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https://www.readbyqxmd.com/read/29676195/in-vitro-inhibitory-effects-of-sophocarpine-on-human-liver-cytochrome-p450-enzymes
#1
Jingwei Zhang, Chuansheng Li, Jingfa Zhang, Fan Zhang
1. Sophocarpine is a biologically active component isolated from the foxtail-like sophora herb and seed that is often orally administered for the treatment of cancer and chronic bronchial asthma. However, whether sophocarpine affects the activity of human liver cytochrome P450 (CYP) enzymes remains unclear. 2. In this study, the inhibitory effects of sophocarpine on the eight human liver CYP isoforms (CYP1A2, 3A4, 2A6, 2E1, 2D6, 2C9, 2C19, and 2C8) were investigated in vitro using human liver microsomes (HLMs)...
April 20, 2018: Xenobiotica; the Fate of Foreign Compounds in Biological Systems
https://www.readbyqxmd.com/read/29659506/in-vitro-inhibitory-effects-of-synthetic-cannabinoid-eam-2201-on-cytochrome-p450-and-udp-glucuronosyltransferase-enzyme-activities-in-human-liver-microsomes
#2
Tae Yeon Kong, Soon-Sang Kwon, Jae Chul Cheong, Hee Seung Kim, Jin Young Kim, Hye Suk Lee
EAM-2201, a synthetic cannabinoid, is a potent agonist of the cannabinoid receptors that is widely abused as an illicit recreational drug in combination with other drugs. To evaluate the potential of EAM-2201 as a perpetrator of drug–drug interactions, the inhibitory effects of EAM-2201 on major drug-metabolizing enzymes, cytochrome P450s (CYPs) and uridine 5′-diphospho-glucuronosyltransferases (UGTs) were evaluated in pooled human liver microsomes using liquid chromatography–tandem mass spectrometry (LC-MS/MS)...
April 16, 2018: Molecules: a Journal of Synthetic Chemistry and Natural Product Chemistry
https://www.readbyqxmd.com/read/29616291/the-role-of-hepatic-cytochrome-p450s-in-the-cytotoxicity-of-dronedarone
#3
Si Chen, Qiangen Wu, Baitang Ning, Matthew Bryant, Lei Guo
Dronedarone is used to treat patients with cardiac arrhythmias and has been reported to be associated with liver injury. Our previous mechanistic work demonstrated that DNA damage-induced apoptosis contributes to the cytotoxicity of dronedarone. In this study, we examined further the underlying mechanisms and found that after a 24-h treatment of HepG2 cells, dronedarone caused cytotoxicity, G1-phase cell cycle arrest, suppression of topoisomerase II, and DNA damage in a concentration-dependent manner. We also investigated the role of cytochrome P450s (CYPs)-mediated metabolism in the dronedarone-induced toxicity using our previously established HepG2 cell lines expressing individually 14 human CYPs (1A1, 1A2, 1B1, 2A6, 2B6, 2C8, 2C9, 2C18, 2C19, 2D6, 2E1, 3A4, 3A5, and 3A7)...
April 3, 2018: Archives of Toxicology
https://www.readbyqxmd.com/read/29614098/a-novel-calcimimetic-agent-evocalcet-mt-4580-khk7580-suppresses-the-parathyroid-cell-function-with-little-effect-on-the-gastrointestinal-tract-or-cyp-isozymes-in-vivo-and-in-vitro
#4
Takehisa Kawata, Shin Tokunaga, Miki Murai, Nami Masuda, Waka Haruyama, Youji Shoukei, Yutaka Hisada, Tetsuya Yanagida, Hiroshi Miyazaki, Michihito Wada, Tadao Akizawa, Masafumi Fukagawa
Cinacalcet hydrochloride (cinacalcet), an oral calcimimetic agent has been widely used for the management of secondary hyperparathyroidism (SHPT) in chronic kidney disease (CKD). In sharp contrast to vitamin D receptor activators, cinacalcet suppresses SHPT without inducing hypercalcemia or hyperphosphatemia. Nevertheless, some patients remain refractory to SHPT with this agent, as the dose cannot be sufficiently increased due to gastrointestinal symptoms. In order to resolve this issue, we have developed a newly synthesized calcimimetic agent, evocalcet (MT-4580/KHK7580)...
2018: PloS One
https://www.readbyqxmd.com/read/29602316/effect-of-cytochrome-p450-cyp-2d6-genetic-polymorphism-on-the-inhibitory-action-of-antidepressants-on-cyp2d6-mediated-dopamine-formation-from-p-tyramine
#5
Toshiro Niwa, Mayumi Yanai, Maya Matsumoto, Marina Shizuku
PURPOSE: The inhibitory effects of antidepressants, such as imipramine, desipramine, and fluvoxamine, on dopamine formation from p-tyramine catalyzed by cytochrome P450 (CYP) 2D6.2 (Arg296Cys, Ser486Thr) and CYP2D6.10 (Pro34Ser, Ser486Thr), were compared with those on dopamine formation catalyzed by CYP2D6.1 (wild type), to investigate the effect of a CYP2D6 polymorphism on neuroactive amine metabolism in the brain. METHODS: Inhibition constants (Ki) of the antidepressants toward dopamine formation catalyzed by CYP2D6...
2018: Journal of Pharmacy & Pharmaceutical Sciences: a Publication of the Canadian Society for Pharmaceutical Sciences
https://www.readbyqxmd.com/read/29600986/molecular-genetic-models-for-prognosis-of-development-of-tumors-of-reproductive-system-in-women-with-family-history-of-cancer
#6
O V Paliychuk, L Z Polishchuk, Z I Rossokha, V F Chekhun
AIM: To develop a prognostic molecular genetic model for assessing the risk of development of benign and malignant tumors of female reproductive organs (FRO) in patients from cancer-affected families. PATIENTS AND METHODS: The work presents the data on a comprehensive clinical examination of 210 women (90 patients with FRO cancer with aggregation of tumor pathology in families, 65 patients with benign pathology of FRO from cancer-affected families, 55 women - control group of healthy women without family history of cancer)...
March 2018: Experimental Oncology
https://www.readbyqxmd.com/read/29595093/synergy-of-clavine-alkaloid-chanoclavine-with-tetracycline-against-multi-drug-resistant-e-coli
#7
Gaurav Raj Dwivedi, Anupam Maurya, Dharmendra Kumar Yadav, Vigyasa Singh, Feroz Khan, Mahendra Kumar Gupta, Mastan Singh, Mahendra P Darokar, Santosh Kumar Srivastava
The emergence of multidrug resistance (MDR) in Gram negative bacteria (GNB) and lack of novel classes of antibacterial agents have raised an immediate need to identify antibacterial agents, which can reverse the phenomenon of MDR. The purpose of present study was to evaluate synergy potential and understanding the drug resistance reversal mechanism of chanoclavine isolated from Ipomoea muricata against the multidrug resistant clinical isolate of Escherichia coli (MDREC). Although chanoclavine did not show antibacterial activity of its own, but in combination, it could reduce the minimum inhibitory concentration (MIC) of tetracycline (TET) up to 16 folds...
March 29, 2018: Journal of Biomolecular Structure & Dynamics
https://www.readbyqxmd.com/read/29588194/using-chemical-bond-based-method-to-predict-site-of-metabolism-for-five-biotransformations-mediated-by-cyp-3a4-2d6-and-2c9
#8
XuYan Fu, ShuaiBing He, Li Du, ZhaoLei Lv, Yi Zhang, Qian Zhang, Yun Wang
Although it has been proposed for decades to predict site of metabolism (SOM) by in silico methods, identifying SOM correctly remains an unsolved fundamental problem and is an active area of research. In our prior works, we proposed a chemical bond-based approach to construction of SOM prediction models by integrating chemical bond descriptors and drug-metabolizing enzymes data. Although it has been evaluated with both 10-fold cross-validation and independent validation, we believe comparisons between this method and prior methods using publicly accessible external datasets are indispensable and more desirable...
March 24, 2018: Biochemical Pharmacology
https://www.readbyqxmd.com/read/29572664/identification-of-cytochrome-p450-mediated-drug-drug-interactions-at-risk-in-cases-of-gene-polymorphisms-by-using-a-quantitative-prediction-model
#9
Nicolas Fermier, Laurent Bourguignon, Sylvain Goutelle, Nathalie Bleyzac, Michel Tod
BACKGROUND AND OBJECTIVE: The magnitude of drug-drug interactions mediated by cytochrome P450 (CYP) may depend on the genotype of polymorphic cytochromes. The objective of this study was to identify drug-drug interactions with greater magnitude in CYP variant groups than in extensive metabolizers. METHODS: The in-vivo mechanistic static model was used to predict the area under the curve ratio of drug-drug interactions. Five cytochromes (CYP3A4/5, 2D6, 2C9, 2C19, 1A2) and five groups of genotypes for each polymorphic cytochrome (CYP2D6, 2C9, 2C19) were considered...
March 23, 2018: Clinical Pharmacokinetics
https://www.readbyqxmd.com/read/29571519/generation-and-validation-of-novel-anti-bovine-cd163-monoclonal-antibodies-abm-1a9-and-abm-2d6
#10
Yoshinori Shimamoto, Junko Nio-Kobayashi, Hiroshi Watarai, Masashi Nagano, Natsuko Saito, Eiki Takahashi, Hidetoshi Higuchi, Atsushi Kobayashi, Takashi Kimura, Hiroshi Kitamura
The scavenger receptor CD163 is widely used as a cell signature for alternatively active "M2" macrophages in mammals. In this study, we generated two monoclonal antibodies, ABM-1A9 and ABM-2D6, against the extracellular region of bovine CD163. Conventional Western blotting using the antibodies yielded immunoreactive bands of bovine CD163 at 130 and 150 kDa in non-reduced and reduced spleen lysates, respectively. The minimum limit of detectable concentration of both antibodies was relatively lower (5...
April 2018: Veterinary Immunology and Immunopathology
https://www.readbyqxmd.com/read/29558929/understanding-human-genetic-factors-influencing-primaquine-safety-and-efficacy-to-guide-primaquine-roll-out-in-a-pre-elimination-setting-in-southern-africa
#11
Shehu S Awandu, Jaishree Raman, Takalani I Makhanthisa, Philip Kruger, John Frean, Teun Bousema, Jandeli Niemand, Lyn-Marie Birkholtz
BACKGROUND: Primaquine (PQ) is recommended as an addition to standard malaria treatments in pre-elimination settings due to its pronounced activity against mature Plasmodium falciparum gametocytes, the parasite stage responsible for onward transmission to mosquitoes. However, PQ may trigger haemolysis in glucose-6-phosphate dehydrogenase (G6PD)-deficient individuals. Additional human genetic factors, including polymorphisms in the human cytochrome P450 2D6 (CYP2D6) complex, may negatively influence the efficacy of PQ...
March 20, 2018: Malaria Journal
https://www.readbyqxmd.com/read/29556194/when-the-safe-alternative-is-not-that-safe-tramadol-prescribing-in-children
#12
REVIEW
Frédérique Rodieux, Laszlo Vutskits, Klara M Posfay-Barbe, Walid Habre, Valérie Piguet, Jules A Desmeules, Caroline F Samer
Children represent a vulnerable population in which management of nociceptive pain is complex. Drug responses in children differ from adults due to age-related differences. Moreover, therapeutic choices are limited by the lack of indication for a number of analgesic drugs due to the challenge of conducting clinical trials in children. Furthermore the assessment of efficacy as well as tolerance may be complicated by children's inability to communicate properly. According to the World Health Organization, weak opioids such as tramadol and codeine, may be used in addition to paracetamol and ibuprofen for moderate nociceptive pain in both children and adults...
2018: Frontiers in Pharmacology
https://www.readbyqxmd.com/read/29555325/genetic-polymorphisms-of-cytochrome-p450-2d6-cyp2d6-are-associated-with-long-term-tramadol-treatment-induced-oxidative-damage-and-hepatotoxicity
#13
Manar Hamed Arafa, Hebatallah Husseini Atteia
Our objective was to figure out whether CYP2D6 gene polymorphisms may account for long term tramadol-induced oxidative stress and hepatotoxicity in 60 patients receiving chronic tramadol treatment in Neurology and Rheumatology Outpatients Clinic, Zagazig University Hospitals, Egypt. As expected, CYP2D6*1 allele (wild type) frequency was significantly greater than CYP2D6*DUP, CYP2D6*4 and CYP2D6*10 alleles in both chronically tramadol-treated and control groups. CYP2D6*DUP allele carriers followed by those carrying CYP2D6*1, displayed higher levels of urinary tramadol major active metabolite O-desmethyltramadol (M1) and serum lipid peroxidation along with lower levels of total antioxidants than those carrying other impaired function alleles (CYP2D6*4&*10) in tramadol-treated patients, suggesting oxidative stress...
March 16, 2018: Toxicology and Applied Pharmacology
https://www.readbyqxmd.com/read/29524040/site-directed-mutagenesis-of-cytochrome-p450-2d6-and-2c19-enzymes-expression-and-spectral-characterization-of-naturally-occurring-allelic-variants
#14
Amelia Nathania Dong, Yan Pan, Uma Devi Palanisamy, Beow Chin Yiap, Nafees Ahemad, Chin Eng Ong
Genetic polymorphism of the cytochrome P450 (CYP) genes particularly affects CYP2D6 and CYP2C19 to a functionally relevant extent, and it is therefore crucial to elucidate the enzyme kinetic and molecular basis for altered catalytic activity of these allelic variants. This study explored the expression and function of the reported alleles CYP2D6*2, CYP2D6*10, CYP2D6*17, CYP2C19*23, CYP2C19*24, and CYP2C19*25 with respect to gene polymorphisms. Site-directed mutagenesis (SDM) was carried out to generate these six alleles...
March 10, 2018: Applied Biochemistry and Biotechnology
https://www.readbyqxmd.com/read/29494843/design-synthesis-and-structure-activity-relationship-of-a-novel-series-of-cxcr4-antagonists
#15
Zhanhui Li, Yujie Wang, Chunyan Fu, Xu Wang, Jun Jun Wang, Yi Zhang, Dongping Zhou, Yuan Zhao, Lusong Luo, Haikuo Ma, Wenfeng Lu, Jiyue Zheng, Xiaohu Zhang
The important roles of the CXCL12/CXCR4 axis in numerous pathogenic pathways involving HIV infection and cancer metastasis make the CXCR4 receptor an attractive target for the development of therapeutic agents. Through scaffold hybridization of a few known CXCR4 antagonists, a series of novel aminopyrimidine derivatives was developed. Compound 3 from this new scaffold demonstrates excellent binding affinity with CXCR4 receptor (IC50  = 54 nM) and inhibits CXCL12 induced cytosolic calcium increase (IC50  = 2...
February 16, 2018: European Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/29472872/pharmacoresistant-severe-mental-health-disorders-in-children-and-adolescents-functional-abnormalities-of-cytochrome-p450-2d6
#16
Susanne Thümmler, Emmanuelle Dor, Renaud David, Graziella Leali, Michele Battista, Alexia David, Florence Askenazy, Céline Verstuyft
Background: Severe mental health disorders in children and adolescents represent a major public health problem. Despite adequate drug treatment, some patients develop pharmacoresistant disease. As a consequence, physicians are confronted with prescribing challenges, prolonged hospitalization and increased risk of adverse events, thus aggravating short-, medium-, and long-term prognosis. The majority of psychotropic treatments, particularly antipsychotics and antidepressants, are metabolized at hepatic level by cytochrome P450 (CYP), particularly by CYP3A4 and CYP2D6...
2018: Frontiers in Psychiatry
https://www.readbyqxmd.com/read/29469947/evaluation-of-the-metabolic-capability-of-primary-human-hepatocytes-in-three-dimensional-cultures-on-microstructural-plates
#17
Satoshi Koyama, Hiroshi Arakawa, Manabu Itoh, Norio Masuda, Kentaro Yano, Hajime Kojima, Takuo Ogihara
The NanoCulture Plate (NCP) is a novel microstructural plate designed as a base for the three-dimensional culture of cells/tissues. Here, we examined whether or not the metabolic capability of human primary hepatocytes is well maintained during culture on NCPs. The hepatocytes formed aggregates after seeding and their ATP content was well maintained during culture for 21 days. Expression of CYP1A2, 2B6, 2C9, 2C19, 2D6, 2E1 and 3A4 mRNAs was detected throughout the 21-day culture period. Addition of CYP substrate drugs (midazolam, diclofenac, lamotrigine and acetaminophen) resulted in the formation of multiple metabolites with a corresponding decrease in the amounts of the unchanged compounds...
February 22, 2018: Biopharmaceutics & Drug Disposition
https://www.readbyqxmd.com/read/29462868/inhibition-of-cytochrome-p450-activities-by-extracts-of-hyptis-verticillata-jacq-assessment-for-potential-herb-drug-interactions
#18
David Picking, Bentley Chambers, James Barker, Iltaf Shah, Roy Porter, Declan P Naughton, Rupika Delgoda
Understanding the potential for adverse drug reactions (ADRs), from herb-drug interactions, is a key aspect of medicinal plant safety, with particular relevance for public health in countries where medicinal plant use is highly prevalent. We undertook an in-depth assessment of extracts of Hyptis verticillata Jacq., via its impact on activities of key cytochrome P450 (CYP) enzymes (CYPs 1A1, 1A2, 1B1, 3A4 and 2D6), its antioxidant properties (determined by DPPH assays) and chemical characterisation (using LC-MS)...
February 15, 2018: Molecules: a Journal of Synthetic Chemistry and Natural Product Chemistry
https://www.readbyqxmd.com/read/29459457/tamoxifen-metabolism-and-efficacy-in-breast-cancer-a-prospective-multicentre-trial
#19
Patrick Neven, Lynn Jongen, Anneleen Lintermans, Kathleen Van Asten, Chantal Blomme, Diether Lambrechts, An Poppe, Hans Wildiers, Anne-Sophie Dieudonné, Olivier Brouckaert, Jan Decloedt, Patrick Berteloot, Didier Verhoeven, Markus Joerger, Peter Vuylsteke, Wim Wynendaele, Minne Casteels, Sabine Van Huffel, Willem Lybaert, Johan Van Ginderachter, Robert Paridaens, Ignace Vergote, Vincent Dezentje, Ben Van Calster, Henk-Jan Guchelaar
PURPOSE: Levels of endoxifen, the most active metabolite of tamoxifen, vary by the highly polymorphic cytochrome P450 (CYP) 2D6 enzyme. We prospectively investigated tamoxifen efficacy by serum endoxifen levels and the tamoxifen activity score (TAS). EXPERIMENTAL DESIGN: A prospective observational multicentre study including postmenopausal women with an oestrogen-receptor (ER)-positive breast cancer receiving first line tamoxifen, 20mg daily in the neo-adjuvant or metastatic setting recruited between February 2009 and May 2014...
February 19, 2018: Clinical Cancer Research: An Official Journal of the American Association for Cancer Research
https://www.readbyqxmd.com/read/29458047/effects-of-cytochrome-p450-single-nucleotide-polymorphisms-on-methadone-metabolism-and-pharmacodynamics
#20
REVIEW
Taha Ahmad, Monica A Valentovic, Gary O Rankin
Methadone is a synthetic, long-acting opioid with a single chiral center forming two enantiomers, (R)-methadone and (S)-methadone, each having specific pharmacological actions. Concentrations of (R)- and (S)-methadone above therapeutic levels have the ability to cause serious, life-threatening, and fatal side effects. This toxicity can be due in part to the pharmacogenetics of an individual, which influences the pharmacokinetic and pharmacodynamic properties of the drug. Methadone is primarily metabolized in the liver by cytochrome P450 (CYP) enzymes, predominately by CYP2B6, followed by CYP3A4, 2C19, 2D6, and to a lesser extent, CYP2C18, 3A7, 2C8, 2C9, 3A5, and 1A2...
February 16, 2018: Biochemical Pharmacology
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