Identification of cyclic hexapeptides natural products with inhibitory potency against Mycobacterium tuberculosis

OBJECTIVE: Our aim was to identify natural products with anti-tubercular activity. RESULTS: A set of ~ 500 purified natural product compounds was screened for inhibition against the human pathogen Mycobacterium tuberculosis. A series of cyclic hexapeptides with anti-tubercular activity was identifie...

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Detalles Bibliográficos
Autores principales: Singh, Sheo B., Odingo, Joshua, Bailey, Mai A., Sunde, Bjorn, Korkegian, Aaron, O’Malley, Theresa, Ovechkina, Yulia, Ioerger, Thomas R., Sacchettini, James C., Young, Katherine, Olsen, David B., Parish, Tanya
Formato: Online Artículo Texto
Lenguaje:English
Publicado: BioMed Central 2018
Materias:
Research Note
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC6022709/
https://www.ncbi.nlm.nih.gov/pubmed/29954459
http://dx.doi.org/10.1186/s13104-018-3526-z
Descripción
Sumario:OBJECTIVE: Our aim was to identify natural products with anti-tubercular activity. RESULTS: A set of ~ 500 purified natural product compounds was screened for inhibition against the human pathogen Mycobacterium tuberculosis. A series of cyclic hexapeptides with anti-tubercular activity was identified. Five analogs from a set of sixteen closely related compounds were active, with minimum inhibitory concentrations ranging from 2.3 to 8.9 μM. Eleven structural analogs had no significant activity (MIC > 20 μM) demonstrating structure activity relationship. Sequencing of resistant mutant isolates failed to identify changes accounting for the resistance phenotype.

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