Osman, K., Evangelopoulos, D., Basavannacharya, C., Gupta, A., McHugh, T.D., Bhakta, S. and Gibbons, S. (2012) An antibacterial from Hypericum acmosepalum inhibits ATP-dependent MurE ligase from Mycobacterium tuberculosis. International Journal of Antimicrobial Agents, 39 (2). pp. 124-129. 10.1016/j.ijantimicag.2011.09.018.
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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.
|Uncontrolled Keywords:||Hypercalin B; Hyperenone A; Hypericum acmosepalum; MurE ligase; Peptidoglycan; Staphylococcus aureus; Tuberculosis|
|Departments, units and centres:||Department of Pharmaceutical and Biological Chemistry > Department of Pharmaceutical and Biological Chemistry|
|Journal or Publication Title:||International Journal of Antimicrobial Agents|
|Deposited By:||Library Staff|
|Deposited On:||23 Mar 2012 11:39|
|Last Modified:||23 Mar 2012 11:39|
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