Results 51 to 60 of about 26,827 (219)

Toxic Evaluations of Calea phyllolepis Extracts Standardized on 6‐epi‐β‐Verbesinol Coumarate and Its In Silico Prediction of the Toxicity

Chemistry &Biodiversity, EarlyView.
In vivo and in silico toxicological effects of Calea phyllolepis extracts Standardized on 6‐epi‐β‐Verbesinol Coumarate. ABSTRACT Medicinal plants are traditionally used in folk medicine. Still, there is a misconception about the safety/efficacy of natural treatments, which results in few studies on the toxic, genotoxic, and mutagenic potential of ...
Suele Bierhals Vencato, Guilherme Borsoi, Cleverson Feistel, Mariele Feiffer Charão, Angélica Rocha Joaquim, Jaqueline Nascimento Picada, Alexandre de Barros Falcão Ferraz   +6 more
wiley   +1 more source

In Vitro Phase I Metabolism of CRV431, a Novel Oral Drug Candidate for Chronic Hepatitis B

Pharmaceutics, 2017
The cytochrome P450-mediated Phase I in vitro metabolism of CRV431 was studied using selective chemical inhibition and recombinant human enzymes. Additionally, the metabolic profile of CRV431 in human, rat, and monkey liver microsomes was investigated ...
Daniel J. Trepanier, Daren R. Ure, Robert T. Foster   +2 more
doaj   +1 more source

Development of Keap1‐Nrf2 Protein–Protein Interaction Inhibitor Activating Intracellular Nrf2 Based on the Naphthalene‐2‐acetamide Scaffold, and its Anti‐Inflammatory Effects

ChemMedChem, EarlyView.
Pyrrolidine‐type naphthalene‐2‐acetamide compound 5i inhibits Kelch‐like ECH‐associated protein 1 (Keap1)‐nuclear factor erythroid 2‐related factor 2 (Nrf2) protein–protein interaction by binding to the Keap1‐DC domain; it subsequently activates intracellular Nrf2 and induces Nrf2‐target genes.
Daisuke Yasuda, Kai Toyoshima, Koujin Kojima, Hanako Ishida, Kazuma Kaitoh, Riyo Imamura, Kayoko Kanamitsu, Hirotatsu Kojima, Megumi Funakoshi‐Tago, Masanori Osawa, Tomoyuki Ohe, Tomoya Hirano   +11 more
wiley   +1 more source

Potent Antisickling Furaldehyde Analogs for Acute Sickle Cell Therapy: Enhanced Efficacy and Intravenous Formulation Potential

ChemMedChem, EarlyView.
This study reports novel 5‐HMF analogs with potent antisickling activities. Lead compound MMA509 enhances hemoglobin oxygen affinity and prevents erythrocyte sickling. Crystal structure of hemoglobin‐MMA509 complex explains MMA509 mechanism of action. An IV formulation is successfully developed, positioning MMA509 as a promising fast‐acting treatment ...
Abdelsattar M. Omar, Moustafa E. El‐Araby, Tarek A. Ahmed, Akua K. Donkor, Albert Opare, Mohini S. Ghatge, Anfal S. Aljahdali, Rana T. Alhashimi, Trevohn N. Robinson, Benita Balogun, Mariana Macias, Salma Roland, Yan Zhang, Faik N. Musayev, Osheiza Abdulmalik, Martin K. Safo   +15 more
wiley   +1 more source

Biosynthesis and Identification of Clenbuterol Metabolites in Urine and In Vitro Microsome Incubation Samples Using UHPLC‐Q‐Exactive Orbitrap Mass Spectrometry: A Comparison Between Human and Bovine Metabolism

Drug Testing and Analysis, EarlyView.
Clenbuterol metabolism was studied in bovine and human urine using LC‐Q‐Exactive‐Orbitrap MS; eight metabolites were identified in human and bovine samples as well as a novel N‐methylated form. Four urinary metabolites specific to cattle were detected and identified.
Anuar Gómez‐Tagle, Claudia Bressan, Rosa Ventura, Alan Álvarez‐Sanchez, Enrique Cardenas‐Yong, Benjamín Velasco‐Bejarano   +5 more
wiley   +1 more source

Interpretation of in vitro concentration‐response data for risk assessment and regulatory decision‐making: Report from the 2022 IWGT quantitative analysis expert working group meeting

Environmental and Molecular Mutagenesis, EarlyView.
Abstract Quantitative risk assessments of chemicals are routinely performed using in vivo data from rodents; however, there is growing recognition that non‐animal approaches can be human‐relevant alternatives. There is an urgent need to build confidence in non‐animal alternatives given the international support to reduce the use of animals in toxicity ...
Marc A. Beal, Guangchao Chen, Kerry L. Dearfield, Min Gi, Bhaskar Gollapudi, Robert H. Heflich, Katsuyoshi Horibata, Alexandra S. Long, David P. Lovell, Barbara L. Parsons, Stefan Pfuhler, John Wills, Andreas Zeller, George Johnson, Paul A. White   +14 more
wiley   +1 more source

In Vitro Metabolism and In Vivo Pharmacokinetics Profiles of Hydroxy-α-Sanshool

Toxics
Hydroxy-α-sanshool (HAS) is the predominant active compound in Zanthoxylum bungeanum Maxim (ZBM). Our present work was aimed to explore the in vitro metabolism characteristics, and in vivo pharmacokinetic (PK) profile of HAS.
Jie Meng, Die Qian, Ruo-Lan Li, Wei Peng, Li Ai   +4 more
doaj   +1 more source

Assay for the terminal enzyme of the stearoyl coenzyme A desaturase system using chick embryo liver microsomes

Journal of Lipid Research, 1977
The NADH-dependent stearoyl CoA desaturase of hepatic microsomes (EC 1.14.99.5) is an enzyme system consisting of cytochrome b5 reductase (EC 1.6.2.2), cytochrome b5, and the terminal desaturase. We have developed a simple method for routine assay of the
V C Joshi, A C Wilson, S J Wakil
doaj   +1 more source

Analysis of in vitro and in vivo metabolism of zidovudine and gemfibrozil in trans‐chromosomic mouse line expressing human UGT2 enzymes

Pharmacology Research & Perspectives, 2022
UDP‐glucuronosyltransferases (UGTs) catalyze the conjugation of various substrates with sugars. Since the UGT2 family forms a large cluster spanning 1.5 Mb, transgenic mouse lines carrying the entire human UGT2 family have not been constructed because of
Kaoru Kobayashi, Tsuneo Deguchi, Satoshi Abe, Naoyo Kajitani, Kanako Kazuki, Shoko Takehara, Kazuomi Nakamura, Atsushi Kurihara, Mitsuo Oshimura, Yasuhiro Kazuki   +9 more
doaj   +1 more source

Activation of HMG-CoA reductase by microsomal phosphatase

Journal of Lipid Research, 1983
HMG-CoA reductase activity can be modulated by a reversible phosphorylation-dephosphorylation with the phosphorylated form of the enzyme being inactive and the dephosphorylated form, active. Phosphatases from diverse sources, including cytosol, have been
K R Feingold, M H Wiley, A H Moser, S R Lear, M D Siperstein   +4 more
doaj   +1 more source