Applications Using C
            <scp>aco</scp>
            ‐2 and
            <scp>TC</scp>
            7 Cells for Drug Metabolism Studies

Ferrec, Eric Le; Fardel, Olivier

doi:10.1002/9780470921920.edm061

Cited by 3 publications

(3 citation statements)

References 53 publications

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“…A step towards the evaluation of bioavailability can be reached in vitro using Caco-2 cells to mimic the transport across the intestinal epithelium. Indeed, Caco-2 cells can be cultivated as monolayers on semipermeable membrane where they develop the morphologic characteristics of epithelium cells, possessing a brush border and tight junctions between adjacent cells[59,60]. In their review, Cui et al mentioned that HT29-MTX goblet cells are sometimes cultured with Caco-2 cells, because they can produce the mucus that otherwise lacks to Caco-2 cells monolayers.They also emphasized the need to evaluate the toxicity of the investigated substance towards Caco-2 cells, before using them, because if the behavior of the Caco-2 cells is compromised, the transmembrane passage could be affected[32].Kang et al attempted to measure the uptake by Caco-2 cells of BDE-28, -47, -99 and -153, respectively, and reported absorption rates of 30%, 26%, 41% and 59% respectively [51].…”

mentioning

confidence: 99%

Oral bioaccessibility of semi-volatile organic compounds (SVOCs) in settled dust: A review of measurement methods, data and influencing factors

Raffy

Mercier

Glorennec

et al. 2018

Journal of Hazardous Materials

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Many semi-volatile organic compounds (SVOCs), suspected of reprotoxic, neurotoxic or carcinogenic effects, were measured in indoor settled dust. Dust ingestion is a non-negligible pathway of exposure to some of these SVOCs, and an accurate knowledge of the real exposure is necessary for a better evaluation of health risks. To this end, the bioaccessibility of SVOCs in dust needs to be considered. In the present work, bioaccessibility measurement methods, SVOCs' oral bioaccessibility data and influencing factors were reviewed. SVOC bioaccessibilities (%) ranged from 11 to 94, 8 to 100, 3 to 92, 1 to 81, 6 to 52, and 2 to 17, for brominated flame retardants, organophosphorus flame retardants, polychlorobiphenyls, phthalates, pesticides and polycyclic aromatic hydrocarbons, respectively. Measurements method produced varying results depending on the inclusion of food and/or sink in the model. Characteristics of dust, e.g., organic matter content and particle size, also influenced bioaccessibility data. Last, results were influenced by SVOC properties, such as octanol/water partition coefficient and migration pathway into dust. Factors related to dust and SVOCs could be used in prediction models. To this end, more bioaccessibility studies covering more substances should be performed, using methods that are harmonized and validated by comparison to in-vivo studies.

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mentioning

confidence: 99%

Oral bioaccessibility of semi-volatile organic compounds (SVOCs) in settled dust: A review of measurement methods, data and influencing factors

Raffy

Mercier

Glorennec

et al. 2018

Journal of Hazardous Materials

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“…To overcome some of the major limitations of the Caco-2 model, researchers have derived a TC7 cell line, which is isolated from Caco-2 subclones. Some major advantages of TC7 include faster growth, relatively lower TEER (150-750 Ω· cm 2) and less heterogeneity [ 34 ]. Moreover, the number of metabolic enzymes at high confluencies, such as UDP-glucuronosyl transferases, hydrolase, sucrase-isomaltase and CYP3A isoenzymes, are also similar to that of the intestinal epithelium of the duodenum and jejunum [ 35 ].…”

Section: D Cell Culture Systems To Evaluate Adme-tox Screeningmentioning

confidence: 99%

Role of in vitro two-dimensional (2D) and three-dimensional (3D) cell culture systems for ADME-Tox screening in drug discovery and development: a comprehensive review

Chunduri¹,

Maddi²

2022

ADMET DMPK

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Drug discovery and development have become a very time-consuming and expensive process. Preclinical animal models have become the gold standard for studying drug pharmacokinetic and toxicity parameters. However, the involvement of a huge number of animal subjects and inter-species pathophysiological variations between animals and humans has provoked a lot of debate, particularly because of ethical concerns. Although many efforts are being established by biotech and pharmaceutical companies for screening new chemical entities in vitro before preclinical trials, failures during clinical trials are still involved. Currently, a large number of two- dimensional (2D) in vitro assays have been developed and are being developed by researchers for the screening of compounds. Although these assays are helpful in screening a huge library of compounds and have shown perception, there is a significant lack in predicting human Absorption, Distribution, Metabolism, Excretion and Toxicology (ADME-Tox). As a result, these assays cannot completely replace animal models. The recent inventions in three-dimensional (3D) cell culture-based assays like organoids and micro-physiological systems have shown great potential alternative tools for predicting the compound pharmacokinetic and pharmacodynamic fate in humans. In this comprehensive review, we have summarized some of the most commonly used 2D in vitro assays and emphasized the achievements in next-generation 3D cell culture-based systems for predicting the compound ADME-Tox.

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“…The researchers need to resort to a new type of intestinal cells to overcome the lack of metabolic enzymes of the Caco-2 cell line was addressed by employing additional cell lines. The TC-7 cell line, one of the Caco-2 cell line subclones, was isolated to overcome the major limitations of the parental line (Ferrec, 2012). There is a good correlation between this subclone and the Caco-2 cell line, indicating that it is an excellent stand-in for Caco-2 monolayers (Grès et al, 1998).…”

Section: Cell-based Enteric Modelmentioning

confidence: 99%

Analyzing the metabolic fate of oral administration drugs: A review and state-of-the-art roadmap

Liu

Liu²,

Zhou³

et al. 2022

Front. Pharmacol.

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The key orally delivered drug metabolism processes are reviewed to aid the assessment of the current in vivo/vitro experimental systems applicability for evaluating drug metabolism and the interaction potential. Orally administration is the most commonly used state-of-the-art road for drug delivery due to its ease of administration, high patient compliance and cost-effectiveness. Roles of gut metabolic enzymes and microbiota in drug metabolism and absorption suggest that the gut is an important site for drug metabolism, while the liver has long been recognized as the principal organ responsible for drugs or other substances metabolism. In this contribution, we explore various experimental models from their development to the application for studying oral drugs metabolism of and summarized advantages and disadvantages. Undoubtedly, understanding the possible metabolic mechanism of drugs in vivo and evaluating the procedure with relevant models is of great significance for screening potential clinical drugs. With the increasing popularity and prevalence of orally delivered drugs, sophisticated experimental models with higher predictive capacity for the metabolism of oral drugs used in current preclinical studies will be needed. Collectively, the review seeks to provide a comprehensive roadmap for researchers in related fields.

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Applications Using C aco ‐2 and TC 7 Cells for Drug Metabolism Studies

Cited by 3 publications

References 53 publications

Oral bioaccessibility of semi-volatile organic compounds (SVOCs) in settled dust: A review of measurement methods, data and influencing factors

Oral bioaccessibility of semi-volatile organic compounds (SVOCs) in settled dust: A review of measurement methods, data and influencing factors

Role of in vitro two-dimensional (2D) and three-dimensional (3D) cell culture systems for ADME-Tox screening in drug discovery and development: a comprehensive review

Analyzing the metabolic fate of oral administration drugs: A review and state-of-the-art roadmap

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