An antibacterial from Hypericum acmosepalum inhibits ATP-dependent MurE ligase from Mycobacterium tuberculosis

Osman, Khadijo, Evangelopoulos, Dimitrios, Basavannacharya, Chandrakala, Gupta, Antima, McHugh, Timothy D., Bhakta, Sanjib and Gibbons, Simon (2012) An antibacterial from Hypericum acmosepalum inhibits ATP-dependent MurE ligase from Mycobacterium tuberculosis. International Journal of Antimicrobial Agents, 39 (2). pp. 124-129. ISSN 0924-8579

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Abstract

In a project to characterise new antibacterial chemotypes from plants, hyperenone A and hypercalin B were isolated from the hexane and chloroform extracts of the aerial parts of Hypericum acmosepalum. The structures of both compounds were characterised by extensive one- and two-dimensional nuclear magnetic resonance (NMR) spectroscopy and were confirmed by mass spectrometry. Hyperenone A and hypercalin B exhibited antibacterial activity against multidrug-resistant strains of Staphylococcus aureus, with minimum inhibition concentration ranges of 2-128 mg/L and 0.5-128 mg/L, respectively. Hyperenone A also showed growth-inhibitory activity against Mycobacterium tuberculosis H37Rv and Mycobacterium bovis BCG at 75 mg/L and 100 mg/L. Neither hyperenone A nor hypercalin B inhibited the growth of Escherichia coli and both were non-toxic to cultured mammalian macrophage cells. Both compounds were tested for their ability to inhibit the ATP-dependent MurE ligase of M. tuberculosis, a crucial enzyme in the cytoplasmic steps of peptidoglycan biosynthesis. Hyperenone A inhibited MurE selectively, whereas hypercalin B did not have any effect on enzyme activity.

Item Type: Article
Uncontrolled Keywords: hypercalin b,hyperenone a,hypericum acmosepalum,mure ligase,peptidoglycan,staphylococcus aureus,tuberculosis,microbiology (medical),infectious diseases,pharmacology (medical) ,/dk/atira/pure/subjectarea/asjc/2700/2726
Faculty \ School: Faculty of Science > School of Pharmacy
Related URLs:
Depositing User: LivePure Connector
Date Deposited: 15 Jul 2020 23:38
Last Modified: 04 Sep 2020 23:56
URI: https://ueaeprints.uea.ac.uk/id/eprint/76099
DOI: 10.1016/j.ijantimicag.2011.09.018

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