ArticleMolecules (Basel, Switzerland)2018
Discovery of Potential Inhibitors of Squalene Synthase from Traditional Chinese Medicine Based on Virtual Screening and In Vitro Evaluation of Lipid-Lowering Effect.
Article in Molecules (Basel, Switzerland), 2018. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 13 papers.
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Who cites it
13 citing papers in PubMed, 25 citations in OpenAlex.
- The Contribution of Cholesterol and Squalene Synthase in Cancer: Molecular Mechanisms, Lipid Rafts and Therapeutic Approaches.Medicinal research reviews · 2026Review
- Hepatoprotective Effect of Cynarin on Alpha-Naphthyl Isothiocyanate-Induced Cholestatic Liver Injury: Associated Modulation of TXNIP/NLRP3 and HMGB1/NF-κB Signaling Cascades.Pharmaceuticals (Basel, Switzerland) · 2026Article
- Herbal Metabolites as Potential Carbonic Anhydrase Inhibitors: Promising Compounds for Cancer and Metabolic Disorders.Journal of obesity & metabolic syndrome · 2023Article
- Review
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- Discovery of New Inhibitors of eEF2K from Traditional Chinese Medicine Based on In Silico Screening and In Vitro Experimental Validation.Molecules (Basel, Switzerland) · 2022Article
- Network Pharmacology Approach for Medicinal Plants: Review and Assessment.Pharmaceuticals (Basel, Switzerland) · 2022Review
- Cynarin attenuates LPS-induced endothelial inflammation via upregulation of the negative regulator MKP-3.Animal cells and systems · 2022Article
- Recent Molecular Mechanisms and Beneficial Effects of Phytochemicals and Plant-Based Whole Foods in Reducing LDL-C and Preventing Cardiovascular Disease.Antioxidants (Basel, Switzerland) · 2021Review
- Geranii Herba as a Potential Inhibitor of SARS-CoV-2 Main 3CLAntibiotics (Basel, Switzerland) · 2020Article
- Paromomycin: A potential dual targeted drug effectively inhibits both spike (S1) and main protease of COVID-19.International journal of infectious diseases : IJID : official publication of the International Society for Infectious Diseases · 2020Article
- Epigenome-Wide Association Study Reveals Duration of Breastfeeding Is Associated with Epigenetic Differences in Children.International journal of environmental research and public health · 2020Article
- Molecular Modeling in Drug Design.Molecules (Basel, Switzerland) · 2019Article
Corrections and comments
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Authors and funding
9 authors at 2 institutions in 1 country.
Funding
No grant is acknowledged in the PubMed record.
Abstract
Squalene synthase (SQS), a key downstream enzyme involved in the cholesterol biosynthetic pathway, plays an important role in treating hyperlipidemia. Compared to statins, SQS inhibitors have shown a very significant lipid-lowering effect and do not cause myotoxicity. Thus, the paper aims to discover potential SQS inhibitors from Traditional Chinese Medicine (TCM) by the combination of molecular modeling methods and biological assays. In this study, cynarin was selected as a potential SQS inhibitor candidate compound based on its pharmacophoric properties, molecular docking studies and molecular dynamics (MD) simulations. Cynarin could form hydrophobic interactions with PHE54, LEU211, LEU183 and PRO292, which are regarded as important interactions for the SQS inhibitors. In addition, the lipid-lowering effect of cynarin was tested in sodium oleate-induced HepG2 cells by decreasing the lipidemic parameter triglyceride (TG) level by 22.50%. Finally. cynarin was reversely screened against other anti-hyperlipidemia targets which existed in HepG2 cells and cynarin was unable to map with the pharmacophore of these targets, which indicated that the lipid-lowering effects of cynarin might be due to the inhibition of SQS. This study discovered cynarin is a potential SQS inhibitor from TCM, which could be further clinically explored for the treatment of hyperlipidemia.
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Registered trials
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