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https://www.readbyqxmd.com/read/28934153/inhibitory-effect-of-selaginellins-from-selaginella-tamariscina-beauv-spring-against-cytochrome-p450-and-uridine-5-diphosphoglucuronosyltransferase-isoforms-on-human-liver-microsomes
#1
Jae-Kyung Heo, Phi-Hung Nguyen, Won Cheol Kim, Nguyen Minh Phuc, Kwang-Hyeon Liu
Selaginella tamariscina (Beauv.) has been used for traditional herbal medicine for treatment of cancer, hepatitis, and diabetes in the Orient. Numerous bioactive compounds including alkaloids, flavonoids, lignans, and selaginellins have been identified in this medicinal plant. Among them, selaginellins having a quinone methide unit and an alkylphenol moiety have been known to possess anticancer, antidiabetic, and neuroprotective activity. Although there have been studies on the biological activities of selaginellins, their modulatory potential of cytochrome P450 (P450) and uridine 5'-diphosphoglucuronosyltransferase (UGT) activities have not been previously evaluated...
September 21, 2017: Molecules: a Journal of Synthetic Chemistry and Natural Product Chemistry
https://www.readbyqxmd.com/read/28933256/combined-effect-of-telmisartan-and-fluvastatin-on-arachidonic-acid-metabolism-in-human-liver-microsomes
#2
Yuka Kato, Yuji Mukai, Anders Rane, Nobuo Inotsume, Takaki Toda
Epoxyeicosatrienoic acids (EETs), metabolites of arachidonic acid (AA) via cytochrome P450s, have a protective effect on the cardiovascular system involving vasodilation. We have previously demonstrated that telmisartan (TEL) inhibits EETs production from AA in vitro. The objectives of the study were to examine the inhibitory effect of fluvastatin (FLU), an inhibitor of CYP2C9, and the combined effect of TEL and FLU on the production of EETs using human liver microsomes. The combined effect of TEL and FLU was evaluated using two methods, the fixed concentration method and the fixed ratio method...
September 21, 2017: Xenobiotica; the Fate of Foreign Compounds in Biological Systems
https://www.readbyqxmd.com/read/28933122/-hepatotoxicity-of-emodin-based-on-ugt1a1-enzyme-mediated-bilirubin-in-liver-microsomes
#3
Qi Wang, Zhong Dai, Yu-Jie Zhang, Shuang-Cheng Ma
To study the hepatotoxicity of emodin based on bilirubin metabolism mediated by glucuronidation of UGT1A1 enzyme. In this study, three different incubation systems were established by using RLM, HLM, and rUGT1A1, with bilirubin as the substrate. Different concentrations of bilirubin and emodin were added in the incubation systems. The double reciprocal Michaelis equation was drawn based on the total amount of bilirubin glucuronidation. The apparent inhibition constant Ki was then calculated with the slope curve to predict the hepatotoxicity...
December 2016: Zhongguo Zhong Yao za Zhi, Zhongguo Zhongyao Zazhi, China Journal of Chinese Materia Medica
https://www.readbyqxmd.com/read/28931913/cell-free-synthesis-of-functional-antibodies-using-a-coupled-in-vitro-transcription-translation-system-based-on-cho-cell-lysates
#4
M Stech, O Nikolaeva, L Thoring, W F M Stöcklein, D A Wüstenhagen, M Hust, S Dübel, S Kubick
Antibodies are indispensable tools for basic research as well as diagnostic and therapeutic applications. Consequently, the development of alternative manufacturing strategies which circumvent the hurdles connected to conventional antibody production technologies is of enormous interest. To address this issue, we demonstrate the synthesis of complex antibody formats, in particular immunoglobulin G (IgG) and single-chain variable fragment Fc fusion (scFv-Fc), in a microsome-containing cell-free system based on translationally active chinese hamster ovary (CHO) cell lysates...
September 20, 2017: Scientific Reports
https://www.readbyqxmd.com/read/28929453/effects-of-long-term-ingestion-of-white-tea-on-oxidation-produced-by-aging-and-acute-oxidative-damage-in-rats
#5
Cristóbal Espinosa Ruiz, Lorena Cabrera, José Ángel López-Jiménez, Salvador Zamora, Francisca Pérez-Llamas
The infusion tea extracted from the leaves of the plant Camellia sinensis can be used in the prevention of cancer, cardiovascular and neurodegenerative diseases, and aging, while adriamycin (ADR) is an anticancer drug that increases oxidative stress in cells. The present study evaluated the protective effect of the long-term consumption of white tea used at two different doses against the oxidative stress produced by aging and acute oxidation caused ADR treatment. At wearing, rats received distilled water (control), or 0...
September 19, 2017: Journal of Physiology and Biochemistry
https://www.readbyqxmd.com/read/28928235/testosterone-protects-high-fat-low-carbohydrate-diet-induced-non-alcoholic-fatty-liver-disease-in-castrated-male-rats-mainly-via-modulating-er-stress
#6
Yue Jia, Jennifer Kuang Yee, Christina Wang, Liana Nikolaenko, Maruja Diaz-Arjonilla, Joshua N Cohen, Samuel W French, Peter Y Liu, YanHe Lue, Wai-Nang Paul Lee, Ronald S Swerdloff
We previously showed that testosterone (T) deficiency enhanced high-fat diet (HFD) induced hepatic steatosis in rats that was independent of insulin resistance, and that T replacement reduced hepatic macrovesicular fat accumulation and inflammation. The present report explores the mechanism of T-protective effects on HFD-induced steatohepatitis. Adult male rats were randomized into four treatment groups for 15 weeks (intact rats on regular chow diet or HFD, and castrated rats on HFD with/without T replacement)...
September 19, 2017: American Journal of Physiology. Endocrinology and Metabolism
https://www.readbyqxmd.com/read/28927781/function-of-38-variants-cyp2c9-polymorphism-on-ketamine-metabolism-in%C3%A2-vitro
#7
Xiang Zheng, Ping Fang, Su-Su Bao, Dan Lin, Jian-Ping Cai, Guo-Xin Hu
BACKGROUND: Cytochrome P450 proteins (CYP 450) is the most important enzyme system of drug phase I metabolism in liver. In previous reports, reduced efficiency or increased risk of adverse events can be affected by primary sequence mutation in CYP450. AIM: To investigate the effect of gene polymorphism on the metabolism of ketamine in vitro, including the new alleles: 2C9*58, *59 and *60. METHOD: Incubation system which was contained insect microsome, b5, NADPH and 1M PBS incubated 10 μM-1000 μM ketamine in 37 °C for 40 min concentration of norketamine was analyzed by ultra-performance liquid chromatography-tandem mass spectrometry system (UPLC-MS/MS)...
September 1, 2017: Journal of Pharmacological Sciences
https://www.readbyqxmd.com/read/28925930/in-vitro-glucuronidation-of-wushanicaritin-by-liver-microsomes-intestine-microsomes-and-expressed-human-udp-glucuronosyltransferase-enzymes
#8
Xiaodan Hong, Yuanru Zheng, Zifei Qin, Baojian Wu, Yi Dai, Hao Gao, Zhihong Yao, Frank J Gonzalez, Xinsheng Yao
Wushanicaritin, a natural polyphenol compound, exerts many biological activities. This study aimed to characterize wushanicaritin glucuronidation by pooled human liver microsomes (HLM), human intestine microsomes and individual uridine diphosphate-glucuronosyltransferase (UGT) enzyme. Glucuronidation rates were determined by incubating wushanicaritin with uridine diphosphoglucuronic acid-supplemented microsomes. Kinetic parameters were derived by appropriate model fitting. Reaction phenotyping, the relative activity factor (RAF) and activity correlation analysis were performed to identify the main UGT isoforms...
September 19, 2017: International Journal of Molecular Sciences
https://www.readbyqxmd.com/read/28925748/the-effect-of-lomitapide-on-cardiovascular-outcome-measures-in-homozygous-familial-hypercholesterolemia-a-modelling-analysis
#9
Robert Leipold, Frederick Raal, Jack Ishak, Kees Hovingh, Helen Phillips
Background Patients with homozygous familial hypercholesterolemia are at high risk of cardiovascular disease due to high low-density lipoprotein (LDL)-cholesterol levels. Cardiovascular disease outcome studies are impossible to conduct, due to the rarity of homozygous familial hypercholesterolemia. We modelled the potential efficacy of lomitapide, a microsomal transfer protein inhibitor, on major adverse cardiovascular events (MACEs) and survival. Design We calculated the effect on cardiovascular outcomes of a 38% plasma LDL-cholesterol reduction induced by lomitapide...
January 1, 2017: European Journal of Preventive Cardiology
https://www.readbyqxmd.com/read/28924233/pharmacological-inhibition-of-camkk2-with-the-selective-antagonist-sto-609-regresses-nafld
#10
Brian York, Feng Li, Fumin Lin, Kathrina L Marcelo, Jianqiang Mao, Adam Dean, Naomi Gonzales, David Gooden, Suman Maity, Cristian Coarfa, Nagireddy Putluri, Anthony R Means
Binding of calcium to its intracellular receptor calmodulin (CaM) activates a family of Ca(2+)/CaM-dependent protein kinases. CaMKK2 (Ca(2+)/CaM-dependent protein kinase kinase 2) is a central member of this kinase family as it controls the actions of a CaMK cascade involving CaMKI, CaMKIV or AMPK. CaMKK2 controls insulin signaling, metabolic homeostasis, inflammation and cancer cell growth highlighting its potential as a therapeutic target for a variety of diseases. STO-609 is a selective, small molecule inhibitor of CaMKK2...
September 18, 2017: Scientific Reports
https://www.readbyqxmd.com/read/28923387/characterization-and-structure-activity-relationship-study-of-iminodipyridinopyrimidines-as-novel-hepatitis-c-virus-inhibitor
#11
Dong-Sik Park, Eunji Jo, Jihyun Choi, MyungEun Lee, Soohyun Kim, Hee-Young Kim, Jiyon Nam, Sujin Ahn, Jong Yeon Hwang, Marc Peter Windisch
Upon high-throughput screening of synthetic small molecule libraries with the infectious hepatitis C virus (HCV) cell culture system, we identified an iminodipyridinopyrimidine (IDPP) scaffold. IDPP did not inhibit HCV replication, but exhibited very potent inhibitory activity on early and late steps of HCV life cycle. Applying an intensive structure-activity relationship (SAR) study, a promising IDPP Lead compound (12c) with excellent potency (EC50 = 10 nM), high safety margin (SI > 2000), and an acceptable stability in human and rat liver microsomes (t1/2 >60 min) was identified...
September 6, 2017: European Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/28919359/human-intestine-and-liver-microsomal-metabolic-differences-between-c19-diester-and-monoester-diterpenoid-alkaloids-from-the-roots-of-aconitum-carmichaelii-debx
#12
Min Zhang, Chong-Sheng Peng, Xiao-Bo Li
The roots of Aconitum carmichaelii Debx. show excellent effects against rheumatism and cardiovascular diseases, but the effective compounds, C19-diester and monoester diterpenoid alkaloids (DDAs and MDAs) are toxic for their narrow therapeutic windows. It is noteworthy to investigate intestinal metabolism of these toxic compounds mainly by oral administration, because gut also express drug-metabolizing enzymes as well as liver. This study initially focused on phase I and phase II metabolism of DDAs (including aconitine, mesaconitine and hypaconitine) and MDAs (including benzoylaconine, benzoylmesaconine and benzoylhypaconine) in human intestine microsomes (HIM), with comparison of metabolism in human liver microsomes (HLM)...
September 14, 2017: Toxicology in Vitro: An International Journal Published in Association with BIBRA
https://www.readbyqxmd.com/read/28916746/high-yield-production-of-difficult-to-express-proteins-in-a-continuous-exchange-cell-free-system-based-on-cho-cell-lysates
#13
Lena Thoring, Srujan K Dondapati, Marlitt Stech, Doreen A Wüstenhagen, Stefan Kubick
Cell-free protein synthesis (CFPS) represents a promising technology for efficient protein production targeting especially so called "difficult-to-express" proteins whose synthesis is challenging in conventional in vivo protein production platforms. Chinese hamster ovary (CHO) cells are one of the most prominent and safety approved cell lines for industrial protein production. In this study we demonstrated the ability to produce high yields of various protein types including membrane proteins and single chain variable fragments (scFv) in a continuous exchange cell-free (CECF) system based on CHO cell lysate that contains endogenous microsomal structures...
September 15, 2017: Scientific Reports
https://www.readbyqxmd.com/read/28912253/physiologically-based-pharmacokinetic-model-predictions-of-panobinostat-lbh589-as-a-victim-and-perpetrator-of-drug-drug-interactions
#14
Heidi J Einolf, Wen Lin, Christina S Won, Lai Wang, Helen Gu, Dung Yu Chun, Handan He, James B Mangold
Panobinostat (Farydak®) is an orally active hydroxamic acid derived histone deacetylase inhibitor for the treatment of relapsed/refractory multiple myeloma. Based upon recombinant cytochrome P450 (CYP) kinetic analyses in vitro, panobinostat oxidative metabolism in human liver microsomes was found to be primarily mediated by CYP3A4 with lower contributions by CYP2D6 and CYP2C19. Panobinostat was also shown to be an in vitro reversible and time-dependent inhibitor of CYP3A4/5, and a reversible inhibitor of CYP2D6 and CYP2C19...
September 14, 2017: Drug Metabolism and Disposition: the Biological Fate of Chemicals
https://www.readbyqxmd.com/read/28911605/7-n-acetylcysteine-pyrrole-conjugate-a-potent-dna-reactive-metabolite-of-pyrrolizidine-alkaloids
#15
Xiaobo He, Liang Ma, Qingsu Xia, Peter P Fu
Plants containing pyrrolizidine alkaloids (PAs) are widespread throughout the world and are the most common poisonous plants affecting livestock, wildlife, and humans. PAs require metabolic activation to form reactive dehydropyrrolizidine alkaloids (dehydro-PAs) that are capable of alkylating cellular DNA and proteins, form (±)-6,7-dihydro-7-hydroxy-1-hydroxymethyl-5H-pyrrolizine (DHP)-DNA and DHP-protein adducts, and lead to cytotoxicity, genotoxicity, and tumorigenicity. In this study, we determined that the metabolism of riddelliine and monocrotaline by human and rat liver microsomes in the presence of N-acetylcysteine both produced 7-N-acetylcysteine-DHP (7-NAC-DHP) and DHP...
October 2016: Journal of Food and Drug Analysis
https://www.readbyqxmd.com/read/28904078/towards-a-systems-approach-to-human-cytochrome-p450-ensemble-interactions-between-cyp2d6-and-cyp2e1-and-their-functional-consequences
#16
Dmitri R Davydov, Nadezhda Y Davydova, John T Rodgers, Thomas H Rushmore, Jeffrey P Jones
Functional cross-talk among human drug-metabolizing cytochromes P450 through their association is a topic of emerging importance. Here we studied the interactions of human CYP2D6, a major metabolizer of psychoactive drugs, with one of the most prevalent human P450 enzymes, ethanol-inducible CYP2E1. Detection of P450-P450 interactions was accomplished through luminescence resonance energy transfer (LRET) between labeled proteins incorporated into human liver microsomes and the microsomes of insect cells containing NADPH-cytochrome P450 reductase...
September 13, 2017: Biochemical Journal
https://www.readbyqxmd.com/read/28903608/influence-of-substrates-on-the-in-vitro-kinetics-of-steviol-glucuronidation-and-interaction-between-steviol-glycosides-metabolites-and-ugt2b7
#17
Jun-Ming Chen, Yong-Mei Xia, Yan-Dong Zhang, Tong-Tong Zhang, Qing-Rui Peng, Yun Fang
Steviol glycosides, a natural sweetener, may perform bioactivities via steviol, their main metabolite in human digestion. The metabolising kinetics, i.e. glucuronidation kinetics and interaction between steviol glycosides or their metabolites and metabolising enzyme, are important for understanding the bioactivity and cytotoxicity. The present study investigated kinetics of steviol glucuronidation in human liver microsome and a recombinant human UDP-glucuronosyltransferases isomer, UGT2B7, along with molecular docking to analyse interaction between UGT2B7 and steviol or glucose...
September 13, 2017: International Journal of Food Sciences and Nutrition
https://www.readbyqxmd.com/read/28893990/cd1d-restricted-pathways-in-hepatocytes-control-local-natural-killer-t-cell-homeostasis-and-hepatic-inflammation
#18
Sebastian Zeissig, Kenneth Peuker, Shankar Iyer, Thomas Gensollen, Stephanie K Dougan, Torsten Olszak, Arthur Kaser, Richard S Blumberg
Invariant natural killer T (iNKT) cells recognize lipid antigens presented by CD1d and play a central role in regulating immunity and inflammation in peripheral tissues. However, the mechanisms which govern iNKT cell homeostasis after thymic emigration are incompletely understood. Here we demonstrate that microsomal triglyceride transfer protein (MTP), a protein involved in the transfer of lipids onto CD1d, regulates liver iNKT cell homeostasis in a manner dependent on hepatocyte CD1d. Mice with hepatocyte-specific loss of MTP exhibit defects in the function of CD1d and show increased hepatic iNKT cell numbers as a consequence of altered iNKT cell apoptosis...
September 11, 2017: Proceedings of the National Academy of Sciences of the United States of America
https://www.readbyqxmd.com/read/28893642/enzyme-inducing-effects-of-berberine-on-cytochrome-p450-1a2-in-vitro-and-in-vivo
#19
Bo Jiang, Liyuan Meng, Feng Zhang, Xiaoling Jin, Guiliang Zhang
AIMS: Berberine (BER) is an important anti-bacterial drug from Chinese herbal medicine and a novel drug candidate for preclinical development in recent years. Here we provide evidence that the effects of berberine on cytochrome P450 (CYP) 1A2 in vitro and in vivo. MAIN METHODS: Real-time polymerase chain reaction and western blotting analysis were employed to evaluate the CYP1A2 mRNA levels and protein expression. The enzyme activity was assessed by the metabolic rate of phenacetin to acetaminophen by LC-MS/MS method...
September 8, 2017: Life Sciences
https://www.readbyqxmd.com/read/28892748/microsomal-glutathione-transferase-2-modulates-ltc4-synthesis-and-ros-production-in-apostichopus-japonicus
#20
Zhen Zhang, Zhimeng Lv, Zhixin Wei, Chenghua Li, Yina Shao, Weiwei Zhang, Xuelin Zhao, Jinbo Xiong
Microsomal glutathione transferase 2 (mGST2) is an integral membrane protein involved in detoxication of xenobiotics, and has also been suggested to catalyze the biosynthesis of pro-inflammatory mediator leukotriene C4 (LTC4) as homologous to LTC4 synthase (LTC4S) in mammals. In the present study, a novel mGST2 homology was identified from Apostichopus japonicus (designated as AjmGST2) by RACE approaches. The full-length cDNA of AjmGST2 was of 1917bp encoding a polypeptide of 161 amino acids residues. Multiple sequences alignment and phylogenetic analysis together supported that AjmGST2 belonged to a new member in invertebrate mGSTs family and close to mammalian LTC4S...
September 8, 2017: Molecular Immunology
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