ArticleThe Biochemical journal2007
Insulin-mimetic and insulin-sensitizing activities of a pentacyclic triterpenoid insulin receptor activator.
Article in The Biochemical journal, 2007. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 29 papers.
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Who cites it
29 citing papers in PubMed, 135 citations in OpenAlex.
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- Recent Advances of Natural Pentacyclic Triterpenoids as Bioactive Delivery System for Synergetic Biological Applications.Foods (Basel, Switzerland) · 2024Review
- Therapeutic Effect of an Ursolic Acid-Based Nutraceutical on Neuronal Regeneration after Sciatic Nerve Injury.International journal of molecular sciences · 2024Article
- Overview of Ursolic Acid Potential for the Treatment of Metabolic Disorders, Autoimmune Diseases, and Cancers via Nuclear Receptor Pathways.Biomedicines · 2023Review
- Exploring of the ameliorative effects of Nerium (Nerium oleander L.) ethanolic flower extract in streptozotocin induced diabetic rats via biochemical, histological and molecular aspects.Molecular biology reports · 2023Article
- Natural products as novel anti-obesity agents: insights into mechanisms of action and potential for therapeutic management.Frontiers in pharmacology · 2023Review
- Serpentine Enhances Insulin Regulation of Blood Glucose through Insulin Receptor Signaling Pathway.Pharmaceuticals (Basel, Switzerland) · 2022Article
- Review
- Anti-Diabetic Potential of Plant-Based Pentacyclic Triterpene Derivatives: Progress Made to Improve Efficacy and Bioavailability.Molecules (Basel, Switzerland) · 2021Review
- Therapeutic Potential of Ursolic Acid in Cancer and Diabetic Neuropathy Diseases.International journal of molecular sciences · 2021Review
- Bioactive Sugarcane Lipids in a Circular Economy Context.Foods (Basel, Switzerland) · 2021Review
- Activation of Insulin Signaling by Botanical Products.International journal of molecular sciences · 2021Review
- Repeated dose (90 days) oral toxicity study of ursolic acid in Han-Wistar rats.Toxicology reports · 2020Article
- Modulation of Lipid Transport and Adipose Tissue Deposition by Small Lipophilic Compounds.Frontiers in cell and developmental biology · 2020Review
- Ursolic acid in health and disease.The Korean journal of physiology & pharmacology : official journal of the Korean Physiological Society and the Korean Society of Pharmacology · 2018Review
- The Effects of Plant-Derived Oleanolic Acid on Selected Parameters of Glucose Homeostasis in a Diet-Induced Pre-Diabetic Rat Model.Molecules (Basel, Switzerland) · 2018Article
- Effects of ursolic acid on sub-lesional muscle pathology in a contusion model of spinal cord injury.PloS one · 2018Article
- Effects of Flavonoids and Triterpene Analogues from Leaves of Eleutherococcus sieboldianus (Makino) Koidz. 'Himeukogi' in 3T3-L1 Preadipocytes.Molecules (Basel, Switzerland) · 2017Article
- Potentiation of insulin-mediated glucose lowering without elevated hypoglycemia risk by a small molecule insulin receptor modulator.PloS one · 2015Article
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Authors and funding
7 authors at 2 institutions in 1 country.
Funding
No grant is acknowledged in the PubMed record.
Abstract
Five pentacyclic triterpenoids isolated from Campsis grandiflora were tested for insulin-mimetic and insulin-sensitizing activity. The compounds enhanced the activity of insulin on tyrosine phosphorylation of the IR (insulin receptor) beta-subunit in CHO/IR (Chinese-hamster ovary cells expressing human IR). Among the compounds tested, CG7 (ursolic acid) showed the greatest enhancement and CG11 (myrianthic acid) the least. We characterized the effect of CG7 further, and showed that it acted as an effective insulin-mimetic agent at doses above 50 mug/ml and as an insulin-sensitizer at doses as low as 1 mug/ml. Additional experiments showed that CG7 increased the number of IRs that were activated by insulin. This indicates that a major mechanism by which CG7 enhances total IR auto-phosphorylation is by promoting the tyrosine phosphorylation of additional IRs. CG7 not only potentiated insulin-mediated signalling (tyrosine phosphorylation of the IR beta-subunit, phosphorylation of Akt and glycogen synthase kinase-3beta), but also enhanced the effect of insulin on translocation of glucose transporter 4 in a classical insulin-sensitive cell line, 3T3-L1 adipocytes. The results of the present study demonstrate that a specific pentacyclic triterpenoid, CG7, exerts an insulin-sensitizing effect as an IR activator in CHO/IR cells and adipocytes. The enhancement of insulin activity by CG7 may be useful for developing a new class of specific IR activators for treatment of Type 1 and Type 2 diabetes.
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