Jump to main content
Jump to site search


A highly selective fluorescent probe for real-time imaging of bacterial NAT2 and high-throughput screening of natural inhibitors for tuberculosis therapy

Author affiliations

Abstract

N-Acetyltransferase 2 (NAT2) is a very important biologically functioning enzyme which plays a key role in the synthesis of cell walls in slowly growing mycobacteria. Thus, it has been widely considered to be a drug-target for anti-mycobacterial therapy. Herein, based on its catalytic characteristics, ARHB was developed for the real-time monitoring and assessment of the activity of NAT2 in different bacteria such as Mycobacterium, Staphylococcus aureus, Lactobacillus, and Pseudomonas aeruginosa. Moreover, using the highly sensitive probe ARHB, a potent natural inhibitor (KSB-4) of NAT2 was found which could effectively inhibit Mycobacterium tuberculosis H37Ra for the first time. Furthermore, the bioactivity of KSB-4 for treating tuberculosis was also evaluated in M. tuberculosis H37Ra, showing a minimum inhibitory concentration (MIC) of 25 μM. After treatment with KSB-4, M. tuberculosis H37Ra grew to be much shorter and its cell wall lysis was observed in scanning electron micrographs. All of the results fully demonstrated that ARHB could serve as a promising molecular tool for the rapid and real-time detection of NAT2 activity in a complex system, providing a novel high-throughput screening method for the discovery of new NAT2 inhibitors.

Graphical abstract: A highly selective fluorescent probe for real-time imaging of bacterial NAT2 and high-throughput screening of natural inhibitors for tuberculosis therapy

Back to tab navigation

Supplementary files

Publication details

The article was received on 16 Oct 2018, accepted on 08 Nov 2018 and first published on 12 Nov 2018


Article type: Research Article
DOI: 10.1039/C8QM00514A
Citation: Mater. Chem. Front., 2019, Advance Article
  •   Request permissions

    A highly selective fluorescent probe for real-time imaging of bacterial NAT2 and high-throughput screening of natural inhibitors for tuberculosis therapy

    Y. Jin, Z. Tian, X. Tian, L. Feng, J. Cui and X. Ma, Mater. Chem. Front., 2019, Advance Article , DOI: 10.1039/C8QM00514A

Search articles by author

Spotlight

Advertisements