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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
#1
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/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
#2
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/29136681/assessment-of-multiple-cytochrome-p450-activities-in-metabolically-inactivated-human-liver-microsomes-and-roles-of-p450-2c-isoforms-in-reaction-phenotyping-studies
#3
Norie Murayama, Kanako Yajima, Mikiko Hikawa, Kanami Shimura, Yu Ishii, Masaki Takada, Yasuhiro Uno, Masahiro Utoh, Kazuhide Iwasaki, Hiroshi Yamazaki
The fraction of substrate metabolized (fm ) can be used to estimate drug interactions and can be determined by comparison of the intrinsic clearances (CLint ) of victim drugs obtained from inhibited and uninhibited hepatic enzymes. Commercially available human liver microsomes were recently developed in which one cytochrome P450 (P450) isoform is selectively inactivated. These inactivated liver microsomes were used to evaluate the roles of P450 2C isoforms in the depletion and oxidation of probe substrates...
November 14, 2017: Biopharmaceutics & Drug Disposition
https://www.readbyqxmd.com/read/29133569/efficacy-of-tilorone-dihydrochloride-against-ebola-virus-infection
#4
Sean Ekins, Mary A Lingerfelt, Jason E Comer, Alexander N Freiberg, Jon C Mirsalis, Kathleen O'Loughlin, Anush Harutyunyan, Claire McFarlane, Carol E Green, Peter B Madrid
Tilorone dihydrochloride (tilorone) is a small-molecule, orally bioavailable drug that is used clinically as an antiviral outside of the US. A machine learning model trained on anti-Ebola virus (EBOV) screening data previously identified tilorone as a potent in vitro EBOV inhibitor, making it a candidate for the treatment of Ebola virus disease (EVD). In the present study, a series of in vitro ADMET (absorption, distribution, metabolism, excretion, toxicity) assays demonstrated the drug has excellent solubility, high Caco-2 permeability, was not a P-glycoprotein substrate and had no inhibitory activity against five human CYP450 enzymes (3A4, 2D6, 2C19, 2C9 and 1A2)...
November 13, 2017: Antimicrobial Agents and Chemotherapy
https://www.readbyqxmd.com/read/29120380/in-vitro-phase-i-metabolism-of-crv431-a-novel-oral-drug-candidate-for-chronic-hepatitis-b
#5
Daniel J Trepanier, Daren R Ure, Robert T Foster
The cytochrome P450-mediated Phase I in vitro metabolism of CRV431 was studied using selective chemical inhibition and recombinant human enzymes. Additionally, the metabolic profile of CRV431 in human, rat, and monkey liver microsomes was investigated. Liver microsomes were incubated for 0-80 min with CRV431, and the metabolite profile was assessed by electrospray ionization liquid chromatography mass spectrometry (ESI-LCMS). CRV431 was extensively metabolized through oxidation to produce various hydroxylated and demethylated species...
November 9, 2017: Pharmaceutics
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
#6
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/29039463/hepatic-differentiation-of-human-ipscs-in-different-3d-models-a-comparative-study
#7
Florian Meier, Nora Freyer, Joanna Brzeszczynska, Fanny Knöspel, Lyle Armstrong, Majlinda Lako, Selina Greuel, Georg Damm, Eva Ludwig-Schwellinger, Ulrich Deschl, James A Ross, Mario Beilmann, Katrin Zeilinger
Human induced pluripotent stem cells (hiPSCs) are a promising source from which to derive distinct somatic cell types for in vitro or clinical use. Existent protocols for hepatic differentiation of hiPSCs are primarily based on 2D cultivation of the cells. In the present study, the authors investigated the generation of hiPSC-derived hepatocyte-like cells using two different 3D culture systems: A 3D scaffold-free microspheroid culture system and a 3D hollow-fiber perfusion bioreactor. The differentiation outcome in these 3D systems was compared with that in conventional 2D cultures, using primary human hepatocytes as a control...
October 16, 2017: International Journal of Molecular Medicine
https://www.readbyqxmd.com/read/29017580/a-retrospective-analysis-of-the-intertan-nail-and-proximal-femoral-nail-anti-rotation-in-the-treatment-of-intertrochanteric-fractures-in-elderly-patients-with-osteoporosis-a-minimum-follow-up-of-3%C3%A2-years
#8
Hui Zhang, Xiaoxiao Zhu, Genwang Pei, Xianshang Zeng, Nan Zhang, Ping Xu, Deng Chen, Weiguang Yu, Xinchao Zhang
BACKGROUND: The study aims to compare the long-term functional and radiographic outcomes of two devices for the treatment of primary intertrochanteric fractures (IFs, OTA 3.1A2.1-A2.3) in elderly patients with osteoporosis. METHODS: Between December 2010 and August 2014, 332 elderly osteoporosis patients with IFs (OTA 3.1A2.1-A2.3) fixed by an InterTAN nail (IT) or a proximal femoral nail anti-rotation (PFNA) device were retrospectively evaluated. Follow-up occurred 1, 3, 6, and 12 months postoperatively and every year thereafter...
October 10, 2017: Journal of Orthopaedic Surgery and Research
https://www.readbyqxmd.com/read/28994497/effects-of-vernonia-cinerea-compounds-on-drug-metabolizing-cytochrome-p450s-in-human-liver-microsomes
#9
Phisit Pouyfung, Songklod Sarapusit, Pornpimol Rongnoparut
Vernonia cinerea has been widely used in traditional medicines for various diseases and shown to aid in smoking abstinence and has anticancer properties. V. cinerea bioactive compounds, including flavonoids and hirsutinolide-type sesquiterpene lactones, have shown an inhibition effect on the nicotine-metabolizing cytochrome P450 2A6 (CYP2A6) enzyme and hirsutinolides reported suppressing cancer growth. In this study, V. cinerea ethanol extract and its bioactive compounds, including four flavonoids and four hirsutinolides, were investigated for an inhibitory effect on human liver microsomal CYPs 1A2, 2A6, 2B6, 2C8, 2C9, 2C19, 2D6, 2E1, and 3A4 using cocktail inhibition assays combined with LC-MS/MS analysis...
October 10, 2017: Phytotherapy Research: PTR
https://www.readbyqxmd.com/read/28992765/phenotyping-of-cyp-4501a2-activity-by-total-overnight-salivary-caffeine-assessment-tosca-in-patients-on-warfarin-treatment-a-cross-sectional-study
#10
Giovanni Tarantino, Domenico Capone, Paola Contaldi, Adriana Gianno, Mosca Teresa, Antonella Tufano
Warfarin is an oral anticoagulant, commonly used for primary and secondary prevention of venous and arterial thromboembolic events. The drug is characterized by narrow therapeutic index, widespread individual variability in clinical response, and high rates of adverse events, particularly bleeding complications. For these reasons, a close monitoring of the dosage, using the frequent assessment of coagulation status by means of International Normalized Ratio value, is mandatory. Warfarin is metabolized by hepatic cytochrome P-450...
January 1, 2017: Clinical and Applied Thrombosis/hemostasis
https://www.readbyqxmd.com/read/28960974/a-chemoproteomic-platform-to-assess-bioactivation-potential-of-drugs
#11
Rui Sun, Fuguo Shi, Keke Liu, Ling Fu, Caiping Tian, Yong Yang, Keri A Tallman, Ned A Porter, Jing Yang
Reactive metabolites (RM) formed from bioactivation of drugs can covalently modify liver proteins and cause mechanism-based inactivation of major cytochrome P450 (CYP450) enzymes. Risk of bioactivation of a test compound is routinely examined as part of lead optimization efforts in drug discovery. Here we described a chemoproteomic platform to assess in vitro and in vivo bioactivation potential of drugs. This platform enabled us to determine reactivity of thousands of proteomic cysteines toward RMs of diclofenac formed in human liver microsomes and living animals...
October 16, 2017: Chemical Research in Toxicology
https://www.readbyqxmd.com/read/28951593/microrna-regulation-of-cyp-1a2-cyp3a4-and-cyp2e1-expression-in-acetaminophen-toxicity
#12
Pritmohinder Gill, Sudeepa Bhattacharyya, Sandra McCullough, Lynda Letzig, Prasun J Mishra, Chunqiao Luo, Harsh Dweep, Laura James
MicroRNAs (miRNAs) that regulate the cytochrome P-450 isoforms involved in acetaminophen (APAP) toxicity were examined in HepaRG cells treated with APAP (20 mM). In-vitro studies found that APAP protein adducts were increased at 1 h, followed by ALT increases at 12 and 24 h. CYP1A2, CYP3A4 and CYP2E1 mRNA levels were decreased, while miRNAs were increased for miR-122-5p, miR-378a-5p, miR-27b-3p at 6 h and miR-125b-5p at 12 h and miR-27b-3p at 24 h. Putative miRNA binding sites on the 3'UTRs of the CYPs were identified in-silico...
September 26, 2017: Scientific Reports
https://www.readbyqxmd.com/read/28945081/direct-detection-of-the-open-shell-singlet-phenyloxenium-ion-an-atom-centered-diradical-reacts-as-an-electrophile
#13
Lili Du, Yunfan Qiu, Xin Lan, Ruixue Zhu, David Lee Phillips, Ming-De Li, Andrew S Dutton, Arthur H Winter
A new photoprecursor to the phenyloxenium ion, 4-methoxyphenoxypyridinium tetrafluoroborate, was investigated using trapping studies, product analysis, computational investigations, and laser flash photolysis experiments ranging from the femtosecond to the millisecond time scale. These experiments allowed us to trace the complete arc of the photophysics and photochemistry of this photoprecursor beginning with the initially populated excited states to its sequential formation of transient intermediates and ultimate formation of stable photoproducts...
October 17, 2017: Journal of the American Chemical Society
https://www.readbyqxmd.com/read/28934216/genetic-polymorphisms-of-cytochrome-p450-1a2-cyp1a2-among-emiratis
#14
Mohammad M Al-Ahmad, Naheed Amir, Subramanian Dhanasekaran, Anne John, Yousef M Abdulrazzaq, Bassam R Ali, Salim M A Bastaki
Cytochrome P450 1A2 (CYP1A2) is one of the CYP450 mixed-function oxidase system that is of clinical importance due to the large number of drug interactions associated with its induction and inhibition. In addition, significant inter-individual differences in the elimination of drugs metabolized by CYP1A2 enzyme have been observed which are largely due to the highly polymorphic nature of CYP1A2 gene. However, there are limited studies on CYP1A2 phenotypes and CYP1A2 genotypes among Emiratis and thus this study was carried out to fill this gap...
2017: PloS One
https://www.readbyqxmd.com/read/28930368/the-importance-of-polymorphic-variants-of-collagen-1a2-gene-col1a2-in-the-development-of-osteopenia-and-osteoporosis-in-postmenopausal-women
#15
Marian Majchrzycki, Joanna Bartkowiak-Wieczorek, Anna Bogacz, Joanna Szyfter-Harris, Hubert Wolski, Andrzej Klejewski, Maciej Goch, Krzysztof Drews, Magdalena Barlik, Marcin Ożarowski, Adam Kamiński, Agnieszka Gryszczyńska, Agnieszka Seremak-Mrozikiewicz
OBJECTIVES: Collagen type I plays an important role in the bone matrix and is encoded by COL1A2 (collagen type I alpha 2) gene that may be a potential candidate for osteoporotic fracture. The aim of this study is to determine whether EcoRI, Del38 and PvuII polymorphisms of COL1A2 are associated with the development of osteoporosis and osteopenia in post-menopausal Polish women. Moreover, analysis of relationship between frequency of COL1A2 gene polymorphic variants and clinical parameters of bone turnover and degree of osteoporosis was performed...
2017: Ginekologia Polska
https://www.readbyqxmd.com/read/28893642/enzyme-inducing-effects-of-berberine-on-cytochrome-p450-1a2-in-vitro-and-in-vivo
#16
Bo Jiang, Liyuan Meng, Feng Zhang, Xiaoling Jin, Guiliang Zhang
AIMS: Berberine (BER) is an important anti-bacterial drug from Chinese herbal medicine and a novel drug candidate for preclinical development in recent years. Here we provide evidence that the effects of berberine on cytochrome P450 (CYP) 1A2 in vitro and in vivo. MAIN METHODS: Real-time polymerase chain reaction and western blotting analysis were employed to evaluate the CYP1A2 mRNA levels and protein expression. The enzyme activity was assessed by the metabolic rate of phenacetin to acetaminophen by LC-MS/MS method...
November 15, 2017: Life Sciences
https://www.readbyqxmd.com/read/28879062/a-modeling-approach-to-evaluate-the-balance-between-bioactivation-and-detoxification-of-meiqx-in-human-hepatocytes
#17
Victorien Delannée, Sophie Langouët, Nathalie Théret, Anne Siegel
BACKGROUND: Heterocyclic aromatic amines (HAA) are environmental and food contaminants that are potentially carcinogenic for humans. 2-Amino-3,8-dimethylimidazo[4,5-f]quinoxaline (MeIQx) is one of the most abundant HAA formed in cooked meat. MeIQx is metabolized by cytochrome P450 1A2 in the human liver into detoxificated and bioactivated products. Once bioactivated, MeIQx metabolites can lead to DNA adduct formation responsible for further genome instability. METHODS: Using a computational approach, we developed a numerical model for MeIQx metabolism in the liver that predicts the MeIQx biotransformation into detoxification or bioactivation pathways according to the concentration of MeIQx...
2017: PeerJ
https://www.readbyqxmd.com/read/28841541/use-of-the-liver-maximum-function-capacity-test-limax-for-the-management-of-liver-resection-in-cirrhosis-a-case-of-hypopharyngeal-cancer-liver-metastasis
#18
S Cammann, F Oldhafer, K I Ringe, W Ramackers, K Timrott, M Kleine, J Klempnauer, F Lehner, H Bektas, F W R Vondran
INTRODUCTION: The presence of liver cirrhosis goes along with a higher chance for the need of liver resection. As established laboratory parameters often underestimate the degree of cirrhosis this is associated with an increased risk for postoperative liver failure due to the preoperatively impaired liver function. Known liver function tests are unlikely to be performed in daily use because of high cost or expenditure of time. Liver maximum function capacity test (LiMAx) provides a novel tool for measurement of liver function and references for the safety of liver resection...
2017: International Journal of Surgery Case Reports
https://www.readbyqxmd.com/read/28834279/the-cytochrome-p450-enzyme-responsible-for-the-production-of-z-norendoxifen-in-vitro
#19
Dabei Tang, Zhong Chu, Jessica Bo Li Lu, Jinzhong Liu, Qingyuan Zhang
BACKGROUND: Norendoxifen, an active metabolite of tamoxifen, is a potent aromatase inhibitor. Little information is available regarding production of norendoxifen in vitro. Here, we conducted a series of kinetic and inhibition studies in human liver microsomes (HLMs) and expressed P450s to study the metabolic disposition of norendoxifen. METHODS: To validate that norendoxifen was the metabolite of endoxifen, metabolites in HLMs incubates of endoxifen were measured using a HPLC/MS/MS method...
August 17, 2017: Chemistry & Biodiversity
https://www.readbyqxmd.com/read/28832650/fructose-diet-alleviates-acetaminophen-induced-hepatotoxicity-in-mice
#20
Sungjoon Cho, Ashutosh Tripathi, George Chlipala, Stefan Green, Hyunwoo Lee, Eugene B Chang, Hyunyoung Jeong
Acetaminophen (APAP) is a commonly used analgesic and antipyretic that can cause hepatotoxicity due to production of toxic metabolites via cytochrome P450 (Cyp) 1a2 and Cyp2e1. Previous studies have shown conflicting effects of fructose (the major component in Western diet) on the susceptibility to APAP-induced hepatotoxicity. To evaluate the role of fructose-supplemented diet in modulating the extent of APAP-induced liver injury, male C57BL/6J mice were given 30% (w/v) fructose in water (or regular water) for 8 weeks, followed by oral administration of APAP...
2017: PloS One
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