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Nigakinone alleviates DSS-induced experimental colitis via regulating bile acid profile and FXR/NLRP3 signaling

Fangle Liu1,2, Yufeng Yao1, Qian Wang1

  • 1School of Pharmaceutical Sciences, Guangzhou University of Chinese Medicine, Guangzhou, PR China.

Phytotherapy Research : PTR
|September 2, 2022
PubMed

Insights

Nigakinone treats ulcerative colitis by regulating bile acid metabolism and the FXR/NLRP3 pathway. This compound reduces inflammation and intestinal damage, offering a potential therapeutic strategy for colitis.

Area of Science:

  • Gastroenterology
  • Pharmacology
  • Molecular Biology

Background:

  • Bile acid (BA) metabolism disorders are linked to ulcerative colitis (UC) pathogenesis.
  • Farnesoid X receptor (FXR) regulates BA homeostasis and inflammation, presenting a therapeutic target for UC.
  • Nigakinone shows potential therapeutic benefits for colitis.

Purpose of the Study:

  • To investigate the anti-UC effects and underlying mechanisms of nigakinone.
  • To explore nigakinone's impact on the nucleotide-binding oligomerization domain, leucine-rich repeat, and pyrin domain-containing 3 (NLRP3) signaling pathway.
  • To elucidate nigakinone's regulation of BA profiles and FXR-mediated pathways in experimental colitis.

Main Methods:

  • Induced colitis in animals using dextran sulfate sodium (DSS).
  • Utilized BA-targeted metabolomics, molecular docking, and dual-luciferase reporter (DLR™) assays.
  • Employed FXR silencing and knockout models in vitro and in vivo.

Main Results:

  • Nigakinone alleviated DSS-induced colitis symptoms, including inflammation and intestinal barrier injury.
  • Nigakinone normalized BA profiles by modulating FXR-controlled cholesterol hydroxylase and transporters, reducing colonic BA accumulation.
  • FXR was identified as a potential direct target of nigakinone, mediating its anti-inflammatory and protective effects.

Conclusions:

  • Nigakinone ameliorates experimental colitis by regulating BA metabolism and the FXR/NLRP3 signaling pathway.
  • FXR activation by nigakinone is critical for its therapeutic effects on colitis.
  • Nigakinone represents a promising therapeutic agent for ulcerative colitis by targeting BA homeostasis and inflammation.
Keywords:
DSS-induced ulcerative colitisFXR-NLRP3 inflammatory signaling pathwaybile acid profilenigakinone

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