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https://www.readbyqxmd.com/read/28220904/recent-advances-in-occupational-and-environmental-health-hazards-of-workers-exposed-to-gasoline-compounds
#1
REVIEW
Christopher E Ekpenyong, Asuquo E Asuquo
The impact of health and environmental hazards, associated with the constituents of gasoline, on occupationally exposed workers has been recorded over the past few decades. However, the scientific literature on their pathogenic potential remains incomplete, which could affect the current understanding of the associated health risks. This review provides current information based on recently improved research techniques to evaluate gasoline toxicity profiles for humans. Our current knowledge provides insight into the intricate mechanism of gasoline-induced adverse effects, including the formation of reactive metabolites via bio-activation and subsequent generation of reactive oxygen species (ROS) and oxidative stress, which are involved in multiple mechanisms that are central to the aetiology of gasoline-induced toxicity...
February 21, 2017: International Journal of Occupational Medicine and Environmental Health
https://www.readbyqxmd.com/read/28213320/comparative-analysis-of-mosquito-diptera-culicidae-aedes-aegypti-liston-responses-to-the-insecticide-temephos-and-plant-derived-essential-oil-derived-from-piper-betle-l
#2
Prabhakaran Vasantha-Srinivasan, Sengottayan Senthil-Nathan, Athirstam Ponsankar, Annamalai Thanigaivel, Edward-Sam Edwin, Selvaraj Selin-Rani, Muthiah Chellappandian, Venkatraman Pradeepa, Jalasteen Lija-Escaline, Kandaswamy Kalaivani, Wayne B Hunter, Veeramuthu Duraipandiyan, Naif Abdullah Al-Dhabi
Resistance to treatments with Temephos or plant derived oil, Pb-CVO, between a field collected Wild Strain (WS) and a susceptible Laboratory Strain (LS) of Ae. aegypti were measured. The Temephos (0.1mg/L) showed the greatest percentage of mosquito mortality compared to Pb-CVO (1.5mg/L) in LS Ae. aegypti. However, WS Ae. aegypti was not significantly affected by Temephos (0.1mg/L) treatment compare to the Pb-CVO (1.5mg/L). However, both strains (LS and WS) when treated with Pb-CVO (1.5mg/L) displayed steady larval mortality rate across all instars...
February 14, 2017: Ecotoxicology and Environmental Safety
https://www.readbyqxmd.com/read/28202360/lycopene-resveratrol-vitamin-c-and-feso4-increase-damage-produced-by-pro-oxidant-carcinogen-4-nitroquinoline-1-oxide-in-drosophila-melanogaster-xenobiotic-metabolism-implications
#3
I E Dueñas-García, M E Heres-Pulido, M R Arellano-Llamas, J De la Cruz-Núñez, V Cisneros-Carrillo, C S Palacios-López, L Acosta-Anaya, L F Santos-Cruz, L Castañeda-Partida, A Durán-Díaz
4-nitroquinoline-1-oxide (4-NQO) is a pro-oxidant carcinogen bioactivated by xenobiotic metabolism (XM). We investigated if antioxidants lycopene [0.45, 0.9, 1.8 μM], resveratrol [11, 43, 172 μM], and vitamin C [5.6 mM] added or not with FeSO4 [0.06 mM], modulate the genotoxicity of 4-NQO [2 mM] with the Drosophila wing spot test standard (ST) and high bioactivation (HB) crosses, with inducible and high levels of cytochromes P450, respectively. The genotoxicity of 4-NQO was higher when dissolved in an ethanol - acetone mixture...
February 12, 2017: Food and Chemical Toxicology
https://www.readbyqxmd.com/read/28197160/digital-gene-expression-analysis-provides-insight-into-the-transcript-profile-of-the-genes-involved-in-aporphine-alkaloid-biosynthesis-in-lotus-nelumbo-nucifera
#4
Mei Yang, Lingping Zhu, Ling Li, Juanjuan Li, Liming Xu, Ji Feng, Yanling Liu
The predominant alkaloids in lotus leaves are aporphine alkaloids. These are the most important active components and have many pharmacological properties, but little is known about their biosynthesis. We used digital gene expression (DGE) technology to identify differentially-expressed genes (DEGs) between two lotus cultivars with different alkaloid contents at four leaf development stages. We also predicted potential genes involved in aporphine alkaloid biosynthesis by weighted gene co-expression network analysis (WGCNA)...
2017: Frontiers in Plant Science
https://www.readbyqxmd.com/read/28186385/activating-nuclear-xenobiotic-receptors-and-triggering-er-stress-and-hepatic-cytochromes-p450-systems-in-quails-coturnix-c-coturnix-during-atrazine-exposure
#5
Zheng-Hai Du, Lei Qin, Jia Lin, Yan-Chun Sun, Jun Xia, Cong Zhang, Xue-Nan Li, Jin-Long Li
Atrazine (ATR) is one of the most widely detected contaminant in the ecosystem. Nuclear xenobiotic receptors are activated by herbicides and induce the transcription of CYP450 isoforms involved in xenobiotic metabolism and transport. However, little is known about hepatic nuclear xenobiotic receptors in birds are responsible for ATR-induced hepatotoxicity via regulating the cytochrome P450 enzyme systems (CYP450s). The objective of this study was to investigate the mechanism of ATR hepatotoxicity in quails...
February 10, 2017: Environmental Toxicology
https://www.readbyqxmd.com/read/28177134/the-influence-of-combination-use-of-cyp450-inducers-on-the-pharmacokinetics-of-voriconazole-a-systematic-review
#6
REVIEW
T-Y Li, W Liu, K Chen, S-Y Liang, F Liu
WHAT IS KNOWN AND OBJECTIVES: Voriconazole is a triazole antifungal agent and is extensively metabolized via cytochrome P450 (CYP450); therefore, special precautions need to be taken when co-administered with a known CYP450 inducer, which may lead to treatment failure. The influence of some CYP450 inducers on the pharmacokinetics of voriconazole has been described in previous studies, but a systematic review was lacking. In this study, we carried out a systematic review to assess the influence of CYP450 inducers on the pharmacokinetic (PK) parameters of voriconazole...
February 8, 2017: Journal of Clinical Pharmacy and Therapeutics
https://www.readbyqxmd.com/read/28173639/bosentan-and-rifampin-interactions-modulate-influx-transporter-and-cytochrome-p450-expression-and-activities-in-primary-human-hepatocytes
#7
Kyoung-Moon Han, Sun-Young Ahn, Hyewon Seo, Jaesuk Yun, Hye Jin Cha, Ji-Soon Shin, Young-Hoon Kim, Hyungsoo Kim, Hye-Kyung Park, Yong-Moon Lee
The incidence of polypharmacy-which can result in drug-drug interactions-has increased in recent years. Drug-metabolizing enzymes and drug transporters are important polypharmacy modulators. In this study, the effects of bosentan and rifampin on the expression and activities of organic anion-transporting peptide (OATP) and cytochrome P450 (CYP450) 2C9 and CYP3A4 were investigated in vitro. HEK293 cells and primary human hepatocytes overexpressing the target genes were treated with bosentan and various concentrations of rifampin, which decreased the uptake activities of OATP transporters in a dose-dependent manner...
February 6, 2017: Biomolecules & Therapeutics
https://www.readbyqxmd.com/read/28172768/p004-stimulation-of-cyp450-mediated-%C3%AF-3-docosahexaenoic-acid-metabolism-via-mfsd2a-as-a-novel-therapy-for-inflammatory-bowel-disease
#8
F Ungaro, C Tacconi, C Correale, L Massimino, P Corsetto, A Piontini, P Fonteyne, F Calcaterra, S Della Bella, A Spinelli, M Carvello, A Rizzo, S Vetrano, G Fiorino, F Furfaro, K R Maddipati, S D'Alessio, S Danese
No abstract text is available yet for this article.
February 1, 2017: Journal of Crohn's & Colitis
https://www.readbyqxmd.com/read/28167220/omega-3-fatty-acids-and-cytochrome-p450-derived-eicosanoids-in-cardiovascular-diseases-which-actions-and-interactions-modulate-hemodynamics
#9
REVIEW
Sara Bonafini, Cristiano Fava
Increasing interest is focused on omega-3 fatty acids (FA) because of their potential beneficial effects, particularly in cardiovascular disease prevention. Eicosapentaenoic acid (EPA) and docosahexaenoic acid (DHA), two major omega-3 FA, are mainly consumed through diet, particularly from fish and seafood intake, whereas alpha-linolenic acid (ALA) is present in high amounts in leafy green vegetables, nuts and seeds. The hypothesis of a cardiovascular protective action of omega-3 FA derives mainly from observational studies, whereas the evidence from interventional studies is not always consistent...
February 3, 2017: Prostaglandins & Other Lipid Mediators
https://www.readbyqxmd.com/read/28152562/a-comparative-evaluation-of-models-to-predict-human-intestinal-metabolism-from-nonclinical-data
#10
Estelle Yau, Carl Petersson, Hugues Dolgos, Sheila Annie Peters
Extensive gut metabolism is often associated with the risk of low and variable bioavailability. Prediction of the fraction of drug escaping gut wall metabolism as well as transporter-mediated secretion (Fg ) has been challenged by the lack of appropriate preclinical models. The purpose of this study is to compare the performance of models that are widely employed in the pharmaceutical industry today to estimate Fg , and based on the outcome to provide recommendations for the prediction of human Fg during drug discovery and early drug development...
February 2, 2017: Biopharmaceutics & Drug Disposition
https://www.readbyqxmd.com/read/28149949/cyp450-enzymes-effect-oxygen-dependent-reduction-of-azide-based-fluorogenic-dyes
#11
Liam J O'Connor, Ishna N Mistry, Sarah L Collins, Lisa K Folkes, Graham Brown, Stuart J Conway, Ester M Hammond
Azide-containing compounds have broad utility in organic synthesis and chemical biology. Their use as powerful tools for the labeling of biological systems in vitro has enabled insights into complex cellular functions. To date, fluorogenic azide-containing compounds have primarily been employed in the context of click chemistry and as sensitive functionalities for hydrogen sulfide detection. Here, we report an alternative use of this functionality: as fluorogenic probes for the detection of depleted oxygen levels (hypoxia)...
January 25, 2017: ACS Central Science
https://www.readbyqxmd.com/read/28139732/intravenous-formulation-of-het0016-decreased-human-glioblastoma-growth-and-implicated-survival-benefit-in-rat-xenograft-models
#12
Meenu Jain, Nipuni-Dhanesha H Gamage, Meshal Alsulami, Adarsh Shankar, Bhagelu R Achyut, Kartik Angara, Mohammad H Rashid, Asm Iskander, Thaiz F Borin, Zhi Wenbo, Roxan Ara, Meser M Ali, Iryna Lebedyeva, Wilson B Chwang, Austin Guo, Hassan Bagher-Ebadian, Ali S Arbab
Glioblastoma (GBM) is a hypervascular primary brain tumor with poor prognosis. HET0016 is a selective CYP450 inhibitor, which has been shown to inhibit angiogenesis and tumor growth. Therefore, to explore novel treatments, we have generated an improved intravenous (IV) formulation of HET0016 with HPßCD and tested in animal models of human and syngeneic GBM. Administration of a single IV dose resulted in 7-fold higher levels of HET0016 in plasma and 3.6-fold higher levels in tumor at 60 min than that in IP route...
January 31, 2017: Scientific Reports
https://www.readbyqxmd.com/read/28112323/mimicking-liver-sinusoidal-structures-and-functions-using-a-3d-configured-microfluidic-chip
#13
Yu Du, Ning Li, Hao Yang, Chunhua Luo, Yixin Gong, Chunfang Tong, Yuxin Gao, Shouqin Lü, Mian Long
Physiologically, four major types of hepatic cells - the liver sinusoidal endothelial cells, Kupffer cells, hepatic stellate cells, and hepatocytes - reside inside liver sinusoids and interact with flowing peripheral cells under blood flow. It is hard to mimic an in vivo liver sinusoid due to its complex multiple cell-cell interactions, spatiotemporal construction, and mechanical microenvironment. Here we developed an in vitro liver sinusoid chip by integrating the four types of primary murine hepatic cells into two adjacent fluid channels separated by a porous permeable membrane, replicating liver's key structures and configurations...
January 23, 2017: Lab on a Chip
https://www.readbyqxmd.com/read/28111763/cytochrome-p450-reaction-phenotyping-and-inhibition-and-induction-studies-of-pinostrobin-in-human-liver-microsomes-and-hepatocytes
#14
Shengnan Tan, Zhimin Dong, Jiashuo Zhang, Thomas Efferth, Yujie Fu, Xin Hua
Pinostrobin (PI, 5-hydroxy-7-methoxyflavanone) is a natural flavonoid known for its rich pharmacological activities. The objective of this study was to identify the human liver cytochrome P450 (CYP450) isoenzymes involved in the metabolism of PI. A single hydoxylated metabolite was obtained from PI after an incubation with pooled human liver microsomes (HLMs). The relative contributions of different CYP450s were evaluated using CYP450-selective inhibitors in HLMs and recombinant human CYP450 enzymes, and the results revealed the major involvement of CYP1A2, CYP2C9 and CYP2E1 in PI metabolism...
November 7, 2016: Biomedical Chromatography: BMC
https://www.readbyqxmd.com/read/28110013/dna-damage-and-translational-response-during-detoxification-from-copper-exposure-in-a-wild-population-of-chironomus-riparius
#15
Paola Bernabò, Matteo Gaglio, Francesco Bellamoli, Gabriella Viero, Valeria Lencioni
Copper is one of the predominant components of pesticides employed in agriculture and known to be highly toxic once it reaches aquatic organisms. The impact of sublethal concentrations of this metal on wild insects is not yet completely understood. Studies addressing alterations in different levels of gene expression are still lacking. We previously demonstrated that in a wild population of Chironomus riparius, HSP and CYP families of genes were up-regulated at the transcriptional level after copper exposure...
January 16, 2017: Chemosphere
https://www.readbyqxmd.com/read/28104494/thoughts-on-interactions-between-pgrmc1-and-diverse-attested-and-potential-hydrophobic-ligands
#16
REVIEW
Michael A Cahill, Amy E Medlock
Progesterone Receptor Membrane Component 1 (PGRMC1) is located in many different subcellular locations with many different attested and probably location-specific functions. PGRMC1 was recently identified in the mitochondrial outer membrane where it interacts with ferrochelatase, the last enzyme in the heme synthetic pathway. It has been proposed that PGRMC1 may act as a chaperone to shuttle newly synthesized heme from the mitochondrion to cytochrome P450 (cyP450) enzymes. Here we consider potential roles that PGRMC1 may play in transferring heme, and other small hydrophobic ligands such as cholesterol and steroids, between the hydrophobic compartment of the membrane lipid bilayer interior to aqueous proteins, and perhaps to the membranes of other organelles...
January 16, 2017: Journal of Steroid Biochemistry and Molecular Biology
https://www.readbyqxmd.com/read/28097507/in-vitro-phase-i-and-phase-ii-drug-metabolism-in-the-liver-of-juvenile-and-adult-g%C3%A3-ttingen-minipigs
#17
Els Van Peer, Frank Jacobs, Jan Snoeys, Jos Van Houdt, Ils Pijpers, Christophe Casteleyn, Chris Van Ginneken, Steven Van Cruchten
PURPOSE: In view of pediatric drug development, juvenile animal studies are gaining importance. However, data on drug metabolizing capacities of juvenile animals are scarce, especially in non-rodent species. Therefore, we aimed to characterize the in vitro biotransformation of four human CYP450 substrates and one UGT substrate in the livers of developing Göttingen minipigs. METHODS: Liver microsomes from late fetal, Day 1, Day 3, Day 7, Day 28, and adult male and female Göttingen minipigs were incubated with a cocktail of CYP450 substrates, including phenacetin, tolbutamide, dextromethorphan, and midazolam...
January 17, 2017: Pharmaceutical Research
https://www.readbyqxmd.com/read/28094799/activation-of-wnt-%C3%AE-catenin-signalling-via-gsk3-inhibitors-direct-differentiation-of-human-adipose-stem-cells-into-functional-hepatocytes
#18
Jieqiong Huang, Xinyue Guo, Weihong Li, Haiyan Zhang
The generation of hepatocytes that are derived from human adipose stem cells (hASCs) represents an alternative to human hepatocytes for individualized therapeutic and pharmaceutical applications. However, the mechanisms facilitating hepatocyte differentiation from hASCs are not well understood. Here, we show that upon exposure to glycogen synthase kinase 3 (GSK3) inhibitors alone, the expression of definitive endoderm specific genes GATA4, FOXA2, and SOX17 in hASCs significantly increased in a manner with activation of Wnt/β-catenin signalling...
January 17, 2017: Scientific Reports
https://www.readbyqxmd.com/read/28075650/pharmacokinetic-evaluation-of-pregabalin-for-the-treatment-of-generalized-anxiety-disorder
#19
Massimiliano Buoli, Alice Caldiroli, Marta Serati
Pregabalin is an alternative compound to SSRIs and SNRIs for the first-line treatment of generalized anxiety disorder (GAD). Areas covered: We describe the pharmacokinetic properties of pregabalin and their implications for the treatment of GAD. A search in the main database sources (Medline, ISI, Web of Knowledge and Medscape) was performed in order to obtain a comprehensive and balanced evaluation about the clinical implications of the pharmacokinetic properties of pregabalin in the treatment of GAD. The word "pregabalin" was associated with "pharmacokinetics", "interactions"', "GAD", "anxiety" and "tolerability"...
March 2017: Expert Opinion on Drug Metabolism & Toxicology
https://www.readbyqxmd.com/read/28073119/in-vitro-inhibition-of-human-cyp450s-1a2-2c9-3a4-5-2d6-and-2e1-by-grandisin
#20
Maísa Daniela Habenschus, Fernanda de Lima Moreira, Norberto Peporine Lopes, Anderson R M de Oliveira
Grandisin, a lignan isolated from many species of plants, such as Virola surinamensis, is a potential drug candidate due to its biological properties, highlighted by its antitumor and trypanocidal activities. In this study, the inhibitory effects of grandisin on the activities of human cytochrome P450 enzymes were investigated by using human liver microsomes. Results showed that grandisin is a competitive inhibitor of CYP2C9 and a competitive and mechanism-based inhibitor of CYP3A4/5. The apparent Ki value for CYP2C9 was 50...
January 10, 2017: Planta Medica
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