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https://www.readbyqxmd.com/read/29233455/genetic-variation-of-cytochrome-p450-in-uyghur-chinese-population
#1
Guangzhao Qi, Duolu Li, Xiaojian Zhang
Interindividual and interethnic variability of drug responses could be attributed to the differences of genetic polymorphisms in the drug metabolizing enzymes and transporters genes among the populations. Here we reviewed the studies of genetic variations in Uyghur Chinese of fifteen CYP450 genes including CYP1A1, CYP1A2, CYP2A6, CYP2B6, CYP2C8, CYP2C9, CYP2C19, CYP2D6, CYP2E1, CYP2J2, CYP2W1, CYP3A4, CYP3A5, CYP4A11, and CYP17A1, which totally covered 277 variants. We also collected the data of 277 variants covered in our study in two extensive population sequencing projects, the International HapMap Project (Hap-Map) and the 1000 Genomes Project and compared them with the data of Uyghur Chinese...
March 6, 2017: Drug Metabolism and Pharmacokinetics
https://www.readbyqxmd.com/read/29232922/study-on-the-correlation-between-gene-expression-and-enzyme-activity-of-seven-key-enzymes-and-ginsenoside-content-in-ginseng-in-over-time-in-ji-an-china
#2
Juxin Yin, Daihui Zhang, Jianjian Zhuang, Yi Huang, Ying Mu, Shaowu Lv
Panax ginseng is a traditional medicine. Fresh ginseng is one of the most important industries related to ginseng development, and fresh ginseng of varying ages has different medicinal properties. Previous research has not systematically reported the correlation between changes in key enzyme activity with changes in ginsenoside content in fresh ginseng over time. In this study, for the first time, we use ginseng samples of varying ages in Ji'an and systematically reported the changes in the activity of seven key enzymes (HMGR, FPS, SS, SE, DS, CYP450, and GT)...
December 11, 2017: International Journal of Molecular Sciences
https://www.readbyqxmd.com/read/29228347/exposure-of-mice-to-1-2-dichloropropane-induces-cyp450-dependent-proliferation-and-apoptosis-of-cholangiocytes
#3
Xiao Zhang, Cai Zong, Lingyi Zhang, Edwin Garner, Shigeyuki Sugie, Chinyen Huang, Wenting Wu, Jie Chang, Toshihiro Sakurai, Masashi Kato, Sahoko Ichihara, Shinji Kumagai, Gaku Ichihara
1, 2-Dichloropropane (1, 2-DCP) has been used as a paint remover in the industry. The International Agency for Research on Cancer reclassified this compound recently to Group 1 (carcinogenic to humans) based on epidemiological studies of cholangiocarcinoma among offset-color proof-printing workers exposed to 1, 2-DCP in Japan. Two-year rodent carcinogenicity bioassays demonstrated that 1, 2-DCP induced tumors in liver and lung, but not in bile duct. The present study was designed to assess the toxic effects of 1, 2-DCP on proliferation and apoptosis in mice bile duct and the role of cytochrome P450 (CYP450) in any such effect...
December 7, 2017: Toxicological Sciences: An Official Journal of the Society of Toxicology
https://www.readbyqxmd.com/read/29227934/gabaa-receptor-activity-modulating-piperine-analogs-in-vitro-metabolic-stability-metabolite-identification-cyp450-reaction-phenotyping-and-protein-binding
#4
Volha Zabela, Timm Hettich, Götz Schlotterbeck, Laurin Wimmer, Marko D Mihovilovic, Fabrice Guillet, Belkacem Bouaita, Bénédicte Shevchenko, Matthias Hamburger, Mouhssin Oufir
In a screening of natural products for allosteric modulators of GABAA receptors (γ-aminobutyric acid type A receptor), piperine was identified as a compound targeting a benzodiazepine-independent binding site. Given that piperine is also an activator of TRPV1 (transient receptor potential vanilloid type 1) receptors involved in pain signaling and thermoregulation, a series of piperine analogs were prepared in several cycles of structural optimization, with the aim of separating GABAA and TRPV1 activating properties...
December 2, 2017: Journal of Chromatography. B, Analytical Technologies in the Biomedical and Life Sciences
https://www.readbyqxmd.com/read/29211346/chemogenomic-active-learning-s-domain-of-applicability-on-small-sparse-qhts-matrices-a-study-using-cyp450-and-nuclear-hormone-receptor-families
#5
Christin Rakers, Rifat Ara Najnin, Ahsan Habib Polash, Shunichi Takeda, J B Brown
Computational models for predicting the activity of small molecules against targets are now routinely developed and used in academia and industry, partially due to public bioactivity databases. While models based on bigger datasets are the trend, recent studies such as chemogenomic active learning have shown that only a fraction of data is needed for effective models in many cases. In this article, the chemogenomic active learning method is discussed and used to newly analyze public databases containing nuclear hormone receptor and cytochrome P450 receptor family bioactivity...
December 6, 2017: ChemMedChem
https://www.readbyqxmd.com/read/29209748/monitoring-cytochrome-p450-activity-in-living-hepatocytes-by-chromogenic-substrates-in-response-to-drug-treatment-or-during-cell-maturation
#6
Jannick Theobald, Xinlai Cheng, Ali Ghanem, Haristi Gaitantzi, Guangqi Song, Edda Klipp, Judith Wodke, Holger Becker, Ralf Mrowka, Katja Breitkopf-Heinlein, Steven Dooley, Stefan Wölfl
The metabolic activity of hepatocytes is a central prerequisite for drug activity and a key element in drug-drug interaction. This central role in metabolism largely depends on the activity of the cytochrome P450 (CYP450) enzyme family, which is not only dependent on liver cell maturation but is also controlled in response to drug and chemical exposure. Here, we report the use of VividDye fluorogenic CYP450 substrates to directly measure and continuously monitor metabolic activity in living hepatocytes. We observed time- and dose-dependent correlation in response to established and putative CYP450 inducers acting through the aryl hydrocarbon receptor and drug combinations...
December 5, 2017: Archives of Toxicology
https://www.readbyqxmd.com/read/29209217/arylacetamide-deacetylase-is-involved-in-vicagrel-bioactivation-in-humans
#7
Jinfang Jiang, Xiaoyan Chen, Dafang Zhong
Vicagrel, a structural analog of clopidogrel, is now being developed as a thienopyridine antiplatelet agent in a phase II clinical trial in China. Some studies have shown that vicagrel undergoes complete first-pass metabolism in human intestine, generating the hydrolytic metabolite 2-oxo-clopidogrel via carboxylesterase-2 (CES2) and subsequently the active metabolite H4 via CYP450s. This study aimed to identify hydrolases other than CES2 that are involved in the bioactivation of vicagrel in human intestine...
2017: Frontiers in Pharmacology
https://www.readbyqxmd.com/read/29209210/critical-role-of-hepatic-cyp450s-in-the-testis-specific-toxicity-of-5r-5-hydroxytriptolide-in-c57bl-6-mice
#8
Cunzhi Yu, Yu Li, Mingxia Liu, Man Gao, Chenggang Li, Hong Yan, Chunzhu Li, Lihan Sun, Liying Mo, Chunyong Wu, Xinming Qi, Jin Ren
Low solubility, tissue accumulation, and toxicity are chief obstacles to developing triptolide derivatives, so a better understanding of the pharmacokinetics and toxicity of triptolide derivatives will help with these limitations. To address this, we studied pharmacokinetics and toxicity of (5R)-5-hydroxytriptolide (LLDT-8), a novel triptolide derivative immunosuppressant in a conditional knockout (KO) mouse model with liver-specific deletion of CYP450 reductase. Compared to wild type (WT) mice, after LLDT-8 treatment, KO mice suffered severe testicular toxicity (decreased testicular weight, spermatocytes apoptosis) unlike WT mice...
2017: Frontiers in Pharmacology
https://www.readbyqxmd.com/read/29207507/zinc-ameliorate-oxidative-stress-and-hormonal-disturbance-induced-by-methomyl-abamectin-and-their-mixture-in-male-rats
#9
Sameeh A Mansour, Mostafa A Abbassy, Hassan A Shaldam
Exposure to mixtures of toxicants (e.g., pesticides) is common in real life and a subject of current concern. The present investigation was undertaken to assess some toxicological effects in male rats following exposure to methomyl (MET), abamectin (ABM), and their combination (MET+ABM), and to evaluate the ameliorative effect of zinc co-administration. Three groups of rats were designated for MET, ABM, and the mixture treatments. Three other groups were designated for zinc in conjunction with the pesticides...
December 3, 2017: Toxics
https://www.readbyqxmd.com/read/29202315/effect-of-enrofloxacin-and-roxarsone-on-cyp450s-in-pig
#10
Yinsheng Li, Meilin Jiang, Michelle Thunders, Xiaojie Ai, Jiangping Qiu
Enrofloxacin (ENR) and roxarsone (ROX) have been widely used in animal breeding. In this study, the daily clinical dosage of ENR and daily additive amount of ROX were administrated to Bama pigs. After 5days, the activity and protein expression of three important enzymes in the cytochrome P450 family were measured in the porcine liver. CYP1A2 was induced by both ENR and ROX independently. CYP2E1 and CYP3A4 were inhibited by ENR, but not affected by ROX. The combined administration of ENR and ROX were antagonistic to CYP1A2 and CYP2E1, but not to CYP3A4...
November 21, 2017: Research in Veterinary Science
https://www.readbyqxmd.com/read/29196123/boosting-11-oxo-%C3%AE-amyrin-and-glycyrrhetinic-acid-synthesis-in-saccharomyces-cerevisiae-via-pairing-novel-oxidation-and-reduction-system-from-legume-plants
#11
Ming Zhu, Caixia Wang, Wentao Sun, Anqi Zhou, Ying Wang, Genlin Zhang, Xiaohong Zhou, Yixin Huo, Chun Li
Glycyrrhetinic acid (GA) and its precursor, 11-oxo-β-amyrin, are typical triterpenoids found in the roots of licorice, a traditional Chinese medicinal herb that exhibits diverse functions and physiological effects. In this study, we developed a novel and highly efficient pathway for the synthesis of GA and 11-oxo-β-amyrin in Saccharomyces cerevisiae by introducing efficient cytochrome P450s (CYP450s: Uni25647 and CYP72A63) and pairing their reduction systems from legume plants through transcriptome and genome-wide screening and identification...
November 28, 2017: Metabolic Engineering
https://www.readbyqxmd.com/read/29185916/drug-drug-interactions-in-cocaine-users-and-their-clinical-implications
#12
Luca Gallelli, Santo Gratteri, Antonio Siniscalchi, Erika Cione, Sabrina Sirico, Paolo Seminara, Giovambattista De Sarro, Maria Cristina Caroleo
Drug-drug interactions (DDIs) are a common problem in clinical practice during drug treatments. DDIs can induce development of adverse drug reactions or reduce clinical efficacy of the drugs. In this review, using PubMed, Embase and Cochrane library we searched articles published until January 10, 2017, and described both pharmacokinetic and pharmacodynamic DDIs in cocaine consumers, focusing the interest on their clinical implications. In this review, the nodal points treated focused on: i) cocaine biochemical metabolism described for both, inactive benzoylecgonine and ecgonine methyl esters and norcocaine active metabolites...
September 20, 2017: Current Drug Abuse Reviews
https://www.readbyqxmd.com/read/29184146/2-3-4-5-tetrahydroxystilbene-2-o-%C3%AE-d-glucoside-exacerbates-acetaminophen-induced-hepatotoxicity-by-inducing-hepatic-expression-of-cyp2e1-cyp3a4-and-cyp1a2
#13
Shangfu Xu, Jie Liu, Jingshan Shi, Zhengtao Wang, Lili Ji
Hepatotoxicity induced by medicinal herb Polygonum multiflorum Thunb. attracts wide attention in the world recently. 2,3,4',5-tetrahydroxystilbene-2-O-β-D-glucoside (TSG) is a main active compound in Polygonum multiflorum Thunb. This study aims to observe TSG-provided the aggravation on acetaminophen (APAP)-induced hepatotoxicity in mice by inducing hepatic expression of cytochrome P450 (CYP450) enzymes. Serum alanine/aspartate aminotransferase (ALT/AST) analysis and liver histological evaluation showed that TSG (200, 400, 800 mg/kg) exacerbated the hepatotoxicity induced by sub-toxic dose of APAP (200 mg/kg) in mice, but TSG alone had no hepatotoxicity...
November 28, 2017: Scientific Reports
https://www.readbyqxmd.com/read/29183580/responses-in-reproductive-organs-steroid-hormones-and-cyp450-enzymes-in-female-mongolian-gerbil-meriones-unguiculatus-over-time-after-quinestrol-treatment
#14
Qian-Qian Su, Yi Chen, Jiao Qin, Tong-Liang Wang, De-Hua Wang, Quan-Sheng Liu
The aim of this study was to assess the effects and reversibility of the synthetic estrogen compound, quinestrol, on the reproductive organs, steroid hormones, and drug-metabolizing enzymes CYP3A4 and CYP1A2 in liver and kidney over time after two quinestrol treatments in female Mongolian gerbils (Meriones unguiculatus). Female gerbils were treated with 4mg/kg quinestrol (9 gerbils/group, 3 treated group) (1 control group, 0mg/kg) for 3days and treated again after 25days. Animals were killed for collection of samples at 5, 10 and 15days after the second treatment ending...
November 2017: Pesticide Biochemistry and Physiology
https://www.readbyqxmd.com/read/29180016/cytochrome-p450-cyp716a254-catalyzes-the-formation-of-oleanolic-acid-from-%C3%AE-amyrin-during-oleanane-type-triterpenoid-saponins-biosynthesis-in-anemone-flaccida
#15
Chuansong Zhan, Shakeel Ahmed, Hu Sheng, Shuang Dong, Qian Cai, Tewu Yang, Xuekui Wang, Xiaohua Li, Xuebo Hu
Anemone flaccida Fr. Shmidt (Ranunculaceae), known as 'Di Wu' in China, is a perennial herb which has long been used to treat arthritis. The rhizome of A. flaccida contains pharmacologically active components i.e. oleanane-type triterpenoid saponins. Oleanolic acid is natural triterpenoid in plants with diverse biological activities. The biosynthesis of oleanolic acid involves cyclization of 2,3-oxidosqualene to the oleanane-type triterpenoid skeleton, followed by a series of oxidation reactions catalyzed by cytochrome P450 monooxygenase (CYP450)...
November 24, 2017: Biochemical and Biophysical Research Communications
https://www.readbyqxmd.com/read/29176550/a-bioreducible-n-oxide-based-probe-for-photoacoustic-imaging-of-hypoxia
#16
Hailey J Knox, Jamila Hedhli, Tae Wook Kim, Kian Khalili, Lawrence W Dobrucki, Jefferson Chan
Hypoxia occurs when limited oxygen supply impairs physiological functions and is a pathological hallmark of many diseases including cancer and ischemia. Thus, detection of hypoxia can guide treatment planning and serve as a predictor of patient prognosis. Unfortunately, current methods suffer from invasiveness, poor resolution and low specificity. To address these limitations, we present Hypoxia Probe 1 (HyP-1), a hypoxia-responsive agent for photoacoustic imaging. This emerging modality converts safe, non-ionizing light to ultrasound waves, enabling acquisition of high-resolution 3D images in deep tissue...
November 27, 2017: Nature Communications
https://www.readbyqxmd.com/read/29169126/effect-of-copper-on-the-translocation-and-transformation-of-polychlorinated-biphenyls-in-rice
#17
Lili Pan, Jianteng Sun, X Chris Le, Lizhong Zhu
Contamination of organic pollutants in the environment is usually accompanied by heavy metals. However, a little information on the influences of heavy metals on the uptake, translocation and transformation of organic pollutants in plants is available. In this study, ten-day hydroponic exposure was conducted to explore the influence of copper (Cu) on the bioaccumulation and biotransformation of polychlorinated biphenyls (PCBs) in intact young rice (Oryza sativa L.). Low dose of Cu (≤100 μmol/L) increased the accumulation of CB-61 in rice plants, while excess concentrations of Cu (>100 μmol/L) inhibited uptake and translocation of CB-61...
November 13, 2017: Chemosphere
https://www.readbyqxmd.com/read/29157826/modulation-of-pregnane-x-receptor-pxr-and-constitutive-androstane-receptor-car-activation-by-ursolic-acid-ua-attenuates-rifampin-isoniazid-cytotoxicity
#18
Hsiao-Yun Chang, Chao-Jung Chen, Wei-Chih Ma, Wai-Kok Cheng, Yen-Ning Lin, Ying-Ray Lee, Jih-Jung Chen, Yun-Ping Lim
BACKGROUND: Interactions between transcriptional inducers of cytochrome P450 (CYP450) enzymes and therapeutic drugs may be prevented by antagonizing the activation of a nuclear receptor (NR), pregnane X receptor (PXR, NR1I2), thus improving therapeutic efficacy. PURPOSE: In the present study, we aim to identify that ursolic acid (UA), a widely distributed pentacyclic triterpene, may act as an effective antagonist of PXR and its sister NR receptor, constitutive androstane receptor (CAR, NR1I3)...
December 1, 2017: Phytomedicine: International Journal of Phytotherapy and Phytopharmacology
https://www.readbyqxmd.com/read/29155484/elevated-difenacoum-metabolism-involved-in-the-difenacoum-resistant-phenotype-observed-in-berkshire-rats-homozygous-for-the-l120q-mutation-in-vkorc1-gene
#19
Maylis Boitet, Abdessalem Hammed, Nolan Chatron, Jean Valéry Debaux, Etienne Benoit, Virginie Lattard
BACKGROUND: After its initial use, resistance to difenacoum has been detected rapidly in rats in north-east Hampshire and north-west Berkshire in England. Resistance to difenacoum has been reported to be stronger in rats from Berkshire than rats from Hampshire. Surprisingly, after the discovery of the Vkorc1 gene, rats from Berkshire and Hampshire were all shown to be homozygous for the L120Q mutation in the Vkorc1. RESULTS: This study aims to evaluate the resistance of Berkshire rats to confirm their extreme resistance and determine mechanisms supporting this resistance...
November 20, 2017: Pest Management Science
https://www.readbyqxmd.com/read/29154136/transcriptional-activity-of-detoxification-genes-is-altered-by-ultraviolet-filters-in-chironomus-riparius
#20
José-Luis Martínez-Guitarte
Ultraviolet (UV) filters are compounds used to prevent the damage produced by UV radiation in personal care products, plastics, etc. They have been associated with endocrine disruption, showing anti-estrogen activity in vertebrates and altering the ecdysone pathway in invertebrates. Although they have attracted the attention of multiple research teams there is a lack of data about how animals activate detoxification systems, especially in invertebrates. Here, analysis of the effects of two UV filters, benzophenone-3 (BP3) and 4-methylbenzylidene camphor (4MBC), on the transcriptional activity of nine genes covering the three steps of the detoxification process has been performed...
November 15, 2017: Ecotoxicology and Environmental Safety
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