Abstract
Tuberculosis has become a major health problem, in particular with the emergence of extremely drug resistant tuberculosis (XDRTB). In our search for new therapeutic leads against TB, we isolated a new triterpene (1) from the plant Rhus taitensis collected in Papua New Guinea. Tetrahydroxysqualene (1) was isolated using bioassay-guided fractionation of the methanolic extract of R. taitensis leaves and twigs. The structure of tetrahydroxysqualene (1) was elucidated on the basis of HRESIMS and 1D and 2D NMR spectra. Tetrahydroxysqualene (1) exhibited antituberculosis activity with an MIC of 10.0 microg/mL, while showing only modest cytotoxicity.
Publication types
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Research Support, N.I.H., Extramural
MeSH terms
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Antitubercular Agents* / chemistry
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Antitubercular Agents* / isolation & purification
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Antitubercular Agents* / pharmacology
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Drug Resistance, Bacterial / drug effects
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Drug Screening Assays, Antitumor
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Humans
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Microbial Sensitivity Tests
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Mycobacterium tuberculosis / drug effects*
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Nuclear Magnetic Resonance, Biomolecular
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Papua New Guinea
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Plant Leaves / chemistry
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Plant Stems / chemistry
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Plants, Medicinal / chemistry*
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Rhus / chemistry*
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Squalene* / analogs & derivatives
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Squalene* / chemistry
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Squalene* / isolation & purification
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Squalene* / pharmacology
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T-Lymphocytes / drug effects
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Tuberculosis / drug therapy
Substances
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Antitubercular Agents
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tetrahydroxysqualene
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Squalene