HOMEPRODUCTSCOMPANYCONTACTFAQResearchDictionaryPharmaSign Up FREE or Login

Halicyclamine A, a marine spongean alkaloid as a lead for anti-tuberculosis agent.

Abstract
In the course of our search for anti-microbial agents against dormant Mycobacterium tuberculosis, halicyclamine A was re-discovered as a lead for anti-tuberculosis agent from a marine sponge of Haliclona sp. on the guidance of the constructed bioassay. Halicyclamine A showed growth inhibition against Mycobacterium smegmatis, Mycobacterium bovis BCG, and M. tuberculosis H37Ra with MICs in the range of 1.0-5.0microg/ml under both aerobic condition and hypoxic condition inducing dormant state. The growth-inhibitory activity of halicyclamine A was bactericidal, and halicyclamine A did not exhibit cross-resistance with the currently used anti-tuberculosis drugs of isoniazid, ethambutol, rifampicin, and streptomycin. Halicyclamine A has been isolated originally as one of the active constituents inhibiting inosine 5'-monophosphate dehydrogenase (IMPDH). Then, in order to elucidate action-mechanism of halicyclamine A, we prepared IMPDH over-expressing strains of M. smegmatis. However, IMPDH was not target for halicyclamine A, because halicyclamine A showed same MIC value against the wild-type M. smegmatis and IMPDH over-expressing strains.
AuthorsMasayoshi Arai, Mari Sobou, Catherine Vilchéze, Anthony Baughn, Hiroyuki Hashizume, Patamaporn Pruksakorn, Shunsuke Ishida, Makoto Matsumoto, William R Jacobs Jr, Motomasa Kobayashi
JournalBioorganic & medicinal chemistry (Bioorg Med Chem) Vol. 16 Issue 14 Pg. 6732-6 (Jul 15 2008) ISSN: 1464-3391 [Electronic] England
PMID18556206 (Publication Type: Journal Article, Research Support, Non-U.S. Gov't)
Chemical References
  • Alkaloids
  • Anti-Bacterial Agents
  • Antitubercular Agents
  • Biological Products
  • Bridged Bicyclo Compounds
  • Piperidines
  • halicyclamine A
  • IMP Dehydrogenase
Topics
  • Alkaloids
  • Animals
  • Anti-Bacterial Agents
  • Antitubercular Agents (pharmacology)
  • Biological Products
  • Bridged Bicyclo Compounds (pharmacology)
  • IMP Dehydrogenase (antagonists & inhibitors)
  • Microbial Sensitivity Tests
  • Mycobacterium (drug effects)
  • Mycobacterium bovis (drug effects)
  • Mycobacterium smegmatis (drug effects)
  • Mycobacterium tuberculosis (drug effects)
  • Piperidines (pharmacology)
  • Porifera
  • Species Specificity

Join CureHunter, for free Research Interface BASIC access!

Take advantage of free CureHunter research engine access to explore the best drug and treatment options for any disease. Find out why thousands of doctors, pharma researchers and patient activists around the world use CureHunter every day.
Realize the full power of the drug-disease research graph!


Choose Username:
Email:
Password:
Verify Password:
Enter Code Shown: