The function of breast cancer resistance protein (BCRP) and its role in drug absorption, distribution, and elimination has recently been evaluated. The objective of the present study was to examine the expression, localization, and functional characteristics of BCRP in Caco-2 cells, a widely used human intestinal epithelial cell model for investigating intestinal drug absorption. The expression...

To further the development of a model for simultaneously assessing intestinal absorption and first-pass metabolism in vitro, Caco-2, LS180, T84, and fetal human small intestinal epithelial cells (fSIECs) were cultured on permeable inserts, and the integrity of cell monolayers, CYP3A4 activity, and the inducibility of enzymes and transporters involved in intestinal drug disposition were measured...

Human organic anion transporting polypeptide OATP-B (OATP2B1) is a pH-sensitive transporter expressed in the apical membranes of small intestinal epithelial cells. In this study, we have examined the contribution of OATP-B to the uptake of [3H]estrone-3-sulfate in Caco-2 cells in comparison with those of its homologs OATP-D (OATP3A1) and OATP-E (OATP4A1). Immunocytochemical study revealed that ...

The intestinal permeability of low-molecular-weight hyaluronan (LMW-HA) was investigated by using cultured monolayers of Caco-2 cells. The amount of LMW-HA that permeated the Caco-2 monolayers was measured by a carbazole assay. The permeability of LMW-HA increased inversely with the molecular size and was dose-dependent. The transport was observed to be energy-independent, and was correlated wi...

Bitter taste receptors (T2Rs) are involved in bitter perception, which is one of the five basic modalities mammals. In this study, a cell co-culture sensor using different proportions Caco-2 cells and SH-SY5Y was proposed. cells, endogenously expressed human T2R38 receptor, T2R16 were co-cultured. Using at constant total concentration 40 K/mL, we designed seven mixtures with [Caco-2]/([Caco-2] ...

A simple, reliable, and user friendly system was established to cultivate Caco-2 cell monolayer for epithelial transport studies. After an initial growth period of 1 week in a CO(2) incubator, Caco-2 cells were cultivated in an automated continuous perfusion system (Minucells and Minutissue, Germany). Medium was constantly renewed at the apical and basal side of the monolayers, which resulted i...

Structured lipids have been proposed as efficient vehicles for the supplementation of essential fatty acids (EFA) to patients with malabsorption. We investigated how a novel structured triglyceride (STG), containing purely octanoic acid in the sn-1/ sn-3 and [14C]linoleic acid in the sn-2 positions, was incorporated into different lipid classes in Caco-2 cells. We also evaluated the contributio...

these tripeptides was studied by using monolayercultured human intestinaJ Caco-2 cells which express rnany enterocyte-Iike functions including the peptide transporter(PepTl)-mediated transport system. ValPro-Pro, an ACE-inhibitors peptide from fermented milk, was used as a model tripeptide. A significant amount of intact Val-Pro-Pro was transported across the Caco-2 cel) monolayer. This transpo...

background: numerous molecules in papaveraceae family display interesting cytotoxic activities against tumor cell lines in vitro and hints of anticancer activities in vivo have been reported in a few cases. objective: numerous molecules in this family display interesting cytotoxic activities against tumor cell lines in vitro and hints of anticancer activities in vivo have been reported in a few...

Introduction: Efforts are made to identify the new potential components such as anticancer drugs. Medicinal plants belonging to Euphorbia genus are widely studied with promising effects. The current study aimed at investigating the effect of ethanolic extract of the root of E. tehranica, grown in Iran, on Caco-2 human colorectal cancer cell-line. Methods: The Caco-2 cells were treated with dif...