The objective of this study was to investigate the influence of physiochemical parameters (such as size, molecular weight, molecular geometry, and number of surface amine groups) of poly (amidoamine) (PAMAM) dendrimers, on their permeability across Caco-2 cell monolayers. The permeability of a series of PAMAM dendrimers, generations 0-4 (G0-G4), was investigated across Caco-2 cell monolayers in...

Hu, Chaobin, and David H. Perlmutter. Regulation of a1-antitrypsin gene expression in human intestinal epithelial cell line Caco-2 by HNF-1a and HNF-4. Am. J. Physiol. 276 (Gastrointest. Liver Physiol. 39): G1181–G1194, 1999.— There is still relatively limited information about mechanisms of gene expression in enterocytes and mechanisms by which gene expression is regulated during enterocyte di...

The IL-1beta-induced increase in intestinal epithelial tight junction (TJ) permeability has been postulated to be an important mechanism contributing to intestinal inflammation of Crohn's disease and other inflammatory conditions of the gut. The intracellular and molecular mechanisms that mediate the IL-1beta-induced increase in intestinal TJ permeability remain unclear. The purpose of this stu...

Previous studies have shown that high concentrations of ethanol (≥40%) cause functional damage of the gastrointestinal epithelial barrier by direct cytotoxic effect on the epithelial cells. The effects of lower noncytotoxic doses of ethanol on epithelial barrier function are unknown. A major function of gastrointestinal epithelial cells is to provide a barrier against the hostile substances in ...

The short-chain fatty acid butyrate was readily taken up by Caco-2 cells. Transport exhibited saturation kinetics, was enhanced by low extracellular pH, and was Na(+) independent. Butyrate uptake was unaffected by DIDS; however, alpha-cyano-4-hydroxycinnamate and the butyrate analogs propionate and L-lactate significantly inhibited uptake. These results suggest that butyrate transport by Caco-2...

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...

The intestinal absorption of chondroitin sulfate (CS) and its hydrolysate, particularly the disaccharides (Di-CS), was investigated by using human intestinal epithelial Caco-2 cell monolayers. Although the transepithelial transport of CS was not detectable, dose- and time-dependent transport of Di-CS was observed. The transport of Di-CS was proved to be energy-independent and its permeability i...

The effect of neuronal cells on the functional properties of intestinal epithelial cells was examined by using an in vitro coculture system. Two cell lines, Caco-2 and PC12, were respectively used as intestinal epithelial and enteric neuronal cell models. Coculture of differentiated Caco-2 cells with PC12 caused a significant decrease in the transepithelial electrical resistance (TER) value of ...

This review examines the use of Caco-2 monolayers in the prediction of intestinal drug absorption. First, the different routes of drug transport in Caco-2 monolayers are compared with those seen in vivo. Second, the prediction of drug absorption in vivo from transport experiments in cell monolayers is discussed for different classes of drugs. Finally, the use of Caco-2 monolayers as a reference...

On interaction with the intestine, the mycotoxin ochratoxin A is know to cause rapid inflammation, diarrhea, and increased bacterial translocation. All these effects are consistent with a decrease in epithelial barrier function. However, this has not been shown directly. We determined that ochratoxin A is able to reduce the barrier properties of the model intestinal cell line Caco-2. Over 24 h,...