Diterpenoids isolated from the Samoan marine sponge Chelonaplysilla sp. inhibit Mycobacterium tuberculosis growth

J Antibiot (Tokyo). 2020 Aug;73(8):568-573. doi: 10.1038/s41429-020-0315-4. Epub 2020 May 13.

Abstract

Crude extracts of the marine sponge Chelonaplysilla sp. collected in Samoa, that were obtained from the NCI Open Repository (NCS 21903), inhibited Mycobacterium tuberculosis growth. Assay-guided fractionation of the extract led to the isolation and structural elucidation of the known diterpenoid macfarlandin D (1) and three new diterpenoids macfarlandins F (2), G (3), and H (4). Macfarlandin D (1) exhibited potent antimicrobial activity against M. tuberculosis with an MIC of 1.2 ± 0.4 µg mL-1. Macfarlandins F (2), G (3), and H (4) exhibited significantly weaker antitubercular activities, revealing SAR for the macfarlandin antitubercular pharmacophore. The structures of compounds 2, 3, and 4 were elucidated via detailed analysis of NMR and MS data.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Animals
  • Antitubercular Agents / chemistry
  • Antitubercular Agents / pharmacology
  • Diterpenes / chemistry*
  • Diterpenes / pharmacology*
  • Magnetic Resonance Spectroscopy / methods
  • Microbial Sensitivity Tests / methods
  • Mycobacterium tuberculosis / drug effects*
  • Porifera / chemistry*

Substances

  • Antitubercular Agents
  • Diterpenes