ArticleDrug design, development and therapy2015
Insight into the mechanism of polyphenols on the activity of HMGR by molecular docking.
Article in Drug design, development and therapy, 2015. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 21 papers.
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Who cites it
21 citing papers in PubMed, 58 citations in OpenAlex.
- Effects of Satureja Khuzestanica supplementation on glycemic indices and lipid profile in type 2 diabetes patients: a randomized controlled clinical-trial.BMC complementary medicine and therapies · 2024Trial
- Repurposing the HMG-CoA reductase inhibitor atorvastatin for SRD5A3-congenital disorder of glycosylation.Communications medicine · 2026Article
- Phenolic compounds and multifunctional properties of thinned apples: revalorizing fruit by-products for industrial applications.Food chemistry: X · 2026Article
- Nano Milling Application of Mutamba (West Indian Elm) Leaves Extract to Enhance itsPharmaceutical nanotechnology · 2026Article
- Bioactive Potential of Arazá (Plants (Basel, Switzerland) · 2025Article
- Inhibitory Effect of Phenolic Compounds on Vascular Endothelial Growth Factor-Induced Retinal Endothelial Permeability and Angiogenesis.Preventive nutrition and food science · 2024Article
- Potential Effect of Baobab's Polyphenols as Antihyperlipidemic Agents: In Silico Study.Molecules (Basel, Switzerland) · 2023Article
- Inactivation Mechanism and Efficacy of Grape Seed Extract for Human Norovirus Surrogate.Applied and environmental microbiology · 2022Article
- Viral Hepatitis, Cholesterol Metabolism, and Cholesterol-Lowering Natural Compounds.International journal of molecular sciences · 2022Review
- Potential dual inhibitors of PCSK-9 and HMG-R from natural sources in cardiovascular risk management.EXCLI journal · 2022Review
- The Effects of Anthocyanin-Rich Bilberry Extract on Transintestinal Cholesterol Excretion.Foods (Basel, Switzerland) · 2021Article
- Review
- Hydromethanolic Extracts fromMolecules (Basel, Switzerland) · 2020Article
- Phytoconstituents of an ethanolic pod extract of Prosopis cineraria triggers the inhibition of HMG-CoA reductase and the regression of atherosclerotic plaque in hypercholesterolemic rabbits.Lipids in health and disease · 2020Article
- Siamese neem flower extract suppresses cholesterol absorption by interfering NPC1L1 and micellar propertyResearch in pharmaceutical sciences · 2019Article
- Computational Molecular Docking and X-ray Crystallographic Studies of Catechins in New Drug Design Strategies.Molecules (Basel, Switzerland) · 2018Review
- In Vitro and In Silico Studies of the Molecular Interactions of Epigallocatechin-3-Molecules (Basel, Switzerland) · 2018Review
- Antihyperlipidemic studies of newly synthesized phenolic derivatives: in silico and in vivo approaches.Drug design, development and therapy · 2018Article
- Flavonoids and Their Metabolites: Prevention in Cardiovascular Diseases and Diabetes.Diseases (Basel, Switzerland) · 2017Article
- Article
Corrections and comments
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Authors and funding
5 authors at 1 institution in 1 country.
Funding
No grant is acknowledged in the PubMed record.
Abstract
Statins are hypolipidemic drugs that are effective in the treatment of hypercholesterolemia by attenuating cholesterol synthesis in the liver via competitive inhibition of 3-hydroxy-3-methylglutaryl-coenzyme A (HMG-CoA) reductase. Recently, dietary changes associated with drug therapy have garnered attention as novel drugs to mitigate or ameliorate hypercholesterolemia. The present study was undertaken to observe different dietary polyphenols that can bind to the active site of HMGR and inhibit it. Results from the 12 dietary polyphenols tested reveal that polyphenols can bind to HMGR and block the binding of nicotinamide adenine dinucleotide phosphate (NADP(+)). We observed that the rigidity of phenolic rings prevents the polyphenols from docking to the enzyme activity site. The presence of an ester linkage between the phenolic rings in (-)-epigallocatechin-3-gallate (EGCG) and the alkyl chain in curcumin allows them to orient in the active site of the HMGR and bind to the catalytic residues. EGCG and curcumin showed binding to the active site residues with a low GRID score, which may be a potential inhibitor of HMGR. Kaempferol showed binding to HMG-CoA, but with low binding affinity. These observations provide a rationale for the consistent hypolipidemic effect of EGCG and curcumin, which has been previously reported in several epidemiological and animal studies. Therefore, this study substantiates the mechanism of polyphenols on the activity of HMGR by molecular docking and provides the impetus for drug design involving further structure-function relationship studies.
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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.