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https://www.readbyqxmd.com/read/28322152/serotonin-receptor-binding-characteristics-of-geissoschizine-methyl-ether-an-indole-alkaloid-in-uncaria-hook
#1
Yasushi Ikarashi, Kyoji Sekiguchi, Kazushige Mizoguchi
Geissoschizine methyl ether (GM) is one of the indole alkaloids in Uncaria hook, and an active ingredient of yokukansan (YKS) that improves behavioral and psychological symptoms of dementia (BPSD) in patients with several types of dementia. The pharmacological action of GM has been related to various serotonin (5-HT) receptor subtypes. Here we describe previous findings and our own data to review the binding characteristics of GM to the 5-HT receptor subtypes. Competitive receptor-binding assays showed that GM bound the following 5-HT receptor subtypes: 5-HT1A, 5-HT1B, 5-HT2A, 5-HT2B, 5-HT2C, 5-HT4, 5-HT5A, 5-HT6, and 5-HT7...
March 20, 2017: Current Medicinal Chemistry
https://www.readbyqxmd.com/read/28301431/cyp3a4-activity-is-markedly-lower-in-patients-with-crohn-s-disease
#2
Aze Wilson, Rommel G Tirona, Richard B Kim
BACKGROUND: Disease-dependent changes in the activity of drug metabolizing enzymes and transporters, such as Cytochrome P450 (CYP) 3A4 and P-glycoprotein (P-gp), are thought to have a major influence on the disposition of shared substrates. However, little is known regarding the in vivo relevance of these 2 proteins during drug therapy for gastrointestinal diseases. Our aim was to elucidate the activity of CYP3A4 and P-gp in subjects with Crohn's disease (CD) and to evaluate their influence on budesonide pharmacokinetics...
March 15, 2017: Inflammatory Bowel Diseases
https://www.readbyqxmd.com/read/28301096/effects-of-tenapanor-on-cytochrome-p450-mediated-drug-drug-interactions
#3
Susanne Johansson, David P Rosenbaum, Marie Ahlqvist, Helen Rollison, Mikael Knutsson, Bergur Stefansson, Marie Elebring
Tenapanor (RDX5791, AZD1722) is an inhibitor of sodium/hydrogen exchanger isoform 3 in development for the treatment of constipation-predominant irritable bowel syndrome and the treatment of hyperphosphatemia in patients with chronic kidney disease on dialysis. We aimed to investigate whether tenapanor inhibits or induces cytochrome P450s (CYPs). In vitro experiments assessing the potential of tenapanor to affect various CYPs indicated that it could inhibit CYP3A4/5 (IC50 0.4-0.7 μM). An open-label, phase 1 clinical study (NCT02140268) evaluated the pharmacokinetics of the CYP3A4 substrate midazolam when administered with and without tenapanor...
March 16, 2017: Clinical Pharmacology in Drug Development
https://www.readbyqxmd.com/read/28272018/genetic-polymorphisms-of-cytochrome-p450-enzymes-cyp2c9-cyp2c19-cyp2d6-cyp3a4-and-cyp3a5-in-the-croatian-population
#4
Lana Ganoci, Tamara Božina, Nikica Mirošević Skvrce, Mila Lovrić, Petar Mas, Nada Božina
BACKGROUND: Data on the frequency of pharmacogenetic polymorphisms in the Croatian population are limited. We determined and analyzed frequencies for the most important CYP2C9, CYP2C19, CYP2D6, CYP3A4, and CYP3A5 genetic variants in the Croatian population. METHODS: 2637 subjects were included. Genotyping was performed by real-time polymerase chain reaction (PCR) using TaqMan® DME or TaqMan® SNP Genotyping Assays, and by PCR, and PCR-RFLP analysis. RESULTS: For CYP2C9, allele frequencies of *2 and *3 variant were 14...
March 1, 2017: Drug Metabolism and Personalized Therapy
https://www.readbyqxmd.com/read/28261841/a-sensitive-quantitative-assay-for-the-determination-of-propafenone-and-two-metabolites-5-hydroxypropafenone-and-n-depropylpropafenone-in-human-k2edta-plasma-using-lc-ms-ms-with-esi-operated-in-a-positive-mode
#5
Harilal Patel, Ashok Ghoghari, Chandrakant Bhatt, Shaival Shah, Anilkumar Jha, Nirmal Desai, Nuggehally R Srinivas
Propafenone is a potent antiarrhythmic agent; clinically propafenone has been used for a number of cardiac arrhythmias because it possesses multiple modes of action, via beta adrenergic receptor blockade and calcium antagonistic activity. Propafenone (PPF) exhibits extensive saturable presystemic biotransformation (first pass effect) resulting into two active metabolites; 5- hydroxypropafenone (5-OH PPF) formed by CYP2D6 and N-depropylpropafenone (NDP) formed by both CYP3A4 and CYP1A2 enzymes. A specific and sensitive LC-MS/MS method was developed and validated for quantitation of PPF, 5-OH PPF and NDP using turboion spray in a positive ion mode...
March 6, 2017: Biomedical Chromatography: BMC
https://www.readbyqxmd.com/read/28260174/effect-of-gevokizumab-on-interleukin-1%C3%AE-mediated-cytochrome-p450-3a4-and-drug-transporter-repression-in-cultured-human-hepatocytes
#6
Amélie Moreau, Marc Le Vée, Elodie Jouan, Claire Denizot, Yannick Parmentier, Olivier Fardel
BACKGROUND AND OBJECTIVES: Gevokizumab is a potent anti-interleukin (IL)-1β neutralizing monoclonal antibody (mAb), which may be used for treating inflammatory or autoimmune diseases. The present study was designed to characterize the potential effects of this mAb towards well-established IL-1β-mediated repression of hepatic drug detoxifying proteins, like cytochrome P450 (CYP) 3A4 and drug transporters. METHODS: Primary cultured human hepatocytes were exposed to various concentrations of IL-1β in the absence or presence of gevokizumab (5 µg/mL); mRNA expression and activity of CYP3A4 and transporters were next determined...
March 4, 2017: European Journal of Drug Metabolism and Pharmacokinetics
https://www.readbyqxmd.com/read/28259126/10-6-plastoquinonyl-decyltriphenylphosphonium-skq1-does-not-increase-the-level-of-cytochromes-p450-in-rat-liver-and-human-hepatocyte-cell-culture
#7
K N Myasoedova, D N Silachev, A D Petrov
Mitochondria-targeted antioxidant SkQ1 did not increase the content of cytochromes P450 in livers of rats that were given SkQ1 in drinking water for 5 days in a dose (2.5 µmol per kg body weight) that exceeded 10 times the SkQ1 therapeutic dose. SkQ1 did not affect the levels of cytochrome P450 forms CYP1A2, CYP2B6, and CYP3A4 in monolayer cultures of freshly isolated human hepatocytes, while specific inducers of these forms (omeprazole, phenobarbital, and rifampicin, respectively) significantly increased expression of the cytochromes P450 under the same conditions...
December 2016: Biochemistry. Biokhimii︠a︡
https://www.readbyqxmd.com/read/28254951/examination-of-the-human-cytochrome-p4503a4-induction-potential-of-pf-06282999-an-irreversible-myeloperoxidase-inactivator-integration-of-preclinical-in-silico-and-biomarker-methodologies-in-the-prediction-of-the-clinical-outcome
#8
Jennifer Dong, James Gosset, Odette Fahmi, Zhiwu Lin, Jeffrey Chabot, Steven Terra, Vu Le, Kristin Chidsey, Parya Nouri, Albert Kim, Leonard Buckbinder, Amit S Kalgutkar
The propensity for cytochrome P450 (CYP)3A4 induction by 2-(6-(5-chloro-2-methoxyphenyl)-4-oxo-2-thioxo-3,4-dihydropyrimidin-1(2H)-yl)acetamide (PF-06282999), an irreversible inactivator of myeloperoxidase, was examined in the present work. Studies using human hepatocytes revealed moderate increases in CYP3A4 messenger RNA (mRNA) and midazolam-1'-hydroxylase activity in a PF-06282999 dose-dependent fashion. At the highest tested concentration of 300 μM, PF-06282999 caused maximal induction in CYP3A4 mRNA and enzyme activity ranging from 56% - 86% and 47% - 72%, respectively, of rifampicin response across the three hepatocyte donor pools...
March 2, 2017: Drug Metabolism and Disposition: the Biological Fate of Chemicals
https://www.readbyqxmd.com/read/28253196/cytotoxicity-and-cytochrome-p450-inhibitory-activities-of-clinacanthus-nutans
#9
Suk Yen Quah, Jin Han Chin, Gabriel Akyirem Akowuah, Shaik Ibrahim Khalivulla, Siew Wei Yeong, Mandumpal Chacko Sabu
BACKGROUND: Clinacanthus nutans Lindau (family: Acanthaceae), also known as "Sabah Snake Grass" or "Belalai Gajah" in Malaysia, has been widely used by Malaysians due to its anticancer property. However, the anticancer activity of C. nutans leaves extract and its safe use need to be further investigated. The objectives of the present study were to evaluate the cytotoxic effects of methanol leaves extract of C. nutans in various human cancer cell lines and to evaluate the in vitro effect of C...
March 1, 2017: Drug Metabolism and Personalized Therapy
https://www.readbyqxmd.com/read/28244811/systematic-screening-for-cyp3a4-genetic-polymorphisms-in-a-han-chinese-population
#10
Guo-Xin Hu, Da-Peng Dai, Hao Wang, Xiang-Xin Huang, Xiao-Yang Zhou, Jie Cai, Hao Chen, Jian-Ping Cai
AIM: To systematically investigate the genetic polymorphisms of the CYP3A4 gene in a Han Chinese population. MATERIALS & METHODS: The promoter and exons of CYP3A4 gene in 1114 unrelated, healthy Han Chinese subjects were amplified and genotyped by direct sequencing. RESULTS: In total, five previously reported alleles (*1G, *4, *5, *18B and *23) were detected, of which one allele (*23) was reported for the first time in Han Chinese population...
March 2017: Pharmacogenomics
https://www.readbyqxmd.com/read/28231276/alterations-in-cellular-pharmacokinetics-and-pharmacodynamics-of-elvitegravir-in-response-to-ethanol-exposure-in-hiv-1-infected-monocytic-u1-cells
#11
Narasimha M Midde, Namita Sinha, Pradeep B Lukka, Bernd Meibohm, Santosh Kumar
Ethanol consumption is negatively associated with antiretroviral therapy (ART) adherence and general health in HIV positive individuals. Previously, we demonstrated ethanol-mediated alterations to metabolism of elvitegravir (EVG) in human liver microsomes. In the current study, we investigated ethanol influence on the pharmacokinetic and pharmacodynamic interactions of EVG in HIV infected monocytic (U1) cells. U1 cells were treated with 5 μM EVG, 2 μM Cobicistat (COBI), a booster drug, and 20 mM ethanol for up to 24 hours...
2017: PloS One
https://www.readbyqxmd.com/read/28224698/determinants-of-the-magnitude-of-interaction-between-tacrolimus-and-voriconazole-posaconazole-in-solid-organ-recipients
#12
Thomas Vanhove, Hanneke Bouwsma, Luuk Hilbrands, Jesse J Swen, Isabel Spriet, Pieter Annaert, Bart Vanaudenaerde, Geert Verleden, Robin Vos, Dirk R J Kuypers
Administration of azole antifungals to tacrolimus-treated solid organ recipients results in a major drug-drug interaction characterized by increased exposure to tacrolimus. The magnitude of this interaction is highly variable but cannot currently be predicted. We performed a retrospective analysis of 126 solid organ recipients (95 lung, 31 kidney) co-treated with tacrolimus and voriconazole (n=100) or posaconazole (n=26). Predictors of the change in tacrolimus dose-corrected trough concentrations (C/D) between baseline and tacrolimus - azole co-therapy were assessed using linear mixed modeling...
February 21, 2017: American Journal of Transplantation
https://www.readbyqxmd.com/read/28221736/individual-pharmacokinetic-variation-leads-to-underdosing-of-ciprofloxacin-in-some-cystic-fibrosis-patients
#13
A N Ø Schultz, N Høiby, X C Nielsen, T Pressler, K Dalhoff, M Duno, A Buchard, H K Johansen, H Wang, C S Dalbøge
Ciprofloxacin (CIP) is frequently used when treating cystic fibrose (CF) patients with intermittent Pseudomonas aeruginosa (P. aeruginosa) lung colonization. However, approximately 20% of the patients progress to chronic infection despite early intervention. The aim of this study, was to investigate the pharmacokinetics of CIP, to evaluate if CYP3A4-related metabolism is involved and to find the optimal dose needed to eradicate intermittently colonizing bacteria in the lungs of CF patients. Methods An open-label, prospective pharmacokinetic study was performed...
March 2017: Pediatric Pulmonology
https://www.readbyqxmd.com/read/28194109/delayed-chemotherapy-induced-nausea-and-vomiting-pathogenesis-incidence-and-current-management
#14
REVIEW
Bernardo L Rapoport
Even when chemotherapy-induced nausea and vomiting (CINV) can be effectively controlled in the acute phase, it may still occur in the delayed phase. Identifying at-risk patients is complex and requires consideration of clinical, personal, demographic, and behavioral factors. Delayed CINV has a significant detrimental effect on patients' daily life and is responsible for significant healthcare resource utilization. Patients who do not experience acute CINV are not necessarily exempt from delayed CINV, and healthcare professionals have been shown to underestimate the incidence of delayed CINV...
2017: Frontiers in Pharmacology
https://www.readbyqxmd.com/read/28185143/characterization-of-1-aminobenzotriazole-and-ketoconazole-as-novel-inhibitors-of-monoamine-oxidase-mao-an-in-vitro-investigation
#15
Abdul Naveed Shaik, Barbara W LeDuc, Ansar A Khan
BACKGROUND AND OBJECTIVES: 1-Aminobenzotriazole, a known time-dependent inhibitor of cytochrome P450 (CYP) enzymes, and ketoconazole, a strong inhibitor of the human CYP3A4 isozyme, are used as standard probe inhibitors to characterize the CYP and/or non-CYP-mediated metabolism of xenobiotics. In the present investigation, 1-Aminobenzotriazole and ketoconazole are characterized as potent monoamine oxidase (MAO) inhibitors in vitro using mouse, rat and human liver microsomes and S9 fractions...
February 9, 2017: European Journal of Drug Metabolism and Pharmacokinetics
https://www.readbyqxmd.com/read/28167419/comparative-pharmacokinetic-profiles-of-selected-irreversible-tyrosine-kinase-inhibitors-neratinib-and-pelitinib-with-apigenin-in-rat-plasma-by-uplc-ms-ms
#16
Hadir M Maher, Nourah Z Alzoman, Shereen M Shehata, Ashwag O Abahussain
Neratinib (NER) and pelitinib (PEL) are irreversible tyrosine kinase inhibitors (TKIs) that have been recently employed in cancer treatment. Apigenin (API), among other flavonoids, is known to have antioxidant, anti-proliferative, and carcinogenic effect. API can potentiate the antitumor effect of chemotherapeutic agents and/or alleviate the side effects of many anticancer agents. Since TKIs are mostly metabolized by CYP3A4 enzymes and that API could alter the enzymatic activity, potential drug interactions could be expected following their co-aministration...
January 31, 2017: Journal of Pharmaceutical and Biomedical Analysis
https://www.readbyqxmd.com/read/28155129/drug-interaction-potential-of-osilodrostat-lci699-based-on-its-effect-on-the-pharmacokinetics-of-probe-drugs-of-cytochrome-p450-enzymes-in-healthy-adults
#17
Sara Armani, Lillian Ting, Nicholas Sauter, Christelle Darstein, Anadya Prakash Tripathi, Lai Wang, Bing Zhu, Helen Gu, Dung Yu Chun, Heidi J Einolf, Swarupa Kulkarni
BACKGROUND AND OBJECTIVES: Osilodrostat (LCI699) is an adrenal steroidogenesis inhibitor currently in late-phase clinical development as a potential treatment for Cushing's disease. This study evaluated the inhibitory effect of osilodrostat on the pharmacokinetics of probe substrates of the cytochrome P450 (CYP) enzymes CYP1A2, CYP2C19, CYP2D6, and CYP3A4. METHODS: Healthy adult volunteers received single-dose cocktail probe substrates [caffeine (100 mg), omeprazole (20 mg), dextromethorphan (30 mg), and midazolam (2 mg)] followed by a 6-day washout...
February 2, 2017: Clinical Drug Investigation
https://www.readbyqxmd.com/read/28153492/sex-and-age-dependent-gene-expression-in-human-liver-an-implication-for-drug-metabolizing-enzymes
#18
Yasuhiro Uno, Ryo Takata, Go Kito, Hiroshi Yamazaki, Kazuko Nakagawa, Yusuke Nakamura, Tetsuya Kamataki, Toyomasa Katagiri
Sex and age differences in hepatic expression of drug-metabolizing enzyme genes could cause variations in drug metabolism, but has not been fully elucidated, especially in Asian population. In this study, the global expression of human hepatic genes was analyzed by microarrays in 40 Japanese subjects (27 males and 13 females). Thirty-five sex-biased genes were identified (P < 0.005). Whereas, 60 age-biased genes in two age groups, <60 years and ≥70 years (P < 0.001), were identified in males...
February 2017: Drug Metabolism and Pharmacokinetics
https://www.readbyqxmd.com/read/28118673/an-appraisal-of-drug-drug-interactions-with-green-tea-camellia-sinensis
#19
Ahmed A Albassam, John S Markowitz
This review summarizes published in vitro, animal, and clinical studies investigating the effects of green tea (Camellia sinensis) extract and associated catechins on drug-metabolizing enzymes and drug transporters. In vitro studies suggest that green tea extract and its main catechin, (-)-epigallocatechin-3-gallate, to varying degrees, inhibit the activity of CYP1A1, CYP1A2, CYP2B6, CYP2C8, CYP2C9, CYP2D6, and CYP3A4. UGT1A1 and UGT1A4 isoforms were also inhibited by (-)-epigallocatechin-3-gallate. Animal studies suggest green tea extract and/or (-)-epigallocatechin-3-gallate significantly increase the bioavailability of diltazem, verapamil, tamoxifen simvastatin, 5-fluorouracil, and nicardipine...
January 24, 2017: Planta Medica
https://www.readbyqxmd.com/read/28117738/in-vitro-biotransformation-of-two-human-cyp3a-probe-substrates-and-their-inhibition-during-early-zebrafish-development
#20
Evy Verbueken, Derek Alsop, Moayad A Saad, Casper Pype, Els M Van Peer, Christophe R Casteleyn, Chris J Van Ginneken, Joanna Wilson, Steven J Van Cruchten
At present, the zebrafish embryo is increasingly used as an alternative animal model to screen for developmental toxicity after exposure to xenobiotics. Since zebrafish embryos depend on their own drug-metabolizing capacity, knowledge of their intrinsic biotransformation is pivotal in order to correctly interpret the outcome of teratogenicity assays. Therefore, the aim of this in vitro study was to assess the activity of cytochrome P450 (CYP)-a group of drug-metabolizing enzymes-in microsomes from whole zebrafish embryos (ZEM) of 5, 24, 48, 72, 96 and 120 h post-fertilization (hpf) by means of a mammalian CYP substrate, i...
January 22, 2017: International Journal of Molecular Sciences
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