中国化学快报(英文版)2024，Vol.35Issue(3) ：358-362.DOI:10.1016/j.cclet.2023.108504

High-throughput fluorescent screening of thioredoxin reductase inhibitors to inhibit Mycobacterium tuberculosis

Fei Yan Xin Zhao Ruibo Li Xiuyan Han Qiulong Yan Lei Feng Xiulan Xin Jingnan Cui Xiaochi Ma
中国化学快报(英文版)2024，Vol.35Issue(3) ：358-362.DOI:10.1016/j.cclet.2023.108504
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High-throughput fluorescent screening of thioredoxin reductase inhibitors to inhibit Mycobacterium tuberculosis

Fei Yan 1Xin Zhao 2Ruibo Li 3Xiuyan Han 1Qiulong Yan 1Lei Feng 4Xiulan Xin 5Jingnan Cui 2Xiaochi Ma6
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作者信息

  • 1. Second Affiliated Hospital,Dalian Medical University,Dalian 116044,China
  • 2. State Key Laboratory of Fine Chemicals,Dalian University of Technology,Dalian 116024,China
  • 3. Jiangsu Key Laboratory of New Drug Research and Clinical Pharmacy,Xuzhou Medical University,Xuzhou 221004,China
  • 4. Second Affiliated Hospital,Dalian Medical University,Dalian 116044,China;School of Chemistry and Chemical Engineering,Henan Normal University,Xinxiang 453007,China
  • 5. College of Bioengineering,Beijing Polytechnic,Beijing 100029,China
  • 6. Second Affiliated Hospital,Dalian Medical University,Dalian 116044,China;Jiangsu Key Laboratory of New Drug Research and Clinical Pharmacy,Xuzhou Medical University,Xuzhou 221004,China
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Abstract

Tuberculosis(TB)is a chronic infectious disease,which is caused by the pathogen Mycobacterium tubercu-losis(Mtb)and reemerged as a global health risk with a significant proportion of multi-drug resistant and extensively drug resistant TB cases.It is very urgent to find some novel high-confidence drug targets in Mtb for discovering the effective anti-TB agents.Thioredoxin reductase(TrxR)has been identified to be a highly viable target for anti-TB drugs for its important role in protecting the pathogen from thiol-specific oxidizing stress,regulating intracellular dithiol/disulfide homeostasis and DNA replication and repair.In the present work,a near-infrared(NIR)fluorescent probe DDAT was developed for the detection of TrxR activity and used to high-throughput screen the TrxR inhibitors from natural products.Two screened TrxR inhibitors from Sappan Lignum and microbial metabolites that were further used to inhibit Mycobacterium tuberculosis.All the results indicate that DDAT is a practical fluorescent molecular tool for the discovery of potential anti-TB drugs.

Key words

Thioredoxin reductase/NIR fluorescent probe/Fluorescence imaging/High-throughput screening inhibitors/Inhibit Mycobacterium tuberculosis

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基金项目

国家自然科学基金(81930112)

国家自然科学基金(82225048)

Open Research Fund of the School of Chemistry and Chemical Engineering,Henan Normal University for support(2021YB07)

Research on National Reference Material and Product Development of Natural Products(SG030801)

Research on National Reference Material and Product Development of Natural Products(Beijing Polytechnic)

出版年

2024
中国化学快报(英文版)
中国化学会

中国化学快报(英文版)

CSTPCDCSCD
影响因子：0.771
ISSN：1001-8417
参考文献量36
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