AIMC Topic: Caco-2 Cells
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Prediction of permeability across intestinal cell monolayers for 219 disparate chemicals using in vitro experimental coefficients in a pH gradient system and in silico analyses by trivariate linear regressions and machine learning.
Biochemical pharmacology
Aug 27, 2021
For medicines, the apparent membrane permeability coefficients (P) across human colorectal carcinoma cell line (Caco-2) monolayers under a pH gradient generally correlate with the fraction absorbed after oral intake. Furthermore, the in vitro P value...
Optimizing Pharmacokinetic Property Prediction Based on Integrated Datasets and a Deep Learning Approach.
Journal of chemical information and modeling
Sep 1, 2020
Oral bioavailability (OBA)-related pharmacokinetic properties, such as aqueous solubility, lipophilicity, and intestinal membrane permeability, play a significant role in drug discovery. However, their measurement is usually costly and time-consuming...
Robotically handled whole-tissue culture system for the screening of oral drug formulations.
Nature biomedical engineering
Apr 27, 2020
Monolayers of cancer-derived cell lines are widely used in the modelling of the gastrointestinal (GI) absorption of drugs and in oral drug development. However, they do not generally predict drug absorption in vivo. Here, we report a robotically hand...
Predictive Multitask Deep Neural Network Models for ADME-Tox Properties: Learning from Large Data Sets.
Journal of chemical information and modeling
Jan 24, 2019
Successful drug discovery projects require control and optimization of compound properties related to pharmacokinetics, pharmacodynamics, and safety. While volume and chemotype coverage of public and corporate ADME-Tox (absorption, distribution, excr...
Effect of potential probiotic Leuconostoc mesenteroides FB111 in prevention of cholesterol absorption by modulating NPC1L1/PPARα/SREBP-2 pathways in epithelial Caco-2 cells.
International microbiology : the official journal of the Spanish Society for Microbiology
Dec 5, 2018
Mustard kimchi consumption reduces cholesterol levels in rats. To identify lactic acid bacteria (LAB) in kimchi which exert this effect, 20 LAB isolates were evaluated for cholesterol reduction in an in vitro screen. The FB111 strain showed the highe...
In vitro intestinal epithelium responses to titanium dioxide nanoparticles.
Food research international (Ottawa, Ont.)
Oct 12, 2018
Titanium dioxide (TiO) is enclosed in many consumer products including pharmaceuticals, cosmetics, and foods. TiO (E171) is daily ingested as mixed nano- and submicron-sized particles since it is approved as a white colorant in Europe in a wide varie...
New 1,5 and 2,5-disubstituted tetrazoles-dependent activity towards surface barrier of Candida albicans.
European journal of medicinal chemistry
Dec 30, 2017
A series of novel tetrazole derivatives was synthetized using N-alkylation or Michael-type addition reactions, and screened for their fungistatic potential against Candida albicans (the lack of endpoint = 100%). Among them, the selected compounds 2d,...
Cytotoxic activity of the bioactive principles from Ficus burtt-davyi.
Journal of environmental science and health. Part. B, Pesticides, food contaminants, and agricultural wastes
Dec 26, 2017
Ficus burtt-davyi (Moraceae) is a medicinal plant species indigenous to Southern Africa. In this study, a phytochemical and cytotoxic investigation on F. burtt-davyi was conducted to evaluate its ethno-medicinal use. The phytochemical study of the fr...
Elevation of serum pyruvate kinase M2 (PKM2) in IBD and its relationship to IBD indices.
Clinical biochemistry
Dec 19, 2017
OBJECTIVES: Endoscopy remains the gold standard to diagnose and evaluate inflammatory bowel disease (IBD) activity. Current biomarkers or their combinations cannot adequately predict IBD risk, diagnosis, progression or relapse, and response to therap...
The addition of inulin and Lactobacillus casei 01 in sheep milk ice cream.
Food chemistry
Dec 5, 2017
The effect of the Lactobacillus casei 01 and inulin addition on sheep milk ice cream during storage (-18 °C, 150 days) was investigated. Control, probiotic and synbiotic ice cream (10% w/w sheep milk cream; 10% w/w sheep milk cream, L. casei 01, 6 lo...
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