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https://www.readbyqxmd.com/read/29158009/effect-of-carbamazepine-on-expression-of-udp-glucuronosyltransferase-1a6-and-1a7-in-rat-brain
#1
Yuki Asai, Yukiko Sakakibara, Masayuki Nadai, Miki Katoh
Because UDP-glucuronosyltransferase (Ugt) 1a6 and Ugt1a7 are highly expressed in the rat brain, changes in Ugt1a6 and Ugt1a7 expression may affect the pharmacokinetics of drugs and endogenous compounds in the brain. The present study aimed to elucidate the effect of carbamazepine (CBZ), a typical UGT inducer, on Ugt1a6 and Ugt1a7 expression in the rat brain. Sprague-Dawley rats were treated intraperitoneally for 7 d with CBZ (100 mg/kg/d). Ugt1a6 and Ugt1a7 mRNAs were induced by CBZ in the cerebellum, piriform cortex, and hippocampus (Ugt1a6: 3...
October 5, 2017: Drug Metabolism and Pharmacokinetics
https://www.readbyqxmd.com/read/29157826/modulation-of-pregnane-x-receptor-pxr-and-constitutive-androstane-receptor-car-activation-by-ursolic-acid-ua-attenuates-rifampin-isoniazid-cytotoxicity
#2
Hsiao-Yun Chang, Chao-Jung Chen, Wei-Chih Ma, Wai-Kok Cheng, Yen-Ning Lin, Ying-Ray Lee, Jih-Jung Chen, Yun-Ping Lim
BACKGROUND: Interactions between transcriptional inducers of cytochrome P450 (CYP450) enzymes and therapeutic drugs may be prevented by antagonizing the activation of a nuclear receptor (NR), pregnane X receptor (PXR, NR1I2), thus improving therapeutic efficacy. PURPOSE: In the present study, we aim to identify that ursolic acid (UA), a widely distributed pentacyclic triterpene, may act as an effective antagonist of PXR and its sister NR receptor, constitutive androstane receptor (CAR, NR1I3)...
December 1, 2017: Phytomedicine: International Journal of Phytotherapy and Phytopharmacology
https://www.readbyqxmd.com/read/29145837/molecular-network-based-analysis-of-the-mechanism-of-liver-injury-induced-by-volatile-oils-from-artemisiae-argyi-folium
#3
Hongjie Liu, Sha Zhan, Yan Zhang, Yan Ma, Liang Chen, Lingxiu Chen, Hanqiu Dong, Min Ma, Zhe Zhang
BACKGROUND: Volatile oils from Artemisiae argyi folium (VOAAF) is reported with hepatotoxicity, but the underlying mechanism is still unclear. METHODS: In the present study this molecular mechanism was explored with the Ingenuity Pathway Analysis (IPA). The chemical components of the VOAAF were searched in the database, and their target proteins were all identified in the PubChem, while drug-induced liver injury (DILI) genes were searched in the PubMed gene databases...
November 16, 2017: BMC Complementary and Alternative Medicine
https://www.readbyqxmd.com/read/29126514/structural-and-functional-evidences-for-the-interactions-between-nuclear-hormone-receptors-and-endocrine-disruptors-at-low-doses
#4
Patrick Balaguer, Vanessa Delfosse, Marina Grimaldi, William Bourguet
Endocrine-disrupting chemicals (EDCs) represent a broad class of exogenous substances that cause adverse effects in the endocrine system mainly by interacting with nuclear hormone receptors (NRs). Humans are generally exposed to low doses of pollutants, and current researches aim at deciphering the mechanisms accounting for the health impact of EDCs at environmental concentrations. Our correlative analysis of structural, interaction and cell-based data has revealed a variety of, sometimes unexpected, binding modes, reflecting a wide range of EDC affinities and specificities...
September 2017: Comptes Rendus Biologies
https://www.readbyqxmd.com/read/29126478/optimization-of-gc-tof-ms-analysis-conditions-for-assessing-host-gut-microbiota-metabolic-interactions-chinese-rhubarb-alters-fecal-aromatic-amino-acids-and-phenol-metabolism
#5
Shan Yin, Pan Guo, Dafu Hai, Li Xu, Jiale Shu, Wenjin Zhang, Muhammad Idrees Khan, Irwin J Kurland, Yunping Qiu, Yumin Liu
In this paper, an optimized method based on gas chromatography/time-of-flight mass spectrometry (GC-TOFMS) platform has been developed for the analysis of gut microbial-host related co-metabolites in fecal samples. The optimization was performed with proportion of chloroform (C), methanol (M) and water (W) for the extraction of specific metabolic pathways of interest. Loading Bi-plots from the PLS regression model revealed that high concentration of chloroform emphasized the extraction of short chain fatty acids and TCA intermediates, while the higher concentration of methanol emphasized indole and phenyl derivatives...
December 1, 2017: Analytica Chimica Acta
https://www.readbyqxmd.com/read/29124635/atropisomers-of-2-2-3-3-6-6-hexachlorobiphenyl-pcb-136-exhibit-stereoselective-effects-on-activation-of-nuclear-receptors-in-vitro
#6
Kateřina Pěnčíková, Petra Brenerová, Lucie Svržková, Eva Hrubá, Lenka Pálková, Jan Vondráček, Hans-Joachim Lehmler, Miroslav Machala
PCB 136 is an environmentally relevant chiral PCB congener, which has been found in vivo to be present in form of rotational isomers (atropisomers). Its atropselective biotransformation or neurotoxic effects linked with sensitization of ryanodine receptor suggest that it might interact also with other intracellular receptors in a stereospecific manner. However, possible atropselective effects of PCB 136 on nuclear receptor transactivation remain unknown. Therefore, in this study, atropselective effects of PCB 136 on nuclear receptors controlling endocrine signaling and/or expression of xenobiotic and steroid hormone catabolism were investigated...
November 9, 2017: Environmental Science and Pollution Research International
https://www.readbyqxmd.com/read/29123941/bile-acids-as-global-regulators-of-hepatic-nutrient-metabolism
#7
Phillip B Hylemon, Kazuaki Takabe, Mikhail Dozmorov, Masayuki Nagahashi, Huiping Zhou
Bile acids (BA) are synthesized from cholesterol in the liver. They are essential for promotion of the absorption of lipids, cholesterol, and lipid-soluble vitamins from the intestines. BAs are hormones that regulate nutrient metabolism by activating nuclear receptors (farnesoid X receptor (FXR), pregnane X receptor, vitamin D) and G protein-coupled receptors (e.g., TGR5, sphingosine-1-phosphate receptor 2 (S1PR2)) in the liver and intestines. In the liver, S1PR2 activation by conjugated BAs activates the extracellular signal-regulated kinase 1/2 and AKT signaling pathways, and nuclear sphingosine kinase 2...
June 2017: Liver Res
https://www.readbyqxmd.com/read/29123032/pregnane-x-receptor-promotes-ethanol-induced-hepatosteatosis-in-mice
#8
Sora Choi, Prince Neequaye, Samuel W French, Frank J Gonzalez, Maxwell A Gyamfi
The pregnane X receptor (PXR, NR1I2) is a xenobiotic-sensing nuclear receptor that modulates the metabolic response to drugs and toxic agents. Both PXR activation and deficiency promote hepatic triglyceride accumulation, a hallmark feature of alcoholic liver disease (ALD). However, the molecular mechanism of PXR-mediated activation of ethanol (EtOH)-induced steatosis is unclear. Here, using male wild type (WT) and Pxr-null mice we examined PXR-mediated regulation of chronic EtOH-induced hepatic lipid accumulation and hepatotoxicity...
November 9, 2017: Journal of Biological Chemistry
https://www.readbyqxmd.com/read/29119010/epigenetic-impact-of-endocrine-disrupting-chemicals-on-lipid-homeostasis-and-atherosclerosis-a-pregnane-x-receptor-centric-view
#9
Robert N Helsley, Changcheng Zhou
Despite the major advances in developing diagnostic techniques and effective treatments, atherosclerotic cardiovascular disease (CVD) is still the leading cause of mortality and morbidity worldwide. While considerable progress has been achieved to identify gene variations and environmental factors that contribute to CVD, much less is known about the role of "gene-environment interactions" in predisposing individuals to CVD. Our chemical environment has significantly changed in the last few decades, and there are more than 100,000 synthetic chemicals in the market...
October 1, 2017: Environmental Epigenetics
https://www.readbyqxmd.com/read/29117101/hepatotoxicity-of-herbal-supplements-mediated-by-modulation-of-cytochrome-p450
#10
REVIEW
Christopher Trent Brewer, Taosheng Chen
Herbal supplements are a significant source of drug-drug interactions (DDIs), herb-drug interactions, and hepatotoxicity. Cytochrome P450 (CYP450) enzymes metabolize a large number of FDA-approved pharmaceuticals and herbal supplements. This metabolism of pharmaceuticals and supplements can be augmented by concomitant use of either pharmaceuticals or supplements. The xenobiotic receptors constitutive androstane receptor (CAR) and the pregnane X receptor (PXR) can respond to xenobiotics by increasing the expression of a large number of genes that are involved in the metabolism of xenobiotics, including CYP450s...
November 8, 2017: International Journal of Molecular Sciences
https://www.readbyqxmd.com/read/29113993/pxr-more-than-just-a-master-xenobiotic-receptor
#11
Peter Oladimeji, Taosheng Chen
Pregnane X receptor (PXR) is a nuclear receptor considered to be a master xenobiotic receptor that coordinately regulates the expression of genes encoding drug-metabolizing enzymes and drug transporters, to essentially detoxify and eliminate xenobiotics and endotoxins from the body. In the past several years, the function of PXR in the regulation of xenobiotic metabolism has been extensively studied, and the role of PXR as a xenobiotic sensor has been well-established. It is now clear, however, that PXR plays many other roles in addition to its xenobiotic sensing function...
November 7, 2017: Molecular Pharmacology
https://www.readbyqxmd.com/read/29112465/high-throughput-screening-identifies-1-4-5-substituted-1-2-3-triazole-analogs-as-potent-and-specific-antagonists-of-pregnane-x-receptor
#12
Wenwei Lin, Asli N Goktug, Jing Wu, Duane G Currier, Taosheng Chen
Human pregnane X receptor (hPXR) is a nuclear receptor that regulates the expression of phase I and phase II drug-metabolism enzymes, as well as that of drug transporters. hPXR is a "xenobiotics sensor" and can be activated by structurally diverse compounds. The activation of hPXR by its agonists increases the clearance of xenobiotics by increasing the expression of drug-metabolism enzymes and drug transporters, possibly leading to drug toxicity, drug resistance, and other adverse drug reactions. Therefore, hPXR antagonists might attenuate agonist-mediated activation of hPXR and reduce the risk of adverse drug reactions...
November 7, 2017: Assay and Drug Development Technologies
https://www.readbyqxmd.com/read/29107179/uptake-and-metabolism-of-water-borne-progesterone-by-the-mussel-mytilus-spp-mollusca
#13
Tamar I Schwarz, Ioanna Katsiadaki, Benjamin H Maskrey, Alexander P Scott
Previous studies have shown that mussels can pick up 17β-estradiol [E2] and testosterone [T] from water, metabolize them and conjugate them to fatty acids (esterification), leading to their accumulation in tissue. A key requirement for the esterification process is that a steroid must have a 'reactive' hydroxyl group to conjugate to a fatty acid (which in T, and probably E2, is the β-hydroxyl group on carbon 17). Progesterone (P) lacks any hydroxyl groups and theoretically cannot be esterified and hence should not accumulate in mussels in the same way as E2 or T...
October 26, 2017: Journal of Steroid Biochemistry and Molecular Biology
https://www.readbyqxmd.com/read/29105855/dicloxacillin-induces-cyp2c19-cyp2c9-and-cyp3a4-in-vivo-and-in-vitro
#14
Tore Bjerregaard Stage, Magnus Graff, Susan Wong, Louise Ladebo Rasmussen, Flemming Nielsen, Anton Pottegård, Kim Brøsen, Deanna L Kroetz, S Cyrus Khojasteh, Per Damkier
AIM: The aim of this study was to study potential cytochrome P450 induction by dicloxacillin. METHODS: We performed an open-label randomized two-phase 5-drug clinical pharmacokinetic cocktail crossover study in 12 healthy men with and without pretreatment with 1g dicloxacillin three times daily for 10 days. Plasma and urine was collected over 24 hours and the concentration of all five drugs and their primary metabolites was determined using a LC-MS/MS method. Cryopreserved primary human hepatocytes were exposed to dicloxacillin for 48h and changes in gene expression and enzyme activity of CYP3A4, CYP2C9, CYP2B6 and CYP1A2 was investigated...
November 4, 2017: British Journal of Clinical Pharmacology
https://www.readbyqxmd.com/read/29100690/diclofenac-exposure-alter-the-expression-of-pxr-and-its-downstream-target-genes-in-mosquito-fish-gambusia-affinis
#15
Shuang Bao, Xiangping Nie, Yang Liu, Chao Wang, Wenlong Li, Sijia Liu
As one of widely used drugs, Diclofenac (DCF) recently has been universally detected in aquatic environment and some negative effects derived from DCF exposure to mammals have been also reported. However, studies about its potential deleterious effects on non-target organisms like fish still require more investigation. In this study an ubiquitous small freshwater invader species in Southern of China, mosquito fish (Gambusia affinis), was employed as test organism. We firstly cloned the crucial partial sequences of nucleus transcriptional factor related genes pregnane X receptor (PXR) and its downstream genes, including P-glycoprotein (P-gp), cytochrome 3A (CYP3A), multidrug resistance protein 2 (MRP2), glutathione peroxidase (GPx) and thioredoxin reductase (TXR) in mosquito fish...
October 31, 2017: Science of the Total Environment
https://www.readbyqxmd.com/read/29096313/regulation-of-pregnane-x-receptor-and-micrornas-on-detoxification-related-genes-expressions-in-mugilogobius-abei-under-the-exposure-to-diclofenac
#16
Peijia Ku, Chao Wang, Xiangping Nie, Ruikang Ou, Kaibing Li
Diclofenac (DCF) has been recognized as an emerging contaminant in aquatic environments. Though many studies have investigated the toxic effects of DCF in human and mammals, limited information is available for the responses of genes associated with detoxification metabolisms in non-target aquatic organisms such as fish. In the present study, a small benthic fish Mugilogobius abei, was chosen as the test organism and the effects of DCF on detoxification-related genes at transcriptional level in M. abei were investigated...
October 30, 2017: Environmental Pollution
https://www.readbyqxmd.com/read/29095659/indirect-activation-of-pregnane-x-receptor-in-the-induction-of-hepatic-cyp3a11-by-high-dose-rifampicin-in-mice
#17
Yuki Yamasaki, Kaoru Kobayashi, Asumi Inaba, Daisuke Uehara, Hiroki Tojima, Satoru Kakizaki, Kan Chiba
Rifampicin (RIF), a typical ligand of human pregnane X receptor (PXR), powerfully induces the expression of cytochrome P450 3A4 (CYP3A4) in humans. Although it is thought that RIF is not a ligand of rodent PXR, treatment with high-dose RIF (e.g., more than 20 mg/kg) increases the expression of CYP3A in the mouse liver. In this study, we investigated whether the induction of CYP3A by high-dose RIF in the mouse liver is mediated via indirect activation of mouse PXR (mPXR). The results showed that high-dose RIF increased the expression of CYP3A11 and other PXR-target genes in the liver of wild-type mice but not PXR-knockout mice...
November 2, 2017: Xenobiotica; the Fate of Foreign Compounds in Biological Systems
https://www.readbyqxmd.com/read/29074825/-update-on-recent-progress-in-vitamin-d-research-vitamin-d-receptor-and-the-nuclear-receptor-superfamily
#18
Makoto Makishima
The vitamin D receptor(VDR)is a ligand-dependent transcription factor of the nuclear receptor superfamily. VDR belongs to the NR1I subfamily along with other nuclear receptors involved in xenobiotic metabolism, such as pregnane X receptor. The oxysterol receptors liver X receptors α/β and the bile acid receptor farnesoid X receptor belong to the NR1H subfamily, which are closely related to the NR1I subfamily. NR1I and NR1H nuclear receptors form heterodimers with retinoid X receptor. The active form of vitamin D, 1α,25-dihydroxyvitamin D3[1,25(OH)2D3], acts as a physiological VDR ligand, and regulates various physiological processes, including calcium and bone metabolism, cellular growth and differentiation, immunity, and cardiovascular function...
2017: Clinical Calcium
https://www.readbyqxmd.com/read/29072505/profiling-of-anthocyanidins-against-transcriptional-activities-of-steroid-and-nuclear-receptors
#19
Barbora Pastorková, Petr Illés, Zdeněk Dvořák
The aim of current study was to evaluate the effect of the most common anthocyanidins (cyanidin, delphinidin, malvidin, pelargonidin, and peonidin) on the transcriptional activity of steroid and nuclear receptors. The activities of steroid receptors - progesterone receptor (PR), estrogen receptor (ER), androgen receptor (AR), glucocorticoid receptor (GR), and nuclear receptors - vitamin D receptor (VDR), retinoid X receptor (RXR), retinoic acid receptor (RAR), pregnane X receptor (PXR), and thyroid receptor (TR) were assessed using either stable transfected luciferase gene reporter cell lines or transiently transfected cell lines...
October 26, 2017: Drug and Chemical Toxicology
https://www.readbyqxmd.com/read/29071751/pxr-mediated-induction-of-cyp3a4-cyp1a2-and-p-gp-by-mitragyna-speciosa-and-its-alkaloids
#20
Vamshi K Manda, Bharathi Avula, Olivia R Dale, Zulfiqar Ali, Ikhlas A Khan, Larry A Walker, Shabana I Khan
Kratom (Mitragyna speciosa), a native herb of Southeast Asia, is widely known for its psychoactive properties. Recent increase in the use of kratom as a recreational drug has increased the risk of its interaction with conventional drugs if taken concomitantly. A few reports are available related to the effects of kratom on the activity of cytochrome P450 enzymes (CYPs), but there are no reports of its effects on pregnane X receptor (PXR), a transcription factor that regulates the expression of CYPs and P-glycoprotein (P-gp)...
October 26, 2017: Phytotherapy Research: PTR
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