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Showing 1 to 20 of 22 for “"metabolic activation"”.
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Development of a new screening assay to identify proteratogenic compounds using Zebrafish Danio rerio embryo combined with an exogenous mammalian metabolic activation system (mDarT)
… (DarT) combined with an exogenous mammalian metabolic activation system (MAS), able to biotransform proteratogenic compounds. Cyclophosphamide, ethanol, benzo[a]pyrene and thalidomide were used as test materials to assess the efficiency of this assay. Briefly, the zebrafish embryos were …
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An investigation into the metabolic activation of novel chloromethylindolines by isoforms of cytochrome P450. Targeting drug metabolising enzymes in cancer: analysis of the role and function of selected cytochrome P450 oxidising novel cancer prodrugs
… cell lines were used to investigate the metabolic profiles with a focus on production of the cytotoxic derivatives of chloromethylindolines. Results Detailed metabolic studies show that (1-(Chloromethyl)-1,2-dihydropyrrolo [3,2-e]indol-3(6H)-yl)(5-methoxy-1H-indol-2-yl) methanone …
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The Mutagenicity of Nutmeg, Mace and Black Pepper and some Oil Constituents
… TA1537, TA1538, TA98 and TAlOO with and without metabolic activation. Safrole, eugenol and myristicinwere tested with metabolic activation. Safrole was shown to be a weak mutagen to TA1535 and TA1538. Mace and black pepper were shown to be weak mutagens to TA1537 with and without metabolic …
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An investigation into the potential mutagenicity of South African traditional medicinal plants
… cell system to detect pro-mutagens that require metabolic activation in order to exert mutagenicity or clastogenicity - directly acting mutagens do not require metabolic activation. A significant mutagenic potential (p 0.01) was evident with the Salmonella reverse mutation assay for three of the …
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Active Inhibition of T Cell Proliferation by Monocytes
… described in their ability to inhibit T cell activation. The most current model is that anti-class II mAb interfere directly with the T cell receptor-major histocompatibility complex crosslinking which is necessary for T cell activation. The anti-CD3 mAb, OKT3, is an MHC class II …
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Modulatory Effects of Citrus Flavonoids Towards the Metabolism and Mutagenicity of Environmental Carcinogens
… NNK generally require internal enzymatic activation. This activation occurs via cytochrome P450 (CYP) enzymes and leads to metabolites that bind to human DNA which may in turn cause mutations which may then in turn lead to carcinogenesis. Certain nonnutritive plant compounds termed …
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The role of ABHD11 in the regulation of the hypoxia inducible transcription factors
… cancers. Critical to understanding this metabolic axis is the recognition that the prolyl hydroxylase enzymes (PHDs), the oxygen sensors within the HIF pathway, are members of a diverse group of enzymes termed 2-oxoglutarate-dependent dioxygenases. These enzymes all require oxygen, iron …
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Modulating macrophage phenotype for obesity therapy
… that macrophages are also involved in beneficial metabolic processes like maintaining energy balance and directing lipid metabolism. Current therapies aim to address health issues arising from obesity by suppressing appetite or decreasing nutrient absorption which can lead to a host of …
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Mechanisms of toxicity and carcinogenicity of three alkylanilines
… published case-control study. Understanding the metabolic activation of and DNA adduct formation by these chemicals is an important first step in elucidating their mechanisms of carcinogenesis and toxicity. Cytochrome P450-mediated metabolism was profiled based on the hypothesis that …
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In vitro chemically-induced DNA damage in cancer patients and healthy individuals. The effect of genotoxic compounds in cells from polyposis coli, colon cancer patients and healthy individuals.
… and alkaline Comet assay with and without metabolic activation.
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Inhibitory Effects of Isothiocyanates on the Mutagenicity and Metabolism of Environmental Carcinogens
… activities. Since NNK, BaP and HCAs all require metabolic activation to be mutagenic, our studies indicated that isothiocyanates inhibited the activity of specific isoenzymes of cytochrome P-450.</p>
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Effects of Pycnogenol on Microsomal Cytochrome P450 Activity and Apoptosis
… in lung microsomes from either age group.</p> <p>Metabolic activation of NNK depends upon cytochrome P450 enzymes (GYP). A second study looked at O-dealkylation of the substrates benzyloxyresorufin (BROD), ethoxyresorufin (EROD) and methoxyresorufin (MROD) linked to CYP2B1,2C6 and 1A2, …
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Estrogenic Activity of the Polybrominated Diphenyl Ether Flame Retardant Mixture DE-71
… the cellular and tissue effects were due to a metabolic activation of individual congeners.
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Free radical formation and DNA damage in the cytotoxicity of alkylaminoanthraquinone antitumour agents.
… of MIT, CI941 and 1,4AQ appears to prevent metabolic activation. In further studies;- i) MIT and CI941 were more potent inhibitors of 3 MCF-7 topoisomerase I activity than other quinones, ii) MIT and DOX-Fe + complexes mediated plasmid DNA strand breakage in the presence of reduced …
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Characterisation of human Haematopoietic Stem Cell differentiation and exit from quiescence at single cell resolution
… model system to comprehensively study HSC activation and to investigate whether HSC self-renewal is lost during quiescence exit or during cell cycle progression. First, I unveil an unexpected degree of intrinsic functional and molecular heterogeneity within the human CD49f+ HSC pool. I …
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The fluroxene mediated degradation of cytochromes P-450
… in methylcholanthrene induced micro-somes. Metabolic activation of cytochromes P-450 by the cyto-chromes P-450 drug metabolising pathway appears to be essential for the fluroxene mediated degradation of cyto-chromes P-450. Since none of the known or proposed metabolites of fluroxene can …
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DEPDC5 is a metabolic checkpoint regulator in the B cell AA-mTORC1 pathway
… is encountered, which simultaneously triggers a metabolic switch enabling enhanced growth, proliferation and differentiation in activated B cells. Central to this metabolic activation is the mechanistic target of rapamycin (mTOR) complex 1 (mTORC1) pathway, which is required for multiple inputs …
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An investigation involving a comparison between the hydrolytic degradation of lovastatin and simvastatin using HPLC
… are administrated as prodrugs that require metabolic activation to form the active acid forms, namely lovastatin hydroxy acid (LVA) and simvastatin hydroxy acid (SVA). Both statins possess similar chemical structures and the only differences is the presence of a 2-methylbutryloxy side chain …
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Improving antibiotic therapy for Mycobacterium tuberculosis
… how combinations of antibiotics influence their metabolic activation and degradation, potentially impacting their therapeutic efficacy. These findings provide valuable insights that could guide the development of optimized combination therapies to enhance patient outcomes. Collectively, my …
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Synthesis and Characterization of Bexarotene Derivatives with Potential Biological Activity // Получаване и охарактеризиране на бексаротенови производни с потенциална биологична активност
… of theoretical approaches, the possibilities for metabolic activation of bexarotene have been successfully identified, also its metabolites and new derivatives evaluated. The mechanisms by which the metabolites of the newly prepared compounds can potentiate liver damage through specific …
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