Aaptamines, marine spongean alkaloids, as anti-dormant mycobacterial substances

J Nat Med. 2014 Apr;68(2):372-6. doi: 10.1007/s11418-013-0811-y. Epub 2014 Jan 12.

Abstract

A new aaptamine class alkaloid, designated 2-methoxy-3-oxoaaptamine (1), together with seven known aaptamines (2-8) were isolated from a marine sponge of Aaptos sp. as anti-mycobacterial substances against active and dormant bacilli. The chemical structure of 1 was determined on the basis of spectroscopic analysis. Compound 1 was anti-mycobacterial against Mycobacterium smegmatis in both active growing and dormancy-inducing hypoxic conditions with a minimum inhibitory concentration (MIC) of 6.25 μg/ml, and compounds 2, 5, 6, and 7 showed anti-mycobacterial activities under hypoxic condition selectively, with MIC values of 1.5-6.25 μg/ml.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Alkaloids / chemistry
  • Alkaloids / isolation & purification
  • Alkaloids / pharmacology
  • Animals
  • Anti-Bacterial Agents / chemistry
  • Anti-Bacterial Agents / isolation & purification
  • Anti-Bacterial Agents / pharmacology*
  • Microbial Sensitivity Tests
  • Mycobacterium smegmatis / drug effects
  • Naphthyridines / chemistry
  • Naphthyridines / isolation & purification
  • Naphthyridines / pharmacology*
  • Porifera / chemistry*

Substances

  • Alkaloids
  • Anti-Bacterial Agents
  • Naphthyridines
  • aaptamine