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https://www.readbyqxmd.com/read/28654297/eriodictyol-not-its-glucuronide-metabolites-attenuates-acetaminophen-induced-hepatotoxicity
#1
Ling Ye, Zhaoyu Wang, Yao Lan, Minghao Chen, Cailing Wen, Yanxian Hu, Zhong Qiu Liu
Acetaminophen (APAP) is one of the most commonly used oral analgesics and antipyretics, but hepatotoxicity including liver failure may occur after overdose. The therapeutic options for treating APAP hepatotoxicity are limited. Eriodictyol, a dietary flavonoid with anti-inflammatory and antioxidant properties, was used here to determine its protective effects against APAP-induced hepatotoxicity in mice. Various administration routes and pharmacokinetics-pharmacodynamics (PK-PD) analyses were used to determine these effects...
June 27, 2017: Molecular Pharmaceutics
https://www.readbyqxmd.com/read/28653847/glucuronides-as-potential-anionic-substrates-of-human-cytochrome-p450-2c8-cyp2c8
#2
Yong Ma, Yue Fu, S Cyrus Khojasteh, Deepak Dalvie, Donglu Zhang
Glucuronidation is in general considered as a terminal metabolic step that leads to direct elimination of drugs and generally abolishes their biological activity. However, there is growing evidence to suggest that glucuronides can be ligands of human CYP2C8, making CYP2C8 distinct from the other CYP isoforms. Several classes of glucuronide conjugates, which include acyl glucuronides, ether glucuronides, N-glucuronides, and carbamoyl glucuronides, have been shown to be substrates or time-dependent inhibitors of CYP2C8...
June 27, 2017: Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/28653752/the-potential-of-epimedium-koreanum-nakai-for-herb-drug-interaction
#3
Qingxiang Zhong, Ziqi Shi, Li Zhang, Rongling Zhong, Zhi Xia, Jing Wang, Hao Wu, Yutong Jiang, E Sun, Yingjie Wei, Liang Feng, Zhenhai Zhang, Dan Liu, Jie Song, Xiaobin Jia
OBJECTIVES: This study aims to investigate potential herb-drug interactions (HDI) of Epimedium koreanum Nakai. METHODS: Human liver microsomes (HLMs) were used to determine the enzyme kinetics of the major human cytochrome P450s (CYPs). Inducible potential of E. koreanum on CYP1A2, 2B6, 2C19 and 3A4 activities of human primary hepatocytes was also examined. KEY FINDINGS: Ethanol extract of E. koreanum showed direct inhibitory potency for CYP1A2 (IC50  = 121...
June 27, 2017: Journal of Pharmacy and Pharmacology
https://www.readbyqxmd.com/read/28652520/biochemical-characterization-of-variants-of-canine-cyp1a1-using-heterologous-3-expression
#4
Hee Jeong Yu, Seung Heon Lee, Seungwoo Lee, Yu Jung Choi, Dayoung Oh, Ki-Hoan Nam, YoungMin Yun, Doug-Young Ryu
Cytochrome P450 1A1 (CYP1A1) is a heme-containing mono-oxygenase involved in metabolism of environmental contaminants. Two variants of dog CYP1A1 with a single residue difference were identified and designated Sap1 and Sap2. Compared with Sap1, Sap2 had a Trp50Leu substitution. The biochemical characteristics of the variants were comparatively analyzed using heterologous expression in Escherichia coli. The membrane fraction of E. coli expressing Sap2 exhibited higher CYP holoprotein and heme contents than the Sap1-containing membranes, although the level of total CYP1A1 protein (i...
June 24, 2017: Journal of Veterinary Medical Science
https://www.readbyqxmd.com/read/28652425/evaluation-of-biological-activity-of-mastic-extracts-based-on-chemotherapeutic-indices
#5
Ryuichiro Suzuki, Hiroshi Sakagami, Shigeru Amano, Kunihiko Fukuchi, Katsuyoshi Sunaga, Taisei Kanamoto, Shigemi Terakubo, Hideki Nakashima, Yoshiaki Shirataki, Mineko Tomomura, Yoshiko Masuda, Satoshi Yokose, Akito Tomomura, Hirofumi Watanabe, Masaki Okawara, Yoshiharu Matahira
BACKGROUND: Most previous mastic investigators have not considered its potent cytotoxicity that may significantly affect the interpretation of obtained data. In the present study, we re-evaluated several biological activities of mastic extracts, based on chemotherapeutic indexes. MATERIALS AND METHODS: Pulverized mastic gum was extracted with n-hexane and then with ethyl acetate or independently with methanol or n-butanol. Tumor specificity (TS) of the extracts was determined by their cytotoxicity against human malignant and non-malignant cells...
July 2017: In Vivo
https://www.readbyqxmd.com/read/28651982/design-and-optimization-of-highly-selective-broad-spectrum-fungal-cyp51-inhibitors
#6
Christopher M Yates, Edward P Garvey, Sammy R Shaver, Robert J Schotzinger, William J Hoekstra
While the orally-active azoles such as fluconazole and posaconazole are effective antifungal agents, they potently inhibit a broad range of off-target human cytochrome P450 enzymes (CYPs) leading to various safety issues (e.g., drug-drug interactions, liver, and reproductive toxicities). Recently we described the rationally-designed, antifungal agent VT-1161 that is more selective for fungal CYP51 than related human CYP enzymes such as CYP3A4. Herein, we describe the use of a homology model of Aspergillus fumigatus to design and optimize a novel series of highly selective, broad spectrum fungal CYP51 inhibitors...
June 15, 2017: Bioorganic & Medicinal Chemistry Letters
https://www.readbyqxmd.com/read/28648140/oxidation-of-1-chloropyrene-by-human-cyp1-family-and-cyp2a-subfamily-cytochrome-p450-enzymes-catalytic-roles-of-two-cyp1b1-and-five-cyp2a13-allelic-variants
#7
Tsutomu Shimada, Norie Murayama, Kensaku Kakimoto, Shigeo Takenaka, Young-Ran Lim, Sora Yeom, Donghak Kim, Hiroshi Yamazaki, F Peter Guengerich, Masayuki Komori
1. Chloropyrene, one of the major chlorinated polycyclic aromatic hydrocarbon contaminants, was incubated with human cytochrome P450 (P450 or CYP) enzymes including CYP1A1, 1A2, 1B1, 2A6, 2A13, 2B6, 2C9, 2D6, 2E1, 3A4, and 3A5. Catalytic differences in 1-chloropyrene oxidation by polymorphic two CYP1B1 and five CYP2A13 allelic variants were also examined. 2. CYP1A1 oxidized 1-chloropyrene at the 6- and 8-positions more actively than at the 3-position, while both CYP1B1.1 and 1B1.3 preferentially catalyzed 6-hydroxylation...
June 26, 2017: Xenobiotica; the Fate of Foreign Compounds in Biological Systems
https://www.readbyqxmd.com/read/28648122/phase-1-study-to-investigate-the-pharmacokinetic-properties-of-dacomitinib-in-healthy-adult-chinese-subjects-genotyped-for-cyp2d6
#8
Xia Chen, Ji Jiang, Nagdeep Giri, Pei Hu
1. This study aimed to characterise the pharmacokinetics of dacomitinib, a pan-human epidermal growth factor receptor tyrosine kinase inhibitor, and its metabolite, PF-05199265, in healthy Chinese subjects. 2. In this open-label, single-centre, nonrandomised study (NCT02097433), 14 subjects received a single dacomitinib 45-mg oral dose. Pharmacokinetic samples for dacomitinib and PF-05199265 were collected pre- and postdose. Subjects were genotyped for cytochrome P450 (CYP)2D6 metaboliser status. Safety was assessed throughout the study...
June 26, 2017: Xenobiotica; the Fate of Foreign Compounds in Biological Systems
https://www.readbyqxmd.com/read/28643580/cyclophilins-less-studied-proteins-with-critical-roles-in-pathogenesis
#9
Khushwant Singh, Mark Winter, Miloslav Zouhar, Pavel Rysanek
Cyclophilins (EC 5.2.1.8) (CYPs) belong to a subgroup of proteins known as immunophilins, which also include FK-506 binding proteins (FKBPs) and parvulins. Members of the immunophilins have two main characteristic properties: I) peptidyl-prolyl cis-trans isomerase activity (PPIases) and II) the ability to bind immunosuppressant molecules of fungal origin. Cyclophilins are some of the most conserved proteins present in eukaryotes and prokaryotes, and they have been implicated in diverse cellular processes and responses to multiple biotic and abiotic stresses...
June 23, 2017: Phytopathology
https://www.readbyqxmd.com/read/28641720/fenofibrate-attenuates-hypertension-in-goldblatt-hypertensive-rats-role-of-20-hydroxyeicosatetraenoic-acid-in-the-nonclipped-kidney
#10
Alexandra Sporková, Věra Čertíková Chábová, Šárka Doleželová, Šárka Jíchová, Libor Kopkan, Zdeňka Vaňourková, Elzbieta Kompanowska-Jezierska, Janusz Sadowski, Hana Maxová, Luděk Červenka
BACKGROUND: There is vast evidence that the renin-angiotensin system is not the sole determinant of blood pressure (BP) elevation in human renovascular hypertension or the relevant experimental models. This study tested the hypothesis that kidney deficiency of 20-hydroxyeicosatetraenoic acid (20-HETE), a product of cytochrome P450 (CYP)-dependent ω-hydroxylase pathway of arachidonic acid metabolism, is important in the pathophysiology of the maintenance phase of 2-kidney, 1-clip (2K1C) Goldblatt hypertension...
June 2017: American Journal of the Medical Sciences
https://www.readbyqxmd.com/read/28641195/biotransformation-in-the-zebrafish-embryo-temporal-gene-transcription-changes-of-cytochrome-p450-enzymes-and-internal-exposure-dynamics-of-the-ahr-binding-xenobiotic-benz-a-anthracene
#11
Agnes Kühnert, Carolina Vogs, Bettina Seiwert, Silke Aulhorn, Rolf Altenburger, Henner Hollert, Eberhard Küster, Wibke Busch
Not much is known about the biotransformation capability of zebrafish (Danio rerio) embryos. For understanding possible toxicity differences to adult fish, it might be crucial to understand the biotransformation of chemicals in zebrafish embryos i.e. as part of toxicokinetics. The biotransformation capabilities were analysed for two different stages of zebrafish embryos in conjunction with the internal concentrations of a xenobiotic. Zebrafish embryos of the late cleavage/early blastula period (2-26 hpf) and the early pharyngula period (26-50 hpf) were exposed for 24 h to the AhR binding compound benz[a]anthracene (BaA)...
June 19, 2017: Environmental Pollution
https://www.readbyqxmd.com/read/28639016/accumulation-properties-of-polychlorinated-biphenyl-congeners-in-yusho-patients-and-prediction-of-their-cytochrome-p450-dependent-metabolism-by-in-silico-analysis
#12
Shusaku Hirakawa, Takashi Miyawaki, Tsuguhide Hori, Jumboku Kajiwara, Susumu Katsuki, Masashi Hirano, Yuka Yoshinouchi, Hisato Iwata, Chikage Mitoma, Masutaka Furue
In what has become known as the Yusho incident, thousands of people in western Japan were poisoned by the accidental ingestion of rice bran oil contaminated with polychlorinated biphenyls (PCBs) and various dioxins and dioxin-like compounds. In this study, we investigated the accumulation patterns of 69 PCB congeners in the blood of Yusho patients in comparison with those of non-exposed controls. The blood samples were collected at medical check-ups in 2004 and 2005. To compare the patterns of PCB congeners, we calculated the concentration ratio of each congener relative to the 2,2',4,4',5,5'-hexaCB (CB153) concentration...
June 21, 2017: Environmental Science and Pollution Research International
https://www.readbyqxmd.com/read/28635628/identification-and-validation-of-reference-genes-for-seashore-paspalum-response-to-abiotic-stresses
#13
Yu Liu, Jun Liu, Lei Xu, Hui Lai, Yu Chen, Zhimin Yang, Bingru Huang
Seashore paspalum (Paspalum vaginatum) is among the most salt- and cadmium-tolerant warm-season perennial grass species widely used as turf or forage. The objective of this study was to select stable reference genes for quantitative real-time polymerase chain reaction (qRT-PCR) analysis of seashore paspalum in response to four abiotic stresses. The stability of 12 potential reference genes was evaluated by four programs (geNorm, NormFinder, BestKeeper, and RefFinder). U2AF combined with glyceraldehyde-3-phosphate dehydrogenase (GAPDH) showed stable expression in Cd-treated leaves and cold-treated roots...
June 21, 2017: International Journal of Molecular Sciences
https://www.readbyqxmd.com/read/28633515/crystal-structure-and-functional-characterization-of-a-cytochrome-p450-bacyp106a2-from-bacillus-sp-pamc-23377
#14
Ki-Hwa Kim, Chang Woo Lee, Bikash Dangi, Sun-Ha Park, Hyun Park, Tae-Jin Oh, Jun Hyuck Lee
Bacterial cytochrome P450 (CYP) steroid hydroxylases are effectively useful in the pharmaceutical industry for introducing hydroxyl groups to a wide range of steroids. We found a putative CYP steroid hydroxylase (BaCYP106A2) from the bacterium Bacillus sp. PAMC 23377 isolated from Kara Sea of the Arctic Ocean, showing 94% sequence similarity with BmCYP106A2 (Bacillus megaterium ATCC 13368). In this study, soluble BaCYP106A2 was overexpressed to evaluate its substrate-binding activity. The substrate affinity (Kd value) to 4-androstenedione was 387 ± 37 µM...
June 21, 2017: Journal of Microbiology and Biotechnology
https://www.readbyqxmd.com/read/28626488/hepatotoxicity-in-rats-induced-by-aqueous-extract-of-polygoni-multiflori-radix-root-of-polygonum-multiflorum-related-to-the-activity-inhibition-of-cyp1a2-or-cyp2e1
#15
Deng-Ke Li, Jing Chen, Zhen-Zhen Ge, Zhen-Xiao Sun
The objective of this study is to investigate the relationship between the hepatotoxicity induced by Polygoni Multiflori Radix (PMR, root of Polygonum multiflorum Thunb., He Shou Wu) and the activity of CYP1A2 or CYP2E1 in the rat liver. Levels of rat serum transaminases ALT and AST were not altered but the activity of CYP1A2 or CYP2E1 in the rat liver was significantly inhibited after oral administration of aqueous extract of PMR under the experimental dosage. However, levels of ALT and AST were significantly increased and the activity of CYP1A2 or CYP2E1 was significantly decreased after injection of specific inhibitor for CYP1A2 or CYP2E1 combined with oral administration of aqueous extract of PMR, especially under the repeated treatment over interval times...
2017: Evidence-based Complementary and Alternative Medicine: ECAM
https://www.readbyqxmd.com/read/28626197/evaluation-of-cyp2d6-protein-expression-and-activity-in-the-small-intestine-to-determine-its-metabolic-capability-in-the-japanese-population
#16
Momoko Kawakami, Sachiko Takenoshita-Nakaya, Yuko Takeba, Yuki Nishimura, Masayuki Oda, Minoru Watanabe, Yuki Ohta, Shinjiro Kobayashi, Takehito Ohtsubo, Shinichi Kobayashi, Naoki Uchida, Naoki Matsumoto
CYP2D6 plays an important role in the metabolism of many drugs such as opioids and antidepressants. Polymorphisms of the CYP2D6 gene are widely observed in the Japanese population, and can affect the first-pass metabolism of orally administered drugs. Several CYP enzymes have been identified in the small intestine of Caucasians, but intestinal CYP enzymes have not been reported in the Japanese population, except for CYP3A4 and CYP2C19. In this study, we evaluated the CYP2D6 metabolic capacity by measurement of CYP2D6 mRNA and protein levels and activity in the small intestine of Japanese individuals...
June 14, 2017: Biological & Pharmaceutical Bulletin
https://www.readbyqxmd.com/read/28625736/use-of-bioconjugation-with-cytochrome-p450-enzymes
#17
REVIEW
Julie Ducharme, Karine Auclair
Bioconjugation, defined as chemical modification of biomolecules, is widely employed in biological and biophysical studies. It can expand functional diversity and enable applications ranging from biocatalysis, biosensing and even therapy. This review summarizes how chemical modifications of cytochrome P450 enzymes (P450s or CYPs) have contributed to improving our understanding of these enzymes. Genetic modifications of P450s have also proven very useful but are not covered in this review. Bioconjugation has served to gain structural information and investigate the mechanism of P450s via photoaffinity labeling, mechanism-based inhibition (MBI) and fluorescence studies...
June 15, 2017: Biochimica et Biophysica Acta
https://www.readbyqxmd.com/read/28623527/updating-the-evidence-of-the-interaction-between-clopidogrel-and-cyp2c19-inhibiting-selective-serotonin-reuptake-inhibitors-a-cohort-study-and-meta-analysis
#18
Katsiaryna Bykov, Sebastian Schneeweiss, Robert J Glynn, Murray A Mittleman, David W Bates, Joshua J Gagne
INTRODUCTION: We previously found that patients who initiate clopidogrel while treated with a cytochrome P450 (CYP) 2C19-inhibiting selective serotonin reuptake inhibitor (SSRI) have a higher risk of subsequent ischemic events than patients treated with other SSRIs. It is not known whether initiating an inhibiting SSRI while treated with clopidogrel will also increase risk of ischemic events. OBJECTIVE: The aim of this study was to assess clinical outcomes following initiation of a CYP2C19-inhibiting SSRI versus initiation of other SSRIs among patients treated with clopidogrel and to update existing evidence on the clinical impact of clopidogrel-SSRI interaction...
June 16, 2017: Drug Safety: An International Journal of Medical Toxicology and Drug Experience
https://www.readbyqxmd.com/read/28622553/toxic-responses-of-cytochrome-p450-sub-enzyme-activities-to-heavy-metals-exposure-in-soil-and-correlation-with-their-bioaccumulation-in-eisenia-fetida
#19
Xiufeng Cao, Ran Bi, Yufang Song
The dose- and time- dependent responses of cytochrome P450 (CYP) sub-enzyme activities to heavy metals in soil, and the relationships between biomarker responses and metal bioaccumulation in Eisenia fetida were evaluated. Earthworms were exposed to soils spiked with increasing doses of Cd, Cu, Pb or Zn for 21 d. Results demonstrated that EROD and CYP3A4 activities responded significantly with increasing dose and exposure duration. EROD activity significantly (P < 0.05) correlated with CYP3A4 activity exposed to Pb and Cu...
June 13, 2017: Ecotoxicology and Environmental Safety
https://www.readbyqxmd.com/read/28620303/effect-of-genetic-variability-in-the-cyp4f2-cyp4f11-and-cyp4f12-genes-on-liver-mrna-levels-and-warfarin-response
#20
J E Zhang, Kathrin Klein, Andrea L Jorgensen, Ben Francis, Ana Alfirevic, Stephane Bourgeois, Panagiotis Deloukas, Ulrich M Zanger, Munir Pirmohamed
Genetic polymorphisms in the gene encoding cytochrome P450 (CYP) 4F2, a vitamin K oxidase, affect stable warfarin dose requirements and time to therapeutic INR. CYP4F2 is part of the CYP4F gene cluster, which is highly polymorphic and exhibits a high degree of linkage disequilibrium, making it difficult to define causal variants. Our objective was to examine the effect of genetic variability in the CYP4F gene cluster on expression of the individual CYP4F genes and warfarin response. mRNA levels of the CYP4F gene cluster were quantified in human liver samples (n = 149) obtained from a well-characterized liver bank and fine mapping of the CYP4F gene cluster encompassing CYP4F2, CYP4F11, and CYP4F12 was performed...
2017: Frontiers in Pharmacology
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