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Journal articles on the topic 'Inhibiteurs du cytochrome P-450 CYP3A'

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1

Baragatti, Barbara, Enrica Ciofini, Francesca Scebba, et al. "Cytochrome P-450 3A13 and endothelin jointly mediate ductus arteriosus constriction to oxygen in mice." American Journal of Physiology-Heart and Circulatory Physiology 300, no. 3 (2011): H892—H901. http://dx.doi.org/10.1152/ajpheart.00907.2010.

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The fetal ductus arteriosus (DA) contracts to oxygen, and this feature, maturing through gestation, is considered important for its closure at birth. We have previously obtained evidence of the involvement of cytochrome P-450, possibly of the 3A subfamily (CYP3A), in oxygen sensing and have also identified endothelin (ET)-1 as the attendant effector for the contraction. Here, we examined comparatively wild-type (WT) and CYP3A-null ( Cyp3a−/−) mice for direct validation of this concept. We found that the CYP3A subfamily is represented only by CYP3A13 in the WT DA. CYP3A13 was also detected in t
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2

Oinonen, T., and K. O. Lindros. "Hormonal regulation of the zonated expression of cytochrome P-450 3A in rat liver." Biochemical Journal 309, no. 1 (1995): 55–61. http://dx.doi.org/10.1042/bj3090055.

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Most cytochrome P-450 enzymes are expressed characteristically in a zonated pattern in the liver. The factors responsible for this heterogenous expression are largely unknown. Here we report how growth hormone and tri-iodothyronine regulate the steroid-hydroxylating cytochrome P-450 (CYP) 3A forms, which are constitutively expressed mainly in the perivenous (downstream) liver region. By comparing cell lysates obtained from the periportal and perivenous acinar regions we observed that the elevated CYP3A expression observed after hypophysectomy was due mainly to a dramatic increase in the normal
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3

Yanagimoto, Toru, Susumu Itoh, Minoru Sawada, Hisashi Hashimoto, and Tetsuya Kamataki. "Molecular cloning and functional expression of a mouse cytochrome P-450 (Cyp3a-13): examination of Cyp3a-13 enzyme to activate aflatoxin B1 (AFB1)." Biochimica et Biophysica Acta (BBA) - General Subjects 1201, no. 3 (1994): 405–10. http://dx.doi.org/10.1016/0304-4165(94)90069-8.

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4

Day, Kimberly C., Charles G. Plopper, and Michelle V. Fanucchi. "Age-specific pulmonary cytochrome P-450 3A1 expression in postnatal and adult rats." American Journal of Physiology-Lung Cellular and Molecular Physiology 291, no. 1 (2006): L75—L83. http://dx.doi.org/10.1152/ajplung.00356.2005.

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A major cause of death and illness in children under the age of five, most living in polluted cities, is respiratory disease. Previous studies have shown that neonatal animals are more susceptible to bioactivated pulmonary cytotoxicants than adults, despite lower expression of the pulmonary cytochrome P-450s (CYP450s) thought to be involved in bioactivation. One CYP450 that is well documented in the bioactivation of many drugs and environmental toxicants in adult lung, but whose expression has not been evaluated during postnatal pulmonary development, is CYP450 3A (CYP3A). We compared age-spec
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5

Givens, Raymond C., Yvonne S. Lin, Amy L. S. Dowling, et al. "CYP3A5 genotype predicts renal CYP3A activity and blood pressure in healthy adults." Journal of Applied Physiology 95, no. 3 (2003): 1297–300. http://dx.doi.org/10.1152/japplphysiol.00322.2003.

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A single-nucleotide polymorphism (A6986G) in the cytochrome P-450 3A5 ( CYP3A5) gene distinguishes an expressor ( *1) and a reduced-expressor ( *3) allele and largely predicts CYP3A5 content in liver and intestine. CYP3A5 is the prevailing CYP3A isoform in kidney. We report that, among renal microsomes from 21 organ donors, those from *1/ *3 individuals had at least eightfold higher mean kidney microsomal CYP3A5 content and 18-fold higher mean CYP3A catalytic activity than did those from *3/ *3 individuals ( P = 0.0001 and P = 0.0137, respectively). We also report significant associations betw
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6

Itoh, Susumu, Mitsuharu Satoh, Yoko Abe, Hisashi Hashimoto, Tom Yanagimoto, and Tetsuya Kamataki. "A Novel Form of Mouse Cytochrome P 450 3A (Cyp3a-16). Its cDNA Cloning and Expression in Fetal Liver." European Journal of Biochemistry 226, no. 3 (1994): 877–82. http://dx.doi.org/10.1111/j.1432-1033.1994.t01-1-00877.x.

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7

Delaforge, Marcel, Denis Servent, Philippe Wirsta, Claire Ducrocq, Daniel Mansuy, and Maryse Lenfant. "Particular ability of cytochrome P-450 CYP3A to reduce glyceryl trinitrate in rat liver microsomes: Subsequent formation of nitric oxide." Chemico-Biological Interactions 86, no. 2 (1993): 103–17. http://dx.doi.org/10.1016/0009-2797(93)90115-f.

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8

Hematheerthani N, Siva Reddy CH, Prameela Rani A, and Suresh Kumar P. "Repercussion of piperine on pharmacokinetics parameters of eletriptan in albino rats: Involvement of CYP3A and P-GP inhibition." International Journal of Research in Pharmaceutical Sciences 12, no. 3 (2021): 2115–22. http://dx.doi.org/10.26452/ijrps.v12i3.4821.

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Eletriptan is at the type of triptan medication suggested for the management of episodes of severe headache with or without aura. Piperine (1-piperoylpiperidine) is a pure alkaloid as well as the basic tanginess material from the pipli and peppercorn. There are signs that piperine inhibits Cytochrome P-450 enzymes and P-glycoprotein, rather than arouses, drug metabolism generally, thus increasing the bioavailability and effect of several medications. The analysis was undertaken to assess the results of Piperine on the pharmacokinetics of Eletriptan. Samples of blood were taken at different tim
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9

Hematheerthani N, Siva Reddy CH, Prameela Rani A, and Suresh Kumar P. "Repercussion of piperine on pharmacokinetics parameters of eletriptan in albino rats: Involvement of CYP3A and P-GP inhibition." International Journal of Research in Pharmaceutical Sciences 11, no. 4 (2020): 8079–86. http://dx.doi.org/10.26452/ijrps.v11i4.4821.

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Eletriptan is at the type of triptan medication suggested for the management of episodes of severe headache with or without aura. Piperine (1-piperoylpiperidine) is a pure alkaloid as well as the basic tanginess material from the pipli and peppercorn. There are signs that piperine inhibits Cytochrome P-450 enzymes and P-glycoprotein, rather than arouses, drug metabolism generally, thus increasing the bioavailability and effect of several medications. The analysis was undertaken to assess the results of Piperine on the pharmacokinetics of Eletriptan. Samples of blood were taken at different tim
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10

Resál, T., K. Farkas, and T. Molnár. "P546 The safety and efficacy of the new-generation budesonide-MMX in the aspect of the cytochrome P-450 enzyme genotype." Journal of Crohn's and Colitis 15, Supplement_1 (2021): S516. http://dx.doi.org/10.1093/ecco-jcc/jjab076.667.

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Abstract Background Unlike previous forms of budesonide absorbing from the ileal and ascending colon region, the new-generation budesonide-MMX contains a formula, that allows absorption throughout the whole colon. Budesonide is degraded in the liver by cytochrome P450 3A enzyme, but so far, there is no study examining the relationship between the budesonide’s effect and the enzyme activity. CYP3A5 is absent in 90% of the European/caucasian population due to a functional loss mutation (CYP3A5*3), whereas patients with the wild-type CYP3A5*1 allele may be expected to have increased metabolism. T
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11

Perdomo, Virginia G., Juan P. Rigalli, Silvina S. M. Villanueva, et al. "Modulation of Biotransformation Systems and ABC Transporters by Benznidazole in Rats." Antimicrobial Agents and Chemotherapy 57, no. 10 (2013): 4894–902. http://dx.doi.org/10.1128/aac.02531-12.

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ABSTRACTThe effect of antichagasic benznidazole (BZL; 100 mg/kg body weight/day, 3 consecutive days, intraperitoneally) on biotransformation systems and ABC transporters was evaluated in rats. Expression of cytochrome P-450 (CYP3A), UDP-glucuronosyltransferase (UGT1A), glutathioneS-transferases (alpha glutathioneS-transferase [GST-α], GST-μ, and GST-π), multidrug-resistance-associated protein 2 (Mrp2), and P glycoprotein (P-gp) in liver, small intestine, and kidney was estimated by Western blotting. Increases in hepatic CYP3A (30%) and GST-μ (40%) and in intestinal GST-α (72% in jejunum and 13
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12

Kim, Young Chul, Chul Won Ahn, Jung Ah Lee, Jae Hak Park, and Young C. Kim. "Alterations in drug metabolizing activities in acute hepatosteatosis induced by intake of a high-carbohydrate/fat-free diet after food deprivation." Functional Foods in Health and Disease 6, no. 1 (2016): 59. http://dx.doi.org/10.31989/ffhd.v6i1.238.

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ABSTRACT Background: Lipid accumulation in hepatocytes constitutes a major component in the pathogenesis of chronic liver injury. However, the impact of lipid deposition in liver on drug metabolizing capacity remains unclear. Purpose of the study: The present study was undertaken to evaluate the changes in hepatic cytochrome P-450 (CYP) enzymes in acute hepatosteatosis.Methods: Rats were fasted for 48 h, and then provided with a high-carbohydrate/fat-free diet (FH) or a normal diet (FN) for 48 h.Results: Hepatic lipid accumulation was significant in the FH group. In the FN group there was a sm
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13

Paulík, Adam, Jiří Grim, and Stanislav Filip. "Predictors of Irinotecan Toxicity and Efficacy in Treatment of Metastatic Colorectal Cancer." Acta Medica (Hradec Kralove, Czech Republic) 55, no. 4 (2012): 153–59. http://dx.doi.org/10.14712/18059694.2015.39.

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The colorectal cancer ranks high among the malignant tumours in incidence and mortality and irinotecan is standardly used in palliative treatment of metastatic disease in every therapeutic line. Unfortunately, the treatment with irinotecan is often associated with severe toxicities, especially neutropenia and diarrhea. The majority of the toxic manifestation is caused by the insufficient deactivation (glucuronidation) of irinotecan active metabolite SN-38 by UGT1A enzyme. The elevated SN-38 plasma concentration is responsible for the hematological and gastrointestinal toxicity that can become
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14

Kiriyama, Akiko, Tomoyuki Nishiura, Hirokazu Yamaji, and Kanji Takada. "Metabolic Characterization of a Tripeptide Human Immunodeficiency Virus Type 1 Protease Inhibitor, KNI-272, in Rat Liver Microsomes." Antimicrobial Agents and Chemotherapy 43, no. 3 (1999): 549–56. http://dx.doi.org/10.1128/aac.43.3.549.

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ABSTRACT KNI-272 is a tripeptide protease inhibitor for treating human immunodeficiency virus type 1 (HIV-1). In in vitro stability studies using rat tissue homogenates, KNI-272 concentrations in the liver, kidney, and brain decreased significantly with time. Moreover, in tissue distribution studies, KNI-272 distributed highly to the liver, kidney, and small intestine in vivo. From these results and reported physiological parameters such as the tissue volume and tissue blood flow rate, we considered the liver to be the main organ which takes part in the metabolic elimination of KNI-272. Then t
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15

Morris, David J., Syed A. Latif, Michael D. Rokaw, Charles O. Watlington, and John P. Johnson. "A second enzyme protecting mineralocorticoid receptors from glucocorticoid occupancy." American Journal of Physiology-Cell Physiology 274, no. 5 (1998): C1245—C1252. http://dx.doi.org/10.1152/ajpcell.1998.274.5.c1245.

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We have confirmed that A6 cells (derived from kidney of Xenopus laevis), which contain both mineralocorticoid and glucocorticoid receptors, do not normally possess 11β-hydroxysteroid dehydroxgenase (11β-HSD1 or 11β-HSD2) enzymatic activity and so are without apparent “protective” enzymes. A6 cells do not convert the glucocorticoid corticosterone to 11-dehydrocorticosterone but do, however, possess steroid 6β-hydroxylase that transforms corticosterone to 6β-hydroxycorticosterone. This hydroxylase is cytochrome P-450 3A (CYP3A). We have now determined the effects of 3α,5β-tetrahydroprogesterone
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16

Goud, Thirumal Eswara, Srinivas Maddi, Nayakanti Devanna, and Thatipamula Rajendra Prasad. "Evaluation of pharmacokinetic and pharmacodynamic interaction between repaglinide and atazanavir in healthy, diabetic and hepatic impaired rats: possible inhibition of CYP3A, OATP, and P-glycoprotein transporters." ADMET and DMPK 4, no. 3 (2016): 269. http://dx.doi.org/10.5599/admet.4.3.328.

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<p>The metabolic syndrome in HIV infected patients is particularly associated with the use protease inhibitors. Atazanavir is an inhibitor of the cytochrome P 450 (CYP) system, in particular CYP3A4 and CYP2C9 which can affect the metabolism of several drugs. To treat metabolic syndrome in HIV patients repaglinide is used and it is a short acting insulin secretagogues undergoing metabolism with CYP 3A4 and CYP 2C8 enzyme system. The purpose of this study was to assess the possible pharmacokinetic and pharmacodynamic drug interaction of repaglinide and atazanavir in healthy, diabetic and i
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17

Chahine, Elias B. "Fostemsavir: The first oral attachment inhibitor for treatment of HIV-1 infection." American Journal of Health-System Pharmacy 78, no. 5 (2021): 376–88. http://dx.doi.org/10.1093/ajhp/zxaa416.

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Abstract Purpose The pharmacology, pharmacokinetics, and role in therapy of fostemsavir in management of HIV-1 infection are reviewed, with an emphasis on clinical efficacy and safety data from phase 2 and phase 3 clinical trials. Summary Fostemsavir (Rukobia, ViiV Healthcare), is a prodrug of temsavir, a novel pyridine compound with potent activity against HIV-1. Fostemsavir, the first oral attachment inhibitor, was approved and granted the breakthrough therapy designation by the Food and Drug Administration for use in combination with other antiretroviral agents for the treatment of HIV-1 in
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18

Tousen, Yuko, Jun Takebayashi, Takashi Kondo, et al. "Safety and Efficacy Assessment of Isoflavones from Pueraria (Kudzu) Flower Extract in Ovariectomised Mice: A Comparison with Soy Isoflavones." International Journal of Molecular Sciences 20, no. 12 (2019): 2867. http://dx.doi.org/10.3390/ijms20122867.

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Numerous Foods with Function Claims that contain the extract of Pueraria flower (kudzu) isoflavones (PFI) are available in the Japanese market. These are labelled with function claims of reducing visceral fat. However, these foods have not undergone proper safety assessment such as the evaluation of their oestrogenic activity and effects on drug-metabolising enzymes (cytochrome P-450: CYP) in the liver. This study evaluated the estrogenic effect and the hepatic CYP activity and mRNA expression in normal female mice as a safety assessment of PFI (Experiment 1). In addition, the bone mineral den
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19

Masuyama, Hisashi, Naoko Suwaki, Yoko Tateishi, Hideki Nakatsukasa, Tomonori Segawa, and Yuji Hiramatsu. "The Pregnane X Receptor Regulates Gene Expression in a Ligand- and Promoter- Selective Fashion." Molecular Endocrinology 19, no. 5 (2005): 1170–80. http://dx.doi.org/10.1210/me.2004-0434.

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Abstract Recent studies have revealed that pregnane X receptor (PXR) can function as a master regulator to control the expression of phase I and phase II drug-metabolizing enzymes, as well as members of the drug transporter family, including multiple drug resistance (MDR) 1, which has a major role in multidrug resistance. Previously, we have demonstrated that steroid/xenobiotics metabolism by tumor tissue through the PXR-cytochrome P-450 3A (CYP3A) pathway might play an important role in endometrial cancer. In this study, we examined which endocrine-disrupting chemicals (EDCs) and anticancer a
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20

Kono, Hiroshi, Blair U. Bradford, Ming Yin, et al. "CYP2E1 is not involved in early alcohol-induced liver injury." American Journal of Physiology-Gastrointestinal and Liver Physiology 277, no. 6 (1999): G1259—G1267. http://dx.doi.org/10.1152/ajpgi.1999.277.6.g1259.

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The continuous intragastric enteral feeding protocol in the rat was a major development in alcohol-induced liver injury (ALI) research. Much of what has been learned to date involves inhibitors or nutritional manipulations that may not be specific. Knockout technology avoids these potential problems. Therefore, we used long-term intragastric cannulation in mice to study early ALI. Reactive oxygen species are involved in mechanisms of early ALI; however, their key source remains unclear. Cytochrome P-450 (CYP)2E1 is induced predominantly in hepatocytes by ethanol and could be one source of reac
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21

Kang, Dongwoo, Julie Passarell, Malaz A. Abutarif, Jeanne Mendell, and Ophelia Yin. "Exposure-Response of Quizartinib Efficacy in Patients with Relapsed/Refractory AML." Blood 134, Supplement_1 (2019): 1263. http://dx.doi.org/10.1182/blood-2019-122582.

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Introduction: Quizartinib is a once-daily, oral, highly potent and selective FLT3 inhibitor that has shown clinical activity in patients with relapsed/refractory acute myeloid leukemia (AML) with FLT3 internal tandem duplications in the phase 3 QuANTUM-R trial (Cortes et al, Lancet Oncol 2019; NCT02039726). In this analysis, exposure-response relationships of select efficacy endpoints of quizartinib were evaluated. Methods: Analysis was conducted for the following 2 studies separately: phase 2 study APS2689-CL-2004 and phase 3 QuANTUM-R study. Phase 2 study APS2689-CL-2004 enrolled 76 patients
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