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Cyp450

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https://www.readbyqxmd.com/read/29027195/tspyl-family-regulates-cyp17a1-and-cyp3a4-expression-potential-mechanism-contributing-to-abiraterone-response-in-metastatic-castration-resistant-prostate-cancer
#1
Sisi Qin, Duan Liu, Manish Kohli, Liguo Wang, Peter T Vedell, David W Hillman, Nifang Niu, Jia Yu, Richard M Weinshilboum, Liewei Wang
The testis-specific Y-encoded-like protein (TSPYL) gene family includes TSPYL1 to TSPYL6. We previously reported that TSPYL5 regulates cytochrome P450 (CYP) 19A1 expression. Here, we show that TSPYLs, especially, TSPYL 1, 2 and 4, can regulate the expression of many CYP genes, including CYP17A1, a key enzyme in androgen biosynthesis, and CYP3A4, an enzyme that catalyzes the metabolism of abiraterone, a CYP17 inhibitor. Furthermore, a common TSPYL1 SNP, rs3828743 (G/A) (Pro62Ser), abolishes TSPYL1's ability to suppress CYP3A4 expression, resulting in reduced abiraterone concentrations and increased cell proliferation...
October 13, 2017: Clinical Pharmacology and Therapeutics
https://www.readbyqxmd.com/read/29023376/altered-protein-expression-of-cardiac-cyp2j-and-hepatic-cyp2c-cyp4a-and-cyp4f-in-a-mouse-model-of-type-ii-diabetes-a-link-in-the-onset-and-development-of-cardiovascular-disease
#2
Benoit Drolet, Sylvie Pilote, Carolanne Gélinas, Alida-Douce Kamaliza, Audrey Blais-Boilard, Jessica Virgili, Dany Patoine, Chantale Simard
Arachidonic acid can be metabolized by cytochrome P450 (CYP450) enzymes in a tissue- and cell-specific manner to generate vasoactive products such as epoxyeicosatrienoic acids (EETs-cardioprotective) and hydroxyeicosatetraenoic acids (HETEs-cardiotoxic). Type II diabetes is a well-recognized risk factor for developing cardiovascular disease. A mouse model of Type II diabetes (C57BLKS/J-db/db) was used. After sacrifice, livers and hearts were collected, washed, and snap frozen. Total proteins were extracted...
October 12, 2017: Pharmaceutics
https://www.readbyqxmd.com/read/28969895/three-dimensional-hydrogel-culture-conditions-promote-the-differentiation-of-human-induced-pluripotent-stem-cells-into-hepatocytes
#3
Ying Luo, Cheng Lou, Sui Zhang, Zhengyan Zhu, Qianzhe Xing, Peng Wang, Tong Liu, Hui Liu, Chenglong Li, Wenxia Shi, Zhi Du, Yingtang Gao
BACKGROUND AIMS: Human induced pluripotent stem cells (hiPSCs) are becoming increasingly popular in research endeavors due to their potential for clinical application; however, such application is challenging due to limitations such as inferior function and low induction efficiency. In this study, we aimed to establish a three-dimensional (3D) culture condition to mimic the environment in which hepatogenesis occurs in vivo to enhance the differentiation of hiPSCs for large-scale culture and high throughput BAL application...
September 29, 2017: Cytotherapy
https://www.readbyqxmd.com/read/28968937/lipid-metabolism-and-pro-oxidant-antioxidant-balance-of-halamphora-oceanica-from-the-gulf-of-mexico-exposed-to-water-accommodated-fraction-of-maya-crude-oil
#4
Hugo F Olivares-Rubio, Lucía Salazar-Coria, Minerva Nájera-Martínez, José Luis Godínez-Ortega, Armando Vega-López
Diatoms play key roles in primary production and carbon fixation at a global scale and in some cases these species live on marine ecosystems impacted by crude oil (CO) spills. Halamphora oceanica, a new diatom species from the Southwest of the Gulf of Mexico was isolated and cultured in the laboratory and was exposed to water accommodated fraction (WAF) of different Maya CO loads at 0.01, 0.1, 1 and 10g/L by 96h. A battery of biomarkers involved in oxidative stress (O2•, H2O2, TBARS, ROOH, RC=O, SOD, CAT, GPx), biotransformation and conjugation (total CYP450 activity and GST) moreover fatty acid (FA) metabolism (FA levels, fatty-acid synthase and acyl-CoA oxidase) were measured...
September 27, 2017: Ecotoxicology and Environmental Safety
https://www.readbyqxmd.com/read/28967508/interactive-effects-of-nutrition-reproductive-state-and-pollution-on-molecular-stress-responses-of-mussels-mytilus-galloprovincialis-lamarck-1819
#5
Carmen González-Fernández, Marina Albentosa, Inna Sokolova
Marine bivalves including mussels Mytilus galloprovincialis are commonly used as sentinels for pollution monitoring and ecosystem health assessment in the coastal zones. Use of biomarkers to assess the pollution effects assumes that the effects of pollutants on the biomarkers exceed the natural background variability; yet this assumption has rarely been tested. We exposed mussels at different reproductive stages and nutritive states to two concentrations of a polycyclic aromatic hydrocarbon (fluoranthene, 3 and 60 μg L(-1)) for three weeks...
September 14, 2017: Marine Environmental Research
https://www.readbyqxmd.com/read/28960974/a-chemoproteomic-platform-to-assess-bioactivation-potential-of-drugs
#6
Rui Sun, Fuguo Shi, Keke Liu, Ling Fu, Caiping Tian, Yong Yang, Keri A Tallman, Ned A Porter, Jing Yang
Reactive metabolites (RM) formed from bioactivation of drugs can covalently modify liver proteins and cause mechanism-based inactivation of major cytochrome P450 (CYP450) enzymes. Risk of bioactivation of a test compound is routinely examined as part of lead optimization efforts in drug discovery. Here we described a chemoproteomic platform to assess in vitro and in vivo bioactivation potential of drugs. This platform enabled us to determine reactivity of thousands of proteomic cysteines toward RMs of diclofenac formed in human liver microsomes and living animals...
October 6, 2017: Chemical Research in Toxicology
https://www.readbyqxmd.com/read/28960401/prediction-of-drug-drug-interactions-using-physiologically-based-pharmacokinetic-models-of-cyp450-modulators-included-in-simcyp-software
#7
Niloufar Marsousi, Jules A Desmeules, Serge Rudaz, Youssef Daali
In recent years, Physiologically-Based PharmacoKinetic (PBPK) modeling has received growing interest as a useful tool for assessment of drug PK. It has demonstrated to be informative and helpful to quantify the modification in drug exposure due to specific physio-pathological conditions, age, genetic polymorphisms, ethnicity and particularly drug-drug interactions (DDIs). In this paper, the prediction success of DDIs involving various cytochrome P450 isoenzyme (CYP) modulators namely ketoconazole (a competitive inhibitor of CYP3A), itraconazole (a competitive inhibitor of CYP3A), clarithromycin (a mechanism-based inhibitor of CYP3A), quinidine (a competitive inhibitor of CYP2D6), paroxetine (a mechanism-based inhibitor of CYP2D6), ciprofloxacin (a competitive inhibitor of CYP1A2), fluconazole (a competitive inhibitor of CYP2C9/2C19) and rifampicin (an inducer of CYP3A) were assessed using Simcyp® software...
September 28, 2017: Biopharmaceutics & Drug Disposition
https://www.readbyqxmd.com/read/28958841/effects-of-dronedarone-amiodarone-and-their-active-metabolites-on-sequential-metabolism-of-arachidonic-acid-to-epoxyeicosatrienoic-and-dihydroxyeicosatrienoic-acids
#8
Aneesh Karkhanis, Nhan Dai Thien Tram, Eric Chun Yong Chan
Cardiac enzymes such as cytochrome P450 2J2 (CYP2J2) metabolize arachidonic acid (AA) to cardioprotective epoxyeicosatrienoic acids (EETs), which in turn are metabolized by soluble epoxide hydrolase (sEH) to dihydroxyeicosatrienoic acids (DHETs). As EETs and less potent DHETs exhibit cardioprotective and vasoprotective functions, optimum levels of cardiac EETs are paramount in cardiac homeostasis. Previously, we demonstrated that dronedarone, amiodarone and their main metabolites, namely N-desbutyldronedarone (NDBD) and N-desethylamiodarone (NDEA), potently inhibit human cardiac CYP2J2-mediated astemizole metabolism in vitro...
September 25, 2017: Biochemical Pharmacology
https://www.readbyqxmd.com/read/28954402/tissue-specific-modulation-of-cyp2c-and-cyp3a-mrna-levels-and-activities-by-diet-induced-obesity-in-mice-the-impact-of-type-2-diabetes-on-drug-metabolizing-enzymes-in-liver-and-extra-hepatic-tissues
#9
Sarah Maximos, Michel Chamoun, Sophie Gravel, Jacques Turgeon, Veronique Michaud
Various diseases such as type 2 diabetes (T2D) may alter drug clearance. The objective of this study was to evaluate the effects of T2D on CYP450 expressions and activities using high-fat diet (HFD) as a model of obesity-dependent diabetes in C57BL6 mice. The cyp450 mRNA expression levels for 15 different isoforms were determined in the liver and extra-hepatic tissues (kidneys, lungs and heart) of HFD-treated animals (n = 45). Modulation of cyp450 metabolic activities by HFD was assessed using eight known substrates for specific human ortholog CYP450 isoforms: in vitro incubations were conducted with liver and extra-hepatic microsomes...
September 26, 2017: Pharmaceutics
https://www.readbyqxmd.com/read/28952270/-effect-of-clinical-doses-of-realgar-indigo-naturalis-formula-and-large-dose-of-realgar-on-cyp450s-of-rat-liver
#10
Huan-Hua Xu, Mei-Xi Wang, Hong-Ling Tan, Yu-Guang Wang, Xiang-Lin Tang, Cheng-Rong Xiao, Hua Li, Yue Gao, Zeng-Chun Ma
To investigate the effect of clinical dose of Realgar-Indigo Naturais formula (RIF) and large-dose of Realgar on main drug-metabolizing enzymes CYP450s of rat liver, as well as its regulatory effect on mRNA expression. Wistar rats were administrated orally with tested drugs for 14 days. A Cocktail method combined with HPLC-MS/MS was used in the determination of 4 cytochrome P450 isozymes (CYP1A2, CYP2B, CYP3A and CYP2C) in liver of the rats, and the mRNA expression levels of the above subtypes were detected by real-time fluorescent quantitative PCR...
February 2017: Zhongguo Zhong Yao za Zhi, Zhongguo Zhongyao Zazhi, China Journal of Chinese Materia Medica
https://www.readbyqxmd.com/read/28949811/characterization-of-maternal-and-fetal-cyp3a-mediated-progesterone-metabolism
#11
Sara K Quinney, Tara Benjamin, Xiaomei Zheng, Avinash S Patil
INTRODUCTION: Progesterone is critical for maintaining pregnancy and onset of labor. We evaluated CYP450-mediated progesterone meta-bolism, specifically the contribution of CYP3A isoforms. MATERIALS AND METHODS: In vitro progesterone metabolism was characterized in human liver microsomes (HLMs) with and without selective cytochrome P450 inhibitors and in recombinant CYP3A4, CYP3A5, and CYP3A7. 6β-hydroxyprogesterone (6β-OHP) and 16α-hydroxyprogesterone (16α-OHP) metabolites were quantified by HPLC/UV and fit to the Michaelis-Menten equation to determine Km and Vmax...
September 26, 2017: Fetal and Pediatric Pathology
https://www.readbyqxmd.com/read/28948743/-effect-of-processed-polygonum-multiflorum-on-mrna-expression-level-of-five-subtypes-of-cyp450-enzymes-in-rat-liver
#12
Chun-Lian Huang, Xue-Mei Fan, Qian Li, Yi-Ming Wang, Shu-Mei Wang, Meng-Juan Gong, Guo-An Luo
To observe the effect of processed Polygonum multiflorum on mRNA expression levels of five subtypes of CYP450 enzymes in rat liver. SD rats were randomly divided into the normal control group, processed P. multiflorum high dose and low dose groups (5.40 g•kg⁻¹ and 1.08 g•kg⁻¹). The rats in administration groups were continuously given with processed P. mutiflorum for 7 days by ig administration, and the rats in normal control group were given with the same volume of distilled water. After successive administration of 7 days, the serum biochemical indications were detected, and Real-time quantitative PCR technology was used to detect the mRNA expression levels of five subtypes of CYP450 enzymes in rat liver...
January 2017: Zhongguo Zhong Yao za Zhi, Zhongguo Zhongyao Zazhi, China Journal of Chinese Materia Medica
https://www.readbyqxmd.com/read/28945086/oleanolic-acid-mediated-inhibition-of-pregnane-x-receptor-and-constitutive-androstane-receptor-attenuates-rifampin-isoniazid-cytotoxicity
#13
Yen-Ning Lin, Chao-Jung Chen, Hsiao-Yun Chang, Wai-Kok Cheng, Ying-Ray Lee, Jih-Jung Chen, Yun-Ping Lim
Interactions between transcriptional inducers of cytochrome P450 (CYP450) and pharmacological agents might decrease drug efficacy and induce side effects. Such interactions could be prevented using an antagonist of the pregnane X receptor (PXR) and constitutive androstane receptor (CAR). Here, we aimed to determine the antagonistic effect of oleanolic acid (OA) on PXR and CAR. OA attenuated the promoter activities, expressions, and enzyme catalytic activities of CYP3A4 and CYP2B6 mediated by rifampin (RIF) and CITCO...
September 25, 2017: Journal of Agricultural and Food Chemistry
https://www.readbyqxmd.com/read/28942133/bush-mint-hyptis-suaveolens-and-spreading-hogweed-boerhavia-diffusa-medicinal-plant-extracts-differentially-affect-activities-of-cyp1a2-cyp2d6-and-cyp3a4-enzymes
#14
Nicholas Ekow Thomford, Kevin Dzobo, Faustina Adu, Shadreck Chirikure, Ambroise Wonkam, Collet Dandara
ETHNO-PHARMACOLOGICAL RELEVANCE: Hyptis suaveolens (L) Poit and Boerhavia diffusa Linn are medicinal herbal plants commonly found in the tropics and sub-tropics. They are used to treat various conditions among them boils, dyslipidaemia, eczema, malaria, jaundice and gonorrhoea. Thus, the herbal medicinal extracts are now found as part of some commercial herbal formulations. There has not been adequate characterization of these medicinal herbs on their effects on drug metabolising enzymes...
September 21, 2017: Journal of Ethnopharmacology
https://www.readbyqxmd.com/read/28940693/hyperbaric-oxygenation-and-20-hete-inhibition-reduce-stroke-volume-in-female-diabetic-sprague-dawley-rats
#15
Mihael Mišir, Marija Renić, Sanja Novak, Martina Mihalj, Anita Ćosić, Monika Vesel, Ines Drenjančević
We evaluated the effects of acute and repetitive hyperbaric oxygenation (HBO2 ), 20-HETE inhibition by N-hydroxy-N'-(4-butyl-2methylphenyl)-formamidine (HET0016) and their combinations on experimental stroke outcomes. Streptozotocin-induced type-1 diabetic Sprague-Dawley female rats (N = 42, N = 7/group), were subjected to 30' transient middle cerebral artery occlusion (t-MCAO) / reperfusion and divided in following groups; (a) Control group, without treatment; and groups exposed to: (b) HBO2 ; (c) multiple HBO2 (HBO2 immediately and second exposure 12 h after t-MCAO); (d) HET0016 pretreatment (1 mg kg(-1) /3 days prior to t-MCAO) combined with HBO2 after t-MCAO; (e) HET0016 treatment (1 h before, during and for 6 hours after t-MCAO); and (f) HET0016 treatment followed by HBO2 after t-MCAO...
September 21, 2017: Experimental Physiology
https://www.readbyqxmd.com/read/28936835/-progress-on-studies-of-impact-on-cyp450-enzymes-activity-of-traditional-chinese-medicine-by-cocktail-probe-substrates-approach
#16
REVIEW
Xi Du, Xin He, Yu-Hong Huang, Zi-Qiang Li
Cocktail probe substrates approach is a fast, sensitive and high through put method to determine cytochrome P450 enzymes activity. It has been widely used to screen early drug development, analyze drug metabolism types and confirm the metabolism pathways, study drug-drug interactions, optimize clinical regimen, evaluate post marketing drugs and help liver/kidney pathological studies. This article reviewed characteristics of Cocktail probe substrates, focused on the application to traditional Chinese medicine to CYP450 system as follows: the metabolic pathway research of Chinese herb active ingredients; processing way and compatibility of medical herbs affect CYP450; find out the metabolic characteristic of Chinese patent medicine, study in pharmacy of national minority; do research in liver protective effect of traditional Chinese medicine and evaluate traditional Chinese medicine syndromes in animal models...
December 2016: Zhongguo Zhong Yao za Zhi, Zhongguo Zhongyao Zazhi, China Journal of Chinese Materia Medica
https://www.readbyqxmd.com/read/28934216/genetic-polymorphisms-of-cytochrome-p450-1a2-cyp1a2-among-emiratis
#17
Mohammad M Al-Ahmad, Naheed Amir, Subramanian Dhanasekaran, Anne John, Yousef M Abdulrazzaq, Bassam R Ali, Salim M A Bastaki
Cytochrome P450 1A2 (CYP1A2) is one of the CYP450 mixed-function oxidase system that is of clinical importance due to the large number of drug interactions associated with its induction and inhibition. In addition, significant inter-individual differences in the elimination of drugs metabolized by CYP1A2 enzyme have been observed which are largely due to the highly polymorphic nature of CYP1A2 gene. However, there are limited studies on CYP1A2 phenotypes and CYP1A2 genotypes among Emiratis and thus this study was carried out to fill this gap...
2017: PloS One
https://www.readbyqxmd.com/read/28927781/function-of-38-variants-cyp2c9-polymorphism-on-ketamine-metabolism-in%C3%A2-vitro
#18
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/28924501/identification-and-analysis-of-cyp450-genes-from-transcriptome-of-lonicera-japonica-and-expression-analysis-of-chlorogenic-acid-biosynthesis-related-cyp450s
#19
Xiwu Qi, Xu Yu, Daohua Xu, Hailing Fang, Ke Dong, Weilin Li, Chengyuan Liang
BACKGROUND: Lonicera japonica is an important medicinal plant that has been widely used in traditional Chinese medicine for thousands of years. The pharmacological activities of L. japonica are mainly due to its rich natural active ingredients, most of which are secondary metabolites. CYP450s are a large, complex, and widespread superfamily of proteins that participate in many endogenous and exogenous metabolic reactions, especially secondary metabolism. Here, we identified CYP450s in L...
2017: PeerJ
https://www.readbyqxmd.com/read/28920579/point-of-care-companion-diagnostic-tests-for-personalizing-psychiatric-medications-fulfilling-an-unmet-clinical-need
#20
Anil S Modak
Over the last decade stable isotope labeled substrates have been used as probes for rapid, point of care, non invasive and user friendly phenotype breath tests to evaluate activity of drug metabolizing enzymes. These diagnostic breath tests can be potentially used as Companion diagnostics (CDx) by physicians to personalize medications especially psychiatric drugs with narrow therapeutic windows, to monitor the progress of disease severity, medication efficacy and to study in vivo the pharmacokinetics of xenobiotics, Several genotype tests have been approved by the FDA over the last 15 years, however, they have not been cleared for use in personalizing medications since they fall woefully short in identifying all non responders to drugs especially for the CYP450 enzymes...
September 18, 2017: Journal of Breath Research
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