A novel in vitro Caco-2 hepatocyte hybrid system was set up and tested for its ability to predict the oral bioavailability (F) in humans of 24 randomly chosen marketed drugs. Caco-2 cells were cultured on the transwell filters to form tight junctions. Pooled cryopreserved human hepatocytes were placed in the basolateral receiver compartment. To evaluate the permeability and hepatic first pass i...

We developed an in vitro screening system for antihyperlipidemic activity by measuring lipoprotein profiles secreted from human intestinal epithelium-like cells from the colon cancer cell line, Caco-2. Sodium (Na) butyrate at 5 mM differentiated Caco-2 cells into intestinal epithelium-like cells and numerous microvilli on the apical side of cells were observed under transmission electron micros...

Butyrate, a short-chain fatty acid, is the major energy fuel for the colonocytes. We have previously reported that monocarboxylate transporter isoform 1 (MCT1) mediates uptake of butyrate by human colonic Caco-2 cells. To better understand the mechanisms of MCT1 expression and regulation in the human intestine, we examined the activity and regulation of MCT1 promoter in Caco-2 cells. The transc...

Although colorectal cancer (CRC) treatment with 5-fluorouracil (5-FU) is the first line of therapy for this debilitating disease, treatment effectiveness is often hampered by the development of drug resistance and toxicity at high doses. ER-β can play an important role in CRC development and possibly in its response to therapy. Pterostilbene (PT) possesses antioxidant and anticancer effects tha...

Adhesive ability was tested in seven lactobacillus solated from the chicken digestive tract after cultivation with CaCo-2 cells (intestinal epithelial cells), MDCK (dog kidney) cells and CEF (chicken embryo fiber) cells. We noted the following important observations regarding the adhesive ability between different lactobacillus strains and three cell types: the adhesive interaction between the ...

κ-carrageenan (κ-CGN) is an important food additive that has been demonstrated to induce colitis in animal models. In the present study, the effects of κ-CGN were assessed using an in vitro co-culture system that contained intestinal epithelial Caco-2 cells and activated macrophage-like THP-1 cells. The results demonstrated that in single cultures of Caco-2 and THP-1 cells treated with κ-CGN, t...

To specify critical factors responsible for Pseudomonas aeruginosa penetration through the Caco-2 cell epithelial barrier, we analyzed transposon insertion mutants that demonstrated a dramatic reduction in penetration activity relative to P. aeruginosa PAO1 strain. From these strains, mutations could be grouped into five classes, specifically flagellin-associated genes, pili-associated genes, h...

We found that the human intestinal isolate Bifidobacterium bifidum MIMBb75 strongly adhered to Caco-2 cells. Proteinase K and lithium chloride treatments showed that proteins play a key role in MIMBb75 adhesion to Caco-2 cells. By studying the cell wall-associated proteins, we identified a surface protein, which we labeled BopA. We purified the protein chromatographically and found that it func...

Of 30 cell lines and primary cells examined, productive severe acute respiratory syndrome coronavirus (Urbani strain) (SARS-CoV) infection after low-multiplicity inoculation was detected in only six: three African green monkey kidney epithelial cell lines (Vero, Vero E6, and MA104), a human colon epithelial line (CaCo-2), a porcine kidney epithelial line [PK(15)], and mink lung epithelial cells...

Generating a phosphate prodrug is one of the common approaches for circumventing poor solubility issues of a parent drug. Alkaline phosphatase (ALP) level was determined in rat intestine mucosa scraps, human colon carcinoma (Caco-2) cells, and Madin-Darby canine kidney (MDCK) cells to characterize in vitro models for ALP-mediated phosphate prodrug conversion. In addition, fosphenytoin and fosfl...