TGR5 Activation by Dietary Bioactives and Related Improvement in Mitochondrial Function for Alleviating Diabetes and

Quanrun He1,2, Xinhang Li1,2, Haimeng Li1,2

  • 1School of Medicine, The Chinese University of Hong Kong, Shenzhen, 2001 Longxiang Boulevard, Longgang District, Shenzhen, Guangdong 518172, P.R. China.

Insights

Dietary compounds can activate Takeda G protein-coupled receptor 5 (TGR5) to help manage diabetes. This review explores how these natural bioactives and their mechanisms offer therapeutic potential for diabetes and its complications.

Area of Science:

  • Endocrinology and Metabolism
  • Nutritional Science
  • Pharmacology

Background:

  • Takeda G protein-coupled receptor 5 (TGR5), also known as GPBAR1, is a key regulator of glucose homeostasis and energy metabolism.
  • TGR5 activation is increasingly recognized for its therapeutic potential in managing diabetes and its associated complications.
  • Dietary bioactive compounds from functional foods and edible plants are emerging as natural activators of TGR5.

Purpose of the Study:

  • To comprehensively review the role of dietary bioactive compounds in activating TGR5 for diabetes management.
  • To analyze the mechanisms by which these compounds modulate TGR5 activity, including direct agonism and indirect pathways.
  • To consolidate scattered research on TGR5 activation by dietary bioactives for therapeutic applications in diabetes.

Main Methods:

  • Systematic literature review of studies investigating dietary bioactives and TGR5 activation.
  • Analysis of mechanisms of TGR5 activation, including direct receptor binding and indirect modulation.
  • Exploration of indirect pathways such as gut microbiota alterations and bile acid metabolism changes.

Main Results:

  • Dietary bioactive compounds demonstrate potential as TGR5 agonists, influencing glucose and energy metabolism.
  • Mechanisms involve both direct interaction with TGR5 and indirect modulation via the gut microbiome and bile acid pool.
  • Evidence suggests TGR5 activation by natural compounds may mitigate diabetic complications.

Conclusions:

  • Dietary bioactives represent a promising avenue for TGR5-targeted diabetes therapy.
  • Understanding the multifaceted mechanisms of TGR5 activation is crucial for developing effective interventions.
  • Further research into specific compounds and their clinical efficacy is warranted for diabetes management.

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