Identification of Antimycobacterial Natural Products from a Library of Marine Invertebrate Extracts

• Published in: Medicines (Basel, Switzerland) Vol. 9; no. 2; p. 9
• Main Authors: Acquah, Kojo Sekyi, Beukes, Denzil R, Seldon, Ronnett, Jordaan, Audrey, Sunassee, Suthananda N, Warner, Digby F, Gammon, David W
• Format: Journal Article
• Language: English
• Published: Switzerland MDPI AG 28.01.2022; MDPI
• Subjects: Analgesics; antitubercular; bengamides; drug discovery; Drugs; heteronemin; Invertebrates; Lipids; marine natural product; Metabolites; molecular networking; Natural products; Tuberculosis; Indian Ocean; Pacific Ocean; heteronemin; antitubercular; drug discovery; molecular networking; marine natural product; bengamides
• ISSN: 2305-6320; 2305-6320
• DOI: 10.3390/medicines9020009

Tuberculosis (TB) remains a public health crisis, requiring the urgent identification of new anti-mycobacterial drugs. We screened several organic and aqueous marine invertebrate extracts for their in vitro inhibitory activity against the causative organism, . Here, we report the results obtained for 54 marine invertebrate extracts. The chemical components of two of the extracts were dereplicated, using H NMR and HR-LCMS with GNPS molecular networking, and these extracts were further subjected to an activity-guided isolation process to purify the bioactive components. yielded heteronemin and was found to produce the bengamide class of compounds, of which bengamides P and Q were isolated, while a new derivative, bengamide S , was putatively identified and its structure predicted, based on the similarity of its MS/MS fragmentation pattern to those of other bengamides. The isolated bioactive metabolites and semi-pure fractions exhibited growth inhibitory activity, in the range <0.24 to 62.50 µg/mL. This study establishes the bengamides as potent antitubercular compounds, with the first report of whole-cell antitubercular activity of bengamides P and Q .