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Drug Metabolism Letters

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https://www.readbyqxmd.com/read/30215338/hepatic-flavin-containing-monooxygenase-and-aldehyde-oxidase-activities-in-male-domestic-pigs-at-different-ages
#1
Steven X Hu
BACKGROUND: Age has significant impact on activities of hepatic metabolizing enzymes in humans and animals. Flavin-containing monooxygenase (FMO) and aldehyde oxidase are two important hepatic enzymes. Understanding of impact of age on these two enzymes is still limited. This work was to investigate growth impact on hepatic FMO and AO activities in domestic male pigs. METHODS: Porcine liver microsomes and cytosol were prepared from the livers of male domestic pigs at ages of 1 day, 2, 5, 10 and 20 weeks...
September 13, 2018: Drug Metabolism Letters
https://www.readbyqxmd.com/read/30210009/formation-of-a-toxic-quinoneimine-metabolite-from-diclofenac-a-quantum-chemical-study
#2
M Ramesh, Prasad V Bharatam
Diclofenac is a non-steroidal antiinflammatory drug. It is predominantly metabolized by CYP2C9. 4̍-hydroxydiclofenac and its quinoneimine are the metabolites of diclofenac. However, few numbers of serious cases of idiosyncratic hepatotoxicity due to diclofenac metabolism were reported. The formation of the quinoneimine metabolite was found to be responsible for this idiosyncratic toxicity. Quinoneimine is an over-oxidized metabolite of diclofenac. In this work, computational studies were conducted to detail the formation of a quinoneimine metabolite from diclofenac...
September 13, 2018: Drug Metabolism Letters
https://www.readbyqxmd.com/read/30124163/a-novel-in-vitro-experimental-system-for-the-evaluation-of-enteric-drug-metabolism-cofactor-supplemented-permeabilized-cryopreserved-human-enterocytes-metmax%C3%A2-cryopreserved-human-enterocytes
#3
Albert P Li, Kirsten Amaral, Ming-Chih David Ho
We report here an evaluation of a novel experimental system- cofactor-supplemented permeabilized cryopreserved human enterocytes (MetMax™ cryopreserved human enterocytes (MMHE), patent pending) for applications in the evaluation of enteric drug metabolism. A major advantage of MMHE over conventional cryopreserved human enterocytes (CCHE) is the simplification of the use procedures including storage at -80o C instead of in liquid nitrogen, and use of the cells immediately after thawing without a need for centrifugation and microscopic evaluation of cell density and viability and cell density adjustment...
August 20, 2018: Drug Metabolism Letters
https://www.readbyqxmd.com/read/30117405/in-vitro-drug-drug-interaction-potential-of-sulfoxide-and-or-sulfone-metabolites-of-albendazole-triclabendazole-aldicarb-methiocarb-montelukast-and-ziprasidone
#4
Poonam Giri, Lakshmikant Gupta, Sneha Naidu, Vipul Joshi, Nirmal Patel, Shyamkumar Giri, Nuggehally R Srinivas
BACKGROUND: The use of poly-pharmacy in the present day clinical therapy has made identification of clinical drug-drug interaction risk an important aspect of drug development process. Although many drugs can be metabolized to sulfoxide and/or sulfone metabolites, seldom is known on the CYP inhibition potential and/or the metabolic fate for such metabolites. OBJECTIVE: The key objectives were: a) to evaluate the in vitro CYP inhibition potential of select parent drugs with sulfoxide/sulfone metabolites; b) to assess the in vitro metabolic fate of the same panel of parent drugs and metabolites...
August 16, 2018: Drug Metabolism Letters
https://www.readbyqxmd.com/read/30070179/using-lc-retention-times-in-organic-structure-determination-drug-metabolite-identification
#5
William L Fitch, S Cyrus Khojasteh, Ignacio Aliagas, Kevin Johnson
BACKGROUND: There is a continued need for improvements in the efficiency of metabolite structure elucidation. OBJECTIVE: We propose to take LC retention time (RT) into consideration during the process of structure determination. METHOD: Herein we develop a simple methodology that employs a chromatographic hydrophobicity index (CHI) framework for standardizing LC conditions and introduce and utilize the concept of a predictable CHI change upon Phase 1 biotransformation (CHIbt)...
August 1, 2018: Drug Metabolism Letters
https://www.readbyqxmd.com/read/29984664/genistein-affects-expression-of-cytochrome-p450-cyp450-genes-in-hepatocellular-carcinoma-hepg2-c3a-cell-line
#6
Sandra Regina Lepri, Daniele Sartori, Simone Cristine Semprebon, Adrivanio Baranoski, Giuliana Castello Coatti, Mario Sergio Mantovani
• Background: Genistein (5,7-Dihydroxy-3-(4-hydroxyphenyl)-4H-1-benzopyran-4-one) is the most abundant isoflavone in soybean, which has been associated with a lower risk of development of cancer and cardiovascular diseases. Of particular interest regarding cancer preventive properties of flavonoids is their interaction with cytochrome P450 enzymes (CYPs). However, contradictory data report the effect of genistein on expression of СYPs enzymes. • Objective: The aim of this study was to investigate the effects of genistein on cytochrome P450 (CYP) gene expression levels in human hepatocellular carcinoma (HepG2/C3A) and colon adenocarcinoma (HT29) cells...
July 9, 2018: Drug Metabolism Letters
https://www.readbyqxmd.com/read/29938623/quantitative-proteomics-reveals-changes-in-transporter-protein-abundance-in-liver-kidney-and-brain-of-mice-by-pregnancy
#7
Michael Z Liao, Chunying Gao, Deepak Kumar Bhatt, Bhagwat Prasad, Qingcheng Mao
BACKGROUND: Few studies have systematically investigated pregnancy-induced changes in protein abundance of drug transporters in organs important for drug/xenobiotic disposition. OBJECTIVE: The goal of this study was to compare protein abundance of important drug/xenobiotic transporters including Abcb1a, Abcg2, Abcc2, and Slco1b2 in the liver, kidney and brain of pregnant mice on gestation day 15 to that of non-pregnant mice. METHODS: The mass spectrometry-based proteomics was used to quantify changes in protein abundance of transporters in tissues from pregnant and non-pregnant mice...
June 25, 2018: Drug Metabolism Letters
https://www.readbyqxmd.com/read/29886840/new-perspectives-on-acyl-glucuronide-risk-assessment-in-drug-discovery-investigation-of-in-vitro-stability-in-situ-reactivity-and-bioactivation
#8
Mithat Gunduz, Upendra A Argikar, Amanda L Cirello, Jennifer L Dumouchel
BACKGROUND: Acyl glucuronides of xenobiotics have been a subject of wide interest from the pharmaceutical industry with respect biochemical reactivity, hepatic disposition, and enterohepatic circulation. The reactivity and lack of stability of an acyl glucuronide for a clinical candidate could pose major developability concerns. To date, multiple in vitro assays have been published to assess the risk associated with acyl glucuronides. Despite this fact, the translation of these findings to predicting clinical safety remains poor...
June 10, 2018: Drug Metabolism Letters
https://www.readbyqxmd.com/read/29886839/effects-of-tobacco-nicotine-derived-nitrosamine-ketone-nnk-exposures-on-brain-alcohol-metabolizing-enzyme-activities
#9
Emine B Yalcin, Ming Tong, Gina Gallucci, Suzanne M de la Monte
BACKGROUND: The high levels of blood alcohol achieved with chronic plus binge alcohol exposures are somewhat reduced by co-administration of tobacco specific Nicotine-Derived Nitrosamine Ketone (NNK) suggesting that NNK may alter alcohol metabolism. OBJECTIVE: To test this hypothesis, we We examined ethanol and acetaldehyde-metabolizing enzyme activities and malondialdehyde adduct formation in rats exposed to ethanol (chronic + binge), NNK, or both. METHODS: 4-week old Long Evans rats were fed liquid diets containing 0% or 26% caloric ethanol for 8 weeks...
June 10, 2018: Drug Metabolism Letters
https://www.readbyqxmd.com/read/30203728/preface
#10
Suresh Balani
No abstract text is available yet for this article.
2018: Drug Metabolism Letters
https://www.readbyqxmd.com/read/29676238/effect-of-cyp2d6-poor-metabolizer-phenotype-on-stereoselective-nebivolol-pharmacokinetics
#11
Carolina P Vieira, Daniel V Neves, Eduardo B Coelho, Vera Lucia Lanchote
BACKGROUND: Nebivolol is a drug available as a racemate of d-nebivolol (SRRR) and lnebivolol (RSSS). In human liver microsomes, CYP2D6 mainly catalyses the metabolism of lnebivolol, while CYP2C19 catalyses the metabolism of d-nebivolol. Nebivolol stereoselective pharmacokinetics has been described only for extensive metabolizers (EM). OBJECTIVE: To describe the stereoseletive nebivolol pharmacokinetics in CYP2D6 poor metabolizers (PM) and to assess whether the phenotype has an impact on nebivolol pharmacokinetics...
2018: Drug Metabolism Letters
https://www.readbyqxmd.com/read/29669508/in-vitro-drug-metabolism-investigation-of-7-ethoxycoumarin-in-human-monkey-dog-and-rat-hepatocytes-by-high-resolution-lc-ms-ms
#12
Wan-Yong Feng, Jenny Wen, Kathe Stauber
BACKGROUND: Recently, it has been an increasing concern on the bioactivation and adverse reactions associated with consumption of herbal and nature products. 7-Ethoxycoumarin is one of coumarin family compounds, but little information is available regarding its potential reactive metabolites. METHOD: 7-ethoxylcoumarin was incubated individually with human, monkey, dog and rat hepatocytes for 2 hr, metabolites were detected, identified and characterized using high resolution liquid chromagraphy - tandem mass spectrometry...
2018: Drug Metabolism Letters
https://www.readbyqxmd.com/read/29658443/evaluation-of-the-effect-of-uremic-serum-on-hepatic-reductase-functional-expression
#13
LETTER
Osama Y Alshogran, Esra A F Al-Obaidi, Belal A Al-Husein, Ashraf O Oweis
BACKGROUND: The nonrenal clearance of drugs mediated by hepatic reduction is selectively altered by kidney disease. This study evaluated the influence of uremic serum on the expression and activity of reductase enzymes. METHODS: Human hepatocellular carcinoma cells (HepG2) were incubated with 5% pooled serum collected from patients with hemodialysis (pre- and post-dialysis session) or control subjects. The mRNA expression of various aldo-keto (AKR1C) and carbonyl (CBR) reductases were measured...
2018: Drug Metabolism Letters
https://www.readbyqxmd.com/read/29595119/cytochrome-p450-3a4-induction-lumacaftor-versus-ivacaftor-potentially-resulting-in-significantly-reduced-plasma-concentration-of-ivacaftor
#14
Elena K Schneider
BACKGROUND & OBJECTIVE: Since the release of ivacaftor-lumacaftor, several red-flags have been raised that highlight the clinical efficacy of this combination strategy that may be limited due to antagonistic drug-drug interactions. METHOD: The effect of ivacaftor, its major metabolites M1 and M6, lumacaftor and the novel cystic fibrosis transmembrane conductance regulator (CFTR) modulator tezacaftor at 10 µg/mL on the enzymatic activity of the major xenobiotic metabolizing enzymes CYP1A2 and CYP3A4 as well as the minor enzymes CYP2B6 and CYP2C9 was assayed...
2018: Drug Metabolism Letters
https://www.readbyqxmd.com/read/29577869/characterization-of-liver-and-cancer-type-organic-anion-transporting-polypeptide-oatp-1b3-messenger-rna-expression-in-normal-and-cancerous-human-tissues
#15
Khondoker Alam, Taleah Farasyn, Kai Ding, Wei Yue
BACKGROUND: Membrane transport protein organic anion transporting polypeptide (OATP) 1B3 mediates the cellular uptake of many clinically important drugs including anti-cancer drugs (e.g., paclitaxel). In addition to the well-recognized hepatic expression and function of OATP1B3 [herein named liver-type (Lt) OATP1B3], OATP1B3 also expresses in cancers and has been postulated to play a role in cancer therapy, presumably by facilitating the influx of anti-cancer drugs. Recently, a cancer type (Ct)-OATP1B3 mRNA variant was identified in colon and lung cancer tissues, which encodes truncated Ct-OATP1B3 with negligible transport activity...
2018: Drug Metabolism Letters
https://www.readbyqxmd.com/read/29542427/evaluation-of-herb-drug-interaction-of-synacinn%C3%A2-and-individual-biomarker-through-cytochrome-450-inhibition-assay
#16
Nur Syukriah Ab Rahman, Fadzilah Adibah Abd Majid, Mohd Effendy Abd Wahid, Ain Nabihah Zainudin, Siti Nurazwa Zainol, Hassan Fahmi Ismail, Tet Soon Wong, Nirbhay Kumar Tiwari, Sanjeev Giri
BACKGROUND: SynacinnTM contains five standardized herbal extracts of Orthosiphon Stamineus (OS), Syzygium polyanthum (SZ), Curcuma xantorrizza (CX), Cinnamomum zeylanicum (CZ) and Andrographis paniculata (AP) and is standardized against phytochemical markers of rosmarinic acid, gallic acid, curcumin, catechin and andrographolide respectively. This herbal medicine has been used as health supplement for diabetes. SynacinnTM is recommended to be consumed as supplement to the diabetic drugs...
2018: Drug Metabolism Letters
https://www.readbyqxmd.com/read/29521215/lc-ms-ms-identification-and-structural-characterization-of-main-biodegradation-products-of-nitroproston-a-novel-prostaglandin-based-pharmaceutical-compound
#17
Natalia V Mesonzhnik, Natalia E Moskaleva, Ksenia M Shestakova, Ksenya O Kurynina, Pavel A Baranov, Natalia M Gretskaya, Igor V Serkov, Igor I Lyubimov, Vladimir V Bezuglov, Svetlana A Appolonova
BACKGROUND: Nitroproston is a novel prostaglandin-based compound modified by NOdonating groups with potential application in obstructive respiratory diseases such as asthma and obstructive bronchitis. Nitroproston has been extensively studied using various pharmacological models. Its biological stability is still uncertain. OBJECTIVE: The aim of the present study was to evaluate Nitroproston stability in vitro, as well as to identify and characterize its major biodegradation products...
2018: Drug Metabolism Letters
https://www.readbyqxmd.com/read/29357810/cytochrome-p450-1a2-messenger-rna-is-a-more-reliable-marker-than-cytochrome-p450-1a2-activity-phenacetin-o-deethylation-for-assessment-of-induction-potential-of-drug-metabolizing-enzymes-using-heparg-cells
#18
Akira Ogasawara, Nozomu Kato, Nao Torimoto, Fumika Aohara, Rikiya Ohashi, Yasuhiro Yamada, Hideki Taniguchi
BACKGROUND: The HepaRG cells have key drug metabolism functionalities comparable to those of primary human hepatocytes. Many studies have reported that this cell line can be used as a reliable in vitro model for human drug metabolism studies, including the assessment of cytochrome P450 (CYP) induction. OBJECTIVES: The objective of this study is to determine whether CYP mRNA level measurement is superior to the CYP enzyme activity measurement as a convenient high-throughput method for evaluating CYP induction potential using HepaRG cells...
2018: Drug Metabolism Letters
https://www.readbyqxmd.com/read/29237391/utility-of-pooled-cryopreserved-human-enterocytes-as-an-in-vitro-model-for-assessing-intestinal-clearance-and-drug-drug-interactions
#19
Zhengyin Yan, Susan Wong, Jane Kelly, Hoa Le, Ning Liu, Mika Kosaka, Suzanne Tey, Peter Vuong, Albert Li
A recent advancement in isolation and cryopreservation has resulted in commercially available primary human enterocytes that express various drug metabolizing enzymes (DMEs) and transporters. The main objective of this study was to further evaluate the utility of pooled cryopreserved enterocytes, specifically MetMax™ cryopreserved human enterocytes (In Vitro ADMET Laboratories), as an in vitro model for assessing intestinal clearance in comparison to hepatocytes. It was found that, for CYP3A4 substrates such as midazolam, amprenavir and loperamide, in vitro metabolic clearance is generally lower in enterocytes compared to that of hepatocytes, which is consistent with the relative abundance of the enzyme between the intestine and liver...
December 12, 2017: Drug Metabolism Letters
https://www.readbyqxmd.com/read/29197321/preface
#20
Suresh K Balani
No abstract text is available yet for this article.
November 17, 2017: Drug Metabolism Letters
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