich fraction from PCP (PGF) were evaluated and characterized.MethodsThe PGF was prepared with 70% ethanol reflux extraction followed by fractional extraction and column chromatography. Pinocembrin-7-O residue components were identified with electrospray ionization mass spectrometry (ESI-MS). Anti-S. aureus activities of the fraction and the main components were evaluated in vitro with serially diluted microbroth assays. Cytotoxicity was evaluated with 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide (MTT) chromogenic assays using the NCTC 1469 cell line.ResultsThis study indicated that the PGF and three components (S1, S2, and S3) presented anti-S. aureus activities, including against clinically isolated MRSA strains. The molecular masses of S1, S2, and S3 were identical to those of pinocembrin-7-O-[4″,6″-hexahydroxydiphenoyl (HHDP)]-β-D-glucose, pinocembrin-7-O-[3″-O-galloyl-4″,6″-(s)-HHDP]-β-D-glucose, and Thonningianin A, respectively. The PGF, S1, S2, and S3 all presented an identical minimum inhibitory concentration (MIC) against S. aureus ATCC 25923 and ATCC 43300, which was 62.5 μg/mL. The minimum bactericidal concentrations (MBCs) of the PGF and S3 against ATCC 25923 were 125 and 250 μg/mL, and the MBCs of the PGF, S2, and S3 against ATCC 43300 were 250, 500, and 250 μg/mL, respectively. A time-kill assay consistently indicated that none of the bacterial clones of ATCC 25923 and ATCC 43300 could survive under 2× and 4× MIC PGF treatment for 24 h, respectively. In contrast, 104 CFU (colony-forming units) of ATCC 25923 and ATCC 43300 were killed by 8× and 4× MIC S3 within 24 h, respectively. Additionally, 1×, 2×, and 4× MIC the PGF presented similar postantibiotic effects (PAEs) on the strain ATCC 25923. However, the PAE of the PGF on the strain ATCC 43300 was concentration dependent (1× < 2× < 4× MIC). Finally, the PGF (200 μg/mL) and S3 (60 μg/mL) showed no cytotoxicity against human hepatoma cells.ConclusionsThe PGF and S3 from PCP present potential for the treatment of S. aureus and MRSA infections. The components S1 and S2 present inhibition activities against S. aureus.

Highlights

  • Methicillin-resistant Staphylococcus aureus (MRSA) causes serious infections in hospitals

  • Pinocembrin-7-O residue-rich fraction in PCP (PGF) component characterization The components in the PGF fraction were analysed by an high-performance liquid chromatography (HPLC) system coupled with a UV monitor (Fig. 1)

  • The major components, S1 (Rt = 17.94 min), S2 (Rt = 20.22), and S3 (Rt = 22.13 min), were identified with HPLC combined with electrospray ionization mass spectrometry (ESI-MS)

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Summary

Introduction

Methicillin-resistant Staphylococcus aureus (MRSA) causes serious infections in hospitals. The anti-Staphylococcus aureus activities in the pinocembrin-7-O residue-rich fraction from PCP (PGF) were evaluated and characterized. Staphylococcus aureus, a gram-positive, facultative anaerobic bacterium with a round shape, is frequently isolated from the skin, eyes, and upper respiratory tract [1]. It is a common opportunistic pathogen and remains a major cause of skin infection. Some of them, such as methicillin, have been widely used against Staphylococcus infection. Methicillin-resistant Staphylococcus aureus (MRSA) was reported very rapidly. Vancomycin is used normally as an alternative antibiotic for MRSA infection treatment [6].

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