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CYP1A1

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https://www.readbyqxmd.com/read/28632937/synthesis-biological-evaluation-and-docking-studies-of-trans-stilbene-methylthio-derivatives-as-cytochromes-p450-family-1-inhibitors
#1
Marcin Wierzchowski, Zbigniew Dutkiewicz, Agnieszka Gielara-Korzańska, Artur Korzański, Anna Teubert, Artur Teżyk, Tomasz Stefański, Wanda Baer-Dubowska, Renata Mikstacka
Cytochromes P450 family 1 (CYP1) are responsible for the metabolism of procarcinogens, e.g. polycyclic aromatic hydrocarbons and aromatic and heterocyclic amines. The inhibition of CYP1 activity is examined in terms of chemoprevention and cancer chemotherapy. We designed and synthesized a series of trans-stilbene derivatives possessing a combination of methoxy and methylthio functional groups attached in different positions to the trans-stilbene skeleton. We determined the effects of synthesized compounds on the activities of human recombinant CYP1A1, CYP1A2 and CYP1B1 and, to explain the variation of inhibitory potency of methoxystilbene derivatives and their methylthio analogs, we employed computational analysis...
June 20, 2017: Chemical Biology & Drug Design
https://www.readbyqxmd.com/read/28623690/candidate-cytochrome-p450-genes-for-ethoxyresorufin-o-deethylase-activity-in-oyster-crassostrea-gigas
#2
Marília Nardelli Siebert, Jacó Joaquim Mattos, Guilherme Toledo-Silva, Guilherme Razzera, Afonso Celso Dias Bainy
Vertebrate cytochrome P450 1 (CYP1) enzymes metabolize endogenous and xenobiotic compounds and usually demonstrate a substrate-inducible response. Ethoxyresorufin O-deethylase activity (EROD) is a common method to quantify CYP1 enzymes activity in these organisms. Despite the absence of this gene family in protostomes, CYP1-like genes were identified in several species, even though no evolutionary relationship has been established with the vertebrate CYP1 family. In the present study, EROD activity was evaluated in microsomal fraction of gills, digestive gland and mantle of Crassostrea gigas...
June 9, 2017: Aquatic Toxicology
https://www.readbyqxmd.com/read/28621325/the-oral-commensal-streptococcus-mitis-activates-the-aryl-hydrocarbon-receptor-in-human-oral-epithelial-cells
#3
Stian A Engen, Gro H Rørvik, Olav Schreurs, Inger Js Blix, Karl Schenck
Streptococcus mitis (S. mitis) is a pioneer commensal bacterial species colonizing many of the surfaces of the oral cavity in healthy individuals. Yet, not much information is available regarding its interaction with the host. We used examination of its transcriptional regulation in oral keratinocytes to elucidate some of its potential roles in the oral cavity. Transcription factor analysis of oral keratinocytes predicted S. mitis-mediated activation of aryl hydrocarbon receptor (AhR). Activation and functionality of AhR was confirmed through nuclear translocation determined by immunofluorescence microscopy and real-time polymerase chain reaction with reverse transcription analysis of CYP1A1, the hallmark gene for AhR activation...
June 16, 2017: International Journal of Oral Science
https://www.readbyqxmd.com/read/28620991/potential-positive-association-between-cytochrome-p450-1a1-gene-polymorphisms-and-recurrent-pregnancy-loss-a-meta-analysis
#4
Jie Li, Yang Chen, Sien Mo, Donghong Nai
In order to discover the potential genetic risks associated with recurrent pregnancy loss (RPL), this meta-analysis was conducted to assess the association between CYP1A1 gene polymorphism and RPL. Studies were retrieved from the databases PubMed, Embase, HuGENet, and CNKI. Four models were then applied. Seven studies, including three datasets for the rs1048943 and five for the rs4646903 single-nucleotide polymorphism (SNP), were included in this analysis, involving 613 cases and 398 controls for the rs1048943; and 864 cases and 842 controls for the rs4646903 SNP...
July 2017: Annals of Human Genetics
https://www.readbyqxmd.com/read/28618207/effect-of-dioxin-and-17%C3%AE-estradiol-on-the-expression-of-cytochrome-p450-1a1-gene-via-an-estrogen-receptor-dependent-pathway-in-cellular-and-xenografted-models
#5
Ryeo-Eun Go, Kyung-A Hwang, Cho-Won Kim, Yong-Sub Byun, Ki-Hoan Nam, Kyung-Chul Choi
Cytochrome P450 (CYP) 1A1 plays a major role in the metabolic activation of procarcinogens to carcinogens via aryl hydrocarbon receptor (AhR) pathway. Especially, 2,3,7,8-tetrachlorodibenzo-p-dioxin (TCDD) is known as an agonist of AhR. In estrogen responsive cancers, 17β-estradiol (E2) may influence on AhR dependent expression of CYP1 family via the interaction between estrogen receptor (ER) and AhR. In the present study, the effect of E2/ER on the expression of AhR and CYP1A1 genes was investigated for MCF-7 clonal variant (MCF-7 CV) breast cancer cells expressing ER...
June 15, 2017: Environmental Toxicology
https://www.readbyqxmd.com/read/28611384/the-correlation-between-the-expression-of-genes-involved-in-drug-metabolism-and-the-blood-level-of-tacrolimus-in-liver-transplant-receipts
#6
Jianhai Wang, Keqiu Li, Xiaoning Zhang, Dahong Teng, Mingyan Ju, Yaqing Jing, Yuxia Zhao, Guang Li
Immunosuppressive medications, such as tacrolimus and mycophenolate mofetil, are commonly used for reducing the risk of organ rejection in receipts of allogeneic organ transplant. The optimal dosages of these drugs are required for preventing rejection and avoiding toxicity to receipts. This study aimed to identify the correlation between the expression profiling of genes involved in drug metabolism and the blood level of tacrolimus in liver transplant receipts. Sixty-four liver transplant receipts were enrolled in this retrospective study...
June 13, 2017: Scientific Reports
https://www.readbyqxmd.com/read/28593185/induction-of-colonic-regulatory-t-cells-by-mesalamine-by-activating-the-aryl-hydrocarbon-receptor
#7
Kyoko Oh-Oka, Yuko Kojima, Koichiro Uchida, Kimiko Yoda, Kayoko Ishimaru, Shotaro Nakajima, Jun Hemmi, Hiroshi Kano, Yoshiaki Fujii-Kuriyama, Ryohei Katoh, Hiroyuki Ito, Atsuhito Nakao
BACKGROUND & AIMS: Mesalamine is a first-line drug for treatment of inflammatory bowel diseases (IBD). However, its mechanisms are not fully understood. CD4(+) Foxp3(+) regulatory T cells (Tregs) play a potential role in suppressing IBD. This study determined whether the anti-inflammatory activity of mesalamine is related to Treg induction in the colon. METHODS: We examined the frequencies of Tregs in the colons of wild-type mice, mice deficient for aryl hydrocarbon receptor (AhR(-/-) mice), and bone marrow-chimeric mice lacking AhR in hematopoietic cells (BM-AhR(-/-) mice), following oral treatment with mesalamine...
July 2017: Cellular and Molecular Gastroenterology and Hepatology
https://www.readbyqxmd.com/read/28585914/glutathione-s-transferase-gene-polymorphisms-and-the-development-of-new-onset-diabetes-after-liver-transplant
#8
Zahra Musavi, Elham Moasser, Neda Zareei, Negar Azarpira, Ali Shamsaeefar
OBJECTIVES: The association between the glutathione S-transferase polymorphisms and the development of new-onset diabetes mellitus after liver transplant was studied. MATERIALS AND METHODS: Peripheral blood samples were collected from 106 liver transplant patients divided into 2 groups: 52 with new-onset diabetes mellitus and 54 without new-onset diabetes mellitus; 169 healthy individuals with no clinical evidence of diabetes mellitus were selected as a control group...
June 5, 2017: Experimental and Clinical Transplantation
https://www.readbyqxmd.com/read/28571624/reprint-of-cyp1a-protein-expression-and-catalytic-activity-in-double-crested-cormorants-experimentally-exposed-to-deepwater-horizon-mississippi-canyon-252-oil
#9
Courtney R Alexander, Michael J Hooper, Dave Cacela, Kim D Smelker, Caleshia S Calvin, Karen M Dean, Steve J Bursian, Fred L Cunningham, Katie C Hanson-Dorr, Katherine E Horak, John P Isanhart, Jane Link, Susan A Shriner, Céline A J Godard-Codding
Double-crested cormorants (Phalacrocorax auritus, DCCO) were orally exposed to Deepwater Horizon Mississippi Canyon 252 (DWH) oil to investigate oil-induced toxicological impacts. Livers were collected for multiple analyses including cytochrome P4501A (CYP1A) enzymatic activity and protein expression. CYP1A enzymatic activity was measured by alkoxyresorufin O-dealkylase (AROD) assays. Activities specific to the O-dealkylation of four resorufin ethers are reported: benzyloxyresorufin O-debenzylase (BROD), ethoxyresorufin O-deethylase (EROD), methoxyresorufin O-demethylase (MROD), and pentoxyresorufin O-depentylase (PROD)...
May 29, 2017: Ecotoxicology and Environmental Safety
https://www.readbyqxmd.com/read/28553516/a-practical-strategy-to-design-and-develop-an-isoform-specific-fluorescent-probe-for-a-target-enzyme-cyp1a1-as-a-case-study
#10
Zi-Ru Dai, Lei Feng, Qiang Jin, Hailing Cheng, Yan Li, Jing Ning, Yang Yu, Guang-Bo Ge, Jing-Nan Cui, Ling Yang
The development of isoform-specific probe(s) for a target enzyme with multiple homologs is always challenging. Herein, a practical strategy was used to design and develop an isoform-specific probe for CYP1A1, a key cytochrome P450 isoenzyme involved in xenobiotic metabolism and bioactivation. On the basis of the subtle differences in 3D structure and substrate preference between CYP1A1 and its homolog CYP1A2, we proposed that it was possible to design a CYP1A1-specific probe via local modification of the reaction site on known CYP1A substrates...
April 1, 2017: Chemical Science
https://www.readbyqxmd.com/read/28535889/unbalanced-expression-of-aryl-hydrocarbon-receptor-in-peripheral-blood-ccr6-cd4-and-cd4-cd25-t-cells-of-rheumatoid-arthritis
#11
Lin Cheng, Long Qian, Yue Tan, Guo-Sheng Wang, Xiao-Mei Li, Xiang-Pei Li, Chao-Yin Luo
OBJECTIVE: The goal of this study was to analyze the role of aryl hydrocarbon receptor in peripheral blood CCR6(+)CD4(+) and CD4(+)CD25(+)T cells of patients with rheumatoid arthritis. METHODS: Flow cytometry was applied to determine the proportion of AhR positive cells in CCR6(+)CD4(+)T, CD4(+)CD25(+)T and peripheral blood peripheral mononuclear cells from each subject. AhR mRNA and CYP1A1 mRNA relative expression levels were tested by real-time PCR. RESULTS: The percentage of AhR positive cells in peripheral blood mononuclear cells was higher in RA group than that in healthy cases [(35...
May 2017: Revista Brasileira de Reumatologia
https://www.readbyqxmd.com/read/28535350/activation-of-phenyl-4-2-oxo-3-alkylimidazolidin-1-yl-benzenesulfonates-prodrugs-by-cyp1a1-as-new-antimitotics-targeting-breast-cancer-cells
#12
Sébastien Fortin, Xavier Charest-Morin, Vanessa Turcotte, Coraline Lauvaux, Jacques Lacroix, Marie-France Côté, Stéphane Gobeil, Rene C-Gaudreault
Prodrug-mediated utilization of the cytochrome P450 (CYP) 1A1 to obtain the selective release of potent anticancer products within cancer tissues is a promising approach in chemotherapy. We herein report the rationale, preparation, biological evaluation and mechanism of action of phenyl 4-(2-oxo-3-alkylimidazolidin-1-yl)benzenesulfonates (PAIB-SOs), that are antimicrotubule prodrugs activated by CYP1A1. Although PAIB-SOs are inert in most cells tested, they are highly cytocidal towards several human breast cancer cells, including hormone-independent and chemoresistant types...
May 23, 2017: Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/28534260/pharmacogenetics-of-cannabinoids
#13
Szymon Hryhorowicz, Michal Walczak, Oliwia Zakerska-Banaszak, Ryszard Słomski, Marzena Skrzypczak-Zielińska
Although the application of medical marijuana and cannabinoid drugs is controversial, it is a part of modern-day medicine. The list of diseases in which cannabinoids are promoted as a treatment is constantly expanding. Cases of significant improvement in patients with a very poor prognosis of glioma or epilepsy have already been described. However, the occurrence of side effects is still difficult to estimate, and the current knowledge of the therapeutic effects of cannabinoids is still insufficient. In our opinion, the answers to many questions and concerns regarding the medical use of cannabis can be provided by pharmacogenetics...
May 22, 2017: European Journal of Drug Metabolism and Pharmacokinetics
https://www.readbyqxmd.com/read/28527150/development-of-in-silico-protocols-to-predict-structural-insights-into-the-metabolic-activation-pathways-of-xenobiotics
#14
M Kalim A Khan, Salman Akhtar, Jamal M Arif
To establish in silico model to predict the structural insight into the metabolic bioactivation pathway of xenobiotics, we considered two specific and one non-specific mammary procarcinogen [e.g., dibenzo[a,l]pyrene (DBP), 7,12-dimethylbenz[a]anthracene (DMBA), and benzo[a]pyrene (BP)]. The CYP1A1, 1B1, 2C9, 1A2 and 2B6 reported in wet-lab studies to actively metabolize DBP also showed strong binding energies (kcal/mol) of -11.50, -10.67, -10.37, -9.76 and -9.72, respectively, with inhibition constants ranging between 0...
May 19, 2017: Interdisciplinary Sciences, Computational Life Sciences
https://www.readbyqxmd.com/read/28513235/impact-of-interaction-between-cyp1a1-genetic-polymorphisms-and-smoking-on-coronary-artery-disease-in-the-han-of-china
#15
Dao-Di Peng, Wei Xie, Zai-Xin Yu
AIMS: To investigate the association of CYP1A1 genotype and additional gene-smoking interaction with coronary artery disease (CAD) risk based on a Chinese case-control study. METHODS: A total of 1862 participants (1134 men, 728 women) were selected, including 620 CAD patients and 1242 normal controls. Logistic regression was performed to investigate association of CYP1A1 genotype, gene-gene, and gene-smoking interaction with CAD. Generalized multifactor dimensionality reduction (GMDR) was used to screen the best gene-gene and gene-smoking interaction combination, cross-validation consistency, the testing balanced accuracy, and the sign test, to assess if each selected interaction was calculated...
2017: Clinical and Experimental Hypertension: CHE
https://www.readbyqxmd.com/read/28499825/induction-of-cytochrome-p450-dependent-mixed-function-oxidase-activities-and-peroxisome-proliferation-by-chloramine-t-in-male-rat-liver
#16
María-Aránzazu Martínez, Irma Ares, Jose-Luís Rodríguez, Marta Martínez, María-Rosa Martínez-Larrañaga, Arturo Anadón
Chloramine-T is an antimicrobial agent recognized for its disinfectant properties widely used in food industry. As an N-chloro-compound, chloramine-T contains electrophilic chlorine and in water it hydrolyses to hypochlorite. Chlorine as hypochlorous acid or hypochlorite is a very reactive chemical which can function as both an oxidant and halogenating agent. Because chloramine-T could be involved in the metabolic activation of drugs, in the present study the effects of chloramine-T on the activities of some drug metabolizing enzymes in rat liver microsomes and peroxisome proliferation were determined in vivo...
May 9, 2017: Food and Chemical Toxicology
https://www.readbyqxmd.com/read/28498411/mitochondrial-activity-and-oxidative-stress-functions-are-influenced-by-the-activation-of-ahr-induced-cyp1a1-overexpression-in-cardiomyocytes
#17
Bing Zhou, Xi Wang, Feng Li, Yingting Wang, Lei Yang, Xiaolong Zhen, Wuhong Tan
There is an endemic cardiomyopathy currently occurring in China, termed, Keshan disease (KD). The authors previously compared mitochondrial‑associated gene expression profiles of peripheral blood mononuclear cells (PBMCs) derived from KD patients and normal controls, using mitochondria‑focused cDNA microarray technology. The results detected an upregulation of the enzyme‑associated CYP1A1 gene, (ratios ≥2.0). The aryl hydrocarbon receptor (AhR) regulates the expression of numerous cytochrome P450 (CYP) genes including members of the CYP1 family; CYP1A1 and CYP1A2...
July 2017: Molecular Medicine Reports
https://www.readbyqxmd.com/read/28494841/quercetin-attenuates-benzo-%C3%AE-pyrene-induced-cyp1a-expression
#18
M L Perepechaeva, T A Seredina, Y A Sidorova, E N Pivovarova, A L Markel, V V Lyakhovich, A Y Grishanova
We studied effects of nutrient quercetin on cytochromes' Р450 1А (CYP1A) activities (measured spectrofluorimetrically using 7-ethoxy-resorufin for CYP1A1 and 7-methoxy-resorufin for CYP1A2 as substrates), on mRNA levels (measured by RT-PCR), and on DNA-binding activities (evaluated by an electrophoretic mobility shift assay) of proteins regulating CYP1A expression in untreated and benzo(α)pyrene (BaP)-treated rats. Wistar rats received quercetin, BaP, or both once daily for 1-3 days. Quercetin did not influence CYP1A1 in untreated rats but inhibited BaP-mediated CYP1A induction on the transcriptional level decreasing positive input (AhR functional activity) and increasing negative input (AhRR/ARNT expression and Oct-1 and C/EBP functional activities)...
April 2017: Biomedical and Environmental Sciences: BES
https://www.readbyqxmd.com/read/28494218/maternal-cigarette-smoking-during-pregnancy-and-offspring-dna-methylation-in-midlife
#19
Parisa Tehranifar, Hui-Chen Wu, Jasmine A McDonald, Farzana Jasmine, Regina M Santella, Irina Gurvich, Julie D Flom, Mary Beth Terry
Maternal smoking in pregnancy (MSP) has been associated with DNA methylation in specific CpG sites in infants and children. We investigated whether MSP, independent of own personal active smoking, was associated with midlife DNA methylation in CpGs that were previously identified in studies of MSP-DNA methylation in children. We used data on MSP collected from pregnant mothers of 89 adult women born in 1959-1964 and measured DNA methylation measured in blood (granulocytes) collected in 2001-2007 (mean age: 43 years)...
May 11, 2017: Epigenetics: Official Journal of the DNA Methylation Society
https://www.readbyqxmd.com/read/28489395/identification-of-potent-and-selective-cyp1a1-inhibitors-via-combined-ligand-and-structure-based-virtual-screening-and-their-in-vitro-validation-in-sacchrosomes-and-live-human-cells
#20
Prashant Joshi, Glen J P McCann, Vinay Sonawane, Ram A Vishwakarma, Bhabatosh Chaudhuri, Sandip B Bharate
Target structure-guided virtual screening (VS) is a versatile, powerful and inexpensive alternative to experimental high-throughput screening (HTS). In order to discover potent CYP1A1 enzyme inhibitors for cancer chemoprevention, a commercially library of 50,000 small molecules was utilized for VS guided by both ligand and structure-based strategies. For experimental validation, 300 ligands were proposed based on combined analysis of fitness scores from ligand based e-pharmacophore screening and docking score, prime MMGB/SA binding affinity and interaction pattern analysis from structure-based VS...
May 10, 2017: Journal of Chemical Information and Modeling
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