Results 31 to 40 of about 12,956 (251)

Metabolism of 2,3-Dehydrosilybin A and 2,3-Dehydrosilybin B: A Study with Human Hepatocytes and Recombinant UDP-Glucuronosyltransferases and Sulfotransferases

open access: yesAntioxidants, 2021
2,3-Dehydrosilybin A and 2,3-dehydrosilybin B are a pair of enantiomers formed by the oxidation of the natural flavonolignans silybin A and silybin B, respectively.
Jiří Vrba   +5 more
doaj   +1 more source

The UDP-glucuronosyltransferases of the blood-brain barrier: their role in drug metabolism and detoxication

open access: yesFrontiers in Cellular Neuroscience, 2014
UDP-glucuronosyltransferases (UGTs) form a multigenic family of membrane-bound enzymes expressed in various tissues, including brain. They catalyze the formation of β-Dglucuronides from structurally unrelated substances (drugs, other xenobiotics, as well
Mohamed eOuzzine   +4 more
doaj   +1 more source

Phase II Metabolism of Asarone Isomers In Vitro and in Humans Using HPLC-MS/MS and HPLC-qToF/MS

open access: yesFoods, 2021
(1) Background: Metabolism data of asarone isomers, in particular phase II, in vitro and in humans is limited so far. For the first time, phase II metabolites of asarone isomers were characterized and human kinetic as well as excretion data after oral ...
Lena Hermes   +3 more
doaj   +1 more source

Glucuronidation: driving factors and their impact on glucuronide disposition

open access: yesDrug Metabolism Reviews, 2017
Glucuronidation is a well-recognized phase II metabolic pathway for a variety of chemicals including drugs and endogenous substances. Although it is usually the secondary metabolic pathway for a compound preceded by phase I hydroxylation, glucuronidation alone could serve as the dominant metabolic pathway for many compounds, including some with high ...
Guangyi, Yang   +15 more
openaire   +3 more sources

SR‐B1‐Mediated Transplacental Transfer of Hydrophobic Toxicants Disrupts Fetal Development During Barriergenesis

open access: yesAdvanced Science, EarlyView.
This study maps the spatiotemporal distribution of hydrophobic toxicants and endogenous metabolites in the developing placenta and fetus. By integrating mass spectrometry imaging with snRNA‐seq, we identify SR‐B1 as a key transporter driving early‐gestation xenobiotic transfer and reveal a critical exposure window associated with persistent fetal ...
Yixuan Huang   +10 more
wiley   +1 more source

Dysregulation of Oral Microbial Eicosapentaenoic Acid Induced by Chronic Restraint Stress Exacerbates Periodontitis via M1 Macrophage Polarization

open access: yesAdvanced Science, EarlyView.
ABSTRACT The intricate interplay between chronic psychological stress and periodontitis, mediated by oral microbiota and macrophage polarization, remains largely enigmatic. Here, we demonstrate that chronic restraint stress (CRS) exacerbates periodontitis by inducing oral microbial dysbiosis and a consequential shift in host metabolism.
Shihong Luo   +13 more
wiley   +1 more source

Integrating Human Intestinal Organoids into FDA'S New Approach Methodologies for Drug Discovery

open access: yesAdvanced Science, EarlyView.
Illustration summarizes how human intestinal organoids (HIOs) are becoming transformative in preclinical research. Preclinical drug discovery pipelines often rely on animal models for ADMET studies, even though interspecies ADME gaps, poor external validity, and high attrition rates are common.
Debarun Patra   +6 more
wiley   +1 more source

Hepatotoxicity Induced by Sophora flavescens and Hepatic Accumulation of Kurarinone, a Major Hepatotoxic Constituent of Sophora flavescens in Rats

open access: yesMolecules, 2017
Our previous study showed that kurarinone was the main hepatotoxic ingredient of Sophora flavescens, accumulating in the liver. This study characterized the mechanism of Sophora flavescens extract (ESF) hepatotoxicity and hepatic accumulation of ...
Peng Jiang   +4 more
doaj   +1 more source

Metabolic fate of drugs of abuse and new psychoactive substances: A pilot study on a novel workflow using a zebrafish embryo model combined with human microdosing

open access: yesBritish Journal of Clinical Pharmacology, EarlyView.
Aim The aim of this study was to develop a novel workflow to identify human urine biomarkers for drugs of abuse and new psychoactive substances. Metabolites of amphetamine, cocaine, LSD, MDMA, methamphetamine, THC, MDMB‐CHMICA, and MDPPP were first identified in a zebrafish embryo (ZE) metabolism study followed by comparison to most abundant human ...
Simon K. Wellenberg   +7 more
wiley   +1 more source

Mapping opioid exposure through prescription data and postmortem analysis of opioid drugs in multiple tissues

open access: yesBritish Journal of Clinical Pharmacology, EarlyView.
Background and Purpose Although opioids are central to end of life (EoL) care, tissue‐level opioid exposure remains poorly understood. The objective of this study was to characterize the relationship between prescription‐derived morphine equivalent daily dose (MEDD) and measured morphine concentrations across multiple organs.
Niamh Higgins   +23 more
wiley   +1 more source

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