Related Experiment Video
Updated: Jun 3, 2026

Using Caco-2 Cells to Study Lipid Transport by the Intestine
Published on: August 20, 2015
ABCA1 and ABCG1 expressions are regulated by statins and ezetimibe in Caco-2 cells
Fabiana D V Genvigir1, Alice C Rodrigues, Alvaro Cerda
1Department of Clinical and Toxicological Analysis, Faculty of Pharmaceutical Sciences, University of Sao Paulo, Sao Paulo, SP, Brazil. fdallavecchia@yahoo.com.br
Background:
Enterocytes play a crucial role in high-density lipoprotein (HDL) biogenesis. Statins and ezetimibe are potent lowering-cholesterol drugs, which can also influence HDL plasma concentrations. We hypothesized that these drugs could modulate the expression of intestinal ABCA1 and ABCG1, two genes involved in HDL metabolism.
Methods:
Caco-2 cells were used as a model of the human intestinal cells and were treated with statins (0.01-1 μmol/L) and/or ezetimibe (0.5-5.0 μmol/L) for 12 h or 24 h. Gene expression was examined using real-time PCR.
Results:
ABCA1 level was more abundant than ABCG1 in Caco-2 cells. ABCA1 was downregulated after 12-h and 24-h treatment with atorvastatin (0.1 and 1.0 μmol/L) or simvastatin (0.01, 0.1 and 1 μmol/L) (p<0.05). In statin-treated cells, ABCG1 levels remained unaltered. Ezetimibe alone did not induce change of ABCA1 or ABCG1 mRNA levels (p>0.05) but 24-h ezetimibe (2.5 or 5.0 μmol/L) plus simvastatin (1 μmol/L) treatment decreased the transcription of ABCA1 and ABCG1 (p<0.05).
Conclusions:
Our findings reveal that, at the concentrations studied, statins isolated or combined with ezetimibe, but not ezetimibe alone, downregulate ABCA1 mRNA expression in Caco-2 cells. Moreover, simvastatin combined with ezetimibe treatment also decrease the ABCG1 levels in these cells.
Related Concept Videos
ABC Transporters: Exporter
Pharmacogenetics of Drug Transporters: P-Glycoprotein and Solute Carrier Transporters
ABC Transporters: Importer
In bacteria, based on the number of transmembrane helices and the chemical nature of their substrates, the ABC importers can be divided into three types:
Carrier-Mediated Transport
Active transport involves two types of membrane-spanning transporters: uptake and efflux. Uptake transporters are expressed in the small...
Cell Specific Gene Expression
Pharmacogenomics: Identification of New Drug Targets

