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具有抗结核分枝杆菌抑制活性的环状六肽天然产物的鉴定

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

作者信息

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

机构信息

Merck & Co., Inc., Infectious Diseases, 770 Sumneytown Pike, West Point, PA, 19486, USA.

SBS Pharma Consulting LLC, Edison, NJ, 08820, USA.

出版信息

BMC Res Notes. 2018 Jun 28;11(1):416. doi: 10.1186/s13104-018-3526-z.

DOI:10.1186/s13104-018-3526-z
PMID:29954459
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC6022709/
Abstract

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.

摘要

目的

我们的目标是鉴定具有抗结核活性的天然产物。

结果

对一组约500种纯化的天然产物化合物进行筛选，以检测其对人类病原体结核分枝杆菌的抑制作用。鉴定出一系列具有抗结核活性的环状六肽。从一组16种密切相关的化合物中得到的5种类似物具有活性，最低抑菌浓度范围为2.3至8.9μM。11种结构类似物无显著活性（MIC>20μM），表明了结构活性关系。对耐药突变株进行测序未能鉴定出导致耐药表型的变化。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/e6a7/6022709/344268d16d0e/13104_2018_3526_Fig1_HTML.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/e6a7/6022709/344268d16d0e/13104_2018_3526_Fig1_HTML.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/e6a7/6022709/344268d16d0e/13104_2018_3526_Fig1_HTML.jpg

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