Abstract
Context: The roots of Lophira lanceolata Van Tiegh. Ex Keay (Ochnaceae) have numerous medicinal values in the Central African region. Even though the MeOH extract of the roots has shown antimycobacterial activities, the constituents responsible for this inhibitory activity remain unknown.Objective: Phytochemical investigation of the MeOH root extract of L. lanceolata and determination of the antimycobacterial activities of that extract and constituents against the growth of Mycobacterium tuberculosis.Materials and methods: Column chromatography was used to provide bioactive phytoconstituents. Those compounds were elucidated using MS and NMR spectroscopic data. Antimycobacterial screening of the extract (4.882–5000 µg/mL in DMSO during 24 h at 37 °C) and isolated compounds (0.244–250 µg/mL in DMSO during 24 h at 37 °C) was performed by microplate alamar blue assay (MABA) against two mycobacterial strains.Results: The investigation of L. lanceolata MeOH roots extract provided of mixture of unseparated biflavonoids with a newly described one, dihydrolophirone A (1a) associated to lophirone A (1b). The bioactive compounds that effectively inhibited the growth of M. tuberculosis AC45 were found to be compounds 1 and 2. They exhibited MIC values of 31.25 and 15.75 µg/mL, respectively, and their MIC was found to be 62.5 µg/mL against resistant strain AC83.Discussion and conclusions: It is clearly evident from the results obtained that the mycobacterial activity of L. lanceolata could be related mainly to its steroid and flavonoid contents. Therefore, this study suggests the potential of the above-mentioned classes of compounds as promising candidate agents for developing new anti-tuberculosis drugs.
Highlights
Tuberculosis (TB) is a chronic contagious and deadly disease that spreads through the air
We report the isolation and identification of a new biflavonoid derivative and other constituents from the methanol extract of Lophira lanceolata with their antitubercular properties
IR spectra were recorded on an Alpha FT-IR Spectrometer from Bruker, while 1D and 2D NMR spectra were obtained on a Bruker DRX 500 (500 MHz for 1H and 125 MHz for 13C spectra) spectrometer (Bruker, Rheinstetten, Germany) with chemical shifts reported in d using TMS as an internal standard
Summary
Tuberculosis (TB) is a chronic contagious and deadly disease that spreads through the air. The high susceptibility of human immunodeficiency virus-infected persons to this illness, the proliferation of HIV/AIDS, and the emergence of multidrug-resistant strains of Mycobacterium tuberculosis (MDR) are contributing to the worsening impact of this disease (Bloom 2002). The first-line regimen for treating TB is considered old and prescribes rifampicin (RMP) and isoniazid (INH) as component drugs. These antibiotics overtime affect the rise of multi-drug resistant (MDR). This increasing drug resistance incidence has led to an urgent need to develop new antitubercular drugs with low toxicity to overcome these limitations and increase the armamentarium of the existing therapeutic drugs
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