High-throughput fluorescent screening of β -lactamase inhibitors to improve antibiotic treatment strategies for tuberculosis

Fei Yan, Shengui He, Xiuyan Han, Jiayue Wang, Xiangge Tian, Chao Wang, Tony James, Jingnan Cui, Xiaochi Ma, Lei Feng

Research output: Contribution to journalArticlepeer-review

5 Citations (SciVal)


Tuberculosis (TB) is an infectious disease caused by Mycobacterium tuberculosis (Mtb), which is a major threat to global public health. Currently, β-lactam antibiotics are rarely used in the treatment of TB, since Mtb naturally expresses β-lactamase (Blac) which renders Mtb resistant to such antibiotics due to β-lactam cleavage. Fortunately, antibiotic resistance can be overcome when β-lactam antibiotics are combined with a Blac inhibitor. With the current research, a near-infrared fluorescent probe LXMB was developed for the real-time detection and imaging of endogenous Blac activity in Mtb. Furthermore, a high-throughput screening platform was established using LXMB to screen Blac inhibitors from herbal medicines. Guided by the visual bioassay, Tannic acid was isolated from Galla Chinensis as a potential Blac inhibitor and was further evaluated in combination with several β-lactam antibiotics which resulted in an enhanced inhibitory effect toward M. tuberculosis H37Ra. Finally, LXMB was used to label live M. tuberculosis H37Ra phagocytosed within macrophages. Consequently, LXMB was a useful fluorescent tool to explore the mechanism of drug resistance based on Blac and can assist in the development of new tuberculosis treatments.

Original languageEnglish
Article number114606
JournalBiosensors and Bioelectronics
Early online date2 Aug 2022
Publication statusPublished - 15 Nov 2022

Bibliographical note

Funding Information:
The authors thank the National Natural Science Foundation of China ( 81930112 ), Dalian Science and Technology Leading Talents Project ( 2019RD15 ), Distinguished professor of Liaoning Province ( XLYC2002008 ), and the Open Research Fund of the School of Chemistry and Chemical Engineering, Henan Normal University for support ( 2020ZD01 and 2021YB07 ).


  • Drug combination
  • Fluorescence imaging
  • High-throughput screening inhibitors
  • NIR fluorescent probe
  • Tuberculosis treatment
  • β-lactamase

ASJC Scopus subject areas

  • Biotechnology
  • Biophysics
  • Biomedical Engineering
  • Electrochemistry


Dive into the research topics of 'High-throughput fluorescent screening of β -lactamase inhibitors to improve antibiotic treatment strategies for tuberculosis'. Together they form a unique fingerprint.

Cite this