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https://www.readbyqxmd.com/read/29150398/glycyrrhiza-glabra-extract-and-quercetin-reverses-cisplatin-resistance-in-triple-negative-mda-mb-468-breast-cancer-cells-via-inhibition-of-cytochrome-p450-1b1-enzyme
#1
Rajni Sharma, Linda Gatchie, Ibidapo S Williams, Shreyans K Jain, Ram A Vishwakarma, Bhabatosh Chaudhuri, Sandip B Bharate
The development of multi-drug resistance to existing anticancer drugs is one of the major challenges in cancer treatment. The over-expression of cytochrome P450 1B1 enzyme has been reported to cause resistance to cisplatin. With an objective to discover cisplatin-resistance reversal agents, herein, we report the evaluation of Glycyrrhiza glabra (licorice) extracts and its twelve chemical constituents for inhibition of CYP1B1 (and CYP1A1) enzyme in Sacchrosomes and live human cells. The hydroalcoholic extract showed potent inhibition of CYP1B1 in both Sacchrosomes as well as in live cells with IC50 values of 21 and 16 µg/mL, respectively...
November 7, 2017: Bioorganic & Medicinal Chemistry Letters
https://www.readbyqxmd.com/read/29145161/cyp450-enzyme-specific-enantioselective-species-specific-response-for-metalaxyl-in-in-vitro-hepatic-cells
#2
Wei Xie, Fangxing Yang
Although enantioselective accumulation of chiral pesticide has been reported in organisms, the mechanisms remain unclear. In this study, the effects of chiral pesticide metalaxyl on CYP1A1, CYP1A2, CYP2B1, CYP2B2, CYP2E1 and CYP3A were investigated in human hepatoma HepG2, rat hepatic H4IIE, chicken hepatic LMH and grass carp hepatic L8824 cells. Moreover, the residual concentrations and enantiomeric ratios (ERs) of metalaxyl were also detected in the medium. The results showed the responses of these CYP450s to metalaxyl were enzyme-dependent and species-dependent in the four cells...
November 13, 2017: Ecotoxicology and Environmental Safety
https://www.readbyqxmd.com/read/29144397/sulforaphane-alters-%C3%AE-naphthoflavone-induced-changes-in-activity-and-expression-of-drug-metabolizing-enzymes-in-rat-hepatocytes
#3
Kateřina Lněničková, Andrea Dymáková, Barbora Szotáková, Iva Boušová
Sulforaphane (SFN), an isothiocyanate found in cruciferous vegetables, exerts many beneficial effects on human health such as antioxidant, anti-inflammatory, and anticancer effects. The effect of SFN alone on drug-metabolizing enzymes (DMEs) has been investigated in numerous in vitro and in vivo models, but little is known about the effect of SFN in combination with cytochrome P450 (CYP) inducer. The aim of our study was to evaluate the effect of SFN on the activity and gene expression of selected DMEs in primary cultures of rat hepatocytes treated or non-treated with β-naphthoflavone (BNF), the model CYP1A inducer...
November 16, 2017: Molecules: a Journal of Synthetic Chemistry and Natural Product Chemistry
https://www.readbyqxmd.com/read/29143794/berberine-activates-aryl-hydrocarbon-receptor-but-suppresses-cyp1a1-induction-through-mir-21-3p-stimulation-in-mcf-7-breast-cancer-cells
#4
Sheng-Nan Lo, Chun-Wei Wang, Yueh-Shieh Chen, Chiung-Chiao Huang, Tian-Shung Wu, Lih-Ann Li, I-Jung Lee, Yune-Fang Ueng
Berberine and the methylenedioxy ring-opening derivatives palmatine and jatrorrhizine are active ingredients in immunomodulatory plants, such as goldenseal. This study aimed to illustrate the effects of protoberberines on aryl hydrocarbon receptor (AhR) activation and cytochrome P450 (CYP) 1 in the estrogen receptor (ER)α(+) MCF-7 breast cancer cells. Among protoberberines at non-cytotoxic concentrations (≤10 μM), berberine had the most potent and statistically significant effects on AhR activation and CYP1A1/1A2/1B1 mRNA induction...
October 28, 2017: Molecules: a Journal of Synthetic Chemistry and Natural Product Chemistry
https://www.readbyqxmd.com/read/29140133/ite-inhibits-growth-of-human-pulmonary-artery-endothelial-cells
#5
Ling-Pin Pang, Yan Li, Qing-Yun Zou, Chi Zhou, Wei Lei, Jing Zheng, Shi-An Huang
AIM: Pulmonary arterial hypertension (PAH), a deadly disorder is associated with excessive growth of human pulmonary artery endothelial (HPAECs) and smooth muscle (HPASMCs) cells. Current therapies primarily aim at promoting vasodilation, which only ameliorates clinical symptoms without a cure. 2-(1'H-indole-3'-carbonyl)-thiazole-4-carboxylic acid methyl ester (ITE) is an endogenous aryl hydrocarbon receptor (AhR) ligand, and mediates many cellular function including cell growth. However, the roles of ITE in human lung endothelial cells remain elusive...
October 2017: Experimental Lung Research
https://www.readbyqxmd.com/read/29138024/-e-3-3-4-5-trimethoxyphenyl-1-pyridin-4-yl-prop-2-en-1-one-a-heterocyclic-chalcone-is-a-potent-and-selective-cyp1a1-inhibitor-and-cancer-chemopreventive-agent
#6
Neill J Horley, Kenneth J M Beresford, Supriya Kaduskar, Prashant Joshi, Glen J P McCann, Ketan C Ruparelia, Ibidapo S Williams, Linda Gatchie, Vinay R Sonawane, Sandip B Bharate, Bhabatosh Chaudhuri
The overexpression of CYP1 family of enzymes is reported to be associated with development of human carcinomas. It has been well reported that CYP1A1 specific inhibitors prevents carcinogenesis. Herein, thirteen pyridine-4-yl series of chalcones were synthesized and screened for inhibition of CYP1 isoforms 1A1, 1B1 and 1A2 in Sacchrosomes™ and live human HEK293 cells. The structure-activity relationship analysis indicated that chalcones bearing tri-alkoxy groups (8a and 8k) on non-heterocyclic ring displayed selective inhibition of CYP1A1 enzyme, with IC50 values of 58 and 65 nM, respectively...
November 6, 2017: Bioorganic & Medicinal Chemistry Letters
https://www.readbyqxmd.com/read/29134945/drug-drug-interaction-potential-of-the-hepatitis-b-and-hepatitis-d-virus-entry-inhibitor-myrcludex-b-assessed-in-vitro
#7
Antje Blank, Katrin Meier, Stephan Urban, Walter Emil Haefeli, Johanna Weiss
BACKGROUND: Myrcludex B is a first-in-class virus entry inhibitor for patients with chronic hepatitis B or B/D infections. In patients it will be co-administered with drugs needed for the disease or comorbidities. We aimed to define the risk of drug-drug interactions by characterizing the influence of myrcludex B on relevant drug transporting and metabolizing enzymes in vitro. METHODS: Inhibition of P-glycoprotein (P-gp, ABCB1), breast cancer resistance protein (BCRP/ABCG2), and the organic anion transporting polypeptides 1B1 and 1B3 (OATP1B1/SLCO1B1 and OATP1B3/SLCO1B3) was measured in cells over-expressing the respective transporter using fluorogenic substrates...
November 14, 2017: Antiviral Therapy
https://www.readbyqxmd.com/read/29126429/rna-sequencing-analysis-of-lung-primary-fibroblast-response-to-eosinophil-degranulation-products-predicts-downstream-effects-on-inflammation-tissue-remodeling-and-lipid-metabolism
#8
Stephane Esnault, Ksenija Bernau, Elizabeth E Torr, Yury A Bochkov, Nizar N Jarjour, Nathan Sandbo
BACKGROUND: The association of eosinophils with inflammation and tissue remodeling is at least partially due to their release of toxic granule proteins and other mediators, including cytokines. Tissue remodeling and consequent functional defects are affected by activity of connective tissue fibroblasts. Exaggerated fibroblast activation, accumulation and change of phenotype may lead to fibrosis and loss of tissue function. So far, little information has been reported on how eosinophils affect inflammation and tissue remodeling via the activation of fibroblasts...
November 10, 2017: Respiratory Research
https://www.readbyqxmd.com/read/29125538/cigarette-smoke-regulates-the-competitive-interactions-between-nrf2-and-bach1-for-heme-oxygenase-1-induction
#9
Wen-Hsin Chang, Philip Thai, Jihao Xu, David C Yang, Reen Wu, Ching-Hsien Chen
Cigarette smoke has been shown to trigger aberrant signaling pathways and pathophysiological processes; however, the regulatory mechanisms underlying smoke-induced gene expression remain to be established. Herein, we observed that two smoke-responsive genes, HO-1 and CYP1A1, are robustly induced upon smoke by different mechanisms in human bronchial epithelia. CYP1A1 is mediated by aryl hydrocarbon receptor signaling, while induction of HO-1 is regulated by oxidative stress, and suppressed by N-acetylcysteine treatment...
November 10, 2017: International Journal of Molecular Sciences
https://www.readbyqxmd.com/read/29121949/quantifying-engineered-nanomaterial-toxicity-comparison-of-common-cytotoxicity-and-gene-expression-measurements
#10
Donald H Atha, Amber Nagy, Andrea Steinbrück, Allison M Dennis, Jennifer A Hollingsworth, Varsha Dua, Rashi Iyer, Bryant C Nelson
BACKGROUND: When evaluating the toxicity of engineered nanomaterials (ENMS) it is important to use multiple bioassays based on different mechanisms of action. In this regard we evaluated the use of gene expression and common cytotoxicity measurements using as test materials, two selected nanoparticles with known differences in toxicity, 5 nm mercaptoundecanoic acid (MUA)-capped InP and CdSe quantum dots (QDs). We tested the effects of these QDs at concentrations ranging from 0.5 to 160 µg/mL on cultured normal human bronchial epithelial (NHBE) cells using four common cytotoxicity assays: the dichlorofluorescein assay for reactive oxygen species (ROS), the lactate dehydrogenase assay for membrane viability (LDH), the mitochondrial dehydrogenase assay for mitochondrial function, and the Comet assay for DNA strand breaks...
November 9, 2017: Journal of Nanobiotechnology
https://www.readbyqxmd.com/read/29115507/cytochrome-p450-1a1-and-1b1-promoter-cpg-island-methylation-regulates-rat-liver-injury-induced-by-isoniazid
#11
Yanhui Li, Yuhong Li, Guoying Zheng, Lingyan Zhu, Jishun Wang, Shasha Mu, Qi Ren, Fumin Feng
DNA methylation is an important component of epigenetics that is involved in the occurrence and development of a variety of diseases. The present study aimed to clarify the relationship between cytochrome P450 (CYP)1A1 and CYP1B1 promoter CpG island methylation and isoniazid‑induced liver injury in rats, and to explore the possible mechanism, rats were given an intragastric dose of isoniazid (55 mg·kg‑1·d‑1). High performance liquid chromatography was used to analyze the DNA methylation level of the whole genome in liver tissue...
October 31, 2017: Molecular Medicine Reports
https://www.readbyqxmd.com/read/29107029/transcriptional-inhibition-of-tcdd-mediated-induction-of-cytochrome-p450-1a1-and-alteration-of-protein-expression-in-a-zebrafish-hepatic-cell-line-following-the-administration-of-tcdd-and-cd-2
#12
Ying Ying Chen, King Ming Chan
We studied the effects of Cd(2+) on TCDD-mediated induction of the cytochrome P450 1A1 (cyp1a1) gene using a zebrafish liver cell line (ZFL). Our results showed that Cd(2+) inhibited the TCDD-mediated induction of the cyp1a1 protein, enzyme activity, and mRNA expression level. Cd(2+) also down-regulated levels of the aryl hydrocarbon receptor (ahr2) and the aryl hydrocarbon receptor nuclear translocator 2b (arnt2b) mRNAs. Compared with TCDD (3nM) treatment alone, co-treatment with Cd(2+) (0-30μM) and TCDD (3nM) significantly inhibited the activity of the luciferase reporter gene constructs harboring the distal promoter region (P-2626/-2009) of CYP1A1 and the synthetic 3XRE gene promoter...
October 26, 2017: Toxicology Letters
https://www.readbyqxmd.com/read/29104633/echinocystic-acid-ameliorates-hyperhomocysteinemia-induced-vascular-endothelial-cell-injury-through-regulating-nf-%C3%AE%C2%BAb-and-cyp1a1
#13
Chuan-Feng Huang, Wei-Na Wang, Cheng-Cao Sun, Yu-Qing Wang, Ling Li, Yin Li, De-Jia Li
The present study investigated the role of echinocystic acid (EA) on the expression of nuclear factor (NF)-κB and cytochrome P450 1A1 (CYP1A1), and aortic morphology, in a rat model of hyperhomocysteinemia (Hhcy). A total of 50 Sprague Dawley rats were randomly divided into five groups as follows: Normal control (NC), model control (MC), vitamin control (VC; folic acid 1 mg/kg + vitamin B2 2 mg/kg + vitamin B12 10u g/kg), EA1 (20 mg/kg EA) and EA2 (40 mg/kg EA). Plasma homocysteine (Hcy) levels were determined via high performance liquid chromatography, and the morphology of the aorta was investigated using hematoxylin and eosin staining...
November 2017: Experimental and Therapeutic Medicine
https://www.readbyqxmd.com/read/29104317/comparison-of-human-cytochrome-p450-1a1-catalysed-oxidation-of-benzo-a-pyrene-in-prokaryotic-and-eukaryotic-expression-systems
#14
Marie Stiborová, Radek Indra, Michaela Moserová, Lucie Bořek-Dohalská, Petr Hodek, Eva Frei, Klaus Kopka, Heinz H Schmeiser, Volker M Arlt
Abstract: Cytochrome P450 (CYP) 1A1 is the most important enzyme activating and detoxifying the human carcinogen benzo[a]pyrene (BaP). In the previous studies, we had shown that not only the canonic NADPH:CYP oxidoreductase (POR) can act as electron donor but also cytochrome b5 and its reductase, NADH:cytochrome b5 reductase. Here, we studied the role of the expression system used on the metabolites generated and the levels of DNA adducts formed by activated BaP. We used an eukaryotic and a prokaryotic cellular system (Supersomes, microsomes isolated from insect cells, and Bactosomes, a membrane fraction of Escherichia coli, each transfected with cDNA of human CYP1A1 and POR)...
2017: Monatshefte Für Chemie
https://www.readbyqxmd.com/read/29101037/hyperoxia-mediated-transcriptional-activation-of-cytochrome-p4501a1-cyp1a1-and-decreased-susceptibility-to-oxygen-mediated-lung-injury-in-newborn-mice
#15
Weiwu Jiang, Paramahamsa Maturu, Yanhong Wei Liang, Lihua Wang, Krithika Lingappan, Xanthi Couroucli
Hyperoxia contributes to the development of bronchopulmonary dysplasia (BPD) in premature infants. In this study, we tested the hypothesis that newborn transgenic mice carrying the human CYP1A1-Luc promoter will display transcriptional activation of the human CYP1A1 promoter in vivo upon exposure to hyperoxia, and that these mice will be less susceptible to hyperoxic lung injury and alveolar simplification than similarly exposed wild type (WT) mice. Newborn WT (CD-1) or transgenic mice carrying a 13.2 kb human CYP1A1 promoter and the luciferase (Luc) reporter gene (CYP1A1-luc) were maintained in room air or exposed to hyperoxia (85% O2) for 7-14 days...
October 31, 2017: Biochemical and Biophysical Research Communications
https://www.readbyqxmd.com/read/29100208/differential-exposure-and-acute-health-impacts-of-inhaled-solid-fuel-emissions-from-rudimentary-and-advanced-cookstoves-in-female-cd-1-mice
#16
Eugene A Gibbs-Flournoy, M Ian Gilmour, Mark Higuchi, James Jetter, Ingrid George, Lisa Copeland, Randy Harrison, Virginia C Moser, Janice A Dye
BACKGROUND: There is an urgent need to provide access to cleaner end user energy technologies for the nearly 40% of the world's population who currently depend on rudimentary cooking and heating systems. Advanced cookstoves (CS) are designed to cut emissions and solid-fuel consumption, thus reducing adverse human health and environmental impacts. STUDY PREMISE: We hypothesized that, compared to a traditional (Tier 0) three-stone (3-S) fire, acute inhalation of solid-fuel emissions from advanced natural-draft (ND; Tier 2) or forced-draft (FD; Tier 3) stoves would reduce exposure biomarkers and lessen pulmonary and innate immune system health effects in exposed mice...
October 31, 2017: Environmental Research
https://www.readbyqxmd.com/read/29100118/in%C3%A2-vitro-effects-of-diosmin-naringenin-quercetin-and-indole-3-carbinol-on-fish-hepatic-cyp1a1-in-the-presence-of-clotrimazole-and-dexamethasone
#17
Sidika Sakalli, Viktoriia Burkina, Nadezhda Pilipenko, Vladimir Zlabek, Galia Zamaratskaia
Phytochemicals are widely present in fruits, vegetables and other plants and have great health benefits owing to their antioxidant properties. They are naturally found in the aquatic environment as well as discharged from sewage treatment plants after their large consumption. Little is known about their impact on fish; particularly in light of their interactions with pharmaceuticals. Therefore, this study was designed to determine the effects of diosmin, naringenin, quercetin and idole-3-carbinol on CYP1A-dependent 7-ethoxyresorufin-O-deethylase (EROD) activity on rainbow trout hepatic microsomes in the presence of two pharmaceuticals: clotrimazole and dexamethasone...
October 23, 2017: Chemosphere
https://www.readbyqxmd.com/read/29098061/%C3%AE-naphthoflavone-induced-mitochondrial-respiratory-damage-in-cyp1-knockout-mouse-and-in-cell-culture-systems-attenuation-by-resveratrol-treatment
#18
Suresh Kumar Anandasadagopan, Naveen M Singh, Haider Raza, Seema Bansal, Venkatesh Selvaraj, Shilpee Singh, Anindya Roy Chowdhury, Nicolae Adrian Leu, Narayan G Avadhani
A number of xenobiotic-inducible cytochrome P450s (CYPs) are now known to be localized in the mitochondrial compartment, though their pharmacological or toxicological roles remain unclear. Here, we show that BNF treatment markedly inhibits liver mitochondrial O2 consumption rate (OCR), ADP-dependent OCR, and also reserve OCR, in wild-type mice but not in Cyp1a1/1a2(-/-) double knockout mice. BNF treatment markedly affected mitochondrial complex I and complex IV activities and also attenuated mitochondrial gene expression...
2017: Oxidative Medicine and Cellular Longevity
https://www.readbyqxmd.com/read/29097115/cytochrome-p450-cyp1-metabolism-of-hydroxylated-flavones-and-flavonols-selective-bioactivation-of-luteolin-in-breast-cancer-cells
#19
Nicola E Wilsher, Randolph R Arroo, Minos-Timotheos Matsoukas, Aristidis M Tsatsakis, Demetrios A Spandidos, Vasilis P Androutsopoulos
Natural flavonoids with methoxy substitutions are metabolized by CYP1 enzymes to yield the corresponding demethylated products. The present study aimed to characterize the metabolism and further antiproliferative activity of the hydroxylated flavonoids apigenin, luteolin, scutellarein, kaempferol and quercetin in CYP1 recombinant enzymes and in the CYP1 expressing cell lines MCF7 and MDA-MB-468, respectively. Apigenin was converted to luteolin and scutellarein, whereas kaempferol was metabolized only to quercetin by recombinant CYP1 enzymes...
October 31, 2017: Food and Chemical Toxicology
https://www.readbyqxmd.com/read/29094188/changes-in-the-expression-of-genes-involved-in-the-ovarian-function-of-rats-caused-by-daily-exposure-to-3-methylcholanthrene-and-their-prevention-by-%C3%AE-naphthoflavone
#20
Eric Alejandro Rhon-Calderón, Carlos Alejandro Toro, Alejandro Lomniczi, Rocío Alejandra Galarza, Alicia Graciela Faletti
Daily exposure to low doses of 3-methylcholanthrene (3MC) during the pubertal period in rats disrupts both follicular growth and ovulation. Thus, to provide new insights into the toxicity mechanism of 3MC in the ovary, here we investigated the effect of daily exposure to 3MC on selected ovarian genes, the role of the aryl hydrocarbon receptor (AhR) and the level of epigenetic remodeling of histone post-transcriptional modifications. Immature rats were daily injected with 3MC (0.1 or 1 mg/kg) and mRNA expression of genes involved in different ovarian processes were evaluated...
November 1, 2017: Archives of Toxicology
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