ArticlePloS one2015
Synthesis and Evaluation of Novel Triterpene Analogues of Ursolic Acid as Potential Antidiabetic Agent.
Article in PloS one, 2015. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 9 papers.
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Who cites it
9 citing papers in PubMed.
- Solvent-dependent metabolite profile and in vitro biological activity of frangipani (3 Biotech · 2025Article
- Artificial intelligence in antidiabetic drug discovery: The advances in QSAR and the prediction of α-glucosidase inhibitors.Computational and structural biotechnology journal · 2024Review
- Potential Pharmacological Properties of Triterpene Derivatives of Ursolic Acid.Molecules (Basel, Switzerland) · 2024Review
- Discovery of triterpenoids as potent dual inhibitors of pancreatic lipase and human carboxylesterase 1.Journal of enzyme inhibition and medicinal chemistry · 2022Article
- Therapeutic Potential of Ursonic Acid: Comparison with Ursolic Acid.Biomolecules · 2020Review
- Design, Synthesis, and Anticancer Evaluation of Novel Indole Derivatives of Ursolic Acid as Potential Topoisomerase II Inhibitors.International journal of molecular sciences · 2020Article
- Ursolic Acid and Its Derivatives as Bioactive Agents.Molecules (Basel, Switzerland) · 2019Review
- Synthesis and biological evaluation of novel ursolic acid analogues as potential α-glucosidase inhibitors.Scientific reports · 2017Article
- Potential Protective Effects of Ursolic Acid against Gamma Irradiation-Induced Damage Are Mediated through the Modulation of Diverse Inflammatory Mediators.Frontiers in pharmacology · 2017Article
Corrections and comments
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Authors and funding
10 authors.
Funding
No grant is acknowledged in the PubMed record.
Abstract
Ursolic acid (UA) is a naturally bioactive compound that possesses potential anti-diabetic activity. The relatively safe and effective molecule intrigued us to further explore and to improve its anti-diabetic activity. In the present study, a series of novel UA analogues was synthesized and their structures were characterized. Their bioactivities against the α-glucosidase from baker's yeast were determined in vitro. The results suggested that most of the analogues exhibited significant inhibitory activity, especially analogues 8b and 9b with the IC50 values of 1.27 ± 0.27 μM (8b) and 1.28 ± 0.27 μM (9b), which were lower than the other analogues and the positive control. The molecular docking and 2D-QSAR studies were carried out to prove that the C-3 hydroxyl could interact with the hydrophobic region of the active pocket and form hydrogen bonds to increase the binding affinity of ligand and the homology modelling protein. Thus, these results will be helpful for understanding the relationship between binding mode and bioactivity and for designing better inhibitors from UA analogues.
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