ArticleNaunyn-Schmiedeberg's archives of pharmacology2017
Ursolic acid activates the TGR5 receptor to enhance GLP-1 secretion in type 1-like diabetic rats.
Article in Naunyn-Schmiedeberg's archives of pharmacology, 2017. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 14 papers.
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Who cites it
14 citing papers in PubMed, 26 citations in OpenAlex.
- Review
- Structure-Based Insights into TGR5 Activation by Natural Compounds: Therapeutic Implications and Emerging Strategies for Obesity Management.Biomedicines · 2025Review
- Guayusa (Molecules (Basel, Switzerland) · 2025Review
- Transformation from passive health to proactive prevention: research progress on glucose-lowering components and its mechanism of food and medicine homology resources.Frontiers in nutrition · 2025Review
- Ursolic acid regulates gut microbiota and corrects the imbalance of Th17/Treg cells in T1DM rats.PloS one · 2022Article
- Therapeutic Potential of Ursolic Acid in Cancer and Diabetic Neuropathy Diseases.International journal of molecular sciences · 2021Review
- Etanercept Ameliorates Cardiac Fibrosis in Rats with Diet-Induced Obesity.Pharmaceuticals (Basel, Switzerland) · 2021Article
- Amelioration of Endothelial Dysfunction in Diabetes: Role of Takeda G Protein-Coupled Receptor 5.Frontiers in pharmacology · 2021Review
- Therapeutic Opportunities of GPBAR1 in Cholestatic Diseases.Frontiers in pharmacology · 2021Review
- Simulating the Post-gastric Bypass Intestinal Microenvironment Uncovers a Barrier-Stabilizing Role for FXR.iScience · 2020Article
- Ursolic Acid and Its Derivatives as Bioactive Agents.Molecules (Basel, Switzerland) · 2019Review
- Bile-ology: from bench to bedside.Journal of Zhejiang University. Science. B · 2019Review
- Differential action of TGR5 agonists on GLP-2 secretion and promotion of intestinal adaptation in a piglet short bowel model.American journal of physiology. Gastrointestinal and liver physiology · 2019Article
- Scutellariae Radix and Coptidis Rhizoma Improve Glucose and Lipid Metabolism in T2DM Rats via Regulation of the Metabolic Profiling and MAPK/PI3K/Akt Signaling Pathway.International journal of molecular sciences · 2018Article
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Authors and funding
6 authors at 4 institutions in 2 countries.
Funding
Abstract
Endogenous Takeda G-protein-coupled receptor 5 (TGR5), G-protein-coupled bile acid receptor 1 (GPBAR1), regulates glucose metabolism. In animals, TGR5 activation by a chemical agonist may increase incretin secretion and reduce the blood sugar level. Recently, betulinic acid has been suggested to activate TGR5. Ursolic acid is a well-known pentacyclic triterpenoid that is similar to betulinic acid. It is of special interest to determine the potential effect of ursolic acid on TGR5. Therefore, we transfected cultured Chinese hamster ovary (CHO-K1) cells with the TGR5 gene. The functions of the transfected cells were confirmed via glucose uptake using a fluorescent indicator. Moreover, NCI-H716 cells that secreted incretin were also investigated, and the glucagon-like peptide (GLP-1) levels were quantified using ELISA kits. In addition, streptozotocin (STZ)-induced type 1-like diabetic rats were used to identify the effect of ursolic acid in vivo. Ursolic acid concentration dependently increased glucose uptake in CHO-K1 cells expressing TGR5. In NCI-H716 cells, ursolic acid induced a concentration-dependent elevation in GLP-1 secretion, which was inhibited by triamterene at the effective concentrations to block TGR5. Ursolic acid also increased the plasma GLP-1 level via TGR5 activation, which was further characterized in vivo with type 1-like diabetic rats. Moreover, ursolic acid is more effective than betulinic acid in reduction of hyperglycemia and increase of GLP-1 secretion. Therefore, we demonstrated that ursolic acid can activate TGR5, enhancing GLP-1 secretion in vitro and in vivo. Therefore, ursolic acid is suitable for use in TGR5 activation.
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Registered trials
Read under generation 80e0d062 · epoch 390. Bibliography from PubMed, PubMed Central and OpenAlex; grants from NIH RePORTER; trial links from ClinicalTrials.gov; estimates, votes and beliefs from the OpenQuestion graph.