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https://www.readbyqxmd.com/read/28302028/quantum-mechanical-qm-calculations-applied-to-admet-drug-prediction-a-review
#1
Edeildo F Silva-Júnior, J X Araújo-Júnior, T M Aquino
The discovery of new drugs is generally considered a long and expensive process, which often leads to molecules with low efficacy and high toxicity, which in many cases can be related to metabolism. In an attempt to reduce these failures and the production costs of a new drug, in silico studies have been used to obtain important information about the behavior of these compounds in the metabolism phases: absorption, distribution, metabolism (or biotransformation) and elimination (or excretion). Quantum Mechanical (QM) calculations are based on Schrödinger's equation can be used to develop models and theoretical parameters able to explain properties observed experimentally...
March 15, 2017: Current Drug Metabolism
https://www.readbyqxmd.com/read/28294491/an-efficient-chemoenzymatic-synthesis-of-dihydroartemisinic-aldehyde
#2
Melodi Demiray, Xiaoping Tang, Thomas Wirth, Juan A Faraldos, Rudolf K Allemann
Artemisinin from the plant Artemisia annua is the most potent pharmaceutical for the treatment of malaria. In the plant, the sesquiterpene cyclase amorphadiene synthase, a cytochrome-dependent CYP450, and an aldehyde reductase convert farnesyl diphosphate (FDP) into dihydroartemisinic aldehyde (DHAAl), which is a key intermediate in the biosynthesis of artemisinin and a semisynthetic precursor for its chemical synthesis. Here, we report a chemoenzymatic process that is able to deliver DHAAl using only the sesquiterpene synthase from a carefully designed hydroxylated FDP derivative...
March 13, 2017: Angewandte Chemie
https://www.readbyqxmd.com/read/28285519/selenomethionine-alleviates-afb1-induced-damage-in-primary-chicken-hepatocytes-by-inhibiting-cyp450-1a5-expression-via-upregulated-selw-expression
#3
Xingxiang Chen, Chaoping Che, Viktor I Korolchuk, Fang Gan, Cuiling Pan, Kehe Huang
This study aims to evaluate the protective effects of selenomethionine (SeMet) on aflatoxin B1 (AFB1)-induced hepatotoxicity in primary chicken hepatocytes. Cell viability and lactic dehydrogenase activity assays revealed the dose dependence of AFB1 toxicity to chicken hepatocytes. AFB1 concentrations of >0.05 μg/mL significantly reduced glutathione and total superoxide dismutase levels and increased the malondialdehyde concentration and cytochrome P450 enzyme 1A5 (CYP450 1A5) mRNA levels (P < 0.05)...
March 21, 2017: Journal of Agricultural and Food Chemistry
https://www.readbyqxmd.com/read/28284116/effects-of-pentachlorophenol-on-the-quail-coturnix-japonica-liver-detoxification-pathway
#4
Peng Jiang, Jianshe Wang, Nan Sheng, Dongbing Wei, Jiayin Dai
Pentachlorophenol (PCP), an extensively used pesticide and biocide, is of critical environmental concern due to its toxicity and recalcitrance to degradation. In this study, the effect of PCP on induction of transcription factors, cytochrome P450 (CYP450) genes, and the antioxidative enzyme system were investigated in the quail liver. A total of 60 (4- to 6-week-old) male quails (Coturnix japonica) were administered 0, 0.05, 0.5, and 5 mg/kg/d PCP orally for 42 d. Following exposure, both absolute and relative liver weights were significantly lower than those of the control...
March 2, 2017: Chemosphere
https://www.readbyqxmd.com/read/28279931/quantitative-chiral-and-achiral-determination-of-ketamine-and-its-metabolites-by-lc-ms-ms-in-human-serum-urine-and-fecal-samples
#5
Mahmoud Hasan, Robert Hofstetter, Georg M Fassauer, Andreas Link, Werner Siegmund, Stefan Oswald
Ketamine (KET) is a widely used anesthetic drug which is metabolized by CYP450 enzymes to norketamine (n-KET), dehydronorketamine (DHNK), hydroxynorketamine (HNK) and hydroxyketamine (HK). Ketamine is a chiral compound and S-ketamine is known to be the more potent enantiomer. Here, we present the development and validation of three LC-MS/MS assays; the first for the quantification of racemic KET, n-KET and DHNK in human serum, urine and feces; the second for the separation and quantification of the S- and R-enantiomers of KET, n-KET and DHNK, and the third for separation and quantification of 2S,6S-hydroxynorketamine (2S,6S-HNK) and 2R,6R-hydroxynorketamine (2R,6R-HNK) in serum and urine with the ability to separate and detect 10 additional hydroxylated norketamine metabolites of racemic ketamine...
February 27, 2017: Journal of Pharmaceutical and Biomedical Analysis
https://www.readbyqxmd.com/read/28266568/elucidation-of-terpenoid-metabolism-in-scoparia-dulcis-by-rna-seq-analysis
#6
Yoshimi Yamamura, Fumiya Kurosaki, Jung-Bum Lee
Scoparia dulcis biosynthesize bioactive diterpenes, such as scopadulcic acid B (SDB), which are known for their unique molecular skeleton. Although the biosynthesis of bioactive diterpenes is catalyzed by a sequence of class II and class I diterpene synthases (diTPSs), the mechanisms underlying this process are yet to be fully identified. To elucidate these biosynthetic machinery, we performed a high-throughput RNA-seq analysis, and de novo assembly of clean reads revealed 46,332 unique transcripts and 40,503 two unigenes...
March 7, 2017: Scientific Reports
https://www.readbyqxmd.com/read/28253826/effect-of-codeine-on-cyp450-isoform-activity-of-rats
#7
Shuanghu Wang, Yanwen Dong, Ke Su, Jing Zhang, Linyi Wang, Anyue Han, Congcong Wen, Xianqin Wang, Yan He
CONTEXT: Codeine, also known as 3-methylmorphine, is an opiate used to treat pain, as a cough medicine and for diarrhoea. No study on the effects of codeine on the metabolic capacity of CYP enzyme is reported. OBJECTIVE: In order to investigate the effects of codeine on the metabolic capacity of cytochrome P450 (CYP) enzymes, a cocktail method was employed to evaluate the activities of CYP2B1, CYP2D1, CYP1A2, CYP3A2 and CYP2C11. MATERIALS AND METHODS: Sprague-Dawley rats were randomly divided into codeine group (low, medium, high) and control group...
December 2017: Pharmaceutical Biology
https://www.readbyqxmd.com/read/28253085/water-pipe-shisha-hookah-arghile-smoking-and-secondhand-tobacco-smoke-effects-on-cyp1a2-and-cyp2a6-phenotypes-as-measured-by-caffeine-urine-test
#8
Şenay Görücü Yılmaz, Adrián Llerena, Fernando De Andrés, Ümit Karakaş, Hasan Gündoğar, Kamile Erciyas, Sabit Kimyon, Alper Mete, Kıvanç Güngör, Vural Özdemir
Public policies to stop or reduce cigarette smoking and exposure to secondhand smoke and associated diseases have yielded successful results over the past decade. Yet, the growing worldwide popularity of another form of tobacco consumption, water pipe smoking, has received relatively less attention. To the best of our knowledge, no study to date has evaluated the effects of water pipe smoking on cytochrome P450 (CYP450) activities and drug interaction potential in humans, whereas only limited information is available on the impact of secondhand smoke on drug metabolism...
March 2017: Omics: a Journal of Integrative Biology
https://www.readbyqxmd.com/read/28239160/insights-into-the-molecular-mechanisms-of-polygonum-multiflorum-thunb-induced-liver-injury-a-computational-systems-toxicology-approach
#9
Yin-Yin Wang, Jie Li, Zeng-Rui Wu, Bo Zhang, Hong-Bin Yang, Qin Wang, Ying-Chun Cai, Gui-Xia Liu, Wei-Hua Li, Yun Tang
An increasing number of cases of herb-induced liver injury (HILI) have been reported, presenting new clinical challenges. In this study, taking Polygonum multiflorum Thunb (PmT) as an example, we proposed a computational systems toxicology approach to explore the molecular mechanisms of HILI. First, the chemical components of PmT were extracted from 3 main TCM databases as well as the literature related to natural products. Then, the known targets were collected through data integration, and the potential compound-target interactions (CTIs) were predicted using our substructure-drug-target network-based inference (SDTNBI) method...
February 27, 2017: Acta Pharmacologica Sinica
https://www.readbyqxmd.com/read/28237650/inhibition-and-inactivation-of-human-cyp2j2-implications-in-cardiac-pathophysiology-and-opportunities-in-cancer-therapy
#10
REVIEW
Aneesh Karkhanis, Yanjun Hong, Eric Chun Yong Chan
Extrahepatic cytochrome P450 enzymes (CYP450) are pivotal in the metabolism of endogenous substrates and xenobiotics. CYP2J2 is a major cardiac CYP450 and primarily metabolizes polyunsaturated fatty acids such as arachidonic acid to cardioactive epoxyeicosatrienoic acids. Due to its role in endobiotic metabolism, CYP2J2 has been actively studied in recent years with the focus on its biological functions in cardiac pathophysiology. Additionally, CYP2J2 metabolizes a number of xenobiotics such as astemizole and terfenadine and is potently inhibited by danazol and telmisartan...
February 23, 2017: Biochemical Pharmacology
https://www.readbyqxmd.com/read/28226256/endocrine-and-cellular-stress-effects-of-zinc-oxide-nanoparticles-and-nifedipine-in-marsh-frogs-pelophylax-ridibundus
#11
Halina Falfushynska, Lesya Gnatyshyna, Oksana Horyn, Inna Sokolova, Oksana Stoliar
Freshwater organisms including amphibians experience increasing exposures to emerging pollutants such as nanoparticles and pharmaceuticals, which can affect their fitness and performance. We studied the effects of two common pollutants extensively used in industry, pharmaceutical and personal care products, nano-zinc oxide (nZnO) and a Ca-channel blocker nifedipine (Nfd), on endocrine status and cellular stress markers of the marsh frog Pelophylax ridibundus. Males were exposed for 14days to nZnO (3.1μM), Zn(2+) (3...
April 2017: Aquatic Toxicology
https://www.readbyqxmd.com/read/28220904/recent-advances-in-occupational-and-environmental-health-hazards-of-workers-exposed-to-gasoline-compounds
#12
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
#13
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 20, 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
#14
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
#15
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
#16
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
#17
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
#18
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
#19
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
#20
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...
January 2017: Prostaglandins & Other Lipid Mediators
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