Your browser doesn't support javascript.
loading
Bengamides display potent activity against drug-resistant Mycobacterium tuberculosis.
Quan, Diana H; Nagalingam, Gayathri; Luck, Ian; Proschogo, Nicholas; Pillalamarri, Vijaykumar; Addlagatta, Anthony; Martinez, Elena; Sintchenko, Vitali; Rutledge, Peter J; Triccas, James A.
Affiliation
  • Quan DH; Discipline of Infectious Diseases and Immunology, Faculty of Medicine and Health, The University of Sydney, Camperdown, NSW, Australia.
  • Nagalingam G; Tuberculosis Research Program, Centenary Institute, Sydney, NSW, Australia.
  • Luck I; Discipline of Infectious Diseases and Immunology, Faculty of Medicine and Health, The University of Sydney, Camperdown, NSW, Australia.
  • Proschogo N; Tuberculosis Research Program, Centenary Institute, Sydney, NSW, Australia.
  • Pillalamarri V; School of Chemistry, Faculty of Science, The University of Sydney, Camperdown, NSW, Australia.
  • Addlagatta A; School of Chemistry, Faculty of Science, The University of Sydney, Camperdown, NSW, Australia.
  • Martinez E; Centre for Chemical Biology, Indian Institute of Chemical Technology, Secunderabad, India.
  • Sintchenko V; Centre for Chemical Biology, Indian Institute of Chemical Technology, Secunderabad, India.
  • Rutledge PJ; Centre for Infectious Diseases and Microbiology, The Westmead Institute, Westmead, NSW, Australia.
  • Triccas JA; Marie Bashir Institute for Infectious Diseases and Biosecurity, The University of Sydney, Camperdown, NSW, Australia.
Sci Rep ; 9(1): 14396, 2019 10 07.
Article in En | MEDLINE | ID: mdl-31591407
Mycobacterium tuberculosis infects over 10 million people annually and kills more people each year than any other human pathogen. The current tuberculosis (TB) vaccine is only partially effective in preventing infection, while current TB treatment is problematic in terms of length, complexity and patient compliance. There is an urgent need for new drugs to combat the burden of TB disease and the natural environment has re-emerged as a rich source of bioactive molecules for development of lead compounds. In this study, one species of marine sponge from the Tedania genus was found to yield samples with exceptionally potent activity against M. tuberculosis. Bioassay-guided fractionation identified bengamide B as the active component, which displayed activity in the nanomolar range against both drug-sensitive and drug-resistant M. tuberculosis. The active compound inhibited in vitro activity of M. tuberculosis MetAP1c protein, suggesting the potent inhibitory action may be due to interference with methionine aminopeptidase activity. Tedania-derived bengamide B was non-toxic against human cell lines, synergised with rifampicin for in vitro inhibition of bacterial growth and reduced intracellular replication of M. tuberculosis. Thus, bengamides isolated from Tedania sp. show significant potential as a new class of compounds for the treatment of drug-resistant M. tuberculosis.
Subject(s)

Full text: 1 Collection: 01-internacional Database: MEDLINE Main subject: Azepines / Drug Resistance, Bacterial / Mycobacterium tuberculosis / Antitubercular Agents Language: En Journal: Sci Rep Year: 2019 Document type: Article Affiliation country: Australia Country of publication: United kingdom

Full text: 1 Collection: 01-internacional Database: MEDLINE Main subject: Azepines / Drug Resistance, Bacterial / Mycobacterium tuberculosis / Antitubercular Agents Language: En Journal: Sci Rep Year: 2019 Document type: Article Affiliation country: Australia Country of publication: United kingdom