ArticleFrontiers in pharmacology2018
Cucurbitacin B Induces Hypoglycemic Effect in Diabetic Mice by Regulation of AMP-Activated Protein Kinase Alpha and Glucagon-Like Peptide-1 via Bitter Taste Receptor Signaling.
Article in Frontiers in pharmacology, 2018. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 28 papers.
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Who cites it
28 citing papers in PubMed, 66 citations in OpenAlex.
- Bitter Compounds in Medicinal Food Plants Based on Traditional Chinese Medicine: Analysis and Regulation Strategies from Chemical Structure to Perception Mechanisms.Molecules (Basel, Switzerland) · 2026Review
- Effects of Different Carriers on the Stability and Pharmacokinetic Performance of Cucurbitacin B Solid Dispersions.AAPS PharmSciTech · 2026Article
- Small molecules targeting regulated cell death for chronic kidney disease therapy.Journal of pharmaceutical analysis · 2026Review
- Parthenolide promotes glucagon-like peptide-1 secreting in human Caco-2 cells via regulation of bitter taste receptor-induced of calcium signaling.Molecular and cellular biochemistry · 2026Article
- Cucurbitacin B Inhibits Hepatocellular Carcinoma by Inducing Ferroptosis and Activating the cGAS-STING Pathway.Current issues in molecular biology · 2026Article
- Pharmacokinetic Profile of Extracts from the Chayote (Molecules (Basel, Switzerland) · 2025Article
- Hypoglycemic Effects ofFoods (Basel, Switzerland) · 2025Review
- The appearance of bitter taste receptors - inspiration from structure, expression, function, and mechanism.Naunyn-Schmiedeberg's archives of pharmacology · 2025Review
- GLP-1-based therapies for type 2 diabetes: from single, dual and triple agonists to endogenous GLP-1 production and L-cell differentiation.Diabetology & metabolic syndrome · 2025Review
- Comparison of the pharmacokinetic profiles of three triterpenoids after oral administration of a cucurbitacin tablet and nanosuspension by UHPLC-MS/MS.Frontiers in pharmacology · 2025Article
- Bitter taste receptors as sensors of gut luminal contents.Nature reviews. Gastroenterology & hepatology · 2025Review
- Bibliometric analysis of research on the utilization of nanotechnology in diabetes mellitus and its complications.Nanomedicine (London, England) · 2024Article
- Genetic mutation of Tas2r104/Tas2r105/Tas2r114 cluster leads to a loss of taste perception to denatonium benzoate and cucurbitacin B.Animal models and experimental medicine · 2024Article
- [Quantitative analysis of differential proteins in renal tissues of rats with chronic intermittent hypoxic exposure based on TMT and PRM technology].Nan fang yi ke da xue xue bao = Journal of Southern Medical University · 2023Article
- Research progress on the relationship between bile acid metabolism and type 2 diabetes mellitus.Diabetology & metabolic syndrome · 2023Review
- Cucurbitacin B Exerts Significant Antidepressant-Like Effects in a Chronic Unpredictable Mild Stress Model of Depression: Involvement of the Hippocampal BDNF-TrkB System.The international journal of neuropsychopharmacology · 2023Article
- Identification and Isolation of α-Glucosidase Inhibitors fromInternational journal of molecular sciences · 2023Article
- Isosinensetin Stimulates Glucagon-like Peptide-1 Secretion via Activation of hTAS2R50 and the GInternational journal of molecular sciences · 2023Article
- Pharmacokinetics and Biological Activity of Cucurbitacins.Pharmaceuticals (Basel, Switzerland) · 2022Review
- Cucurbitacin B-induced G2/M cell cycle arrest of conjunctival melanoma cells mediated by GRP78-FOXM1-KIF20A pathway.Acta pharmaceutica Sinica. B · 2022Article
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Authors and funding
6 authors at 1 institution in 1 country.
Funding
No grant is acknowledged in the PubMed record.
Abstract
Taste receptors exist in several organs from tongue to colon and have diverse functions dependent on specific cell type. In enteroendocrine L-cells, stimulation of taste receptor signaling induces incretin hormones. Among incretin hormones, glucagon-like peptide-1 (GLP-1) induces insulinotropic action by activating GLP-1 receptor of pancreatic β-cells. However, GLP-1 mimetic medicines have reported clinical side effects, such as autoimmune hepatitis, acute kidney injury, pancreatitis, and pancreatic cancer. Here, we hypothesized that if natural components in ethnomedicines can activate agonistic action of taste receptor; they may stimulate GLP-1 and therefore, could be developed as safe and applicable medicines to type 2 diabetes mellitus (T2DM) with minimal side effects. Cucurbitacin B (CuB) is composed of triterpenoid structure and its structural character, that represents bitterness, can stimulate AMP-activated protein kinase (AMPK) pathway. CuB ameliorated hyperglycemia by activating intestinal AMPK levels and by inducing plasma GLP-1 and insulin release in diabetic mice. This hypoglycemic action was decreased in dorsomorphin-injected mice and α-gustducin null mice. Moreover, systemic inhibition study in differentiated NCI-H716 cell line showed that CuB-mediated GLP-1 secretion was involved in activation of AMPK through α-gustducin and Gβγ-signaling of taste receptors. In summary, we conclude that, CuB represents novel hypoglycemic agents by activation of AMPK and stimulation of GLP-1 in differentiated enteroendocrine L-cells. These results suggest that taste receptor signaling-based therapeutic agents within tremendously diverse ethnomedicines, could be applied to developing therapeutics for T2DM patients.
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