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Colleen P Chin, YiXin Ren, Joan Berry, Stanley A Knott, Craig C McLauchlan, Lisa F Szczepura
Novel oxazine, oxazoline and carboxamide cluster complexes were prepared when different nucleophilic oxygen species reacted with nitriles coordinated to the Lewis acidic [Re6 Se8 ]2+ cluster core. Reaction of ICH2 CH2 O- (generated in situ) with [Re6 Se8 (PEt3 )5 (NCR)]A2 (1A2 (R = Me) and 2A2 (R = Ph) where A = BF4 - ), leads to the formation of [Re6 Se8 (PEt3 )5 (2-methyloxazoline)]2+ (32+ ) and [Re6 Se8 (PEt3 )5 (2-phenyloxazoline)]2+ (42+ ). Similarly, reaction of BrCH2 CH2 CH2 O- with the same nitrile complexes, 1A2 and 2A2 (where A = BF4 - or SbF6 - ) leads to the corresponding oxazine complexes, [Re6 Se8 (PEt3 )5 (2-methyloxazine)]2+ (52+ ) and [Re6 Se8 (PEt3 )5 (2-phenyloxazine)]2+ (62+ )...
March 12, 2018: Dalton Transactions: An International Journal of Inorganic Chemistry
Chi Zhang, Bo Xu, Guanzhao Liang, Xianshang Zeng, Dan Zeng, Deng Chen, Zhe Ge, Weiguang Yu, Xinchao Zhang
Objectives To compare the functional and radiographic outcomes of InterTAN nail (IT) and proximal femoral nail anti-rotation (PFNA) for managing primary AO/OTA 31-A2 intertrochanteric hip fractures (IHFs) in older osteoporotic patients. Methods Patients aged 60 years or older who received surgical treatment for IHFs (AO/OTA 3.1A2.1-A2.3) with IT or PFNA were retrospectively evaluated. The primary outcome was the postoperative treatment failure rate. The secondary outcome was the Harris Hip Score (HHS). Results A total of 326 osteoporotic cases (326 hips: IT, n = 162; PFNA, n = 164) were assessed with a mean follow-up of 43...
January 1, 2018: Journal of International Medical Research
Ching Feng Wu, Ricardo Fernandez, de la Torre Mercedes, Maria Delgado, Eva Fieira, Ching Yang Wu, Ming Ju Hsieh, Marina Paradela, Yun-Hen Liu, Diego Gonzalez-Rivas
OBJECTIVES: Single-port video-assisted thoracoscopic surgery (SPVATS) anatomical resection has been shown to be a feasible technique for lung cancer patients. Whether SPVATS has equivalent or better oncological outcomes for lung cancer patients remains controversial. The purpose of this study was to evaluate the perioperative and mid-term survival outcomes of SPVATS in 2 different medical centres. METHODS: We retrospectively reviewed patients who underwent SPVATS anatomical resections between January 2014 and February 2017 in Coruña University Hospital's Minimally Invasive Thoracic Surgery Unit (Spain) and Chang Gung Memorial Hospital (Taiwan)...
March 3, 2018: European Journal of Cardio-thoracic Surgery
Chris Schiering, Anne Vonk, Srustidhar Das, Brigitta Stockinger, Emma Wincent
The aryl hydrocarbon receptor (AHR)controls interleukin 22 production by T helper 17 cells (Th17). IL-22contributes to intestinalhomeostasis but has also been implicated inchronic inflammatory disorders and colorectal cancer, highlighting the need for appropriate regulation of IL-22 production. Upon activation, the AHR induces expression of cytochrome P4501 (CYP1) enzymes that in turn play an important feedback role that curtails the duration of AHR signaling by metabolizingAHRligands. Recently we described how agents that inhibit CYP1 function potentiate AHR signalingby disruptingmetabolic clearance of the endogenous ligand 6-formylindolo[3,2-b]carbazole (FICZ)...
February 28, 2018: Biochemical Pharmacology
Huaqiao Tang, Nana Long, Lin Lin, Yao Liu, Jianlong Li, Fenghui Sun, Lijuan Guo, Fen Zhang, Min Dai
Background: Methicillin-resistant Staphylococcus aureus (MRSA) is a very damaging and widespread pathogen, which is associated with many diseases and causes serious infections. MRSA infection can modulate the effects of drugs, which may occur through an influence on cytochrome P450 (CYP450), the drug-metabolizing enzyme in the liver. In this study, we evaluated the underlying mechanism of drug failure or poisoning in MRSA infection. Materials and methods: Mice were infected with three different doses of MRSA and the changes in CYP450 expression, cytokines, and oxidative stress markers were evaluated...
2018: Infection and Drug Resistance
Seong Eun Jin, Hyekyung Ha, Chang-Seob Seo, Hyeun-Kyoo Shin, Soo-Jin Jeong
Objective: The aim of this study was to investigate the possible herb-drug interactions between the traditional herbal formula Guibi-tang (GBT; Guipi-tang , Kihi-to ) and conventional drugs. Materials and Methods: GBT was orally administered to either male or female Sprague Dawley (SD) rats once daily at doses of 1000, 2000, or 5000 mg/kg/day for 13 weeks. The messenger ribonucleic acid (mRNA) expression of drug-metabolizing enzyme cytochrome P450 isozymes (cytochrome P450s; CYP1A1, 1A2, 2B1/2, 2C11, 2E1, 3A1, 3A2, and 4A1) was analyzed in hepatic tissues by reverse transcription-polymerase chain reaction...
January 2018: Pharmacognosy Magazine
Osamu Abe, Tomoyuki Ono, Hideyuki Sato, Fabian Müller, Hiroshi Ogata, Itaru Miura, Yayoi Shikama, Hirooki Yabe, Satomi Onoue, Martin F Fromm, Junko Kimura, Shingen Misaka
PURPOSE: The aim of the present study is to investigate a possible role of a single dose of (-)-epigallocatechin gallate (EGCG), the major catechin in green tea, for the pharmacokinetic interaction between green tea and nadolol in humans. METHODS: In a randomized three-phase crossover study, 13 healthy volunteers received single doses of 30 mg nadolol orally with water (control), or an aqueous solution of EGCG-concentrated green tea extract (GTE) at low or high dose...
February 26, 2018: European Journal of Clinical Pharmacology
David Picking, Bentley Chambers, James Barker, Iltaf Shah, Roy Porter, Declan P Naughton, Rupika Delgoda
Understanding the potential for adverse drug reactions (ADRs), from herb-drug interactions, is a key aspect of medicinal plant safety, with particular relevance for public health in countries where medicinal plant use is highly prevalent. We undertook an in-depth assessment of extracts of Hyptis verticillata Jacq., via its impact on activities of key cytochrome P450 (CYP) enzymes (CYPs 1A1, 1A2, 1B1, 3A4 and 2D6), its antioxidant properties (determined by DPPH assays) and chemical characterisation (using LC-MS)...
February 15, 2018: Molecules: a Journal of Synthetic Chemistry and Natural Product Chemistry
Taha Ahmad, Monica A Valentovic, Gary O Rankin
Methadone is a synthetic, long-acting opioid with a single chiral center forming two enantiomers, (R)-methadone and (S)-methadone, each having specific pharmacological actions. Concentrations of (R)- and (S)-methadone above therapeutic levels have the ability to cause serious, life-threatening, and fatal side effects. This toxicity can be due in part to the pharmacogenetics of an individual, which influences the pharmacokinetic and pharmacodynamic properties of the drug. Methadone is primarily metabolized in the liver by cytochrome P450 (CYP) enzymes, predominately by CYP2B6, followed by CYP3A4, 2C19, 2D6, and to a lesser extent, CYP2C18, 3A7, 2C8, 2C9, 3A5, and 1A2...
February 16, 2018: Biochemical Pharmacology
Ochuko L Erukainure, Rahman M Hafizur, Nurul Kabir, M Iqbal Choudhary, Olubunmi Atolani, Priyanka Banerjee, Robert Preissner, Chika I Chukwuma, Aliyu Muhammad, Eric O Amonsou, Md Shahidul Islam
Type 2 diabetes is the most prominent of all diabetes types, contributing to global morbidity and mortality. Availability and cost of treatment with little or no side effect especially in developing countries, remains a huge burden. This has led to the search of affordable alternative therapies especially from medicinal plants. In this study, the antidiabetic effect of the methanolic extract, dichloromethane (DCM), butanol (BuOH) and aqueous fractions of Clerodendrum volubile leaves were investigated in type 2 diabetic rats for their effect on glucose homeostasis, serum insulin level and hepatic biomarkers, lipid profile, pancreatic redox balance and Ca 2+ levels, and β-cell distribution and function...
2018: Frontiers in Pharmacology
Yosuke Hashimoto, Tomoyuki Hata, Minoru Tada, Manami Iida, Akihiro Watari, Yoshiaki Okada, Takefumi Doi, Hiroki Kuniyasu, Kiyohito Yagi, Masuo Kondoh
Claudin-2 (CLDN-2), a pore-forming tight-junction protein with a tetra-transmembrane domain, is involved in carcinogenesis and the metastasis of some cancers. Although CLDN-2 is highly expressed in the tight junctions of the liver and kidney, whether CLDN-2 is a safe target for cancer therapy remains unknown. We recently generated a rat monoclonal antibody (mAb, clone 1A2) that recognizes the extracellular domains of human and mouse CLDN-2. Here, we investigated the safety of CLDN-2-targeted cancer therapy by using 1A2 as a model therapeutic antibody...
February 12, 2018: European Journal of Pharmaceutical Sciences
Yanhong Sun, Shuqi Wang, Jianbo Ji, Guangxi Zhai, Jie Xing
Naphthoquine (NQ) is one of important partner drugs of Artemisinin-based combination therapy (ACT), which is recommended for the treatment of uncomplicated Plasmodium falciparum. NQ shows a high cure rate after a single oral administration. It is absorbed quickly (Tmax 2-4 h) and has a long elimination half-life (255 h). However, the metabolism of NQ has not been clarified. In this work, the metabolite profiling of NQ was studied in six liver microsomal incubates (human, cynomolgus monkey, beagle dog, mini pig, rat and CD1 mouse), seven recombinant CYP enzymes (1A2, 2B6, 2C8, 2C9, 2C19, 2D6 and 3A4) and rat (plasma, urine, bile and feces ) using liquid chromatography tandem high-resolution LTQ-Orbitrap mass spectrometry (HRMSn ) in conjunction with online H/D exchange...
February 12, 2018: Biomedical Chromatography: BMC
Henrik Berg Rasmussen, Majbritt Busk Madsen
The carboxylesterase 1 gene (CES1) encodes a hydrolase that metabolizes commonly used drugs. The CES1-related pseudogene, carboxylesterase 1 pseudogene 1 (CES1P1), has been implicated in gene exchange with CES1 and in the formation of hybrid genes including the carboxylesterase 1A2 gene (CES1A2). Hence, the CES1 region is complex. Using in silico PCR and alignment, we assessed the specificity of PCR-assisted procedures for genotyping CES1, CES1A2 and CES1P1 in studies identified in PubMed. We identified 33 such studies and excluded those that were not the first to use a procedure or lacked sequence information...
February 10, 2018: Drug Metabolism and Personalized Therapy
Jiří Vrba, Barbora Papoušková, Lenka Roubalová, Martina Zatloukalová, David Biedermann, Vladimír Křen, Kateřina Valentová, Jitka Ulrichová, Jan Vacek
This study examined the in vitro biotransformation of eight structurally related flavonolignans, namely silybin, 2,3-dehydrosilybin, silychristin, 2,3-dehydrosilychristin, silydianin, 2,3-dehydrosilydianin, isosilybin A and isosilybin B. The metabolic transformations were performed using primary cultures of human hepatocytes and recombinant human cytochromes P450 (CYPs 1A2, 2A6, 2B6, 2C8, 2C9, 2C19, 2D6, 2E1 and 3A4). The metabolites produced were analyzed by ultra-performance liquid chromatography coupled with tandem mass spectrometry...
January 30, 2018: Journal of Pharmaceutical and Biomedical Analysis
Breann T Colter, Helen Frances Garber, Sheila M Fleming, Jocelyn Phillips Fowler, Gregory D Harding, Molly Kromme Hooven, Amy Ashworth Howes, Smitha Krishnan Infante, Anna L Lang, Melinda Curran MacDougall, Melinda Stegman, Kelsey Rae Taylor, Christine Perdan Curran
Polychlorinated biphenyls (PCBs) are persistent organic pollutants known to cause adverse health effects and linked to neurological deficits in both human and animal studies. Children born to exposed mothers are at highest risk of learning and memory and motor deficits. We developed a mouse model that mimics human variation in the aryl hydrocarbon receptor and cytochrome P450 1A2 (CYP1A2) to determine if genetic variation increases susceptibility to developmental PCB exposure. In our previous studies, we found that high-affinity AhrbCyp1a2(-/-) and poor-affinity AhrdCyp1a2(-/-) knockout mice were most susceptible to learning and memory deficits following developmental PCB exposure compared with AhrbCyp1a2(+/+) wild type mice (C57BL/6J strain)...
January 30, 2018: Neurotoxicology
Tomoki Yamashita, Kazuo Takayama, Fuminori Sakurai, Hiroyuki Mizuguchi
Human induced pluripotent stem (iPS) cell-derived hepatocyte-like cells are expected to be utilized in drug screening and regenerative medicine. However, hepatocyte-like cells have not been fully used in such applications because it is difficult to produce such cells on a large scale. In this study, we tried to establish a method to mass produce hepatocyte-like cells using a three-dimensional (3D) cell culture bioreactor called the Rotary Cell Culture System (RCCS). RCCS enabled us to obtain homogenous hepatocyte-like cells on a billion scale (>109 cells)...
February 1, 2018: Biochemical and Biophysical Research Communications
Matt Albertolle, Thanh T N Phan, Ambra Pozzi, F Peter Guengerich
The lumen of the endoplasmic reticulum (ER) provides an oxidizing environment to aid in the formation of disulfide bonds, which is tightly regulated by both antioxidant proteins and small molecules. On the cytoplasmic side of the ER, cytochrome P450 (P450) proteins have been identified as a superfamily of enzymes that are important in the formation of endogenous chemicals as well as in the detoxication of xenobiotics. Our previous report described oxidative inhibition of P450 Family 4 enzymes via oxidation of the heme-thiolate cysteine to a sulfenic acid (-SOH) (Albertolle, M...
January 26, 2018: Molecular & Cellular Proteomics: MCP
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...
January 18, 2018: Drug Metabolism Letters
Mohammad Usman Mirza, Nazia Ikram, Nauman Mazhar, Kanzal Iman, Mehwish Riaz, Mohammad A Kamal
Alzheimer disease (AD) is a hot research topic currently across the world, characterized by the formation of β-amyloid plaques and neurofibrillary tangles. Inhibition of acetylcholinesterase (AChE) has gained much importance since the discovery of the involvement of peripheral anionic site (PAS) as an allosteric regulator of AChE. Progression of this neurodegenerative disorder causes a deficit in the cholinergic activity that leads towards cognitive decline. Therapeutic interventions in AD are largely focused upon AChE inhibitors designed essentially to prevent the loss of cholinergic function...
January 15, 2018: CNS & Neurological Disorders Drug Targets
Munirah Ahmad, Shazlan-Noor Suhaimi, Tai-Lin Chu, Norazlin Abdul Aziz, Noor-Kaslina Mohd Kornain, D S Samiulla, Kwok-Wai Lo, Chew-Hee Ng, Alan Soo-Beng Khoo
Copper(II) ternary complex, [Cu(phen)(C-dmg)(H2O)]NO3 was evaluated against a panel of cell lines, tested for in vivo efficacy in nasopharyngeal carcinoma xenograft models as well as for toxicity in NOD scid gamma mice. The Cu(II) complex displayed broad spectrum cytotoxicity against multiple cancer types, including lung, colon, central nervous system, melanoma, ovarian, and prostate cancer cell lines in the NCI-60 panel. The Cu(II) complex did not cause significant induction of cytochrome P450 (CYP) 3A and 1A enzymes but moderately inhibited CYP isoforms 1A2, 2C9, 2C19, 2D6, 2B6, 2C8 and 3A4...
2018: PloS One
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