In Vitro Metabolism
Mostrando 1-12 de 1135 artigos, teses e dissertações.
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1. CYP450 Metabolism of a Semisynthetic Naphthoquinone, an Anticancer Drug Candidate, by Human Liver Microsomes
CNFD (6b,7-dihydro-5H-cyclopenta[b]naphtho[2,1-d]furan-5,6(9aH)-dione) is a semisynthetic naphthoquinone derived from lawsone that has cytotoxic action in different tumor lines and anticancer activity in vivo. Therefore, this molecule is a relevant candidate for drug development, but there is still no information on its human metabolism and systemic eliminat
Journal of the Brazilian Chemical Society. Publicado em: 2022
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2. DFT, Molecular Docking, and ADME/Tox Screening Investigations of Market-Available Drugs against SARS-CoV-2
A series of drugs was investigated to determine structural, electronic and pharmacological properties, as well as the molecular affinity for the main protease of severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2). The drugs were submitted to density functional theory calculations to optimize structures and predict binding preferences. The optimized
J. Braz. Chem. Soc.. Publicado em: 2021-08
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3. In vitro metabolism of copalic and kaurenoic acids in rat and human liver microsomes
Copalic (CA) and kaurenoic (KA) acids are the main diterpenes found in the oleoresin extracted from the copaiba tree (Copaifera sp). This study aimed to characterize the metabolism of CA and KA in rat and human liver microsomes using liquid chromatography with tandem mass spectrometry (LC-MS/MS). The in vitro assays showed deviations from the Michaelian kine
Quím. Nova. Publicado em: 2021-06
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4. Synthesis, in silico Study and Antimicrobial Activity of New Piperine Derivatives Containing Substituted δ-Esters
A series of fifteen new piperine-derived diesters was synthesized through the substitution reaction between the salt of piperic acid, obtained through piperine basic hydrolysis, with the δ-chloro-esters, obtained through the cleavage of tetrahydrofuran (THF) with acyl chlorides in the presence of ZnCl2. The final compounds were obtained with yields ranging
J. Braz. Chem. Soc.. Publicado em: 2020-12
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5. EFEITO DO PARASITISMO POR Haemonchus contortus SOBRE O METABOLISMO OXIDATIVO DE LEUCÓCITOS DE OVINOS
Resumo A resposta imune tardia direcionada para eliminação da hemoncose pode ser modulada pelo perfil Th2, sendo os eosinófilos as principais células efetoras responsáveis pela eficiente eliminação do parasita; ou modulada pelo perfil Th1, sendo os neutrófilos as principais células efetoras, que promovem eliminação parasitária mais deficiente, po
Ciênc. anim. bras.. Publicado em: 13/12/2019
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6. Meta-topolin: an alternative for the prevention of oxidative stress in sugarcane micropropagation
RESUMO A influência de duas citocininas aromáticas (CKs), 6-benzilaminopurina (BAP) e meta-topolina (mT) na propagação in vitro e no metabolismo redox da cana-de-açúcar (Saccharum spp., variedade RB98710) foi investigada. As plantas foram cultivadas em meio Murashige e Skoog (MS) suplementado com mT (5 µmol.L-1) ou BAP (5 ou 6,66 µmol.L-1) por 40 dia
Hoehnea. Publicado em: 21/10/2019
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7. Preparation and evaluation of 2-methoxyestradiol-loaded pH-sensitive liposomes
The development and clinical application of 2-methoxyestradiol (2-ME) as a new type of antitumor drug are limited due to its poor solubility, rapid metabolism in vivo, and large oral dosage. 2-ME-loaded pH-sensitive liposomes (2-ME-PSLs) was prepared containing the lipids, Lipoid E-80 (E-80), cholesteryl hemisuccinate (CHEMS), and cholesterol (CHOL) via thin
Braz. J. Pharm. Sci.. Publicado em: 03/10/2019
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8. Effect of iguratimod on diclofenac metabolism by CYP2C9 in rats and human recombinant CYP2C9 yeast cells
Iguratimod (IGU, also known as T-614), a novel disease modifying antirheumatic drug intended to cure patients with rheumatoid arthritis (RA). The purpose of this study is to evaluate the effect of IGU on the pharmacokinetics of CYP2C9 probe drug diclofenac and its metabolite 4′-hydroxy diclofenac in vivo and in vitro. In in vivo experiments, 24 rats were r
Braz. J. Pharm. Sci.. Publicado em: 09/09/2019
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9. Isolation and characterization of a human cementocyte-like cell line, HCY-23
Abstract Cementum is the mineralized tissue covering the tooth root that functions in tooth attachment and post-eruptive adjustment of tooth position. It has been reported to be highly similar to bone in several respects but remains poorly understood in terms of development and regeneration. Here, we investigate whether cementocytes, the residing cells in ce
Braz. oral res.. Publicado em: 15/08/2019
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10. NMR-Based Metabolomic Screening for Metabolites Associated with Resistance to Meloidogyne javanica in Annona muricata Roots
The resistance of Annona muricata roots to the nematode Meloidogyne javanica was investigated by nuclear magnetic resonance (NMR)-based metabolomics in combination with principal component analysis (PCA). Metabolic changes in roots exposed and not exposed to the nematode were evaluated and compared. In addition, the presence of nematicidal compounds in the r
J. Braz. Chem. Soc.. Publicado em: 23/05/2019
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11. Pyrazolyl-Tetrazoles and Imidazolyl-Pyrazoles as Potential Anticoagulants and their Integrated Multiplex Analysis Virtual Screening
This article reports a novel virtual screening algorithm seeking the rational identification of novel lead anticoagulants. Seven 5-(3-methyl-1-aryl-1H-pyrazol-4-yl)-1H-tetrazoles and seven novel 1-aryl-4-(4,5-dihydro-1H-imidazol-2-yl)-3-methyl-1H-pyrazoles were obtained in three steps starting from arylhydrazine hydrochlorides as raw materials in good yields
J. Braz. Chem. Soc.. Publicado em: 2019-01
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12. Efficacy of sertraline against Trypanosoma cruzi: an in vitro and in silico study
Abstract Background: Drug repurposing has been an interesting and cost-effective approach, especially for neglected diseases, such as Chagas disease. Methods: In this work, we studied the activity of the antidepressant drug sertraline against Trypanosoma cruzi trypomastigotes and intracellular amastigotes of the Y and Tulahuen strains, and investigated its
J. Venom. Anim. Toxins incl. Trop. Dis. Publicado em: 29/11/2018