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Cytochrome 450

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https://www.readbyqxmd.com/read/28412920/neuropsychiatric-and-general-interactions-of-natural-and-synthetic-cannabinoids-with-drugs-of-abuse-and-medicines
#1
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
#2
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...
March 3, 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
#3
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
https://www.readbyqxmd.com/read/28377716/human-cytochrome-p450-3a4-as-a-biocatalyst-effects-of-the-engineered-linker-in-modulation-of-coupling-efficiency-in-3a4-bmr-chimeras
#4
Danilo Degregorio, Serena D'Avino, Silvia Castrignanò, Giovanna Di Nardo, Sheila J Sadeghi, Gianluca Catucci, Gianfranco Gilardi
Human liver cytochrome P450 3A4 is the main enzyme involved in drug metabolism. This makes it an attractive target for biocatalytic applications, such as the synthesis of pharmaceuticals and drug metabolites. However, its poor solubility, stability and low coupling have limited its application in the biotechnological context. We previously demonstrated that the solubility of P450 3A4 can be increased by creating fusion proteins between the reductase from Bacillus megaterium BM3 (BMR) and the N-terminally modified P450 3A4 (3A4-BMR)...
2017: Frontiers in Pharmacology
https://www.readbyqxmd.com/read/28367588/effect-of-long-term-in-vitro-lithium-exposure-on-mrna-levels-of-claudin-3-cyp1a1-abcg2-and-gstm3-genes-in-the-hcmec-d3-human-brain-endothelial-cell-line
#5
Ramzi Shawahna, Kayathiri Ganeshamoorthy, Luo Huilong, Jean-Michel Scherrmann, Pierre-Olivier Couraud, Xavier Declèves
BACKGROUND AND OBJECTIVES: Lithium chloride (LiCl) has been shown to improve the tightness of brain endothelial cell monolayers in vitro by inhibition of the GSK-3β enzyme, activation of the Wnt/beta-catenin pathway and regulation of tight junction (TJ) protein expression. However, the effect of LiCl on the drug transporters and drug-metabolizing enzymes has not been addressed so far. The hCMEC/D3 cell line is a validated in vitro BBB model expressing transporters and drug-metabolizing enzymes (phase 1 and 2)...
April 3, 2017: European Journal of Drug Metabolism and Pharmacokinetics
https://www.readbyqxmd.com/read/28346481/edaravone-protects-against-hyperosmolarity-induced-oxidative-stress-and-apoptosis-in-primary-human-corneal-epithelial-cells
#6
Yanwei Li, Haifeng Liu, Wei Zeng, Jing Wei
An increase in the osmolarity of tears induced by excessive evaporation of the aqueous tear phase is a major pathological mechanism behind dry eye. Exposure of epithelial cells on the surface of the human eye to hyperosmolarity leads to oxidative stress, mitochondrial dysfunction, and apoptosis. Edaravone, a hydroxyl radical scavenging agent, is clinically used to reduce neuronal damage following ischemic stroke. In this study, we found that treatment with hyperosmotic media at 400 and 450 mOsM increased the levels of ROS and mitochondrial oxidative damage, which were ameliorated by edaravone treatment in a dose-dependent manner...
2017: PloS One
https://www.readbyqxmd.com/read/28322174/acanthocotyle-gurgesiella-n-sp-monogenea-acanthocotylidae-from-the-deep-sea-skate-gurgesiella-furvescens-rajidae-in-the-south-eastern-pacific
#7
L A Ñacari, F A Sepulveda, R Escribano, M E Oliva
Little is known about the diversity of parasites of the deep-sea fish of the world's oceans. Here, a new species of monogenean parasite of the deep-sea skate Gurgesiella furvescens is described. Specimens of parasites were obtained from the skin of two specimens of the dusky finless skate, G. furvescens (Rajidae), in the vicinity of Valparaiso (33°S, 72°W), central Chile, from midwater trawl fishing at depths of 350-450 m. Both morphological and molecular analyses were conducted to provide a full description of the new species, named Acanthocotyle gurgesiella...
March 21, 2017: Journal of Helminthology
https://www.readbyqxmd.com/read/28275327/insecticide-resistance-and-cytochrome-p450-activation-in-unfed-and-blood-fed-laboratory-and-field-populations-of-culex-pipiens-pallens
#8
Kyu-Sik Chang, Heung-Chul Kim, Terry A Klein, Young Ran Ju
Understanding the mechanisms of insecticide resistance to vector mosquitoes is critical for the implementation of effective control measures. A nulliparous susceptible Culex pipiens pallens (KSCP) laboratory colony and two field strains from Paju (PAJ) and Jeonju (JEO) Korea were evaluated for susceptibility to five pesticides by microapplication techniques. Unfed PAJ and JEO females demonstrated increased resistance compared to unfed KSCP females, respectively. While blood-fed KSCP females demonstrated <10-fold decreased susceptibility to pesticides compared to unfed KSCP females, blood-fed PAJ and JEO females demonstrated 25...
2017: Journal of Pest Science
https://www.readbyqxmd.com/read/28250275/optimization-of-albumin-secretion-and-metabolic-activity-of-cytochrome-p450-1a1-of-human-hepatoblastoma-hepg2-cells-in-multicellular-spheroids-by-controlling-spheroid-size
#9
Tomoko Nishikawa, Yutaro Tanaka, Makiya Nishikawa, Yuka Ogino, Kosuke Kusamori, Narumi Mizuno, Yuya Mizukami, Kazunori Shimizu, Satoshi Konishi, Yuki Takahashi, Yoshinobu Takakura
Multicellular spheroids are useful as three-dimensional cell culture systems and for cell-based therapies. Their successful application requires an understanding of the consequences of spheroid size for cellular functions. In the present study, we prepared multicellular spheroids of different sizes using the human hepatoblastoma HepG2 cells, as hepatocytes are frequently used for in vitro drug screening and cell-based therapy. Precise polydimethylsiloxane-based microwells with widths of 360, 450, 560, and 770 µm were fabricated using a micromolding technique...
2017: Biological & Pharmaceutical Bulletin
https://www.readbyqxmd.com/read/28219593/betel-nut-chewing-is-associated-with-reduced-tacrolimus-concentration-in-taiwanese-liver-transplant-recipients
#10
W-Y Chen, C-Y Lee, P-Y Lin, C-E Hsieh, C-J Ko, K-H Lin, C-C Lin, Y-Z Ming, Y-L Chen
PURPOSE: Studies have shown that arecoline, the major alkaloid component of betel nuts, alters the activity of enzymes in the cytochrome P450 (CYP-450) family. Tacrolimus, an immunosuppressant that protects against organ rejection in transplant recipients, not only is mainly metabolized by CYP3A enzymes but also has a narrow therapeutic range. We aimed to investigate whether dose-adjusted blood trough levels of tacrolimus differed over time between betel nut-chewing and non-betel nut-chewing liver transplant recipients...
March 2017: Transplantation Proceedings
https://www.readbyqxmd.com/read/28215696/recurrent-venous-thrombosis-under-rivaroxaban-and-carbamazepine-for-symptomatic-epilepsy
#11
Claudia Stöllberger, Josef Finsterer
BACKGROUND: The direct oral anticoagulant (DOAC) rivaroxaban, an oral Factor Xa inhibitor, is increasingly used as an alternative to vitamin-K-antagonists (VKAs). Absorption and elimination of DOACs are dependent on the permeability glycoprotein (P-gp) efflux transporter protein system, and DOACs are substrates of the hepatic cytochrome P 450 3A4 (CYP3A4) enzymes. Therefore, drug-interactions may occur when DOACs are administered with drugs affecting the activity of P-gp or CYP3A4 systems...
March 2017: Neurologia i Neurochirurgia Polska
https://www.readbyqxmd.com/read/28210286/bilastine-in-allergic-rhinoconjunctivitis-and-urticaria-a-practical-approach-to-treatment-decisions-based-on-queries-received-by-the-medical-information-department
#12
REVIEW
Amalia Leceta, Ander Sologuren, Román Valiente, Cristina Campo, Luis Labeaga
BACKGROUND: Bilastine is a safe and effective commonly prescribed non-sedating H1-antihistamine approved for symptomatic treatment in patients with allergic disorders such as rhinoconjunctivitis and urticaria. It was evaluated in many patients throughout the clinical development required for its approval, but clinical trials generally exclude many patients who will benefit in everyday clinical practice (especially those with coexisting diseases and/or being treated with concomitant drugs)...
2017: Drugs in Context
https://www.readbyqxmd.com/read/28195395/heterologous-expression-of-helicoverpa-armigera-cytochrome-p450-cyp6b7-in-pichia-pastoris-and-interactions-of-cyp6b7-with-insecticides
#13
Chunqing Zhao, Genmiao Song, Hongxia Duan, Tao Tang, Chen Wang, Lihong Qiu
BACKGROUND: Previous studies indicated that constitutive overexpression of cytochrome P450 CYP6B7 was involved in fenvalerate resistance in Helicoverpa armigera. In this study, the CYP6B7 gene from H. armigera (namely HaCYP6B7), was heterologously expressed in Pichia pastoris GS115. A vector pPICZA-HaCYP6B7 was constructed and transformed into P. pastoris GS115, the transformant of pPICZA-HaCYP6B7-GS115 was then cultured and induced by 1% (v/v) methanol and the heterologous expression of HaCYP6B7 protein in P...
February 13, 2017: Pest Management Science
https://www.readbyqxmd.com/read/28182799/in-vivo-acrylamide-exposure-may-cause-severe-toxicity-to-mouse-oocytes-through-its-metabolite-glycidamide
#14
Duru Aras, Zeynep Cakar, Sinan Ozkavukcu, Alp Can, Ozgur Cinar
High acrylamide (ACR) content in heat-processed carbohydrate-rich foods, as well as roasted products such as coffee, almonds etc., has been found to be as a risk factor for carcinogenicity and genotoxicity by The World Health Organization. Glycidamide (GLY), the epoxide metabolite of ACR, is processed by the cytochrome P-450 enzyme system and has also been found to be a genotoxic agent. The aim of this study was to determine whether ACR and/or GLY have any detrimental effect on the meiotic cell division of oocytes...
2017: PloS One
https://www.readbyqxmd.com/read/28154783/leptin-influences-estrogen-metabolism-and-increases-dna-adduct-formation-in-breast-cancer-cells
#15
Samia Shouman, Mohamed Wagih, Marwa Kamel
OBJECTIVE: The elevated incidence of obesity has been paralleled with higher risks of breast cancer. High adiposity increases leptin secretion from adipose tissue, which in turn increases cancer cell proliferation. The interplay between leptin and estrogen is one of the mechanisms through which leptin influences breast carcinogenesis. An unbalanced estrogen metabolism increases the formations of catechol estrogen quinones, DNA adducts, and cancer mutations. This study aims to investigate the effect of leptin on some estrogen metabolic enzymes and DNA adduction in breast cancer cells...
December 2016: Cancer Biology & Medicine
https://www.readbyqxmd.com/read/28135009/atp-binding-cassette-subfamily-b-member-1-1236c-t-polymorphism-significantly-affects-the-therapeutic-outcome-of-tacrolimus-in-patients-with-refractory-ulcerative-colitis
#16
Motoyuki Onodera, Katsuya Endo, Yoichi Kakuta, Masatake Kuroha, Tomoya Kimura, Keiichiro Hiramoto, Yoshitake Kanazawa, Kenichi Negoro, Hisashi Shiga, Yoshitaka Kinouchi, Tooru Shimosegawa
BACKGROUND AND AIM: Tacrolimus is now considered to be one of the main therapeutic options for refractory ulcerative colitis. Both cytochrome P-450 3A5 (CYP3A5) and ATP-binding cassette subfamily B member 1 (ABCB1) associated with tacrolimus metabolism are known to have several genetic polymorphisms. However, it remains controversial whether these polymorphisms affect the therapeutic efficacy for ulcerative colitis. We aimed to investigate the influence of both CYP3A5 and ABCB1 polymorphisms on the efficacy of tacrolimus in ulcerative colitis treatment under the tight dose-adjusting strategy...
January 30, 2017: Journal of Gastroenterology and Hepatology
https://www.readbyqxmd.com/read/28129335/reduction-of-aflatoxin-b1-toxicity-by-lactobacillus-plantarum-c88-a-potential-probiotic-strain-isolated-from-chinese-traditional-fermented-food-tofu
#17
Li Huang, Cuicui Duan, Yujuan Zhao, Lei Gao, Chunhua Niu, Jingbo Xu, Shengyu Li
In this study, we investigated the potential of Lactobacillus plantarum isolated from Chinese traditional fermented foods to reduce the toxicity of aflatoxin B1 (AFB1), and its subsequent detoxification mechanism. Among all the investigated L. plantarum strains, L. plantarum C88 showed the strongest AFB1 binding capacity in vitro, and was orally administered to mice with liver oxidative damage induced by AFB1. In the therapy groups, the mice that received L. plantarum C88, especially heat-killed L. plantarum C88, after a single dose of AFB1 exposure, showed an increase in unabsorbed AFB1 in the feces...
2017: PloS One
https://www.readbyqxmd.com/read/28122753/edoxaban-a-direct-oral-anticoagulant
#18
REVIEW
Mara Poulakos, Jacqueline N Walker, Umima Baig, Tosin David
PURPOSE: The pharmacology, pharmacokinetics, pharmacodynamics, clinical efficacy, safety, and place in therapy of edoxaban for prevention of stroke in patients with nonvalvular atrial fibrillation (AF) and treatment of venous thromboembolism (VTE) are reviewed. SUMMARY: Although warfarin has been an established therapy for stroke prevention in AF and VTE, the need for agents with less monitoring requirements, fewer food and drug interactions, and a lower risk of major bleeding led to the development of direct oral anticoagulants (DOACs)...
February 1, 2017: American Journal of Health-system Pharmacy: AJHP
https://www.readbyqxmd.com/read/28118749/warfarin-interaction-with-hepatic-cytochrome-p-450-enzyme-inducing-anticonvulsants
#19
Nathan P Clark, Kim Hoang, Thomas Delate, John R Horn, Daniel M Witt
BACKGROUND: Initiation of cytochrome P-450 (CYP)-inducing anticonvulsant medications during warfarin therapy may decrease anticoagulant effect and necessitate frequent warfarin dose adjustments to maintain therapeutic response measured by the international normalized ratio (INR). Clinical information regarding interactions between warfarin and these medications is limited. This study investigated warfarin dose and INR response following CYP-inducing anticonvulsant initiation among chronic warfarin users...
January 1, 2017: Clinical and Applied Thrombosis/hemostasis
https://www.readbyqxmd.com/read/28081510/gestational-and-lactational-exposure-to-di-isobutyl-phthalate-via-diet-in-maternal-mice-decreases-testosterone-levels-in-male-offspring
#20
Xiaoyang Wang, Nan Sheng, Ruina Cui, Hongxia Zhang, Jianshe Wang, Jiayin Dai
Phthalates are a large family of ubiquitous environmental chemicals suspected of being endocrine disruptors, with exposure to these chemicals during prenatal and postnatal development possibly resulting in reproductive disorders. Di-isobutyl phthalate (DiBP) is widely used in consumer and industrial products, and although its exposure in the general population has increased in recent years, the mechanisms behind DiBP-induced reproductive disorders in male offspring remain unclear. Here, pregnant mice were exposed to 0 or 450 mg/kg bw/day DiBP via diet from gestation day (GD) 0 to GD21...
April 2017: Chemosphere
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