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Drug Metabolism Letters

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https://www.readbyqxmd.com/read/28137210/the-metabolism-of-methazolamide-in-immortalized-human-keratinocytes-hacat-cells
#1
Tetsuo Sasabe, Shinichiro Maeda, Kenichi Kishida, Mariko Yamano, Yoshihiro Miwa, Toshihiro Sugiyama
OBJECTIVE: Drug therapy is occasionally accompanied by an idiosyncratic severe toxicity, which occurs very rarely, but can lead to patient mortality. Methazolamide, an anti-glaucomatous agent, could cause severe skin eruptions called Stevens-Johnson syndrome/toxic epidermal necrolyis (SJS/TEN). Its precise etiology is still uncertain. In this study, the metabolism of methazolamide was investigated in immortalized human keratinocytes to reveal the possible mechanism which causes SJS/TEN...
January 27, 2017: Drug Metabolism Letters
https://www.readbyqxmd.com/read/28103788/pharmacokinetics-metabolism-and-disposition-of-14c-xq-1h-after-intravenous-administration-to-male-rats
#2
Yinlin Qin, Tao Chen, Qiu Jin, Kai Guo, Hao Feng, Dennis Heller, Zheming Gu
This study describes the in vivo pharmacokinetics and metabolism of [14C]labeled XQ-1H in male rats. XQ-1H is a methanesulfonate of XQ, 10-O-(N,N-dimethylaminoethyl)-ginkgolide B is a derivative of ginkgolide B (GB) with enhanced water solubility. Since it is very difficult to synthesize radiolabeled GB, the results obtained in this study may provide helpful insight to further ADME investigation of GB and its analogue compounds. After an i.v. administration of [14C]XQ-1H to male rats, XQ (the freebase form of XQ-1H) was extensively hydrolyzed, moderately metabolized, and mainly excreted in feces (71...
January 18, 2017: Drug Metabolism Letters
https://www.readbyqxmd.com/read/28093968/quantification-of-etodolac-in-human-plasma-for-pharmacokinetics-and-bioequivalence-studies-in-27-korean-subjects
#3
Il-Dong Song, Je-Seop Kang, Hyun-Jin Kim, Se-Mi Kim, Dong-Xu Zhao, Shin-Hee Kim, Min-Young Chun, Kyuhyun Lee
We developed a simple and validated liquid chromatography tandem mass spectrometry(LC-MS/MS) for quantification of etodolac using pioglitazone as an internal standard (IS) to assess pharmacokinetics and to appraise bioequivalence of two formulations of etodolac (reference and tested) in 27 healthy Korean subjects. Isocratic mobile phase consisted of 10 mM ammonium formate and acetonitrile were used to separate the analytes on a Gemini C18 column. Also, analytes were analyzed by MS/MS in multiple reaction monitoring (MRM) mode using the transitions of (M+H)+ ions, m/z 288...
16, 2017: Drug Metabolism Letters
https://www.readbyqxmd.com/read/28029084/variability-of-zaleplon-5-oxidase-activity-in-mice-and-humans-and-inhibition-by-raloxifene
#4
Chiaki Tanoue, Kazumi Sugihara, Yoshitaka Tayama, Naoto Uramaru, Yoko Watanabe, Shigeru Ohta, Shigeyuki Kitamura
Zaleplon (ZAL) is a sedative-hypnotic agent, which is mainly metabolized to inactive 5-oxidized zaleplon (5-oxo-ZAL) and N-des-ethylated ZAL (des-ethyl-ZAL) in mice and humans. The former reaction is considered to be catalyzed by aldehyde oxidase present in liver cytosol. Here, we examined sex and strain differences of ZAL metabolism to 5-oxo-ZAL among four strains of mice, as well as the inter-individual variation in humans, in order to evaluate the variability of 5-oxo-ZAL-forming activity and its relationship with aldehyde oxidase activity...
December 27, 2016: Drug Metabolism Letters
https://www.readbyqxmd.com/read/28000546/ortho-methylarylamines-as-time-dependent-inhibitors-of-cytochrome-p450-1a1-enzyme
#5
Jayalakshmi Sridhar, Jiawang Liu, Rajesh Komati, Richard Schroeder, Quan Jiang, Phan Tram, Kevin Riley, Maryam Foroozesh
Members of the cytochrome P450 1A family metabolize many procarcinogens such as polycyclic aromatic hydrocarbons and heterocyclic amines. Inactivation of these enzymes is prerequisite for cancer prevention and treatment in certain cases. Mechanism-based inhibition (time and co-factor dependent) is an effective method for the inactivation of these enzymes. Our recent study on emodin analogs revealed an anthraquinone with ortho-methylarylamine moiety that exhibited time-dependent inhibition of P450 enzymes 1A1 and 1A2...
December 20, 2016: Drug Metabolism Letters
https://www.readbyqxmd.com/read/27908259/a-novel-liquid-chromatography-tandem-mass-spectrometry-method-for-the-estimation-of-bilirubin-glucuronides-and-its-application-to-in-vitro-enzyme-assays
#6
Siva Prasad Putluru, Murali Krishna Matta, Deepak Ahire, Murali Subramanian, Michael Sinz, Sandhya Mandlekar
Bilirubin is a toxic waste product of metabolism, eliminated mainly through UGT1A1 mediated conjugation to mono- and di-glucuronides. Due to the potentially low Km value of bilirubin glucuronidation, the quantitative sensitivity obtained with most UV/visible light detection methods are not sufficient to accurately calculate UGT1A1 enzyme kinetics and inhibition properties of new chemical entities at low bilirubin concentrations. In addition, bilirubin, as well as its metabolites, are unstable during sample preparation and bioanalysis...
November 24, 2016: Drug Metabolism Letters
https://www.readbyqxmd.com/read/27842485/cytochrome-p450-2a6-phenotyping-using-dietary-caffeine-salivary-metabolite-ratios-and-genotyping-using-blood-on-storage-cards-in-non-smoking-japanese-volunteers
#7
Norie Murayama, Makiko Shimizu, Kenta KObayashi, Izumi KIshimoto, Hiroshi Yamazaki
BACKGROUND: A simple method of genotyping and phenotyping cytochrome P450 2A6 (CYP2A6) was previously reported using individual blood samples and urinary caffeine metabolite ratios of 1,7-dimethyluric acid (17U) to 1-methylxanthine (1X). OBJECTIVE: Blood spotted onto storage cards and salivary caffeine metabolites were analyzed in 27 healthy non-smoking Japanese volunteers with no prior abstention from dietary caffeine intake. METHODS: 1,7-Dimethylxanthine (17X), 17U, 1X, and caffeine levels in spot saliva samples were determined in Japanese non-smokers by high-performance liquid chromatography under normal dietary caffeine consumption...
November 14, 2016: Drug Metabolism Letters
https://www.readbyqxmd.com/read/27842484/strong-induction-of-cytochrome-p450-1a-3a-but-not-p450-2b-in-cultured-hepatocytes-from-common-marmosets-and-cynomolgus-monkeys-by-typical-human-p450-inducing-agents
#8
Shotaro Uehara, Yasuhiro Uno, Takako Suzuki, Takashi Inoue, Masahiro Utoh, Erika Sasaki, Hiroshi Yamazaki
BACKGROUND: Common marmosets (Callithrix jacchus) and cynomolgus monkeys (Macaca fascicularis) are used as non-human primate models in preclinical studies for drug development. OBJECTIVE: The assessment of P450 induction in hepatocytes from marmosets and cynomolgus monkeys was performed using typical P450 inducers. METHODS: Induction of cytochrome P450 1-4 family enzymes was analyzed in two lots of cultured hepatocytes from common marmosets and cynomolgus monkeys after 24-h treatment with typical human P450 inducing agents by real-time reverse transcription-polymerase chain reaction...
November 14, 2016: Drug Metabolism Letters
https://www.readbyqxmd.com/read/27774888/genipin-inhibits-the-induction-of-inducible-nitric-oxide-synthase-through-the-inhibition-of-nf-%C3%AE%C2%BAb-activation-in-rat-hepatocytes
#9
Richi Nakatake, Takumi Tsuda, Takashi Matsuura, Hirokazu Miki, Hideki Hishikawa, Hideyuki Matsushima, Morihiko Ishizaki, Kosuke Matsui, Masaki Kaibori, Mikio Nishizawa, Tadayoshi Okumura, Masanori Kon
BACKGROUND/AIMS: Genipin is a component of Japanese traditional herbal medicine (Kampo), inchinkoto, and is used for the treatment of various liver injuries. However, there are few scientific evidence for its anti-inflammatory effects and mechanisms. In inflamed liver, proinflammatory cytokines including tumor necrosis factor (TNF)-α and interleukin (IL)-1β stimulate liver cells, followed by the expression of inducible nitric oxide synthase (iNOS). Excessive levels of NO produced by iNOS have been implicated as one of the factors in liver injury...
October 20, 2016: Drug Metabolism Letters
https://www.readbyqxmd.com/read/27449528/the-uremic-toxin-indoxyl-3-sulfate-induces-cyp1a2-in-primary-human-hepatocytes
#10
Rangaraj Narayanan, Lisa Liu, Matthew Hoffmann, Sekhar Surapaneni
: Chronic kidney disease (CKD) generally impacts clearance of renally eliminated drugs but growing evidence shows that it can influence clearance of hepatically eliminated drugs and a complete mechanistic understanding of this phenomenon is still lacking. CKD leads to accumulation of uremic toxins, including indoxyl-3-sulfate (3-INDS) and indole-3-acetic acid (3-IAA). OBJECTIVE: In this study, we evaluated the potential of 3-INDS and 3-IAA (10, 30 and 100 μM) to induce liver cytochrome P450 (CYP) enzymes CYP1A2, 2B6 and 3A4/5 using cultured primary human hepatocytes following once daily treatment for 3 days...
July 19, 2016: Drug Metabolism Letters
https://www.readbyqxmd.com/read/27604990/application-of-a-fit-for-purpose-pbpk-model-to-investigate-the-cyp3a4-induction-potential-of-enzalutamide
#11
Rangaraj Narayanan, Matthew Hoffmann, Gondi Kumar, Sekhar Surapaneni
BACKGROUND: Oncology therapy typically involves drug combinations since monotherapy seldom provides the desired outcome. But combination therapy presents the potential for drug-drug interactions (DDIs). Due to the narrow window between therapeutic concentrations and onset of toxicity often observed with oncology therapeutics, managing DDIs with combination therapy in cancer is critical. Physiologically based pharmacokinetic (PBPK) modeling can be effectively used for predicting DDIs and guiding dose-selection, but requires development of PBPK models of cancer drugs...
2016: Drug Metabolism Letters
https://www.readbyqxmd.com/read/27550199/new-screening-criteria-setting-on-evaluation-of-cytochrome-p450-induction-using-heparg-cells-with-multiplex-branched-dna-technologies-in-early-drug-discovery
#12
Akira Ogasawara, Nao Torimoto, Naoki Tsuda, Fumika Aohara, Rikiya Ohashi, Yasuhiro Yamada, Hideki Taniguchi
BACKGROUND: Cytochrome P450 (CYP) enzymes are induced by some therapeutic drugs, leading to interactions reducing drug plasma concentrations. Recently, an assessment of CYP induction using messenger RNA (mRNA) levels has shown advantages over measurement of enzymatic activity; it has a larger dynamic range of induction and enables us to measure the intrinsic induction potential of time-dependent CYP inhibitors. In order to minimize the late-stage attrition of new chemical entities (NCE), it is important to evaluate CYP induction potency at mRNA levels in the early stage of drug development...
2016: Drug Metabolism Letters
https://www.readbyqxmd.com/read/27515451/cyp2b6-and-oprm1-receptor-polymorphisms-at-methadone-clinics-and-novel-oprm1-haplotypes-a-cross-sectional-study
#13
Ahmad Abdulrahman AlMeman, Rusli Ismail, Markus Perola
INTRODUCTION: Methadone is accepted as an alternative therapy in opioid use disorders worldwide. Methadone responsiveness, however, is affected by a range of CYP450 enzymes and OPRM1 polymorphisms. OBJECTIVE: This study sought to detect CYP2B6 and OPRM1 variants and their genotypes, as major contributors to inter-variability in methadone responsiveness and methadone dose requirements. METHODS: We carried out a prospective experimental one-phase pharmacogenetic study in four addiction clinics in Malaysia...
2016: Drug Metabolism Letters
https://www.readbyqxmd.com/read/27456669/intracellular-retention-of-three-quinuclidine-derivatives-in-caco-2-permeation-experiments-mechanisms-and-impact-on-estimating-permeability-and-active-efflux-ratio
#14
Hong Jin, Sudarshan Kapadnis, Ting Chen, Dooyoung Lee, Andrew McRiner, Andrew Cook, Duane A Burnett, Gerhard Koenig, Cuyue Tang
BACKGROUND: Three quinuclidine derivatives (FRM-1, FRM-2 and FRM-3) were subject to significant mass loss to cellular retention in Caco-2 permeation experiments. The apparent permeability coefficient (Papp) calculated with either 'sink' (Papp,sink) or 'non-sink' (Papp,nonsink) method was significantly biased. As a result, a simplified 3-compartmental distribution model was applied in this study to derive the 'intrinsic' Papp (Papp,int) and to understand the impact of cellular retention on estimating Papp and active efflux ratio (ER) values...
2016: Drug Metabolism Letters
https://www.readbyqxmd.com/read/27456668/uhplc-quantitation-method-for-new-thiazolidinedione-lpsf-gq-02-and-in-vitro-in-vivo-kinetic-studies
#15
Carla Monalizi Vieira, Michel Leandro de Campos, Elias Carvalho Padilha, Marina Pitta, Ivan da Rocha Pitta, Maria do Carmo Alves de Lima, Rosângela Gonçalves Peccinini
BACKGROUND: LPSF/GQ-02 is a promising benzylidene thiazolidinedione that has demonstrated antidiabetic, antidyslipidemic, anti-atherosclerotic properties and can also treat non-alcoholic fatty liver disease. Despite all activity studies of the new compound, its pharmacokinetics are not yet described. OBJECTIVE: The aim of this study was to perform its first pharmacokinetic profile. METHODS: For this purpose a bioanalytical method for the quantitation of 5-(4- Chloro-benzylidene)-3-(4-methylbenzyl)-thiazolidine-2,4-dione (LPSF/GQ-02) was developed and validated...
2016: Drug Metabolism Letters
https://www.readbyqxmd.com/read/27449410/identification-and-characterization-of-the-human-cytosolic-sulfotransferases-mediating-the-sulfation-of-clioquinol-and-iodoquinol
#16
Akihiro Yamamoto, Maame Debrah-Pinamang, Nicholas J DiModica, Katsuhisa Kurogi, Ali A Naqvi, Ying Hui, Yoichi Sakakibara, Masahito Suiko, Ming-Cheh Liu
OBJECTIVE: The aim of the current study was to identify the human cytosolic sulfotransferases (SULTs) that are capable of sulfating clioquinol and iodoquinol, and to verify the presence of clioquinol/ iodoquinol-sulfating activity in human organ homogenates and cultured cells. METHOD: An established sulfotransferase assay was employed to analyze clioquinol/iodoquinolsulfating activity of thirteen known human SULTs, as well as cytosols of human kidney, liver, lung, and small intestine...
2016: Drug Metabolism Letters
https://www.readbyqxmd.com/read/27449409/the-uremic-toxin-indoxyl-3-sulfate-induces-cyp1a2-in-primary-human-hepatocytes
#17
Hong Liu, Rangaraj Narayanan, Matthew Hoffmann, Sekhar Surapaneni
: Chronic kidney disease (CKD) generally impacts clearance of renally eliminated drugs but growing evidence shows that it can influence clearance of hepatically eliminated drugs and a complete mechanistic understanding of this phenomenon is still lacking. CKD leads to accumulation of uremic toxins, including indoxyl- 3-sulfate (3-INDS) and indole-3-acetic acid (3-IAA). OBJECTIVE: In this study, we evaluated the potential of 3-INDS and 3-IAA (10, 30 and 100 μM) to induce liver cytochrome P450 (CYP) enzymes CYP1A2, 2B6 and 3A4/5 using cultured primary human hepatocytes following once daily treatment for 3 days...
2016: Drug Metabolism Letters
https://www.readbyqxmd.com/read/27331219/preface
#18
Suresh K Balani
No abstract text is available yet for this article.
2016: Drug Metabolism Letters
https://www.readbyqxmd.com/read/27292117/inhibition-of-procarcinogen-activating-enzyme-cyp1a2-activity-and-free-radical-formation-by-caffeic-acid-and-its-amide-analogues
#19
Paitoon Narongchai, Kanokporn Niwatananun, Siripun Narongchai, Winthana Kusirisin, Churdsak Jaikang
OBJECTIVES: Caffeic acid (CAF) and its amide analogues, ethyl 1-(3',4'-dihydroxyphenyl) propen amide (EDPA), phenethyl 1-(3',4'-dihydroxyphenyl) propen amide (PEDPA), phenmethyl 1- (3',4'-dihydroxyphenyl) propen amide (PMDPA) and octyl 1-(3',4'-dihydroxyphenyl) propen amide (ODPA) were investigated for the inhibition of procarcinogen activating enzyme. METHODS: CYP1A2 and scavenging activity on formation of nitric oxide, superoxide anion, DPPH radical and hydroxyl radical...
2016: Drug Metabolism Letters
https://www.readbyqxmd.com/read/27280599/effect-of-cardiovascular-injury-on-catabolism-of-adenosine-and-adenosine-5-triphosphate-in-systemic-blood-in-a-freely-moving-rat-model-in-vivo
#20
Pollen K Yeung, Shyam S Kolathuru, Remigius U Agu
BACKGROUND: Previous studies have shown that catabolism of adenosine 5'-triphosphate (ATP) in red blood cell (RBC) may be a key factor for cardiovascular protection and maintaining cardiovascular homeostasis. OBJECTIVE: To investigate the effect of cardiovascular injury on adenosine and ATP catabolism in systemic blood using a freely moving rat model in vivo. METHOD: After acclimatized to the experimental environment, Sprague Dawley (SD) rats were each given either isoproterenol (30 mg/kg) or saline (1 mL/kg) by subcutaneous (sc) injection...
2016: Drug Metabolism Letters
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