Antitubercular evaluation of root extract and isolated phytochemicals from Lophira lanceolata against two resistant strains of Mycobacterium tuberculosis

Pharm Biol. 2018 Dec;56(1):318-324. doi: 10.1080/13880209.2018.1476559.

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.

Keywords: Ochnaceae; antitubercular activity; biflavonoids; dihydrolophirone A; steroids.

MeSH terms

  • Antitubercular Agents / isolation & purification
  • Antitubercular Agents / pharmacology*
  • Drug Evaluation, Preclinical / methods
  • Drug Resistance, Multiple, Bacterial / drug effects*
  • Drug Resistance, Multiple, Bacterial / physiology
  • Humans
  • Microbial Sensitivity Tests / methods
  • Mycobacterium tuberculosis / drug effects*
  • Mycobacterium tuberculosis / physiology
  • Ochnaceae*
  • Phytochemicals / isolation & purification
  • Phytochemicals / pharmacology*
  • Plant Extracts / isolation & purification
  • Plant Extracts / pharmacology*

Substances

  • Antitubercular Agents
  • Phytochemicals
  • Plant Extracts

Grants and funding

The authors gratefully acknowledge financial support from the Swiss National Science Foundation (SNSF) (No.: IZK0Z2-157272) for research fellowships in Switzerland to D. S. Ngono Bikobo. The authors also acknowledge the DAAD/STIBET Doktoranden Scholarship for financial support and travel grants for Mr. Mbabi to Germany.