Abstract

With the occurrence of antibiotic-resistant Staphylococcus aureus strains, identification of new anti-staphylococcal drugs has become a necessity. It has long been demonstrated that plants are a large and diverse source of antibacterial compounds. Psiloxylon mauritianum, an endemic medicinal plant from Reunion Island, was chemically investigated for its reported biological activity against S. aureus. Aspidin VB, a phloroglucinol derivative never before described, together with Aspidin BB, were first isolated from the ethyl acetate extract of P. mauritianum leaves. Their structures were elucidated from spectroscopic data. Aspidin VB exhibited strong antibacterial activity against standard and methicillin-resistant S. aureus strains, with a minimal inhibition concentration (MIC) of 0.25 μg/mL, and no cytotoxicity was observed at 10−5 M in MRC5 cells. Due to its biological activities, Aspidin VB appears to be a good natural lead in the fight against S. aureus.

Highlights

  • Staphylococcus aureus is a Gram-positive bacterium and the major cause of hospital-acquired infections, often resulting in longer stays and increases in patient mortality [1]

  • Our results indicated that compound 2 has the same minimal inhibition concentration (MIC) as oxacillin against S. aureus chain (2 additional carbons) on the acylfilinic acid moiety is correlated with 4- to 8-fold stronger and was 16-fold more potent than the standard antibiotic vancomycin against Methicillin-resistant Staphylococcus aureus (MRSA)

  • Chemical investigation of the ethyl acetate extraction of P. mauritianum leaves led to the first report of the known compounds Aspidin BB (1), ursolic acid (3) and oleanic acid (4) in this plant

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Summary

Introduction

Staphylococcus aureus is a Gram-positive bacterium and the major cause of hospital-acquired infections, often resulting in longer stays and increases in patient mortality [1]. Such S. aureus infections, promoted by the use of ventilators or venous catheters, affect the bloodstream, lower respiratory tract, and the skin and soft tissues [2]. The microbial world is ruled by adaptation to environmental pressure, and S. aureus has developed very effective tools to resist antibiotics since the introduction of penicillin in the 1940s to cure infections. The selective pressure of antibiotics continually promotes the emergence of drug-resistant strains of S. aureus, which have dramatically increased and spread around the world [3]. Due to the rapidity and extent of its spread, as well as the high diversity among clones and strain virulence, the WHO has classified MRSA as a high priority target for new antibiotic development [4]

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