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https://www.readbyqxmd.com/read/28454244/proliferation-of-sphere-forming-hepatocellular-carcinoma-cells-is-suppressed-in-a-medium-without-glucose-and-arginine-but-with-galactose-and-ornithine
#1
Minoru Tomizawa, Fuminobu Shinozaki, Yasufumi Motoyoshi, Takao Sugiyama, Shigenori Yamamoto, Naoki Ishige
Resistance to sorafenib in hepatocellular carcinoma (HCC) cells exhibiting stemness was evaluated using a sphere formation assay. A hepatocyte selection medium (HSM) deficient in glucose and arginine was used to suppress the proliferation of cell spheres composed of HLF and PLC/PRF/5 HCC cells, which were subjected to a sphere formation assay. Cell spheres were cultured with sorafenib and subjected to a cell proliferation assay and the expression levels of cytochrome P450 (CYP3A4) were analyzed in RNA extracted from sphere-forming cells using reverse transcription-quantitative polymerase chain reaction...
March 2017: Oncology Letters
https://www.readbyqxmd.com/read/28449367/metoprolol-pridopidine-drug-drug-interaction-and-food-effect-assessments-of-pridopidine-a-new-drug-for-treatment-of-huntington-disease
#2
Laura Rabinovich-Guilatt, Lilach Steiner, Hussein Hallak, Gina Pastino, Pierandrea Muglia, Ofer Spiegelstein
AIM: Pridopidine is an oral drug in clinical development for treatment of patients with Huntington disease. This study examined the interactions of pridopidine with in vitro cytochrome P450 activity and characterized the effects of pridopidine on CYP2D6 activity in healthy volunteers using metoprolol as a probe substrate. The effect of food on pridopidine exposure was assessed. METHODS: The ability of pridopidine to inhibit and/or induce in vitro activity of drug metabolising enzymes was examined in human liver microsomes and fresh hepatocytes...
April 27, 2017: British Journal of Clinical Pharmacology
https://www.readbyqxmd.com/read/28448819/construction-of-three-dimensional-vascularized-functional-human-liver-tissue-using-a-layer-by-layer-cell-coating-technique
#3
Kazuki Sasaki, Takami Akagi, Tadafumi Asaoka, Hidetoshi Eguchi, Yasunari Fukuda, Yoshifumi Iwagami, Daisaku Yamada, Takehiro Noda, Hiroshi Wada, Kunihito Gotoh, Koichi Kawamoto, Yuichiro Doki, Masaki Mori, Mitsuru Akashi
The creation of artificial liver tissue is an active area of research due to the shortage of donors for liver transplantation. Here we investigated whether a simple and efficient cell coating technique developed in our laboratory could be used to generate functional vascularized liver tissue. This technique creates three-dimensional tissue by loading cells sterically onto other cells that have been coated with layer-by-layer (LbL) nanofilms of fibronectin and gelatin, two extracellular matrix proteins. We used this technique to construct homogenous, dense, well-vascularized liver tissue from cryopreserved human primary hepatocytes, human umbilical vein endothelial cells, and normal human dermal fibroblasts...
February 28, 2017: Biomaterials
https://www.readbyqxmd.com/read/28448172/the-macrophage-stimulating-anti-cancer-agent-rrx-001-protects-against-ischemia-reperfusion-injury
#4
Pedro Cabrales, Scott Caroen, Arnold Oronsky, Corey Carter, Jane Trepel, Thomas Summers, Tony Reid, Neil Oronsky, Michelle Lybeck, Bryan Oronsky
Introduction RRx-001, a clinical macrophage-stimulating anti-cancer agent that also produces nitric oxide (NO) was studied in a model of ischemia-reperfusion injury. Methods The production of NO is dependent on the oxygen tension because nitric oxide synthases convert l-arginine to NO and l-citrulline in the presence of O2. Since the P450 enzymes, which metabolize nitrate esters such as nitroglycerin are dependent on oxygen, the generation of 'exogenous' NO is also sensitive to alterations in tissue PO2. I/R injury was studied in a hamster chamber window, with compression of the periphery of the window for 1 hour to induce ischemia...
April 27, 2017: Expert Review of Hematology
https://www.readbyqxmd.com/read/28447451/improvement-of-a-p450-based-recombinant-e-coli-whole-cell-system-for-the-production-of-oxygenated-sesquiterpene-derivatives
#5
Thuy Thi Bich Ly, Alexander Schifrin, Bach Duc Nguyen, Rita Bernhardt
Sesquiterpenes are common constituents of essential oil in plants. Their oxygenated derivatives often possess desirable flavor, fragrant and pharmaceutical properties. Recently, the CYP264B1-based recombinant E. coli whole-cell system has been constructed for the oxidation of sesquiterpenes. However, limiting factors of this system related to the high volatility of substrates and the suitability of the P450 redox partner need to be addressed. In this work, the improvement of the system was implemented with (+)-α-longipinene as a model substrate...
April 27, 2017: Journal of Agricultural and Food Chemistry
https://www.readbyqxmd.com/read/28447323/observation-of-clinically-relevant-drug-interaction-in-chimeric-mice-with-humanized-livers-the-case-of-valproic-acid-and-carbapenem-antibiotics
#6
Eiko Suzuki, Kumiko Koyama, Daisuke Nakai, Ryoya Goda, Hiroshi Kuga, Kan Chiba
BACKGROUND AND OBJECTIVE: Human in vitro and dog in vitro/in vivo researches indicate that the drug-drug interaction (DDI) of decreased plasma valproic acid (VPA) concentration by co-administration of carbapenem antibiotics is caused by inhibition of acylpeptide hydrolase (APEH)-mediated VPA acylglucuronide (VPA-G) hydrolysis by carbapenems. In this study, we investigated VPA disposition and APEH activities in TK-NOG chimeric mice, whose livers were highly replaced with human hepatocytes, to evaluate the utility of this animal model and the clinical relevance of the DDI mechanism...
April 26, 2017: European Journal of Drug Metabolism and Pharmacokinetics
https://www.readbyqxmd.com/read/28446877/exploring-the-role-of-cyp3a4-mediated-drug-metabolism-in-the-pharmacological-modulation-of-nitric-oxide-production
#7
José Pérez-Del Palacio, Caridad Díaz, Noemí Vergara, Francesca Algieri, Alba Rodríguez-Nogales, Nuria de Pedro, M Elena Rodríguez-Cabezas, Olga Genilloud, Julio Gálvez, Francisca Vicente
Nitric-oxide synthase, the enzyme responsible for mammalian nitric oxide generation, and cytochrome P450, the major enzymes involved in drug metabolism, share striking similarities. Therefore, it makes sense that cytochrome P450 drug mediated biotransformations might play an important role in the pharmacological modulation of nitric oxide synthase. In this work, we have undertaken an integrated in vitro assessment of the hepatic metabolism and nitric oxide modulation of previously described dual inhibitors (imidazoles and macrolides) of these enzymes in order assess the implication of CYP450 activities over production of nitric oxide...
2017: Frontiers in Pharmacology
https://www.readbyqxmd.com/read/28446509/inhibition-of-the-all-trans-retinoic-acid-hydroxylases-cyp26a1-and-cyp26b1-results-in-dynamic-tissue-specific-changes-in-endogenous-atra-signaling
#8
Faith Stevison, Cathryn Hogarth, Sasmita Tripathy, Travis Kent, Nina Isoherranen
all-trans-retinoic acid (atRA), the active metabolite of vitamin A, is a ligand for several nuclear receptors and acts as a critical regulator of many physiological processes. The cytochrome P450 family 26 (CYP26) enzymes are responsible for atRA clearance, and are potential drug targets to increase concentrations of endogenous atRA in a tissue-specific manner. Talarozole is a potent inhibitor of CYP26A1 and CYP26B1, and has shown some success in clinical trials. Yet, it is not known what magnitude of change is needed in tissue atRA concentrations to promote atRA signaling changes...
April 26, 2017: Drug Metabolism and Disposition: the Biological Fate of Chemicals
https://www.readbyqxmd.com/read/28445040/chemoenzymatic-total-synthesis-of-the-proposed-structures-of-putaminoxins-b-and-d
#9
Carolin Bisterfeld, Claudia Holec, Dietrich Böse, Patrick Marx, Jörg Pietruszka
Different enzymatic and nonenzymatic approaches were tested and compared to afford enantiopure homoallylic and allylic alcohols as building blocks in a total synthesis showcase. Thereby, highly enantioselective alcohol dehydrogenases and the P450 BM3 monooxygenase variant A74G L188Q were compared to classical asymmetric reagent-controlled allyl additions. Thus, the first total syntheses of the proposed structures for putaminoxins B/D and their respective enantiomers were accomplished. Detailed spectroscopic analysis of the newly synthesized compounds unraveled a discrepancy with respect to the reported structures of putaminoxins B/D...
April 26, 2017: Journal of Natural Products
https://www.readbyqxmd.com/read/28444958/role-of-cytochrome-p450-3a4-and-1a2-phenotyping-in-patients-with-advanced-non-small-cell-lung-cancer-nsclc-receiving-erlotinib-treatment
#10
Zinnia P Parra-Guillen, Peter B Berger, Manuel Haschke, Massimiliano Donzelli, Daria Winogradova, Bogumila Pfister, Martin Früh, Charlotte Kloft, Stephan Krähenbühl, Silke Gillessen, Markus Joerger
Erlotinib is metabolized by cytochrome p450 (CYP) 3A and CYP1A. This study assessed CYP3A4 (midazolam) and CYP1A2 (caffeine) phenotyping in plasma and dried blood spots (DBS) for predicting the pharmacokinetics and toxicity of erlotinib in 36 patients with advanced NSCLC. On day 1, erlotinib 150 mg OD. was initiated, and the 2 oral probe drugs midazolam (2mg) and caffeine (100mg) were added on day 1. Plasma and DBS were collected for erlotinib, OSI-420 and probe drugs for up to 6 hr on day 1 and 2-weekly up to week 10...
April 26, 2017: Basic & Clinical Pharmacology & Toxicology
https://www.readbyqxmd.com/read/28444482/synthesis-pharmacological-evaluation-and-molecular-docking-of-pyranopyrazole-linked-1-4-dihydropyridines-as-potent-positive-inotropes
#11
Rakesh Kumar, Neha Yadav, Rodolfo Lavilla, Daniel Blasi, Jordi Quintana, José Manuel Brea, María Isabel Loza, Jordi Mestres, Mamta Bhandari, Ritu Arora, Rita Kakkar, Ashok K Prasad
1,4-Dihydropyridines are well-known calcium channel blockers, but variations in the substituents attached to the ring have resulted in their role reversal making them calcium channel activators in some cases. We describe the microwave-assisted eco-friendly approach for the synthesis of pyranopyrazole-1,4-dihydropyridines, a new class of 1,4-DHPs, under solvent-free conditions in good yield, and screen them for various in silico, in vitro and in vivo activities. The in vivo experimentation results show that the compounds possess positive inotropic effect, and the docking results validate their good binding with calcium channels...
April 25, 2017: Molecular Diversity
https://www.readbyqxmd.com/read/28443803/a-strategy-for-early-risk-predictions-of-clinical-drug-drug-interactions-involving-the-gastroplus-tm-ddi-module-for-time-dependent-cyp-inhibitors
#12
Anna-Karin Sohlenius-Sternbeck, Gabrielle Meyerson, Ann-Louise Hagbjörk, Sanja Juric, Ylva Terelius
1. A set of reference compounds for time-dependent inhibition (TDI) of cytochrome P450 with available literature data for kinact and KI was used to predict clinical implications using the GastroPlus(TM) software. Comparisons were made to in vivo literature interaction data. 2. The predicted AUC ratios (AUC+inhibitor/AUCcontrol) could be compared with the observed ratios from literature for all compounds with detailed information about in vivo administration, pharmacokinetics and in vivo interactions (N = 21)...
April 26, 2017: Xenobiotica; the Fate of Foreign Compounds in Biological Systems
https://www.readbyqxmd.com/read/28443179/inhibition-of-carcinogen-activating-cytochrome-p450-enzymes-by-xenobiotic-chemicals-in-relation-to-antimutagenicity-and-anticarcinogenicity
#13
REVIEW
Tsutomu Shimada
A variety of xenobiotic chemicals, such as polycyclic aromatic hydrocarbons (PAHs), aryl- and heterocyclic amines and tobacco related nitrosamines, are ubiquitous environmental carcinogens and are required to be activated to chemically reactive metabolites by xenobiotic-metabolizing enzymes, including cytochrome P450 (P450 or CYP), in order to initiate cell transformation. Of various human P450 enzymes determined to date, CYP1A1, 1A2, 1B1, 2A13, 2A6, 2E1, and 3A4 are reported to play critical roles in the bioactivation of these carcinogenic chemicals...
April 2017: Toxicological Research
https://www.readbyqxmd.com/read/28443122/membrane-proteomics-of-arabidopsis-glucosinolate-mutants-cyp79b2-b3-and-myb28-29
#14
Islam Mostafa, Mi-Jeong Yoo, Ning Zhu, Sisi Geng, Craig Dufresne, Maged Abou-Hashem, Maher El-Domiaty, Sixue Chen
Glucosinolates (Gls) constitute a major group of natural metabolites represented by three major classes (aliphatic, indolic and aromatic) of more than 120 chemical structures. In our previous work, soluble proteins and metabolites in Arabidopsis mutants deficient of aliphatic (myb28/29) and indolic Gls (cyp79B2B3) were analyzed. Here we focus on investigating the changes at the level of membrane proteins in these mutants. Our LC/MS-MS analyses of tandem mass tag (TMT) labeled peptides derived from the cyp79B2/B3 and myb28/29 relative to wild type resulted in the identification of 4,673 proteins, from which 2,171 are membrane proteins...
2017: Frontiers in Plant Science
https://www.readbyqxmd.com/read/28442937/simultaneous-administration-of-fluoxetine-and-simvastatin-ameliorates-lipid-profile-improves-brain-level-of-neurotransmitters-and-increases-bioavailability-of-simvastatin
#15
Abdulrahman K Al-Asmari, Zabih Ullah, Aqeel Salman Al Masoudi, Ishtiaque Ahmad
Simvastatin (STT), a 3-hydroxy-3-methylglutaryl coenzyme A reductase inhibitor, is widely prescribed for dyslipidemia, whereas fluoxetine (FLX) is the first-choice drug for the treatment of depression and anxiety. A recent report suggests that selective serotonin reuptake inhibitors can interact with the cytochrome P450 3A4 substrate, and another one suggests that STT enhances the antidepressant activity of FLX. However, the data are inconclusive. The present study was designed to explore the pharmacokinetic and pharmacodynamic consequences of coadministration of STT and FLX in experimental animals...
2017: Journal of Experimental Pharmacology
https://www.readbyqxmd.com/read/28442500/high-fat-diet-feeding-alters-expression-of-hepatic-drug-metabolizing-enzymes-in-mice
#16
Miaoran Ning, Hyunyoung Jeong
Medical conditions accompanying obesity often require drug therapy, but whether and how obesity alters the expression of drug-metabolizing enzymes and thus drug pharmacokinetics is poorly defined. Previous studies have shown that high fat diet (HFD) feeding and subsequent obesity in mice lead to altered expression of transcriptional regulators for cytochrome P450 (CYP) 2D6, including hepatocyte nuclear factor 4α (HNF4α, a transcriptional activator of CYP2D6) and small heterodimer partner (SHP, a transcriptional repressor of CYP2D6)...
April 25, 2017: Drug Metabolism and Disposition: the Biological Fate of Chemicals
https://www.readbyqxmd.com/read/28442442/prostaglandins-and-other-lipid-mediators-polm-special-issue-of-the-6th-european-workshop-on-lipid-mediators-role-of-m%C3%A3-ller-cell-cytochrome-p450-2c44-in-murine-retinal-angiogenesis
#17
Jiong Hu, Alexandra Geyer, Sarah Dziumbla, Khader Awwad, Darryl C Zeldin, Wolf-Hagen Schunck, Rüdiger Popp, Timo Frömel, Ingrid Fleming
Polyunsaturated fatty acids (PUFA) and their cytochrome P450 (CYP450) metabolites have been linked to angiogenesis and vessel homeostasis. However, the role of individual CYP isoforms and their endogenous metabolites in those processes are not clear. Here, we focused on the role of Cyp2c44 in postnatal retinal angiogenesis and report that Cyp2c44 is highly expressed in Müller glial cells in the retina. The constitutive as well as inducible postnatal genetic deletion of Cyp2c44 resulted in an increased vessel network density without affecting vessel radial expansion during the first postnatal week...
April 22, 2017: Prostaglandins & Other Lipid Mediators
https://www.readbyqxmd.com/read/28442026/neuromodulatory-effect-of-oestradiol-in-the-metabolism-of-ovarian-progesterone-and-oestradiol-during-dioestrus-ii-participation-of-the-superior-mesenteric-ganglion
#18
Adriana Vega Orozco, Cynthia Bronzi, Sandra Vallcaneras, Zulema Sosa, Marilina Casais
The aims of the present study were to determine: (1) whether oestradiol (E2) in the superior mesenteric ganglion (SMG) modifies the release of ovarian progesterone (P4), androstenedione (A2) and E2, the activity and gene expression of 3β-hydroxysteroid dehydrogenase (3β-HSD) and 20α-HSD and the expression of P450 aromatase (Cyp19a1) and (2) whether any such modifications are related to changes in ovarian nitric oxide (NO) and noradrenaline (NA) levels during dioestrus II. Using an ex vivo SMG-ovarian nervous plexus-ovary system, ovarian P4 release was measured following the addition E2 plus tamoxifen (Txf) (10-6M) to the ganglion, whereas A2, E2, NA and NO were measured following the addition of E2 alone...
April 26, 2017: Reproduction, Fertility, and Development
https://www.readbyqxmd.com/read/28441709/association-of-cyp3a5-3-and-cyp1a1-2c-polymorphism-with-development-of-acute-myeloid-leukemia-in-egyptian-patients
#19
Nahed Abd El Wahab, Nevine F Shafik, Roxan E Shafik, Sherin A Taha, Hanan E Shafik, Amira D Darwish
Aim: Cytochrome P450 (CYP) enzyme catalyzes the phase I metabolism reaction which metabolize endogenous and exogenous DNA-reactive chemical compounds and xenobiotics which could induce genotoxicity and increase the risk for leukemia. We aimed to detect frequency of CYP3A5*3 and CYP1A1*2C polymorphisms in Egyptian acute myeloid leukemia (AML) patients and to determine role of allele’s variants as a risk factor for developing leukemia. Patients and Methods: A case-control study was conducted on seventy acute myeloid leukemia patients and thirty control subjects...
March 1, 2017: Asian Pacific Journal of Cancer Prevention: APJCP
https://www.readbyqxmd.com/read/28441608/phylogenetic-signals-in-detoxification-pathways-in-cyprinid-and-centrarchid-species-in-relation-to-sensitivity-to-environmental-pollutants
#20
Peter van den Hurk, Lindsay E Gerzel, Peter Calomiris, Dennis C Haney
Observations in a previous study on biomarker responses in fish collected from urban creeks in Greenville, SC, indicated that there might be considerable differences in the expression of biotransformation enzymes in chub and sunfish species. To further investigate these species differences a dosing experiment was performed in which bluehead and creek chub (Nocomis leptocephalus and Semotilus atromaculatus), and redbreast sunfish, pumpkinseed, and bluegill (Lepomis auritus, L. gibbosus, and L. macrochirus) were injected with benzo[a]pyrene (BaP) as a model compound for common pollutants in urban creeks...
April 13, 2017: Aquatic Toxicology
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