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Antimycobacterials from Lovage Root (Ligusticum officinale Koch)

Authors

  • Juan David Guzman,

    1. Mycobacteria Research Laboratory, Department of Biological Sciences, Institute of Structural and Molecular Biology, Birkbeck, University of London, London, UK
    2. Department of Pharmaceutical and Biological Chemistry, UCL School of Pharmacy, London, UK
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  • Dimitrios Evangelopoulos,

    1. Mycobacteria Research Laboratory, Department of Biological Sciences, Institute of Structural and Molecular Biology, Birkbeck, University of London, London, UK
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  • Antima Gupta,

    1. Mycobacteria Research Laboratory, Department of Biological Sciences, Institute of Structural and Molecular Biology, Birkbeck, University of London, London, UK
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  • Jose M. Prieto,

    1. Department of Pharmaceutical and Biological Chemistry, UCL School of Pharmacy, London, UK
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  • Simon Gibbons,

    Corresponding author
    • Department of Pharmaceutical and Biological Chemistry, UCL School of Pharmacy, London, UK
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  • Sanjib Bhakta

    Corresponding author
    • Mycobacteria Research Laboratory, Department of Biological Sciences, Institute of Structural and Molecular Biology, Birkbeck, University of London, London, UK
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Correspondence to: Professor Simon Gibbons, Department of Pharmaceutical and Biological Chemistry, UCL School of Pharmacy, 29–39 Brunswick Square, London WC1N 1AX, UK; Dr Sanjib Bhakta, Mycobacteria Research Laboratory, Department of Biological Sciences, Institute of Structural and Molecular Biology, Birkbeck, University of London, Malet Street, London WC1E 7HX, UK.

E-mail: simon.gibbons@ucl.ac.uk; s.bhakta@bbk.ac.uk

Abstract

The n-hexane extract of Lovage root was found to significantly inhibit the growth of both Mycobacterium smegmatis mc2155 and Mycobacterium bovis BCG, and therefore a bioassay-guided isolation strategy was undertaken. (Z)-Ligustilide, (Z)-3-butylidenephthalide, (E)-3-butylidenephthalide, 3-butylphthalide, α-prethapsenol, falcarindiol, levistolide A, psoralen and bergapten were isolated by chromatographic techniques, characterized by NMR spectroscopy and MS, and evaluated for their growth inhibition activity against Mycobacterium tuberculosis H37Rv using the whole-cell phenotypic spot culture growth inhibition assay (SPOTi). Cytotoxicity against RAW 264.7 murine macrophage cells was employed for assessing their degree of selectivity. Falcarindiol was the most potent compound with a minimum inhibitory concentration (MIC) value of 20 mg/L against the virulent H37Rv strain; however, it was found to be cytotoxic with a half-growth inhibitory concentration (GIC50) in the same order of magnitude (SI < 1). Interestingly the sesquiterpene alcohol α-prethapsenol was found to inhibit the growth of the pathogenic mycobacteria with an MIC value of 60 mg/L, being more specific towards mycobacteria than mammalian cells (SI ~ 2). Colony forming unit analysis at different concentrations of this phytochemical showed mycobacteriostatic mode of action. Copyright © 2012 John Wiley & Sons, Ltd.

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