Global ETD Search
Search theses and dissertations gathered from participating repositories worldwide. Every result links back to the library that holds it. No account is needed.
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Showing 1 to 20 of 20 for “"Microsome"”.
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Melatonin-Tamoxifen Drug Conjugates as Breast Cancer Drugs: Pharmacological Evaluation in Phenotypically Diverse Breast Cancer Models and Pharmacokinetic Assessment in Liver Microsome and Female Mouse Models
<p>Tamoxifen is a first-generation selective estrogen receptor modulator, which reduces the risk of both invasive and non-invasive breast cancer (BC) as well as tumor recurrence in several clinical trials. However, chronic use of tamoxifen can increase uterine cancer risk and induce tamoxifen …
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Species-specific Myoglobin Oxidation
… redox stability was investigated in HNE- and microsome containing models. HNE enhanced ovine OxyMb oxidation at all pH/temperature conditions studied and adduction of HNE to Mb was identified at amino acid residue His 120, His 25 and His 65. The ovine microsome model study found that elevated …
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Inhibitory Effects of Isothiocyanates on the Mutagenicity and Metabolism of Environmental Carcinogens
… by F344 rat and male Syrian golden hamster liver microsomes were investigated. In addition, the alkyl chain-length effects of BITC and PEITC, together with phenyl isothiocyanate (PITC) and phenylpropyl isothiocyanate (PPITC) on the metabolism and mutagenicity of NNK, and on the metabolism of …
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IN VITRO AND IN VIVO KINETIC MODELING OF DIAZEPAM METABOLISM
… specific CYP enzyme sources, including rat liver microsome (RLM), human liver microsome (HLM), purified CYP enzyme isoforms and rat hepatocytes. All saturation curves display non-Michaelis-Menten kinetics, form multiple primary metabolites, and are sequentially metabolized to secondary …
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Influence of Chlorination and the Distribution System on Mutagens in a Potable Water Supply
… of these concentrates with the Ames Salmonella/microsome reversion assay showed both promutagenic and direct-acting responses in TA98. Examination of the water at the groundwater source, following treatment and after passage through the distribution system, revealed that the level of both direct …
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From the Endoplasmic Reticulum to the Golgi Apparatus : In Vitro and In Vivo Approaches to Understanding COPII Vesicle Function in Plant Cells
… vitro formation of COPII vesicle using ER-rich microsome, 30% (NH4)2SO4 cytosol GMP-PNP and ATP regenerating system. The vesicle budding was enhanced when ER-rich microsome from a Sec12 overproducer and more Sar1p are available in the budding mixture. Putative COPII vesicles were isolated from a …
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ACUTE CELLULAR UPTAKE OF ABNORMAL PRION PROTEIN IS CELL TYPE AND SCRAPIE STRAIN INDEPENDENT
… taken up more efficiently then PrP-res in either microsome or partially purified preparations. Our results suggest that PrP-res aggregate size, the PrP-res microenvironment, and/or host cell-specific factors can all influence whether or not a cell takes up PrP-res following exposure to TSE …
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ACUTE CELLULAR UPTAKE OF ABNORMAL PRION PROTEIN IS CELL TYPE AND SCRAPIE STRAIN INDEPENDENT
… taken up more efficiently then PrP-res in either microsome or partially purified preparations. Our results suggest that PrP-res aggregate size, the PrP-res microenvironment, and/or host cell-specific factors can all influence whether or not a cell takes up PrP-res following exposure to TSE …
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Determination of Absolute Protein Content of Hepatic CYP4F Enzymes in Human Liver Microsomes Using LC/MS/MS Methodology and Comparison with Immunoquantification and Enzyme Activity
… (CYP) enzymes in individual donor human liver microsome (HLM) samples. The CYP4F subfamily of enzymes have recently been identified to be involved in the metabolism of endogenous compounds (arachidonic acid, leukotriene B4), nutrients (vitamin K1 and vitamin E), and xenobiotics (parfuramidine …
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Content and Activity of Cytochrome P450 3A in Rat Brain Microsomes and Mitochondria
<p>The potential contribution of CYP3A in brain microsomes and mitochondria is crucial to designing appropriate therapeutic strategies and preventing toxicities. Until recently, there has been limited data reported in the literature with respect to CYP3A activity and its expression in the brain …
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Regulation of Highly Unsaturated Fatty Acid Metabolism
… and HUFAs increased the PE/PC ratio in rat liver microsome and the change of PE/PC ratio was inversely correlated with both mature SREBP-1 and D6D mRNA in rat liver and in HepG2 cells. D6D promoter-luciferase assay in HepG2 cells demonstrated that sterol regulatory element is required for …
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Metabolic Factors Determining Outcome in Chemotherapy: Studies with Pazopanib
… techniques used in this work include liver microsome preparations and drug <br/>stability assays in vitro, pharmacokinetic profiling of drugs, and syngeneic tumour <br/>growth studies in vivo. Drug stability studies in vitro identified a species difference in pazopanib metabolism between …
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Effect of Dietary Factors on Mutagenesis, Metabolism, and Binding to DNA of Benzo [a] pyrene and Benzo [a] pyrene 7, 8-dihydrodiol
… to those suggested for EA.</p> <p>Hepatic microsomes from rats which had been given 30% glucose in drinking water 48 hrs prior to sacrifice inhibited B[a]P-induced mutagenesis by 27% and B[a]P 7,8- DHD-induced mutagenesis by 55% in Salmonella tvphimurium TA 100. Microsomes from …
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Impact of CYP2C8 single nucleotide polymorphisms on in-vitro metabolism of imatinib to N-desmethyl imatinib
… by CYP3A4 and CYP2C8. In vitro human liver microsome (HLM) studies indicate imatinib autoinhibition of CYP3A4-mediated metabolism, suggesting a more significant role for CYP2C8 upon chronic dosing. CYP2C8 is polymorphic and functional effects of the major CYP2C8 polymorphisms CYP2C8*3 and …
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Characterising the anticancer effects of a small molecule with potential to inhibit nuclear import via karyopherin beta1
… however, rapid clearance was shown by liver microsome assay. In vivo repeated dose toxicology studies showed that C53 is tolerable in nude mice. Taken together, the data presented in this study shows that a novel small molecule, C53 has a negative effect on the proliferation of cancer cells, …
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Metabolomics and chemical library screening for antibacterial drug discovery
… involved generating and screening a human liver microsome metabolized drug library in parallel with the original library to identify intrinsically active drugs and drugs with antibacterial metabolites. Several drugs demonstrated improved antibacterial activities against MRSA after microsomal …
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Characterization of the first steryl ester transporter in biology, Yol075c, and its pleiotropic effects
… plasma membrane, nucleus, vacuole, mitochondria, microsome, peroxisome, and whole cells saponified the lipids and measured sterol amount using UV absorbance spectroscopy. The overall sterol content for whole cells in both wild type and Yol075c was identical. The organelles, in contrast, showed a …
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In Vitro SSAT Enzyme Activity Study Using Rat and Mouse Liver Tissue Preparations
Spermidine/spermine N1-acetyltransferase (SSAT) is the enzyme which acetylates spermidine (Spd) to acetylspermidine (AcSpd). SSAT is also capable of acetylating polyamine analogues such as triethylenetetramine (TETA) to acetyltriethylenetetramine (MAT). However, this process is debatable because …
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Library Screening and Focused Multiomics of Antibacterial Action on Vancomycin-Resistant Enterococci faecium
… in both its original (unmetabolized; UM) and its microsome metabolized (pre-metabolized; PM) forms, and in the absence and presence of vancomycin. This allows the identification of agents with active metabolites and agents that can act synergistically with the resistant-to-antibiotic. 2 x 2 …
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The Biogenesis of Peroxisomal Catalase in Rat Liver
… reached the peroxisomes were found partly in the microsome-rich fractions and largely at the top of the gradients where the layer was applied. Many experiments were performed to clarify the early events in catalase biosynthesis and transport, but they did not succeed in completely solving the …