ArticleDrug metabolism and disposition: the biological fate of chemicals2016
Functional Comparison of Human Colonic Carcinoma Cell Lines and Primary Small Intestinal Epithelial Cells for Investigations of Intestinal Drug Permeability and First-Pass Metabolism.
Article in Drug metabolism and disposition: the biological fate of chemicals, 2016. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 29 papers.
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The abstract states no effect estimate the extractor could read, or names no intervention and outcome on the map, so this paper lights no cell and moves no belief. It is still indexed, cited and linked below.
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Trials whose registry record cites this paper, or whose number appears in the abstract. A trial that started after this paper was published is citing it as background, not reporting it.
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Who cites it
29 citing papers in PubMed, 52 citations in OpenAlex.
- Glycoprotein Mucin 13 Expression as a Theranostic Target in Colorectal Cancer.Clinical cancer research : an official journal of the American Association for Cancer Research · 2026Article
- Modeling Early Events in Food Sensitization: Complementary Insights from Caco-2 and T84 Epithelial Barriers Exposed to Peanut Allergens.Foods (Basel, Switzerland) · 2026Article
- The scientific basis of synergy in traditional Chinese medicine: physicochemical, pharmacokinetic, and pharmacodynamic perspectives.Chinese medicine · 2026Review
- Human intestinal enteroids: Nonclinical applications for predicting oral drug disposition, toxicity, and efficacy.Pharmacology & therapeutics · 2025Review
- Article
- Complexification of In Vitro Models of Intestinal Barriers, A True Challenge for a More Accurate Alternative Approach.International journal of molecular sciences · 2023Review
- Development of 3D-Bioprinted Colitis-Mimicking Model to Assess Epithelial Barrier Function Using Albumin Nano-Encapsulated Anti-Inflammatory Drugs.Biomimetics (Basel, Switzerland) · 2023Article
- Evaluation of Caco-2 and human intestinal epithelial cells asBiochemistry and biophysics reports · 2022Article
- Establishment and Characterization of Novel Human Intestinal In Vitro Models for Absorption and First-Pass Metabolism Studies.International journal of molecular sciences · 2022Article
- Intestinal Models for Personalized Medicine: from Conventional Models to Microfluidic Primary Intestine-on-a-chip.Stem cell reviews and reports · 2022Review
- Organoid-derived intestinal epithelial cells are a suitable model for preclinical toxicology and pharmacokinetic studies.iScience · 2022Article
- Preclinical In Vitro Model to Assess the Changes in Permeability and Cytotoxicity of Polarized Intestinal Epithelial Cells during Exposure Mimicking Oral or Intravenous Routes: An Example of Arsenite Exposure.International journal of molecular sciences · 2022Article
- Gutsy science: In vitro systems of the human intestine to model oral drug disposition.Pharmacology & therapeutics · 2022Review
- Magnetically-propelled fecal surrogates for modeling the impact of solid-induced shear forces on primary colonic epithelial cells.Biomaterials · 2021Article
- Hyperglycemia minimally alters primary self-renewing human colonic epithelial cells while TNFα-promotes severe intestinal epithelial dysfunction.Integrative biology : quantitative biosciences from nano to macro · 2021Article
- Bypassing P-glycoprotein mediated efflux of afatinib by cyclodextrin complexation - Evaluation of intestinal absorption and anti-cancer activity.Journal of molecular liquids · 2021Article
- Cytochrome P450 expression, induction and activity in human induced pluripotent stem cell-derived intestinal organoids and comparison with primary human intestinal epithelial cells and Caco-2 cells.Archives of toxicology · 2021Article
- Next-Generation Intestinal Toxicity Model of Human Embryonic Stem Cell-Derived Enterocyte-Like Cells.Frontiers in veterinary science · 2021Article
- Protective Effect of an Exopolysaccharide Produced byFrontiers in microbiology · 2021Article
- Robotically handled whole-tissue culture system for the screening of oral drug formulations.Nature biomedical engineering · 2020Article
Corrections and comments
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Authors and funding
5 authors at 1 institution in 1 country.
Funding
Abstract
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. Caco-2, T84, and fSIECs all formed tight junctions, as assessed by immunofluorescence microscopy for zonula occludens-1, which was well organized into circumscribing strands in T84, Caco-2, and fSIECs but was diffuse in LS180 cells. The transepithelial electrical resistance value for LS180 monolayers was lower than that for Caco-2, T84, and fSIECs. In addition, the apical-to-basolateral permeability of the paracellular marker Lucifer yellow across LS180 monolayers was greater than in fSIECs, T84, and Caco-2 monolayers. The transcellular marker propranolol exhibited similar permeability across all cells. With regard to metabolic capacity, T84 and LS180 cells showed comparable basal midazolam hydroxylation activity and was inducible by rifampin and 1α,25(OH)2D3 in LS180 cells, but only marginally so in T84 cells. The basal CYP3A4 activity of fSIECs and Caco-2 cells was much lower and not inducible. Interestingly, some of the drug transporters expressed in LS180 and Caco-2 cells were induced by either 1α,25(OH)2D3 or rifampin or both, but effects were limited in the other two cell lines. These results suggest that none of the cell lines tested fully replicated the drug disposition properties of the small intestine and that the search for an ideal screening tool must continue.
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Registered trials
Read under generation 80e0d062 · epoch 390. Bibliography from PubMed, PubMed Central and OpenAlex; grants from NIH RePORTER; trial links from ClinicalTrials.gov; estimates, votes and beliefs from the OpenQuestion graph.