With current progress in science, there is growing interest in developing and applying Physiologically Based Kinetic (PBK) models in chemical risk assessment, as knowledge of internal exposure to chemicals is critical to understanding potential effects in vivo. In particular, a new generation of PBK models is being developed in which the model parameters are derived from in silico and in vitro methods. To increase the acceptance and use of these "Next Generation PBK models", there is a need to demonstrate their validity. However, this is challenging in the case of data-poor chemicals that are lacking in kinetic data and for which predictive capacity cannot, therefore, be assessed. The aim of this work is to lay down the fundamental steps in using a read across framework to inform modellers and risk assessors on how to develop, or evaluate, PBK models for chemicals without in vivo kinetic data. The application of a PBK model that takes into account the absorption, distribution, metabolism and excretion characteristics of the chemical reduces the uncertainties in the biokinetics and biotransformation of the chemical of interest. A strategic flow-charting application, proposed herein, allows users to identify the minimum information to perform a read-across from a data-rich chemical to its data-poor analogue(s). The workflow analysis is illustrated by means of a real case study using the alkenylbenzene class of chemicals, showing the reliability and potential of this approach. It was demonstrated that a consistent quantitative relationship between model simulations could be achieved using models for estragole and safrole (source chemicals) when applied to methyleugenol (target chemical). When the PBK model code for the source chemicals was adapted to utilise input values relevant to the target chemical, simulation was consistent between the models. The resulting PBK model for methyleugenol was further evaluated by comparing the results to an existing, published model for methyleugenol, providing further evidence that the approach was successful. This can be considered as a "read-across" approach, enabling a valid PBK model to be derived to aid the assessment of a data poor chemical.
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http://dx.doi.org/10.1016/j.comtox.2021.100159 | DOI Listing |
Food Chem Toxicol
January 2025
Department of Health Sciences and Technology, ETH Zurich, Switzerland. Electronic address:
Hop extracts containing prenylated polyphenols such as 8-prenylnaringenin (8-PN) and its precursor isoxanthohumol (iXN) are popular among women seeking natural alternatives to hormone therapy for postmenopausal symptoms. Due to structural similarities with estrogens, these compounds act as estrogen receptor agonists. Especially 8-PN, described as the most potent phytoestrogen known to date, poses a potential risk for endocrine disruption.
View Article and Find Full Text PDFPflugers Arch
January 2025
Gangarosa Department of Environmental Health, Rollins School of Public Health, Emory University, Atlanta, GA, 30322, USA.
Plasma thyroid hormone (TH) binding proteins (THBPs), including thyroxine-binding globulin (TBG), transthyretin (TTR), and albumin (ALB), carry THs to extrathyroidal sites, where THs are unloaded locally and then taken up via membrane transporters into the tissue proper. The respective roles of THBPs in supplying THs for tissue uptake are not completely understood. To investigate this, we developed a spatial human physiologically based kinetic (PBK) model of THs, which produces several novel findings.
View Article and Find Full Text PDFArch Toxicol
December 2024
Division of Toxicology, Wageningen University and Research, Stippeneng 4, 6708 WE, Wageningen, The Netherlands.
Systemic bile acid homeostasis plays an important role in human health. In this study, a physiologically based kinetic (PBK) model that includes microbial bile acid deconjugation and intestinal bile acid reuptake via the apical sodium-dependent bile acid transporter (ASBT) was applied to predict the systemic plasma bile acid concentrations in human upon oral treatment with the antibiotic tobramycin. Tobramycin was previously shown to inhibit intestinal deconjugation and reuptake of bile acids and to affect bile acid homeostasis upon oral exposure of rats.
View Article and Find Full Text PDFRegul Toxicol Pharmacol
December 2024
Division of Toxicology, Wageningen University, PO Box 8000, 6700 EA Wageningen, the Netherlands.
Pyrrolizidine alkaloids N-oxides (PA-N-oxides) are predominant in plants and herbal foods, and are converted to pyrrolizidine alkaloids (PAs) upon consumption, leading to toxicity. The effect of interindividual kinetic differences on the relative potency values of PA-N-oxides compared to their PAs (REP) was studied, with riddelliine N-oxide (RIDO) and riddelliine (RID) as model compounds. In vitro kinetic data measured in incubations with 30 fecal and 25 liver S9 donor samples showed high variation across individuals, where the interindividual variability was captured with Bayesian multilevel regression.
View Article and Find Full Text PDFBiol Direct
December 2024
Department of Liver Diseases, Shuguang Hospital, Shanghai University of Traditional Chinese Medicine, Shanghai, 201203, China.
Background: Disulfidptosis, identified as an innovative form of cellular death subsequent to cuproptosis, is currently under investigation for its mechanisms in oncological contexts. In-depth analyses exploring the relationship between disulfidptosis-related genes (DRGs) and hepatocellular carcinoma (HCC) are currently limited.
Methods: Transcriptomic data and clinical information were retrieved from the TCGA and GEO databases (GSE76427 and GSE54236), concentrating on the expression levels of 24 DRGs.
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