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Antimycobacterials from Lovage Root ( Ligusticum officinale Koch)

2013, Phytotherapy Research

The n-hexane extract of Lovage root was found to significantly inhibit the growth of both Mycobacterium smegmatis mc 2 155 and Mycobacterium bovis BCG, and therefore a bioassay-guided isolation strategy was undertaken. (Z)-Ligustilide, (Z)-3-butylidenephthalide, (E)-3-butylidenephthalide, 3-butylphthalide, a-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 H 37 Rv 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 H 37 Rv strain; however, it was found to be cytotoxic with a half-growth inhibitory concentration (GIC 50) in the same order of magnitude (SI < 1). Interestingly the sesquiterpene alcohol a-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.