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https://www.readbyqxmd.com/read/28652425/evaluation-of-biological-activity-of-mastic-extracts-based-on-chemotherapeutic-indices
#1
Ryuichiro Suzuki, Hiroshi Sakagami, Shigeru Amano, Kunihiko Fukuchi, Katsuyoshi Sunaga, Taisei Kanamoto, Shigemi Terakubo, Hideki Nakashima, Yoshiaki Shirataki, Mineko Tomomura, Yoshiko Masuda, Satoshi Yokose, Akito Tomomura, Hirofumi Watanabe, Masaki Okawara, Yoshiharu Matahira
BACKGROUND: Most previous mastic investigators have not considered its potent cytotoxicity that may significantly affect the interpretation of obtained data. In the present study, we re-evaluated several biological activities of mastic extracts, based on chemotherapeutic indexes. MATERIALS AND METHODS: Pulverized mastic gum was extracted with n-hexane and then with ethyl acetate or independently with methanol or n-butanol. Tumor specificity (TS) of the extracts was determined by their cytotoxicity against human malignant and non-malignant cells...
July 2017: In Vivo
https://www.readbyqxmd.com/read/28628909/nonalcoholic-fatty-liver-disease-impairs-the-cytochrome-p-450-dependent-metabolism-of-%C3%AE-tocopherol-vitamin-e
#2
Desirée Bartolini, Pierangelo Torquato, Carolina Barola, Angelo Russo, Chiara Rychlicki, Danilo Giusepponi, Guido Bellezza, Angelo Sidoni, Roberta Galarini, Gianluca Svegliati-Baroni, Francesco Galli
This study aims to investigate in in vivo and in vitro models of nonalcoholic fatty liver disease (NAFLD) the enzymatic metabolism of α-tocopherol (vitamin E) and its relationship to vitamin E-responsive genes with key role in the lipid metabolism and detoxification of the liver. The experimental models included mice fed a high-fat diet combined or not with fructose (HFD+F) and HepG2 human hepatocarcinoma cells treated with the lipogenic agents palmitate, oleate or fructose. CYP4F2 protein, a cytochrome P-450 isoform with proposed α-tocopherol ω-hydroxylase activity, decreased in HFD and even more in HFD+F mice liver; this finding was associated with increased hepatic levels of α-tocopherol and decreased formation of the corresponding long-chain metabolites α-13-hydroxy and α-13-carboxy chromanols...
June 7, 2017: Journal of Nutritional Biochemistry
https://www.readbyqxmd.com/read/28617523/electrochemical-characterization-of-geobacter-lovleyi-identifies-limitations-of-microbial-fuel-cell-performance-in-constructed-wetlands
#3
Clara Corbella, Rebecca P Steidl, Jaume Puigagut, Gemma Reguera
Power generation in microbial fuel cells implemented in constructed wetlands (CW-MFCs) is low despite the enrichment of anode electricigens most closely related to Geobacter lovleyi. Using the model representative G. lovleyi strain SZ, we show that acetate, but not formate or lactate, can be oxidized efficiently but growth is limited by the high sensitivity of the bacterium to oxygen. Acetate and highly reducing conditions also supported the growth of anode biofilms but only at optimal anode potentials (450 mV vs...
June 2017: International Microbiology: the Official Journal of the Spanish Society for Microbiology
https://www.readbyqxmd.com/read/28603032/%C3%AE-2-adrenergic-receptor-mediated-in-vitro-regulation-of-human-hepatic-drug-transporter-expression-by-epinephrine
#4
Abdullah Mayati, Amélie Moreau, Claire Denizot, Bruno Stieger, Yannick Parmentier, Olivier Fardel
The catecholamine epinephrine is known to repress expression of hepatic drug metabolizing enzymes such as cytochromes P-450. The present study was designed to determine whether epinephrine may also target expression of main hepatic drug transporters, that play a major role in liver detoxification and are commonly coordinately regulated with drug detoxifying enzymes. Treatment of primary human hepatocytes with 10μM epinephrine for 24h repressed mRNA expression of various transporters, such as the sinusoidal influx transporters NTCP, OATP1B1, OATP2B1, OAT2, OAT7 and OCT1 and the efflux transporters MRP2, MRP3 and BSEP, whereas it induced that of MDR1, but failed to alter that of BCRP...
August 30, 2017: European Journal of Pharmaceutical Sciences
https://www.readbyqxmd.com/read/28571502/liver-toxicity-mechanisms-of-herbs-commonly-used-in-latin-america
#5
Sofía López-Gil, Natalia Nuño-Lámbarri, Norberto Chávez-Tapia, Misael Uribe, Varenka J Barbero-Becerra
Mexico owns approximately 4500 medicinal plants species, a great diversity that position it at the second place after China. According to the Mexican health department, 90% of common population consumes them to treat various diseases. Additionally, herbal remedies in Latin America are considered a common practice, but the frequency of use and the liver damage related to its consumption is still unknown. Despite the high prevalence and indiscriminate herbal consumption, the exact mechanism of hepatotoxicity and adverse effects is not fully clarified and is still questioned...
June 2, 2017: Drug Metabolism Reviews
https://www.readbyqxmd.com/read/28557353/generation-of-carbamoyl-phosphate-synthetase-1-reporter-cell-lines-for-the-assessment-of-ammonia-metabolism
#6
Yi Wang, Le Chang, Jiahui Zhai, Qiao Wu, Donggen Wang, Yunfang Wang
Both primary hepatocytes and stem cells-derived hepatocyte-like cells (HLCs) are major sources for bioartificial liver (BAL). Maintenance of hepatocellular functions and induction of functional maturity of HLCs are critical for BAL's support effect. It remains difficult to assess and improve detoxification functions inherent to hepatocytes, including ammonia clearance. Here, we aim to assess ammonia metabolism and identify ammonia detoxification enhancer by developing an imaging strategy. In hepatoma cell line HepG2, and immortalized hepatic cell line LO2, carbamoyl phosphate synthetase 1 (CPS1) gene, the first enzyme of ammonia-eliminating urea cycle, was labelled with fluorescence protein via CRISPR/Cas9 system...
May 30, 2017: Journal of Cellular and Molecular Medicine
https://www.readbyqxmd.com/read/28541669/effects-of-polychlorinated-biphenyls-pcbs-and-their-hydroxylated-metabolites-oh-pcbs-on-arabidopsis-thaliana
#7
Srishty Subramanian, Jerald L Schnoor, Benoit Van Aken
Plants metabolize polychlorinated biphenyls (PCBs) into hydroxylated derivatives (OH-PCBs), which are sometimes more toxic than the parent PCBs. The objective of this research was to compare the toxicity of a suite of PCBs and OH-PCBs toward the model plant, Arabidopsis thaliana. While parent PCBs and higher-chlorinated OH-PCBs exhibited a low or nondetectable toxicity, lower-chlorinated OH-PCBs significantly inhibited the germination rate and plant growth, with inhibition concentration 50% (IC50) ranging from 1...
June 8, 2017: Environmental Science & Technology
https://www.readbyqxmd.com/read/28513969/effect-of-steady-state-faldaprevir-on-pharmacokinetics-of-atorvastatin-or-rosuvastatin-in-healthy-volunteers-a-prospective-open-label-fixed-sequence-crossover-study
#8
Fenglei Huang, Kristell Marzin, Rüdiger Koenen, Klaus Peter Kammerer, Natalja Strelkowa, Mabrouk Elgadi, Anne-Marie Quinson, Sebastian Haertter
Faldaprevir (FDV) is a potent, orally administered inhibitor of hepatitis C virus protease. It inhibits multiple cytochrome P-450 enzymes and multiple membrane transporters. The objective of this study was to evaluate the effect of steady-state faldaprevir on the pharmacokinetics (PK) of a single dose of atorvastatin or rosuvastatin. In this single-center, open-label, fixed-sequence crossover study, 33 healthy adult male and female volunteers were given either atorvastatin 10 mg (n = 16) or rosuvastatin 10 mg (n = 17) on day 1...
May 17, 2017: Journal of Clinical Pharmacology
https://www.readbyqxmd.com/read/28513222/the-contribution-of-cyp2c-gene-subfamily-involved-in-epoxygenase-pathway-of-arachidonic-acids-metabolism-to-hypertension-susceptibility-in-russian-population
#9
Alexey Polonikov, Marina Bykanova, Irina Ponomarenko, Svetlana Sirotina, Anna Bocharova, Kseniya Vagaytseva, Vadim Stepanov, Mikhail Churnosov, Olga Bushueva, Maria Solodilova, Yaroslav Shvetsov, Vladimir Ivanov
Numerous studies demonstrated an importance of cytochrome P-450 epoxygenase pathway of arachidonic acids metabolism for the pathogenesis of essential hypertension (EH). The present study was designed to investigate whether common single-nucleotide polymorphisms (SNP) of CYP2C gene subfamily such as CYP2C8 (rs7909236 and rs1934953), CYP2C9 (rs9332242), and CYP2C19 (rs4244285) are associated with susceptibility to EH in Russian population. A total of 816 unrelated Russian individuals comprising 425 EH patients and 391 normotensive controls were included into the study...
2017: Clinical and Experimental Hypertension: CHE
https://www.readbyqxmd.com/read/28501544/the-dna-methylation-status-alteration-of-two-steroidogenic-genes-in-gonads-of-rare-minnow-after-bisphenol-a-exposure
#10
Ting Zhang, Yan Liu, Hong Chen, Jiancao Gao, Yingying Zhang, Cong Yuan, Zaizhao Wang
Both cytochrome P450c17 (CYP17A1) and P-450 side chain cleavage (CYP11A1) play important roles in steroid biosynthesis. According to our previous studies, bisphenol A (BPA) could regulate the mRNA expression of cyp17a1 and cyp11a1 in rare minnow Gobiocypris rarus. However, the potential mechanism of the regulation is barely understood. In the present study, aiming to explore how BPA affects the mRNA expression of cyp17a1 and cyp11a1 in testes and ovaries of G. rarus, we firstly cloned 340-bp fragment of 5' flanking region of cyp11a1 and then detected the methylation level of CpG loci involved in 5' flanking of cyp11a1 and cyp17a1 and their mRNA expression levels...
May 10, 2017: Comparative Biochemistry and Physiology. Toxicology & Pharmacology: CBP
https://www.readbyqxmd.com/read/28501210/determination-of-tocopherols-and-their-metabolites-by-liquid-chromatography-coupled-with-tandem-mass-spectrometry-in-human-plasma-and-serum
#11
Danilo Giusepponi, Pierangelo Torquato, Desirée Bartolini, Marta Piroddi, Marc Birringer, Stefen Lorkowski, Carmelo Libetta, Gabriele Cruciani, Simone Moretti, Giorgio Saluti, Francesco Galli, Roberta Galarini
Several studies are increasingly underlying the biological role of vitamin E metabolites as bioactive compounds with anti-inflammatory, anti-proliferative and anti-atherogenic activity. A quantitative method for the simultaneous determination in human plasma and serum of vitamin E (α-tocopherol, α-T and γ-tocopherol, γ-T) and its cytochrome P-450 metabolites: 13'-hydroxychromanol (α-13'-OH), 13'-carboxychromanol (α-13'-COOH) and carboxyethyl hydroxychromanols (α-CEHC and γ-CEHC), was developed and validated...
August 1, 2017: Talanta
https://www.readbyqxmd.com/read/28495029/the-pharmacokinetics-of-the-cyp3a-substrate-midazolam-after-steady-state-dosing-of-delafloxacin
#12
Susan K Paulson, Rebecca N Wood-Horrall, Randall Hoover, Megan Quintas, Laura E Lawrence, Sue K Cammarata
PURPOSE: Delafloxacin is a novel anionic fluoroquinolone in Phase III development for the treatment of serious skin infections. The objective of this study was to evaluate the effects of delafloxacin on the pharmacokinetics of midazolam, a cytochrome P450 (CYP) 3A substrate. METHODS: CYP3A activity using midazolam as a probe was assessed before and after multiple doses of delafloxacin to reach steady state. In this nonrandomized, open-label, single-sequence, Phase I study, 22 healthy male and female subjects were administered a single 5-mg oral dose of midazolam on days 1 and 8, with oral delafloxacin 450 mg every 12 hours administered from days 3 to 8...
June 2017: Clinical Therapeutics
https://www.readbyqxmd.com/read/28494841/quercetin-attenuates-benzo-%C3%AE-pyrene-induced-cyp1a-expression
#13
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/28492277/association-study-and-expression-analysis-of-cyp4a11-gene-copy-number-variation-in-chinese-cattle
#14
Mingjuan Yang, Jingqiao Lv, Liangzhi Zhang, Mingxun Li, Yang Zhou, Xianyong Lan, Chuzhao Lei, Hong Chen
The identification of copy number variations (CNVs) allow us to explore genomic polymorphisms. In recent years, significant progress in understanding CNVs has been made in studies of human and animals, however, association and expression studies of CNVs are still in the early stage. It was previously reported that the Cytochrome P-450 4A11 (CYP4A11) gene is located within a copy number variable region (CNVR) that encompasses quantitative trait loci (QTLs) for economic traits like meat quality and milk production...
May 11, 2017: Scientific Reports
https://www.readbyqxmd.com/read/28469395/cytochrome-p-450-1b1-leu432val-polymorphism-does-not-show-association-with-breast-cancer-in-northern-iranian-women-with-a-history-of-infertility
#15
Maryam Ghanbari Andarieh, Ebrahim Zabihi, Dariush Moslemi, Mouloud Agajani Delavar, Mahmoud Haji-Ahmadi, Ali Shabestani Monfared, Seyed Gholam Ali Jorsaraei, Masoumeh Ghasemi, Sedighe Esmaeilzadeh
The Cytochrome P-4501B1 (CYP1B1) Leu432Val polymorphism has been previously shown to be associated with some types of cancer and affects CYP1B1-mediated metabolism of various infertility drugs. To establish the frequency of CYP1B1 Leu432Val polymorphism among women with a history of infertility drug use, we studied the genotypes of 147 patients with breast cancer with a history of infertility and 150 cancer-free, infertile women (control group) in Northern Iran. A polymerase chain reaction-based restriction fragment length polymorphism assay was used to detect GG (Val/Val), CG (Leu/Val), and CC (Leu/Leu) genotype frequencies, which did not vary significantly between the 2 patient groups (P = ...
2017: Biomarker Insights
https://www.readbyqxmd.com/read/28461126/benzo-a-pyrene-induced-dna-damage-associated-with-mutagenesis-in-primary-human-activated-t-lymphocytes
#16
Marie Liamin, Elisa Boutet-Robinet, Emilien L Jamin, Morgane Fernier, Laure Khoury, Benjamin Kopp, Eric Le Ferrec, Julien Vignard, Marc Audebert, Lydie Sparfel
Polycyclic aromatic hydrocarbons (PAHs), such as benzo[a]pyrene (B[a]P), are widely distributed environmental contaminants exerting toxic effects such as genotoxicity and carcinogenicity, mainly associated with aryl hydrocarbon receptor (AhR) activation and the subsequent induction of cytochromes P-450 (CYP) 1-metabolizing enzymes. We previously reported an up-regulation of AhR expression and activity in primary cultures of human T lymphocyte by a physiological activation. Despite the suggested link between exposure to PAHs and the risk of lymphoma, the potential of activated human T lymphocytes to metabolize AhR exogenous ligands such as B[a]P and produce DNA damage has not been investigated...
August 1, 2017: Biochemical Pharmacology
https://www.readbyqxmd.com/read/28459658/enhanced-oral-bioavailability-of-domperidone-with-piperine-in-male-wistar-rats-involvement-of-cyp3a1-and-p-gp-inhibition
#17
Bhargavi Latha Athukuri, Prasad Neerati
PURPOSE: Domperidone is a commonly used antiemetic drug. The oral bioavailability of domperidone is very low due to its rapid first pass metabolism in the intestine and liver. Piperine, the main alkaloid present in black pepper has been reported to show inhibitory effects on Cytochrome P-450 (CYP-450) enzymes and P-glycoprotein (P-gp). In the present study we investigated the effect of piperine pretreatment on the intestinal transport and oral bioavailability of domperidone in male Wistar rats...
2017: Journal of Pharmacy & Pharmaceutical Sciences: a Publication of the Canadian Society for Pharmaceutical Sciences
https://www.readbyqxmd.com/read/28412920/neuropsychiatric-and-general-interactions-of-natural-and-synthetic-cannabinoids-with-drugs-of-abuse-and-medicines
#18
Ana Lucia Arellano, Esther Papaseit, Anna Romaguera, Marta Torrens, Magi Farré
Cannabis is the most widely used illicit drug. The two most important natural cannabinoids are delta-9-tetrahydrocannabinol (THC) and cannabidiol (CBD). The THC content of cannabis has been increasing during the last years and recently appeared in the market a series of synthetic cannabinoids with potent agonist activity. Recreational users frequently combine cannabis with other drugs of abuse as alcohol, amphetamines and derivatives, nicotine and cocaine. In addition these subjects can be taking medicines for acute and chronic medical conditions...
April 13, 2017: CNS & Neurological Disorders Drug Targets
https://www.readbyqxmd.com/read/28404946/cyp-genes-in-osteosarcoma-their-role-in-tumorigenesis-pulmonary-metastatic-microenvironment-and-treatment-response
#19
Alini Trujillo-Paolillo, Francine Tesser-Gamba, Antonio Sergio Petrilli, Maria Teresa de Seixas Alves, Reynaldo Jesus Garcia Filho, Renato de Oliveira, Silvia Regina Caminada de Toledo
Osteosarcoma (OS) is the most common malignant bone tumor in children and adolescents. The present study investigated the expression of Cytochrome P-450 (CYP) genes: CYP1A2, CYP3A4 and CYP3A5 by qRT-PCR in 135 specimens obtained from OS patients, including biopsy (pre-chemotherapy), tumor resected in surgery (post-chemotherapy), adjacent bone to tumor (nonmalignant tissue), pulmonary metastasis and adjacent lung to metastasis (nonmalignant tissue). Normal bone and normal lung tissues were used as control. We also investigated in five OS cell lines the modulation of CYPs expression by cisplatin, doxorubicin and methotrexate...
June 13, 2017: Oncotarget
https://www.readbyqxmd.com/read/28377720/curcumin-successfully-inhibited-the-computationally-identified-cyp2a6-enzyme-mediated-bioactivation-of-aflatoxin-b1-in-arbor-acres-broiler
#20
Ishfaq Muhammad, Xiaoqi Sun, He Wang, Wei Li, Xinghe Wang, Ping Cheng, Sihong Li, Xiuying Zhang, Sattar Hamid
Cytochrome P450 enzymes are often responsible for the toxic and carcinogenic effects of toxicants, such as aflatoxin B1 (AFB1). The human hepatic CYP2A6 enzyme mediates the oxidative metabolism of several procarcinogens. In this study, we characterized a partial sequence of CYP2A6 gene from Arbor Acres (AA) broiler and studied its role in AFB1 bioactivation. Moreover, the effect of curcumin on CYP2A6 is illustrated. Six groups of AA broiler were treated for 28 days including the control group (fed only basal diet), curcumin alone-treated group (450 mg/kg feed), the group fed AFB1-contaminated feed (5 mg/kg feed) plus the low (150 mg), medium (300 mg) or high (450 mg) of curcumin, and the group fed AFB1-contaminated diet alone (5 mg/kg feed)...
2017: Frontiers in Pharmacology
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