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Metabolism

1051

Spectral and mass characterization of kinetic conversion from retinoids to retinoic acid in an in vitro 3-D human skin equivalent model

To investigate the effect of retinoids, such as retinol (ROL), retinal (RAL), and retinyl palmitate (RP), on epidermal integrity, skin deposition, and bioconversion to retinoic acid (RA). 3-D human skin equivalent model (EpiDermFT™) was used. Epidermal cellular integrity measured by TEER values was significantly higher for a topical treatment of ROL and RAL than RP […]
1027

Kinetic conversion of BIOGF1K enriched in compound K from in vitro 3-D human tissue model

The purposes of current study were to investigate the effect of ginsenosides from BIOGF1K enriched in compound K (CK) and compound Y (CY) on the skin barrier function, the deposition in in vitro 3-D human tissue model (EpiDermFT™ Full Thickness 400), and to identify and quantify kinetic bioconversion of the ginsenosides in artificial skin by utilizing the […]
931

Demonstration of the first-pass metabolism in the skin of the hair dye, 4-amino-2-hydroxytoluene, using the Chip2 skin–liver microphysiological model

We used TissUse’s HUMIMIC Chip2 microfluidic model, incorporating reconstructed skin models and liver spheroids, to investigate the impact of consumer-relevant application scenarios on the metabolic fate of the hair dye, 4-amino-2-hydroxytoluene (AHT). After a single topical or systemic application of AHT to Chip2 models, medium was analysed for parent and metabolites over 5 days. The […]
915

Human small intestinal organotypic culture model for drug permeation, inflammation, and toxicity assays

The gastrointestinal tract (GIT), in particular, the small intestine, plays a significant role in food digestion, fluid and electrolyte transport, drug absorption and metabolism, and nutrient uptake. As the longest portion of the GIT, the small intestine also plays a vital role in protecting the host against pathogenic or opportunistic microbial invasion. However, establishing polarized […]
912

A Systems Biology Approach Reveals the Dose- and Time-Dependent Effect of Primary Human Airway Epithelium Tissue Culture After Exposure to Cigarette Smoke In Vitro

To establish a relevant in vitro model for systems toxicology-based mechanistic assessment of environmental stressors such as cigarette smoke (CS), we exposed human organotypic bronchial epithelial tissue cultures at the air liquid interface (ALI) to various CS doses. Previously, we compared in vitro gene expression changes with published human airway epithelia in vivo data to […]
839

Human 3D Gastrointestinal Microtissue Barrier Function As a Predictor of Drug-Induced Diarrhea

Drug-induced gastrointestinal toxicities (GITs) rank among the most common clinical side effects. Preclinical efforts to reduce incidence are limited by inadequate predictivity of in vitro assays. Recent breakthroughs in in vitro culture methods support intestinal stem cell maintenance and continual differentiation into the epithelial cell types resident in the intestine. These diverse cells self-assemble into microtissues with in […]
798

A four-organ-chip for interconnected long-term co-culture of human intestine, liver, skin and kidney equivalents

Systemic absorption and metabolism of drugs in the small intestine, metabolism by the liver as well as excretion by the kidney are key determinants of efficacy and safety for therapeutic candidates. However, these systemic responses of applied substances lack in most in vitro assays. In this study, a microphysiological system maintaining the functionality of four organs over 28 […]
282

NAD(P)H:QUINONE REDUCTASE ACTIVITY IN HUMAN EPIDERMAL KERATINOCYTES AND RECONSTRUCTED EPIDERMAL MODELS.

Reconstructed epidermal models may provide a suitable and relevant model for screening compounds such as quinones, which affect the activities of phase I and II enzymes involved in epidermal detoxification. Reconstructed epidermis may also allow the study of the metabolism of topically applied compounds by the phase I and II enzymes. We demonstrate that NAD(P)H:quinone […]
281

COMPARISON OF ACTIVITIES DEPENDENT ON GLUTATHIONE S-TRANSFERASE AND CYTOCHROME P-450 IA1 IN CULTURED KERATINOCYTES AND RECONSTRUCTED EPIDERMAL MODELS.

There is an increasing need for in vitro testing of compounds for topical application. Reconstructed epidermal models may provide a suitable and relevant model for screening compounds that may affect the activities of phase I and II enzymes involved in epidermal detoxification. In this study, we measured the activity of a phase I enzyme, cytochrome […]
456

AN IN VITRO MODEL OF HUMAN AIRWAY EPITHELIUM (EPIAIRWAY) FOR IN VITRO METABOLISM, TOXICITY SCREENING AND DRUG DELIVERY APPLICATIONS.

This study by Mattek Corp. scientists demonstrated that the EpiAirway in vitro human tracheal/bronchial tissue equivalent possesses the in vivo-like physical and biochemical attributes necessary for evaluating the delivery of drugs, metabolism, airway irritation, and toxicity potential of environmental/occupational chemicals. In vitro airway models are urgently needed as alternatives to animal testing for compliance with […]
517

DERMAL PENETRATION AND METABOLISM OF p-AMINOPHENOL AND p-PHENYLENEDIAMINE: APPLICATION OF THE EPIDERM HUMAN RECONSTRUCTED EPIDERMIS MODEL.

This study by scientists at Procter & Gamble Co. demonstrated that Mattek’s EpiDerm in vitro human skin tissue equivalent showed excellent correlation to in vivo results for skin penetration and metabolism of two hair dye ingredients, further strengthening the evidence for the use of the EpiDerm reconstructed human skin micronucleus assay as a replacement for […]