ArticleActa pharmacologica Sinica2009
The expression of efflux and uptake transporters are regulated by statins in Caco-2 and HepG2 cells.
Article in Acta pharmacologica Sinica, 2009. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 22 papers, 1 of them a synthesis that pooled it.
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Who cites it
22 citing papers in PubMed, 1 synthesis or guideline pooled it, 64 citations in OpenAlex.
- The Effect of Statin Therapy on Serum Uric Acid Levels: A Systematic Review and Meta-analysis.Current medicinal chemistry · 2024Pooled it
- Mechanisms, precision therapies, and technological frontiers in coronary atherosclerosis: a comprehensive review.Acta pharmacologica Sinica · 2026Review
- HepG2 cells do not express xanthine oxidoreductase (XOR): Implications for XOR and uric acid-related research.Free radical biology & medicine · 2025Article
- Cancer Stem Cells in Carcinogenesis and Potential Role in Pancreatic Cancer.Current stem cell research & therapy · 2024Review
- OCT1-dependent uptake of structurally diverse pyrrolizidine alkaloids in human liver cells is crucial for their genotoxic and cytotoxic effects.Archives of toxicology · 2023Article
- A Study on Pharmacokinetic Functionalities and Safety Margins of an Optimized Simvastatin Nanoformulation.Pharmaceuticals (Basel, Switzerland) · 2023Article
- Article
- In Vitro Safety, Off-Target and Bioavailability Profile of the Antiviral Compound Silvestrol.Pharmaceuticals (Basel, Switzerland) · 2022Article
- SLCO1B1 Phenotype and CYP3A5 Polymorphism Significantly Affect Atorvastatin Bioavailability.Journal of personalized medicine · 2021Article
- Rifampicin Induces Gene, Protein, and Activity of P-Glycoprotein (ABCB1) in Human Precision-Cut Intestinal Slices.Frontiers in pharmacology · 2021Article
- The Role of Structure and Biophysical Properties in the Pleiotropic Effects of Statins.International journal of molecular sciences · 2020Review
- Article
- Sorafenib Activity and Disposition in Liver Cancer Does Not Depend on Organic Cation Transporter 1.Clinical pharmacology and therapeutics · 2020Article
- Review
- ABC Transport Proteins in Cardiovascular Disease-A Brief Summary.Molecules (Basel, Switzerland) · 2017Review
- Atorvastatin attenuation of ABCB1 expression is mediated by microRNA miR-491-3p in Caco-2 cells.European journal of pharmaceutical sciences : official journal of the European Federation for Pharmaceutical Sciences · 2016Article
- Intestinal absorption characteristics of imperialine: in vitro and in situ assessments.Acta pharmacologica Sinica · 2015Article
- Atorvastatin induces bile acid-synthetic enzyme Cyp7a1 by suppressing FXR signaling in both liver and intestine in mice.Journal of lipid research · 2014Article
- The genetics of hyperuricaemia and gout.Nature reviews. Rheumatology · 2012Review
- Intestinal absorption of forsythoside A in in situ single-pass intestinal perfusion and in vitro Caco-2 cell models.Acta pharmacologica Sinica · 2012Article
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
aimStatin disposition and response are greatly determined by the activities of drug metabolizing enzymes and efflux/ uptake transporters. There is little information on the regulation of these proteins in human cells after statin therapy. In this study, the effects of atorvastatin and simvastatin on mRNA expression of efflux (ABCB1, ABCG2 and ABCC2) and uptake (SLCO1B1, SLCO2B1 and SLC22A1) drug transporters in Caco-2 and HepG2 cells were investigated.
methodsQuantitative real-time PCR was used to measure mRNA levels after exposure of HepG2 and Caco-2 cells to statins.
resultsDifferences in mRNA basal levels of the transporters were as follows: ABCC2>ABCG2>ABCB1>SLCO1B1>>>SLC22A1>SLC O2B1 for HepG2 cells, and SLCO2B1>>ABCC2>ABCB1>ABCG2>>>SLC22A1 for Caco-2 cells. While for HepG2 cells, ABCC2, ABCG2 and SLCO2B1 mRNA levels were significantly up-regulated at 1, 10 and 20 micromol/L after 12 or 24 h treatment, in Caco-2 cells, only the efflux transporter ABCB1 was significantly down-regulated by two-fold following a 12 h treatment with atorvastatin. Interestingly, whereas treatment with simvastatin had no effect on mRNA levels of the transporters in HepG2 cells, in Caco-2 cells the statin significantly down-regulated ABCB1, ABCC2, SLC22A1, and SLCO2B1 mRNA levels after 12 or 24 h treatment.
conclusionThese findings reveal that statins exhibits differential effects on mRNA expression of drug transporters, and this effect depends on the cell type. Furthermore, alterations in the expression levels of drug transporters in the liver and/or intestine may contribute to the variability in oral disposition of statins.Acta Pharmacologica Sinica (2009) 30: 956-964; doi: 10.1038/aps.2009.85; published online 22 June 2009.
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