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https://www.readbyqxmd.com/read/27918128/mulberroside-a-suppresses-pxr-mediated-transactivation-and-gene-expression-of-p-gp-in-ls174t-cells
#1
Yuhua Li, Ling Huang, Jiahong Sun, Xiaohua Wei, Jinhua Wen, Guoping Zhong, Min Huang, Huichang Bi
Mulberroside A (Mul A) is the main bioactive constituents of Sangbaipi, which is officially listed in the Chinese Pharmacopoeia. The pregnane X receptor (PXR) has been recognized as the critical mediator of human P-glycoprotein (P-gp) gene transactivation. In this study, the effect of Mul A on PXR-mediated transactivation and gene expression of P-gp was investigated. It was found that Mul A significantly suppressed PXR-mediated P-gp luciferase activity induced by rifampicin (Rif). Furthermore, Rif induced an elevation of P-gp expression and transport activity, which was apparently suppressed by Mul A...
December 5, 2016: Journal of Biochemical and Molecular Toxicology
https://www.readbyqxmd.com/read/27899892/age-dependent-hepatic-udp-glucuronosyltransferase-gene-expression-and-activity-in-children
#2
Elizabeth Neumann, Huma Mehboob, Jacqueline Ramírez, Snezana Mirkov, Min Zhang, Wanqing Liu
UDP-glucuronosyltransferases (UGTs) are important phase II drug metabolism enzymes. The aim of this study was to explore the relationship between age and changes in mRNA expression and activity of major human hepatic UGTs, as well as to understand the potential regulatory mechanism underlying this relationship. Using previously generated data, we investigated age-dependent mRNA expression levels of 11 hepatic UGTs (UGT1A1, UGT1A3, UGT1A4, UGT1A5, UGT1A6, UGT1A9, UGT2B4, UGT2B7, UGT2B10, UGT2B15, and UGT2B17) and 16 transcription factors (AHR, AR, CAR, ESR2, FXR, GCCR, HNF1a, HNF3a, HNF3b, HNF4a, PPARA, PPARG, PPARGC, PXR, SP1, and STAT3) in liver tissue of donors (n = 38) ranging from 0 to 25 years of age...
2016: Frontiers in Pharmacology
https://www.readbyqxmd.com/read/27878971/pregnane-x-receptors-regulate-cyp2c8-and-p-glycoprotein-to-impact-on-the-resistance-of-nsclc-cells-to-taxol
#3
Yan Chen, Wandan Huang, Feiyu Chen, Guoping Hu, Fenglei Li, Jianhua Li, Aiguo Xuan
Cytochrome P450 2C8 (CYP2C8) is one of the enzymes that primarily participate in producing metabolisms of medications and P-glycoprotein (P-gp) has been regarded as one of the important molecules in chemotherapeutically induced multidrug resistance (MDR). In addition, the pregnane X receptor (PXR) is involved in regulating both CYP2C8 and P-gp. We aim to research the effect of PXR on Taxol-resistant non-small-cell lung cancer (NSCLC cells) via regulating CYP2C8 and P-gp. NSCLC cells were treated with SR12813, LY335979, or PXR siRNA...
November 22, 2016: Cancer Medicine
https://www.readbyqxmd.com/read/27876007/effect-of-pregnane-x-receptor-1b-genetic-polymorphisms-on-postoperative-analgesia-with-fentanyl-in-chinese-patients-undergoing-gynecological-surgery
#4
Jing-Jing Yuan, Xiao-Jing Ma, Zhi-Song Li, Yan-Zi Chang, Wei Zhang, Quan-Cheng Kan, Jun-Kai Hou, Li-Rong Zhang
BACKGROUND: The purpose of the study was to investigate the effects of the pregnane X receptor (PXR)*1B polymorphisms on CYP3A4 enzyme activity and postoperative fentanyl consumption in Chinese patients undergoing gynecological surgery. METHODS: A total of 287 females of Han ethnicity, aged 20 to 50 years old, ASA I or II, scheduled to abdominal total hysterectomy or myomectomy under general anesthesia were enrolled. The analgesic model used was fentanyl consumption via patient-controlled intravenous analgesia (PCIA) in the post-operative period...
November 23, 2016: BMC Medical Genetics
https://www.readbyqxmd.com/read/27871908/acetylated-deoxycholic-dca-and-cholic-ca-acids-are-potent-ligands-of-pregnane-x-pxr-receptor
#5
Alejandro Carazo, Lucie Hyrsova, Jan Dusek, Hana Chodounska, Alzbeta Horvatova, Karel Berka, Vaclav Bazgier, Hongying Gan-Schreier, Waleé Chamulitrat, Eva Kudova, Petr Pavek
The Pregnane X (PXR), Vitamin D (VDR) and Farnesoid X (FXR) nuclear receptors have been shown to be receptors of bile acids controlling their detoxification or synthesis. Chenodeoxycholic (CDCA) and lithocholic (LCA) acids are ligands of FXR and VDR, respectively, whereas 3-keto and acetylated derivates of LCA have been described as ligands for all three receptors. In this study, we hypothesized that oxidation or acetylation at position 3, 7 and 12 of bile acids DCA (deoxycholic acid), LCA, CA (cholic acid), and CDCA by detoxification enzymes or microbiome may have an effect on the interactions with bile acid nuclear receptors...
November 18, 2016: Toxicology Letters
https://www.readbyqxmd.com/read/27871799/molecular-mechanisms-of-pfoa-induced-toxicity-in-animals-and-humans-implications-for-health-risks
#6
REVIEW
Kan Li, Peng Gao, Ping Xiang, Xuxiang Zhang, Xinyi Cui, Lena Q Ma
As an emerging persistent organic pollutant (POP), perfluorooctanoate (PFOA) is one of the most abundant perfluorinated compounds (PFCs) in the environment. This review summarized the molecular mechanisms and signaling pathways of PFOA-induced toxicity in animals and humans as well as their implications for health risks in humans. Traditional PFOA-induced signal pathways such as peroxisome proliferating receptor alpha (PPARα), constitutive androstane receptor (CAR), farnesoid X receptor (FXR), and pregnane-X receptor (PXR) may not be important for PFOA-induced health effects on humans...
November 18, 2016: Environment International
https://www.readbyqxmd.com/read/27856527/role-of-glucocorticoid-receptor-and-pregnane-x-receptor-in-dexamethasone-induction-of-rat-hepatic-aryl-hydrocarbon-receptor-nuclear-translocator-and-nadph-cytochrome-p450-oxidoreductase
#7
Sarah R Hunter, Alex Vonk, Anne K Mullen Grey, David S Riddick
The aryl hydrocarbon receptor (AHR) nuclear translocator (ARNT), as the AHR's heterodimerization partner, and NADPH-cytochrome P450 oxidoreductase (POR), as the key electron donor for all microsomal P450s, are independent and indispensable components in the adaptive and toxic responses to polycyclic aromatic hydrocarbons. Expression of both ARNT and POR in rat liver is induced by dexamethasone (DEX), a synthetic glucocorticoid known to activate both the glucocorticoid receptor (GR) and the pregnane X receptor (PXR)...
November 16, 2016: Drug Metabolism and Disposition: the Biological Fate of Chemicals
https://www.readbyqxmd.com/read/27853109/a-crucial-role-of-constitutive-androstane-receptor-car-in-liver-tumor-development-by-imazalil-in-mice
#8
Kei Tamura, Kaoru Inoue, Miwa Takahashi, Saori Matsuo, Yukio Kodama, Midori Yoshida
To clarify the major pathway of liver tumor development induced by imazalil (IMA), an imidazole fungicide, male constitutive androstane receptor (CAR)-knockout (CARKO) and wild-type (WT) mice were treated with IMA at 500 ppm in the diet up to 27 weeks after initiation by diethylnitrosamine. After 27 weeks of treatment, neither altered foci nor adenomas were significantly increased in CARKO mice, whereas both eosinophilic altered foci and adenomas were increased in WT mice. After 4 or 13 weeks of IMA treatment, liver hypertrophy was observed at the tumor-inducible dose without differences among genotypes or durations...
2016: Journal of Toxicological Sciences
https://www.readbyqxmd.com/read/27836114/66034t-c-polymorphism-of-the-human-pregnane-x-receptor-hpxr-as-potential-risk-factor-for-drug-resistance-in-epilepsy-preliminary-study
#9
Alicja Kozera-Kępniak, Karol Jastrzębski, Jakub Walenczak, Andrzej Klimek, Andrzej Głąbiński
INTRODUCTION AND OBJECTIVES: Recent research has suggested that genetic factors may play an important role in the development of drug resistance in epilepsy. It is not clear which gene loci are responsible for the drug-resistant phenotype. Studying certain nuclear receptors may be helpful in predicting drug response, as they regulate drug transporting proteins and enzymes involved in their metabolism. This study focuses on one of these receptors, the human pregnane X receptor (hPXR). The objective was to examine the link between selected single nucleotide polymorphisms (SNPs) 69789A/G rs 7643645 and 66034T/C rs 13059232 hPXR and the lack of response to epilepsy treatment...
October 17, 2016: Neurologia i Neurochirurgia Polska
https://www.readbyqxmd.com/read/27833556/increased-motor-impairing-effects-of-the-neuroactive-steroid-pregnanolone-in-mice-with-targeted-inactivation-of-the-gabaa-receptor-%C3%AE-2-subunit-in-the-cerebellum
#10
Elli Leppä, Anni-Maija Linden, Maria I Aller, Peer Wulff, Olga Vekovischeva, Bernhard Luscher, Hartmut Lüddens, William Wisden, Esa R Korpi
Endogenous neurosteroids and neuroactive steroids have potent and widespread actions on the brain via inhibitory GABAA receptors. In recombinant receptors and genetic mouse models their actions depend on the α, β, and δ subunits of the receptor, especially on those that form extrasynaptic GABAA receptors responsible for non-synaptic (tonic) inhibition, but they also act on synaptically enriched γ2 subunit-containing receptors and even on αβ binary receptors. Here we tested whether behavioral sensitivity to the neuroactive steroid agonist 5β-pregnan-3α-ol-20-one is altered in genetically engineered mouse models that have deficient GABAA receptor-mediated synaptic inhibition in selected neuronal populations...
2016: Frontiers in Pharmacology
https://www.readbyqxmd.com/read/27833169/effects-of-periplocoside-p-from-periploca-sepium-on-the-midgut-transmembrane-potential-of-mythimna-separata-larvae
#11
YingYing Wang, Zhijun Qi, Meng Qi, Zhaonong Hu, Wenjun Wu
Periplocoside P (PSP) isolated from the root bark of Periploca sepium contains a pregnane glycoside skeleton and possesses high insecticidal properties. Preliminary studies indicated that PSP disrupts epithelial functions in the midgut of lepidopteran larvae. In the present study, we examined the effects of PSP on the apical and basolateral membrane voltages, Va and Vbl, respectively, of cells from (1) midguts isolated from the larvae of the oriental armyworm Mythimna separata that were in vitro incubated with toxins and (2) midguts isolated from M...
November 11, 2016: Scientific Reports
https://www.readbyqxmd.com/read/27815157/excretion-and-measurement-of-corticosterone-and-testosterone-metabolites-in-bank-voles-myodes-glareolus
#12
Saana Sipari, Hannu Ylönen, Rupert Palme
The bank vole is a commonly used model species in behavioral and ecophysiological studies. Thus, presenting a validated method for noninvasive monitoring of corticosterone and testosterone secretion is of high relevance. Here, we evaluated the effect of time of day and an ACTH challenge test on measured fecal corticosterone (FCM) and testosterone (FTM) metabolites in both sexes. Furthermore, we performed radiometabolism experiments for both steroids and sexes to study metabolism and excretion of (3)H-corticosterone and (3)H-testosterone...
November 1, 2016: General and Comparative Endocrinology
https://www.readbyqxmd.com/read/27803452/mechanism-for-increased-expression-of-ugt2b-in-the-liver-of-mice-with-neuropathic-pain
#13
Mitsumasa Kaneta, Wataru Ochiai, Marina Nagae, Wataru Suto, Mika Hanagata, Haruka Suzuki, Satoshi Kitaoka, Jo Hatogai, Nobutomo Ikarashi, Kiyoshi Sugiyama
Approximately 30% of patients with cancer pain experience concurrent neuropathic pain. Since these patients are not sufficiently responsive to morphine, the development of an effective method of pain relief is urgently needed. Decreased function of the μ opioid receptor, which binds to the active metabolite of morphine M-6-G in the brain, has been proposed as a mechanism for morphine resistance. Previously, we pharmacokinetically examined morphine resistance in mice with neuropathic pain, and demonstrated that the brain morphine concentration was decreased, expression level of P-glycoprotein (P-gp) in the small intestine was increased, and expression level and activity of uridine diphosphate glucuronosyltransferase (UGT)2B in the liver were increased...
2016: Biological & Pharmaceutical Bulletin
https://www.readbyqxmd.com/read/27802245/progesterone-treatment-shows-greater-protection-in-brain-vs-retina-in-a-rat-model%C3%A2-of-middle-cerebral-artery-occlusion-progesterone-receptor-levels-may-play-an-important-role
#14
Rachael S Allen, Iqbal Sayeed, Yuliya Oumarbaeva, Katherine C Morrison, Paul H Choi, Machelle T Pardue, Donald G Stein
BACKGROUND/OBJECTIVE: To determine whether inflammation increases in retina as it does in brain following middle cerebral artery occlusion (MCAO), and whether the neurosteroid progesterone, shown to have protective effects in both retina and brain after MCAO, reduces inflammation in retina as well as brain. METHODS: MCAO rats treated systemically with progesterone or vehicle were compared with shams. Protein levels of cytosolic NF-κB, nuclear NF-κB, phosphorylated NF-κB, IL-6, TNF-α, CD11b, progesterone receptor A and B, and pregnane X receptor were assessed in retinas and brains at 24 and 48 h using western blots...
October 13, 2016: Restorative Neurology and Neuroscience
https://www.readbyqxmd.com/read/27799961/heterozygous-inactivation-of-the-nuclear-receptor-pxr-nr1i2-in-a-patient-with-anabolic-steroid-induced-intrahepatic-cholestasis
#15
Roman Liebe, Marcin Krawczyk, Joanna Raszeja-Wyszomirska, Beata Kruk, Rebecca Preis, Jocelyn Trottier, Olivier Barbier, Piotr Milkiewicz, Frank Lammert
INTRODUCTION: The incidence of liver damage due to steroid consumption is increasing due to the omnipresence of the idealized body image and the widespread availability of drugs via the Internet. The genetic factors underlying individual susceptibility are not presently known. CASE PRESENTATION: A male patient developed cholestatic liver injury two weeks after a two-month course of anabolic steroids. Next-generation sequencing (NGS) of 24 cholestasis-related genes revealed a heterozygous two-basepair deletion in exon 1 of the pregnane X receptor gene (PXR)...
August 2016: Hepatitis Monthly
https://www.readbyqxmd.com/read/27795941/a-molecular-aspect-in-the-regulation-of-drug-metabolism-does-pxr-induced-enzyme-expression-always-lead-to-functional-changes-in-drug-metabolism
#16
Yuan Wei, Chenxiao Tang, Vinayak Sant, Song Li, Samuel M Poloyac, Wen Xie
Pregnane X receptor (PXR, NR112) is a xenobiotic receptor whose primary function is to regulate the expression of drug-metabolizing enzymes (DMEs) and drug transporters. Drug-induced PXR activation and subsequent enzyme and transporter induction has been proposed to be an important mechanism for the drug-drug interactions. In addition to activating PXR, many pharmaceutical chemicals can also function as reversible or irreversible inhibitors of DMEs, which may also impact the pharmacokinetics and pharmacodynamics (PK/PD) of drugs...
August 2016: Current Pharmacology Reports
https://www.readbyqxmd.com/read/27773686/differential-modulation-of-fxr-activity-by-chlorophacinone-and-ivermectin-analogs
#17
Chia-Wen Hsu, Jui-Hua Hsieh, Ruili Huang, Dirk Pijnenburg, Thai Khuc, Jon Hamm, Jinghua Zhao, Caitlin Lynch, Rinie van Beuningen, Xiaoqing Chang, René Houtman, Menghang Xia
Chemicals that alter normal function of farnesoid X receptor (FXR) have been shown to affect the homeostasis of bile acids, glucose, and lipids. Several structural classes of environmental chemicals and drugs that modulated FXR transactivation were previously identified by quantitative high-throughput screening (qHTS) of the Tox21 10K chemical collection. In the present study, we validated the FXR antagonist activity of selected structural classes, including avermectin anthelmintics, dihydropyridine calcium channel blockers, 1,3-indandione rodenticides, and pyrethroid pesticides, using in vitro assay and quantitative structural-activity relationship (QSAR) analysis approaches...
December 15, 2016: Toxicology and Applied Pharmacology
https://www.readbyqxmd.com/read/27732883/optical-isomers-of-dihydropyridine-calcium-channel-blockers-display-enantiospecific-effects-on-the-expression-and-enzyme-activities-of-human-xenobiotics-metabolizing-cytochromes-p450
#18
Martina Štěpánková, Kristýna Krasulová, Aneta Dořičáková, Ondřej Kurka, Pavel Anzenbacher, Zdeněk Dvořák
Dihydropyridine calcium channel blockers (CCBs) are used as anti-hypertensives and in the treatment of angina pectoris. Structurally, CCBs have at least one chiral center in the molecule, thereby existing in two or more different enantiomers. In the current paper we examined effects of benidipine, felodipine and isradipine enantiomers on the expression and enzyme activities of human xenobiotics-metabolizing cytochromes P450. All CCBs dose-dependently activated aryl hydrocarbon receptor (AhR) and pregnane X receptor (PXR), as revealed by gene reporter assays...
October 9, 2016: Toxicology Letters
https://www.readbyqxmd.com/read/27732639/transactivation-assays-to-assess-canine-and-rodent-pregnane-x-receptor-pxr-and-constitutive-androstane-receptor-car-activation
#19
Marija Pinne, Elsa Ponce, Judy L Raucy
The pregnane X receptor (PXR/SXR, NR1I2) and constitutive androstane receptor (CAR, NR1I3) are nuclear receptors (NRs) involved in the regulation of many genes including cytochrome P450 enzymes (CYPs) and transporters important in metabolism and uptake of both endogenous substrates and xenobiotics. Activation of these receptors can lead to adverse drug effects as well as drug-drug interactions. Depending on which nuclear receptor is activated will determine which adverse effect could occur, making identification important...
2016: PloS One
https://www.readbyqxmd.com/read/27714977/the-long-chain-%C3%AE-tocopherol-metabolite-%C3%AE-13-cooh-and-%C3%AE-tocotrienol-induce-p-glycoprotein-expression-and-activity-by-activation-of-the-pregnane-x-receptor-in-the-intestinal-cell-line-ls-180
#20
Maren C Podszun, Metta Jakobi, Marc Birringer, Johanna Weiss, Jan Frank
SCOPE: Members of the vitamin E family or their metabolites may induce the xenobiotic transporter P-glycoprotein (P-gp), which can limit the bioavailability of drugs and phytochemicals. This study aimed to investigate if α- and γ-tocopherol, α- and γ-tocotrienol, the long chain metabolite α-tocopherol-13'-COOH, the short chain metabolites α- and γ-carboxyethylhydroxychromanol and plastochromanol-8 activate the pregnane X receptor (PXR) and thereby modulate P-gp expression and/or activity...
October 6, 2016: Molecular Nutrition & Food Research
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