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Ping-Ping Lin, Xue-Ning Li, Fei Yuan, Wei-Li Chen, Meng-Jie Yang, Hong-Rong Xu
Huperzine A (HupA), one of the reversible and selective acetylcholinesterase inhibitors derived from Chinese herb Huperzia Serrata, possesses affirmative action of ameliorating cognitive dysfunction of Alzheimer's disease. Up to now, the effects of HupA on human cytochrome P450s (CYPs) have not been fully elucidated. The purpose of the present study was to clarify the metabolic pathway of HupA in vitro and in vivo, and to evaluate the CYPs inhibition/induction profile of HupA in vitro. The catalytic activity of CYP enzymes (CYP1A2, 2A6, 2C9, 2C19, 2D6, 2E1 and 3A4) was measured by the quantification of specific enzyme substrates using validated liquid chromatography-tandem mass spectrometry (LC/MS/MS) methods...
October 14, 2016: Biochemical and Biophysical Research Communications
Frank F Vincenzi, Philippe Lunetta
While SCUBA diving, a 44-year-old Caucasian patient had an abnormal cardiac rhythm, presumably Torsade de Pointes (TdP), during the initial descent to depth. Upon surfacing, she developed ventricular fibrillation and died. The patient had been treated for mild depression for nearly a year with citalopram 60 mg per day, a drug known to cause prolonged QT interval. She had also been treated with two potentially hepatotoxic drugs. Liver impairment causes selective loss of cytochrome P450 (CYP) 2C19 activity, the major pathway for metabolism of citalopram...
December 2015: Drug Saf Case Rep
Dal-Sik Kim, Yunjeong Kim, Ji-Young Jeon, Min-Gul Kim
BACKGROUND: We evaluated the drug interaction profile of Red Ginseng (RG) with respect to the activities of major cytochrome P450 (CYP) enzymes and the drug transporter P-glycoprotein (P-gp) in healthy Korean volunteers. METHODS: This article describes an open-label, crossover study. CYP probe cocktail drugs, caffeine, losartan, dextromethorphan, omeprazole, midazolam, and fexofenadine were administered before and after RG supplementation for 2 wk. Plasma samples were collected, and tolerability was assessed...
October 2016: Journal of Ginseng Research
Hirotaka Amano, Daichi Kazamori, Kenji Itoh
Three major organosulfur compounds of aged garlic extract, S-allyl-L-cysteine (SAC), S-methyl-L-cysteine (SMC), and trans-S-1-propenyl-L-cysteine (S1PC), were examined for their effects on the activities of five major isoforms of human CYP enzymes: CYP1A2, 2C9, 2C19, 2D6, and 3A4. The metabolite formation from probe substrates for the CYP isoforms was examined in human liver microsomes in the presence of organosulfur compounds at 0.01-1 mM by using liquid chromatography-tandem mass spectrometry (LC-MS/MS) analysis...
2016: Biological & Pharmaceutical Bulletin
D D Nabinger, L E Mazzoleni, G B Sander, F Mazzoleni, M C Osório, M G Klein, T F Rech, L Basso da Silva, G S de Moraes, R A Cristovam, E F Nardelli, C F M Francesconi, D Simon
The aim of this study was to examine the effect of polymorphisms in the cytochrome P450 (CYP) 2C19 gene (CYP2C19) on the Helicobacter pylori eradication rate in Brazilian patients with functional dyspepsia. Adults diagnosed with functional dyspepsia based on the ROME III criteria and infected with H. pylori were recruited to this study. The patients were subjected to gastrointestinal endoscopy and the H. pylori status was defined when both urease test and histopathology results were negative or positive. The patients were treated with proton pump inhibitor-based triple therapy (omeprazole, amoxicillin, and clarithromycin)...
September 16, 2016: Genetics and Molecular Research: GMR
Tomonori Akasaka, Daisuke Sueta, Yuichiro Arima, Noriaki Tabata, Seiji Takashio, Yasuhiro Izumiya, Eiichiro Yamamoto, Megumi Yamamuro, Kenichi Tsujita, Sunao Kojima, Koichi Kaikita, Ayami Kajiwara, Kazunori Morita, Kentaro Oniki, Junji Saruwatari, Kazuko Nakagawa, Yasuhiro Ogata, Kunihiko Matsui, Seiji Hokimoto
BACKGROUND: Categorization as a cytochrome P450 (CYP) 2C19 poor metabolizer (PM) is reported to be an independent risk factor for cardiovascular disease. Epoxyeicosatrienoic acids (EETs) are metabolites of arachidonic acid by CYP2C19 epoxygenases and anti-inflammatory properties, especially in microvascular tissues. We examined the impact of CYP2C19 polymorphisms and EETs on microvascular angina (MVA) caused by coronary microvascular dysfunction. METHODS AND RESULTS: We examined CYP2C19 genotypes in patients with MVA (n=71) and healthy subjects as control (n=71)...
September 23, 2016: American Journal of Physiology. Heart and Circulatory Physiology
Shotaro Uehara, Mirai Kawano, Norie Murayama, Yasuhiro Uno, Masahiro Utoh, Takashi Inoue, Erika Sasaki, Hiroshi Yamazaki
Racemic omeprazole has been used for clinically treating gastric acid-related diseases and also as a typical human cytochrome P450 (P450) 2C19 probe substrate in preclinical studies. S-Omeprazole has been developed as a single enantiomer medicine, which has been reported not to be associated with polymorphic human P450 2C19 phenotypes. In this study, 5-hydroxylation and sulfoxidation activities, with respect to stereoselective R- and S-omeprazole oxidations by liver microsomes from experimental animals including non-human primates and humans, were investigated in vitro...
September 15, 2016: Biochemical Pharmacology
Pui Shen Lau, Kenny Voon Gah Leong, Chin Eng Ong, Amelia Nathania Hui Min Dong, Yan Pan
Cytochrome P450 (CYP) 2C19 is essential for the metabolism of clinically used drugs including omeprazole, proguanil, and S-mephenytoin. This hepatic enzyme exhibits genetic polymorphism with inter-individual variability in catalytic activity. This study aimed to characterise the functional consequences of CYP2C19*23 (271 G>C, 991 A>G) and CYP2C19*24 (991 A>G, 1004 G>A) in vitro. Mutations in CYP2C19 cDNA were introduced by site-directed mutagenesis, and the CYP2C19 wild type (WT) as well as variants proteins were subsequently expressed using Escherichia coli cells...
August 30, 2016: Biochemical Genetics
B A L M Deiman, P A L Tonino, K Kouhestani, C E M Schrover, V Scharnhorst, L R C Dekker, N H J Pijls
AIM: This study explores clinical outcome in cytochrome P450 2C19 (CYP2C19)-related poor metaboliser patients treated with either clopidogrel or prasugrel after percutaneous coronary intervention (PCI) and investigates whether this could be cost-effective. METHODS AND RESULTS: This single-centre, observational study included 3260 patients scheduled for elective PCI between October 2010 and June 2013 and followed for adverse cardiovascular events until October 2014...
October 2016: Netherlands Heart Journal
Satoshi Asakura, Taiji Hayano, Atsushi Hagino, Tsukasa Koyama
PURPOSE: To investigate the safety, tolerability, and effectiveness of escitalopram in patients with social anxiety disorder in Japan. METHODS: A 52-week, open-label study was conducted in Japanese patients with social anxiety disorder with a total score ≥60 on the Liebowitz Social Anxiety Scale - Japanese Version (LSAS-J) and ≥4 on the Clinical Global Impression - Severity Scale. Escitalopram 10 mg/day was administered for the first week and could be increased to 20 mg/day...
2016: Neuropsychiatric Disease and Treatment
Hong Sun, Xiao-Ya Lou, Xiao-Ying Wu, Huan Wang, Qiang Qu, Shen-Lan Tan, Jun-Shan Ruan, Jian Qu, Hui Chen
BACKGROUND: Cytochrome P450 2C19 (CYP2C19) is an important drug-metabolizing enzyme (DME), which is responsible for the biotransformation of several kinds of drugs such as proton pump inhibitors, platelet aggregation inhibitors and antidepressants. Previous studies showed that Buchang NaoXinTong capsules (NXT) increased the CYP2C19 metabolic activity in vitro and enhanced the antiplatelet effect of clopidogrel in vivo. However, the underlying molecular mechanism remained unclear. In the present study, we examined whether Pregnane X receptor (PXR) plays a role in NXT-mediated regulation of CYP2C19 expression...
2016: PloS One
Subrata Pandit, Satyajyoti Kanjilal, Anshumali Awasthi, Anika Chaudhary, Dipankar Banerjee, B N Bhatt, Avinash Narwaria, Rahul Singh, Kakoli Dutta, Manu Jaggi, Anu T Singh, Neena Sharma, Chandra Kant Katiyar
ETHNOPHARMACOLOGICAL RELEVANCE: Arishtas are Ayurvedic formulation made with decoction of herbs. Arjunarishta formulation is being used in Ayurveda for cardio-protective activity. Ashwagandharishta formulation possesses antioxidant, anti-atherosclerotic and anti-stress properties. Ridayarishta, a novel empirical formulation was prepared using combination of selected ingredients from these two formulations to support healthy heart functions and to reduce stress. AIM OF THE STUDY: Aim of the Study was to investigate herb-drug interaction (HDI) of Ridayarishta formulation through human hepatic cytochrome P450 (CYP450) enzyme inhibition assay...
July 22, 2016: Journal of Ethnopharmacology
Wenfang Ma, Yan Liang, Jun Zhu, Tao Chen, Guangxun Feng, Yanmin Yang, Xin Liu, Xingyu Wang
BACKGROUND AND AIMS: Asians have very different genotype distributions of cytochrome P450 2C19 (CYP2C19), ATP-binding cassette, sub-family B, member 1 (ABCB1), and paraoxonase-1 (PON1), in whom relevant studies based on large samples are scarce. The purpose of this study was to evaluate the effects of these genes on outcomes of in-stent restenosis and re-stenting in Chinese patients after coronary stenting. METHODS: A total of 2569 acute coronary syndrome (ACS) patients were enrolled in a gene database study...
August 2016: Atherosclerosis
Steeve Gress, Claire Laurant, Nicolas Defarge, Carine Travert, Gilles-Éric Séralini
BACKGROUND: Plant medicinal extracts may be claimed to prevent or cure chemical intoxications. Few of these are tested for their mechanisms of actions in vivo and for their cellular impacts. In 2011, we demonstrated that hepatic cell mortality induced by environmentally realistic levels of the widely used herbicide Roundup (R) in vitro can be almost entirely prevented by plant extracts called Dig1 (D, Digeodren). METHODS: We tested the in vivo effects of D alone (1...
2016: BMC Complementary and Alternative Medicine
Chang Seon Ryu, Soo Jin Oh, Jung Min Oh, Ji-Yoon Lee, Sang Yoon Lee, Jung-Woo Chae, Kwang-Il Kwon, Sang Kyum Kim
Although propolis is one of the most popular functional foods for human health, there have been no comprehensive studies of herb-drug interactions through cytochrome P450 (CYP) inhibition. The purpose of this study was to determine the inhibitory effects of propolis on the activities of CYP1A2, 2A6, 2B6, 2C9, 2C19, 2D6, 2E1 and 3A4 using pooled human liver microsomes (HLMs). Propolis inhibited CYP1A2, CYP2E1 and CYP2C19 with an IC50 value of 6.9, 16.8, and 43.1 μg/mL, respectively, whereas CYP2A6, 2B6, 2C9, 2D6, and 3A4 were unaffected...
July 2016: Toxicological Research
Li Zhu, Roger J Brüggemann, Jonathan Uy, Angela Colbers, Matthew W Hruska, Ellen Chung, Karen Sims, Blisse Vakkalagadda, Xiaohui Xu, Ron H N van Schaik, David M Burger, Richard J Bertz
Voriconazole, a broad-spectrum triazole antifungal agent, is metabolized by cytochrome P450 (CYP) 2C19 and to a lesser extent by CYP3A. Genetic polymorphism of CYP2C19 not only plays a prominent role in its disposition but may also influence potential drug interactions with CYP450 modulators such as ritonavir. This study assessed 2-way drug interactions of voriconazole added-on to ritonavir-boosted atazanavir in both CYP2C19 extensive metabolizer (EM) and poor metabolizer (PM) healthy subjects. Each subject received voriconazole alone on days 1-3 followed by a 7-day washout...
July 19, 2016: Journal of Clinical Pharmacology
Christian Stratz, Timo Bömicke, Iris Younas, Anja Kittel, Michael Amann, Christian M Valina, Thomas Nührenberg, Dietmar Trenk, Franz-Josef Neumann, Willibald Hochholzer
BACKGROUND: Previous data suggest that reticulated platelets significantly affect antiplatelet response to thienopyridines. It is unknown whether parameters describing reticulated platelets can predict antiplatelet response to thienopyridines. OBJECTIVES: The authors sought to determine the extent to which parameters describing reticulated platelets can predict antiplatelet response to thienopyridine loading compared with established predictors. METHODS: This study randomized 300 patients undergoing elective coronary stenting to loading with clopidogrel 600 mg, prasugrel 30 mg, or prasugrel 60 mg...
July 19, 2016: Journal of the American College of Cardiology
Xiaofei Li, Caiyuan Yu, Tiansheng Wang, Ken Chen, Suodi Zhai, Huilin Tang
BACKGROUND: Genetic polymorphisms of cytochrome P450 enzymes, especially CYP2C19, could influence voriconazole pharmacokinetics. The association between CYP2C19 polymorphisms and voriconazole clinical outcomes is not well established. The aim of this meta-analysis was to evaluate the effect of CYP2C19 polymorphisms on clinical outcomes in patients treated with voriconazole. METHODS: PubMed, EMBASE, CENTRAL,, and three Chinese databases were searched from their inception to January 2016 to identify eligible trials that reported voriconazole exposure and clinical outcomes of voriconazole according to CYP2C19 polymorphisms...
October 2016: European Journal of Clinical Pharmacology
Manisha Bhateria, Rachumallu Ramakrishna, Santosh Kumar Puttrevu, Anil K Saxena, Rabi Sankar Bhatta
A significant number of new chemical entities (NCEs) fail in drug discovery due to inhibition of Cytochrome P450 (CYP) enzymes. Therefore, to avert costly drug failure at the clinical phase it becomes indispensable to evaluate the CYP inhibition profile of NCEs early in drug discovery. In light of these concerns, we envisioned to investigate the inhibitory effects of S002-333 [2-(4-methoxy-benzenesulfonyl)-2,3,4,9-tetrahydro-1H-b-carboxylic acid amide], a novel and potent antithrombotic agent, on nine major CYP enzymes (CYP1A2, 2A6, 2B6, 2C8, 2C9, 2C19, 2D6, 2E1 and 3A4) of human liver microsomes (HLM)...
August 25, 2016: Chemico-biological Interactions
Viktoria Moschetti, Katja Boland, Ulrich Feifel, Anja Hoch, Heike Zimdahl-Gelling, Michael Sand
AIMS: The aim of the present study was to investigate the safety, tolerability, dose proportionality and relative bioavailability of tablet and oral solution formulations of BI 409306 in healthy male subjects, and to compare the safety and pharmacokinetics in subjects who were extensive metabolizers (EMs) or poor metabolizers (PMs) of cytochrome P450 (CYP)-2C19. METHODS: The present randomized, double-blind, placebo-controlled, single-centre study evaluated single rising doses of BI 409306 (0...
July 4, 2016: British Journal of Clinical Pharmacology
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