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Published on: January 23, 2018
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.
Abstract:
Takeda G protein-coupled receptor 5 (TGR5), also known as G protein-coupled bile acid receptor 1 (GPBAR1), is a cell surface receptor involved in key physiological processes, including glucose homeostasis and energy metabolism. Recent research has focused on the role of TGR5 activation in preventing or treating diabetes while also highlighting its potential impact on the progression of diabetic complications. Functional foods and edible plants have emerged as valuable sources of natural compounds that can activate TGR5, offering potential therapeutic benefits for diabetes management. Despite growing interest, studies on the activation of TGR5 by dietary bioactive compounds remain scattered. This Review aims to provide a comprehensive analysis of how dietary bioactives act as potential agents for TGR5 activation in managing diabetes and its complications. It explores the mechanisms of TGR5 activation through both direct agonistic effects and indirect pathways via modulation of the gut microbiota and bile acid metabolism.
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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