PUBLICATION

Degarelix limits the survival of mycobacteria and granuloma formation

Authors
Li, J., Gao, J., Gao, Y., Shi, C., Guo, X., Huang, H., Wang, J., Huang, X., Chen, H., Huang, J., Wang, W., Yang, H.
ID
ZDB-PUB-241022-11
Date
2024
Source
Microbial pathogenesis   197: 107046 (Journal)
Registered Authors
Keywords
Degarelix, Mycobacterium, Treatment, Tuberculous granuloma, Zebrafish
MeSH Terms
  • Disease Models, Animal
  • Granuloma*/drug therapy
  • Granuloma*/microbiology
  • Zebrafish*
  • Antitubercular Agents/pharmacology
  • Autophagy/drug effects
  • Animals
  • Mice
  • Microbial Viability/drug effects
  • Mycobacterium Infections, Nontuberculous/drug therapy
  • Mycobacterium Infections, Nontuberculous/microbiology
  • Tuberculosis/drug therapy
  • Tuberculosis/microbiology
  • Mycobacterium marinum*/drug effects
  • Mycobacterium marinum*/pathogenicity
  • Macrophages*/drug effects
  • Macrophages*/microbiology
  • Oligopeptides/pharmacology
  • Interferon-gamma/metabolism
  • Drug Repositioning
  • Rifampin/pharmacology
  • Rifampin/therapeutic use
  • Humans
  • Mycobacterium tuberculosis/drug effects
  • Mycobacterium tuberculosis/genetics
PubMed
39433139 Full text @ Microb. Pathog.
Abstract
Tuberculosis (TB), caused by Mycobacterium tuberculosis (Mtb) infection, is a serious health hazard, characterized by tuberculous granuloma formation, which may facilitate bacterial survival. At the same time, the identification of multidrug-resistant and extremely drug-resistant Mtb strains, and the progressive accumulation of mutations in biological targets of frontline antimicrobials, has made TB treatments more difficult. Therefore, new and rapid drug development for TB is warranted. Recently, drug repurposing has received considerable attention. In this study, we applied the anticancer drug degarelix to anti-TB research and found that it inhibits mycobacteria survival and pathological damage in Mycobacterium marinum-infected zebrafish and Mtb-infected mice. Supplementation of degarelix matched the bactericidal activities of rifampicin (RFP) toward M. marinum in zebrafish. Mechanistically, degarelix significantly increased interferon (IFN)-γ levels in M. marinum-infected zebrafish. Degarelix had no direct anti-mycobacterial activity in vitro but significantly reduced the survival of H37Rv in macrophages. The effect of degarelix could be reversed by 3-methyladenine (3-MA), which inhibits the class III phosphatidylinositol (PI) 3 kinase required for autophagy initiation. However, no effect on later steps in autophagy could be detected. Our findings demonstrate the potential of degarelix on limiting mycobacterial survival and granuloma formation, which may generate novel TB therapeutics.
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