keyword
MENU ▼
Read by QxMD icon Read
search

cyp

keyword
https://www.readbyqxmd.com/read/29040392/%C3%AE-cypermethrin-and-its-metabolite-3-phenoxybenzoic-acid-exhibit-immunotoxicity-in-murine-macrophages
#1
Xia Wang, Bingnan He, Baida Kong, Lai Wei, Rong Wang, Chenqian Zhou, Yiyan Shao, Jiajia Lin, Yuanxiang Jin, Zhengwei Fu
β-Cypermethrin (β-CYP), one of most important pyrethroids, is widely used to control insects, and has been detected in organisms, including human. Pyrethroids have been shown to pose neurotoxicity, hepatotoxicity, endocrine disruption and reproductive risks in mammals. However, research in immunotoxicity of pyrethroids, especially their metabolites, is limited. A common metabolite of pyrethroids is 3-phenoxybenzoic acid (3-PBA) in mammals. Thus, in this study, we evaluated the immunotoxicity of β-CYP and 3-PBA in mouse macrophages, RAW 264...
October 11, 2017: Acta Biochimica et Biophysica Sinica
https://www.readbyqxmd.com/read/29035734/comparison-of-constitutive-and-thiabendazole-induced-expression-of-five-cytochrome-p450-genes-in-fourth-stage-larvae-of-haemonchus-contortus-isolates-with-different-drug-susceptibility-identifies-one-gene-with-high-constitutive-expression-in-a-multi-resistant
#2
Esra Yilmaz, Sabrina Ramünke, Janina Demeler, Jürgen Krücken
Benzimidazoles (BZs) remain amongst the most widely used anthelmintic drug classes against gastro-intestinal nematode infections, although their efficacy is increasingly compromised by resistance. The primary underlying mechanisms for BZ resistance are single-nucleotide polymorphisms (SNPs) in the isotype 1 β-tubulin gene causing the substitutions F167Y, E198A or F200Y. However, resistance is believed to be multi-genic and previous studies have shown that isolates carrying 90-100% F200Y can vary considerably in their resistance level in the egg hatch assay (EHA)...
October 7, 2017: International Journal for Parasitology, Drugs and Drug Resistance
https://www.readbyqxmd.com/read/29035537/discovery-of-a-novel-piperidine-based-inhibitor-of-cholesteryl-ester-transfer-protein-cetp-that-retains-activity-in-hypertriglyceridemic-plasma
#3
Ken Yamada, Margaret Brousseau, Wataru Honma, Akiko Iimura, Hidetomo Imase, Yuki Iwaki, Toshio Kawanami, Daniel LaSala, Guiqing Liang, Hironobu Mitani, Kazuhiko Nonomura, Osamu Ohmori, Meihui Pan, Dean F Rigel, Ichiro Umemura, Kayo Yasoshima, Guoming Zhu, Muneto Mogi
Herein we describe the discovery and characterization of a novel, piperidine-based inhibitor of cholesteryl ester transfer protein (CETP) with a core structure distinct from other reported CETP inhibitors. A versatile synthesis starting from 4-methoxypyridine enabled an efficient exploration of the SAR, giving a lead molecule with potent CETP inhibition in human plasma. The subsequent optimization focused on improvement of pharmacokinetics and mitigation of off-target liabilities, such as CYP inhibition, whose improvement correlated with increased lipophilic efficiency...
October 16, 2017: Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/29030652/evidence-for-a-complex-formation-between-cyp2j5-and-meh-in-living-cells-by-fret-analysis-of-membrane-protein-interaction-in-the-endoplasmic-reticulum-fampir
#4
Anette Carolina Orjuela Leon, Anne Marwosky, Michael Arand
The potential complex formation between microsomal epoxide hydrolase (mEH) and cytochrome P450-dependent monooxygenase (CYP) has been a subject of research for many decades. Such an association would enable efficient substrate channeling between CYP and mEH and as such represent an attractive strategy to prevent deleterious accumulation of harmful metabolic by-products such as CYP-generated epoxide intermediates. However, such complex formation is experimentally difficult to prove, because CYP and mEH are membrane-bound proteins that are prone to unspecific aggregation after solubilization...
October 13, 2017: Archives of Toxicology
https://www.readbyqxmd.com/read/29030272/impact-of-fasting-followed-by-short-term-exposure-to-interleukin-6-on-cytochrome-p450-mrna-in-mice
#5
Martin Krøyer Rasmussen, Lærke Bertholdt, Anders Gudiksen, Henriette Pilegaard, Jakob G Knudsen
mRNA expression of the cytochrome P450 (CYP) enzyme family is regulated by numerous factors. Fasting has been shown to induce increased hepatic CYP mRNA in both humans and animals. However, the coordinated regulation of CYP, CYP-regulating transcription factors, and transcriptional co-factors in the liver linking energy metabolism to detoxification has never been investigated. Interleukin-6 (IL-6) has been suggested to be released during fasting and has been shown to regulate CYP expression. The present study investigated the mRNA content of selected CYP, AhR, CAR, PXR and PPARα in mice fasted for 18hours and subsequently exposed to IL-6...
October 10, 2017: Toxicology Letters
https://www.readbyqxmd.com/read/29027939/nicotine-component-of-cigarette-smoke-extract-cse-decreases-the-cytotoxicity-of-cse-in-beas-2b-cells-stably-expressing-human-cytochrome-p450-2a13
#6
Minghui Ji, Yudong Zhang, Na Li, Chao Wang, Rong Xia, Zhan Zhang, Shou-Lin Wang
Cytochrome P450 2A13 (CYP2A13), an extrahepatic enzyme mainly expressed in the human respiratory system, has been reported to mediate the metabolism and toxicity of cigarette smoke. We previously found that nicotine inhibited 4-(methylnitrosamino)-1-(3-pyridyl)-1-butanone (NNK) metabolism by CYP2A13, but its influence on other components of cigarette smoke remains unclear. The nicotine component of cigarette smoke extract (CSE) was separated, purified, and identified using high-performance liquid chromatography (HPLC) and ultra-performance liquid chromatography tandem mass spectrometry (UPLC-MS/MS), splitting CSE into a nicotine section (CSE-N) and nicotine-free section (CSE-O)...
October 13, 2017: International Journal of Environmental Research and Public Health
https://www.readbyqxmd.com/read/29027845/the-potent-mechanism-based-inactivation-of-cyp2d6-and-cyp3a4-with-fusidic-acid-in-in-vivo-bioaccumulation
#7
Xiu-Xian Lin, Guang-Hui Lian, Ying Xu, Qing Zhao, Jian Xiao, Shi-Fang Peng, Mei-Fang Xiao, Dong-Sheng Ouyang, Zhi-Rong Tan, Yi-Cheng Wang, Jing-Bo Peng, Wei Zhang, Yao Chen
1. The accumulation of fusidic acid (FA) after multiple doses of FA has been reported on in previous studies but the related mechanisms have not been clarified fully. In the present study, we explain the mechanisms related to the mechanism-based inactivation of CYP2D6 and CYP3A4. 2. The irreversible inhibitory effects of FA on CYP2D6 and CYP3A4 were examined via a series of experiments, including: a) time-, concentration- and NADPH-dependent inactivation, b) substrate protection in enzyme inactivation and c) partition ratio with recombinant human CYP enzymes...
October 13, 2017: Xenobiotica; the Fate of Foreign Compounds in Biological Systems
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
#8
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/29027194/predictive-performance-of-physiologically-based-pharmacokinetic-pbpk-modeling-of-drugs-extensively-metabolized-by-major-cytochrome-p450s-in-children
#9
Wangda Zhou, Trevor N Johnson, Khanh H Bui, S Y Amy Cheung, Jianguo Li, Hongmei Xu, Nidal Al-Huniti, Diansong Zhou
The accuracy of physiologically-based pharmacokinetic (PBPK) model prediction in children, especially those younger than 2 years old has not been systematically evaluated. The aim of this study was to characterize the pediatric predictive performance of the PBPK approach for ten drugs extensively metabolized by CYP1A2 (theophylline), CYP2C8 (desloratidine, montelukast), CYP2C9 (diclofenac), CYP2C19 (esomeprazole, lansoprazole), CYP2D6 (tramadol) and CYP3A4 (itraconazole, ondansetron, sufentanil). Model performance in children was evaluated by comparing simulated plasma concentration-time profiles with observed clinical results for each drug and age group...
October 13, 2017: Clinical Pharmacology and Therapeutics
https://www.readbyqxmd.com/read/29025271/psychotropic-drugs-and-cyp2d6-in-late-life-psychiatric-and-neurological-disorders-what-do-we-know
#10
Davide Seripa, Madia Lozupone, Eleonora Stella, Giulia Paroni, Paola Bisceglia, Maddalena La Montagna, Grazia D'onofrio, Carolina Gravina, Maria Urbano, Maria Giovanna Priore, Angela Lamanna, Antonio Daniele, Antonello Bellomo, Giancarlo Logroscino, Antonio Greco, Francesco Panza
Late-life psychiatric and neurological disorders (LLPND) are interesting models to understand the potential role of pharmacogenetics in drug management, since several pharmacological approaches for treating LLPND have proven to be ineffective or deleterious, thus resulting in therapeutic failures (TF) and adverse drug reactions (ADR). Common variants in the genes encoding the cytochrome P450 (CYP) enzyme system, the 'engine room' of drug metabolism, together with well-known age-related increased polypharmacy also contributed to the prevalence of TF and ADR observed in these patients, also rising number and time of hospital readmissions and rate of institutionalizations...
October 12, 2017: Expert Opinion on Drug Safety
https://www.readbyqxmd.com/read/29024742/cyp-mediated-drug-metabolism-in-the-brain-impacts-drug-response
#11
REVIEW
Douglas M McMillan, Rachel F Tyndale
The functional role of cytochrome P450 (CYP) enzymes in the brain is an exciting and evolving field of research. CYPs are present and active in the brain, with heterogeneous patterns of expression, activity, and sensitivity to modulation across cell types, regions, and species. Despite total brain CYP expression being a fraction of hepatic CYP expression, the expanding literature of in vitro and in vivo experiments have provided evidence that brain CYPs can impact acute and chronic drug response, susceptibility to damage by neurotoxins, and are associated with altered personality, behaviour, and risk of neurological disease...
October 9, 2017: Pharmacology & Therapeutics
https://www.readbyqxmd.com/read/29022838/pharmacogenomics-of-triazole-antifungal-agents-implications-for-safety-tolerability-and-efficacy
#12
Jarrett R Amsden, Paul O Gubbins
Introduction Triazole antifungal agents are prescribed to treat invasive fungal infections in neutropenic and non-neutropenic patients. These antifungal agents are substrates and inhibitors of cytochrome P450 (CYP). Genetic polymorphisms in CYP2C9, CYP2C19 and CYP3A5 can lead to large population-specific variations in drug efficacy and safety, optimal dosing, or contribute to drug interactions associated with this class. Areas covered This manuscript reviews the pharmacogenomics (i.e. the influence of genetics on drug disposition) of triazole antifungal agents related to their CYP-mediated metabolism and summarizes their implications on triazole efficacy, safety, and tolerability...
October 12, 2017: Expert Opinion on Drug Metabolism & Toxicology
https://www.readbyqxmd.com/read/29022765/polymorphisms-in-genes-involved-in-vasoactive-eicosanoids-synthesis-affect-cardiovascular-risk-in-renal-transplant-recipients
#13
Guillermo Gervasini, Enrique Luna, Guadalupe Garcia-Pino, Lilia Azevedo, Sonia Mota-Zamorano, Juan José Cubero
OBJECTIVE: Arachidonic acid metabolism by cytochrome P450 (CYP) epoxygenases lead to epoxyeicosatrienoic acids (EETs), which eicosanoids with vasodilator and anti-inflammatory properties. We aim to determine whether genetic variability in these routes may contribute to cardiovascular (CV) risk in renal transplant recipients. METHODS: In a cohort of 355 patients, we determined the presence of two polymorphisms, CYP2C8*3 and CYP2J2*7, known to affect eicosanoids levels...
October 12, 2017: Current Medical Research and Opinion
https://www.readbyqxmd.com/read/29020013/in-utero-and-lactational-exposure-to-low-doses-of-the-pyrethroid-insecticide-cypermethrin-leads-to-neurodevelopmental-defects-in-male-mice-an-ethological-and-transcriptomic-study
#14
Anthony Laugeray, Ameziane Herzine, Olivier Perche, Olivier Richard, Céline Montecot-Dubourg, Arnaud Menuet, Séverine Mazaud-Guittot, Laurianne Lesné, Bernard Jegou, Stéphane Mortaud
Accumulating evidence suggests that developmental exposure to environmental chemicals may modify the course of brain development, ultimately leading to neuropsychiatric / neurodegenerative disorders later in life. In the present study, we assessed the impact of one of the most frequently used pesticides in both residential and agricultural applications - the synthetic pyrethroid cypermethrin (CYP) - on developmental neurotoxicity (DNT). Female mice were perinatally exposed to low doses of CYP (5 and 20 mg/kg body weight) from gestation to postnatal day 15...
2017: PloS One
https://www.readbyqxmd.com/read/29019074/in-vitro-inhibitory-effect-of-gymnema-sylvestre-extracts-and-total-gymnemic-acids-fraction-on-select-cytochrome-p450-activities-in-rat-liver-microsomes
#15
Madhuri Vaghela, Krishna Iyer, Nancy Pandita
BACKGROUND AND OBJECTIVES: Gymnema sylvestre R. Br. is a well-known Indian medicinal herb. Gymnemic acids are pentacyclic triterpenes saponins and active phytoconstituents of Gymnema sylvestre. The study aimed at evaluation of the in vitro rat liver cytochrome P450 (CYP) inhibition potential of extracts and total gymnemic acid (TA)-enriched fractions from G. sylvestre. METHODS: Standardization of G. sylvestre [ethanolic (EL), hydroethanolic (HE), total acid of ethanolic (TAE), total acid of hydroethanolic (TAHE) and total acid of aqueous (TAAQ) extract] was done with respect to deacyl gymnemic acid (DAGA), using reverse phase-high performance liquid chromatography (RP-HPLC)...
October 10, 2017: European Journal of Drug Metabolism and Pharmacokinetics
https://www.readbyqxmd.com/read/29018789/cost-effectiveness-of-a-family-planning-voucher-program-in-rural-pakistan
#16
Edward Ivor Broughton, Waqas Hameed, Xaher Gul, Shabnum Sarfraz, Imam Yar Baig, Monica Villanueva
INTRODUCTION: This study reports on the effectiveness and efficiency from the program funder's perspective of the Suraj Social Franchise (SSF) voucher program in which private health-care providers in remote rural areas were identified, trained, upgraded, and certified to deliver family planning services to underserved women of reproductive age in 29 districts of Sindh and 3 districts of Punjab province, Pakistan between October 2013 and June 2016. METHOD: A decision tree compared the cost of implementing SSF to the program funder and its effects of providing additional couple years of protection (CYPs) to targeted women, compared to business-as-usual...
2017: Frontiers in Public Health
https://www.readbyqxmd.com/read/29017403/protective-effect-of-zizyphus-lotus-jujube-fruits-against-cypermethrin-induced-oxidative-stress-and-neurotoxicity-in-mice
#17
Khazri Abdelhafidh, Lazher Mhadhbi, Ali Mezni, Sellami Badreddine, Hamouda Beyrem, Ezzeddine Mahmoudi
CONTEXT: Cypermethrin (CYP) is a synthetic pyrethroid insecticide used worldwide in agriculture, home pest control. The toxicity of CYP is well studied in many organisms Objective: The aim of present study was to investigate the protective effect of Zizyphus lotus (Zizyp) fruit against neurotoxicity and oxidative stress induced by CYP in mice. MATERIALS AND METHODS: Mice were divided into four groups of six each: groups I and II were used as control and CYP control (20mg/kg body weight)...
October 11, 2017: Biomarkers: Biochemical Indicators of Exposure, Response, and Susceptibility to Chemicals
https://www.readbyqxmd.com/read/29016726/genetic-polymorphisms-of-alcohol-metabolizing-enzymes-and-alcohol-consumption-are-associated-with-asymptomatic-cardiac-remodeling-and-subclinical-systolic-dysfunction-in-large-community-dwelling-asians
#18
Chung-Lieh Hung, Shun-Chuan Chang, Sheng-Hsiung Chang, Po-Ching Chi, Yu-Jun Lai, Shih-Wei Wang, Yih-Jer Wu, Hung-I Yeh, Shing-Jong Lin, Che-Hong Chen, Daria Mochly-Rosen, Li-Yu Wang
Aims: Excessive consumption of alcoholic beverages is associated with cardiac remodeling and cardiomyopathy. We examined the possible association of alcohol use, common Asian genetic variants in genes involved in alcohol metabolism, and cardiac structures/functions alterations. Methods: A prospective, community-dwelling survey among individuals with available complete echocardiography examined the associations of alcohol use, cardiac structure/functions, and three common alcohol metabolizing genetic variants, including aldehyde dehydrogenase 2 (ALDH2), alcohol dehydrogenase 1B (ADH1B) and cytochrome P450 (CYP) isoform 2E1 (CYP2E1)...
August 31, 2017: Alcohol and Alcoholism: International Journal of the Medical Council on Alcoholism
https://www.readbyqxmd.com/read/28994497/effects-of-vernonia-cinerea-compounds-on-drug-metabolizing-cytochrome-p450s-in-human-liver-microsomes
#19
Phisit Pouyfung, Songklod Sarapusit, Pornpimol Rongnoparut
Vernonia cinerea has been widely used in traditional medicines for various diseases and shown to aid in smoking abstinence and has anticancer properties. V. cinerea bioactive compounds, including flavonoids and hirsutinolide-type sesquiterpene lactones, have shown an inhibition effect on the nicotine-metabolizing cytochrome P450 2A6 (CYP2A6) enzyme and hirsutinolides reported suppressing cancer growth. In this study, V. cinerea ethanol extract and its bioactive compounds, including four flavonoids and four hirsutinolides, were investigated for an inhibitory effect on human liver microsomal CYPs 1A2, 2A6, 2B6, 2C8, 2C9, 2C19, 2D6, 2E1, and 3A4 using cocktail inhibition assays combined with LC-MS/MS analysis...
October 10, 2017: Phytotherapy Research: PTR
https://www.readbyqxmd.com/read/28993551/usefulness-of-two-compartment-model-assisted-and-static-overall-inhibitory-activity-method-for-prediction-of-drug-drug-interaction
#20
Katsumi Iga, AKiko Kiriyama
Our study of drug-drug interaction (DDI) started with the clarification of unusually large DDI observed between ramelteon (RAM) and fluvoxamine (FLV). The main cause of this DDI was shown to be the extremely small hepatic availability of RAM (vFh). Traditional DDI prediction assuming the well-stirred hepatic extraction kinetic ignores the relative increase of vFh by DDI, while we could solve this problem by use of the tube model. Ultimately, we completed a simple and useful method for prediction of DDI. Currently, DDI prediction becomes more complex and difficult when examining issues such as dynamic changes in perpetrator level, inhibitory metabolites, etc...
October 7, 2017: Biological & Pharmaceutical Bulletin
keyword
keyword
18466
1
2
Fetch more papers »
Fetching more papers... Fetching...
Read by QxMD. Sign in or create an account to discover new knowledge that matter to you.
Remove bar
Read by QxMD icon Read
×

Search Tips

Use Boolean operators: AND/OR

diabetic AND foot
diabetes OR diabetic

Exclude a word using the 'minus' sign

Virchow -triad

Use Parentheses

water AND (cup OR glass)

Add an asterisk (*) at end of a word to include word stems

Neuro* will search for Neurology, Neuroscientist, Neurological, and so on

Use quotes to search for an exact phrase

"primary prevention of cancer"
(heart or cardiac or cardio*) AND arrest -"American Heart Association"