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https://www.readbyqxmd.com/read/28646165/selective-inhibition-of-sterolo-acyltransferase-1-isozyme-by-beauveriolide-iii-in-intact-cells
#1
Taichi Ohshiro, Keisuke Kobayashi, Mio Ohba, Daisuke Matsuda, Lawrence L Rudel, Takashi Takahashi, Takayuki Doi, Hiroshi Tomoda
Beauveriolide III (BeauIII) inhibited sterol O-acyltransferases 1 and 2 (SOAT1 and SOAT2), which are endoplasmic reticulum (ER) membrane proteins, in an enzyme-based assay, and selectively inhibited SOAT1 in a cell-based assay using SOAT1-/SOAT2-CHO cells. This discrepancy in SOAT inhibition by BeauIII was investigated. In the enzyme-based assay, BeauIII inhibited SOAT1 and SOAT2 to a similar extent using microsomes prepared from cells disrupted under the strongest sonication condition. In semi-intact SOAT1-/SOAT2-CHO cells prepared by a treatment with digitonin (plasma membrane permeabilized), BeauIII selectively inhibited SOAT1 (IC50; 5...
June 23, 2017: Scientific Reports
https://www.readbyqxmd.com/read/28644971/simultaneous-silencing-of-ghfad2-1-and-ghfatb-enhances-the-quality-of-cottonseed-oil-with-high-oleic-acid
#2
Feng Liu, Yan-Peng Zhao, Hua-Guo Zhu, Qian-Hao Zhu, Jie Sun
Cottonseed oil has become an important source of edible oil due to its significant cost advantage. However, there is a growing concern over its fatty acid composition and nutritional value. In Gossypium hirsutum, GhFAD2-1 and GhFATB encoding the microsomal oleate desaturase and palmitoyl-acyl carrier protein thioesterase, respectively, play critical roles in regulating the proportions of saturated and polyunsaturated fatty acids in cottonseed lipids. In this study, RNAi technology was used to simultaneously inhibit the expression levels of GhFAD2-1 and GhFATB to improve the quality of cottonseed oil by increasing oleic acid content...
June 15, 2017: Journal of Plant Physiology
https://www.readbyqxmd.com/read/28644704/numerical-analysis-of-time-dependent-inhibition-kinetics-comparison-between-rat-liver-microsomes-and-rat-hepatocyte-data-for-mechanistic-model-fitting
#3
Chuong Pham, Swati Nagar, Ken Korzekwa
Time dependent inhibition (TDI) may confound drug interaction predictions. Recently, models were generated for an array of TDI kinetic schemes using numerical analysis of microsomal assays. Additionally, a distinct terminal inactivation step was identified for certain mechanism based inhibitors (MBI) following reversible metabolite intermediate complex (MIC) formation. Longer hepatocyte incubations potentially allow analysis of slow TDI and terminal inactivation. In the experiments presented here, we compared the quality of TDI parameterization by numerical analysis between hepatocyte and microsomal data...
June 23, 2017: Xenobiotica; the Fate of Foreign Compounds in Biological Systems
https://www.readbyqxmd.com/read/28642035/improving-the-efficacy-of-hormone-therapy-in-breast-cancer-the-role-ofcholesterol-metabolism-in-serm-mediated-autophagy-cell-differentiation-and-death
#4
REVIEW
Julie Leignadier, Florence Dalenc, Marc Poirot, Sandrine Silvente-Poirot
Breast cancer (BC) is one of the most common female cancers in the world, with estrogen receptor (ER)-positive BC the most frequent subtype. Tamoxifen (Tam) is an effective drug that competitively binds to the ER and is routinely used for the treatment of ER-positive BC. However, a number of ER-positive BC do not respond to Tam treatment and acquired resistance is often observed, constituting a major challenge for extending patient life expectancy. The mechanisms responsible for these treatment failures remain unclear, indicating the requirement for other targets and better predictors for patient response to Tam...
June 19, 2017: Biochemical Pharmacology
https://www.readbyqxmd.com/read/28638985/glucuronidation-of-deoxynivalenol-don-by-different-animal-species-identification-of-iso-don-glucuronides-and-iso-deepoxy-don-glucuronides-as-novel-don-metabolites-in-pigs-rats-mice-and-cows
#5
Heidi E Schwartz-Zimmermann, Christian Hametner, Veronika Nagl, Iris Fiby, Lukas Macheiner, Janine Winkler, Sven Dänicke, Erica Clark, James J Pestka, Franz Berthiller
The Fusarium mycotoxin deoxynivalenol (DON) is a frequent contaminant of cereal-based food and feed. Mammals metabolize DON by conjugation to glucuronic acid (GlcAc), the extent and regioselectivity of which is species-dependent. So far, only DON-3-glucuronide (DON-3-GlcAc) and DON-15-GlcAc have been unequivocally identified as mammalian DON glucuronides, and DON-7-GlcAc has been proposed as further DON metabolite. In the present work, qualitative HPLC-MS/MS analysis of urine samples of animals treated with DON (rats: 2 mg/kg bw, single bolus, gavage; mice: 1 mg/kg bw, single i...
June 21, 2017: Archives of Toxicology
https://www.readbyqxmd.com/read/28637871/phosphorylation-at-serine-31-targets-tyrosine-hydroxylase-to-vesicles-for-transport-along-microtubules
#6
Ana Jorge-Finnigan, Rune Kleppe, Kunwar Jung-Kc, Ming Ying, Michael Marie, Ivan Rios-Mondragon, Michael F Salvatore, Jaakko Saraste, Aurora Martinez
Tyrosine hydroxylase (TH) catalyzes the conversion of L-tyrosine into L-Dopa, which is the rate-limiting step in the synthesis of catecholamines, particularly dopamine in dopaminergergic neurons. Low dopamine levels and death of the dopaminergic neurons are hallmarks of Parkinson's disease (PD), where α-synuclein is also a key player. TH is highly regulated, notably by phosphorylation of several Ser/Thr residues in the N-terminal tail. However, the functional role of TH phosphorylation at the Ser31 site (THpSer31) remains unclear...
June 21, 2017: Journal of Biological Chemistry
https://www.readbyqxmd.com/read/28636885/differential-changes-in-the-pharmacokinetics-of-statins-in-collagen-induced-arthritis-rats
#7
Chun-Han Lin, Ke-Wei Hsu, Chia-Hao Chen, Yow-Shieng Uang, Chun-Jung Lin
The elevated systemic levels of cytokines in rheumatoid arthritis (RA) can change the expression of metabolic enzymes and transporters. Given that statins are lipid-lowering agents frequently used in RA patients with concurrent cardiovascular diseases, the objective of the present study was to investigate the impacts of RA on the pharmacokinetics of statins of different disposition properties in rats with collagen-induced arthritis (CIA). The expression of metabolic enzymes and transporters in tissues of CIA rats were analyzed by RT-qPCR...
June 18, 2017: Biochemical Pharmacology
https://www.readbyqxmd.com/read/28634818/sg2na-is-a-regulator-of-endoplasmic-reticulum-er-homeostasis-as-its-depletion-leads-to-er-stress
#8
Buddhi Prakash Jain, Shweta Pandey, Nikhat Saleem, Goutam K Tanti, Shalini Mishra, Shyamal K Goswami
SG2NA belongs to a three-member striatin subfamily of WD40 repeat superfamily of proteins. It has multiple protein-protein interaction domains involved in assembling supramolecular signaling complexes. Earlier, we had demonstrated that there are at least five variants of SG2NA generated by alternative splicing, intron retention, and RNA editing. Such versatile and dynamic mode of regulation implicates it in tissue development. In order to shed light on its role in cell physiology, total proteome analysis was performed in NIH3T3 cells depleted of 78 kDa SG2NA, the only isoform expressing therein...
June 21, 2017: Cell Stress & Chaperones
https://www.readbyqxmd.com/read/28634536/telavancin-a-novel-semisynthetic-lipoglycopeptide-agent-to-counter-the-challenge-of-resistant-gram-positive-pathogens
#9
REVIEW
Biswadeep Das, Chayna Sarkar, Debasmita Das, Amit Gupta, Arnav Kalra, Shubham Sahni
Telavancin (TD-6424), a semisynthetic lipoglycopeptide vancomycin-derivative, is a novel antimicrobial agent developed by Theravance for overcoming resistant Gram-positive bacterial infections, specifically methicillin-resistant Staphylococcus aureus (MRSA). The US Food and Drug Administration (USFDA) had approved telavancin in 2009 for the treatment of complicated skin and skin structure infections (cSSSIs) caused by Gram-positive bacteria, including MRSA (S. aureus, Streptococcus agalactiae, Streptococcus pyogenes, Streptococcus anginosus group, or Enterococcus faecalis)...
March 2017: Therapeutic Advances in Infectious Disease
https://www.readbyqxmd.com/read/28633475/cloning-and-characterization-of-cheilanthifoline-and-stylopine-synthase-genes-from-chelidonium-majus
#10
Mahdi Yahyazadeh, Purwanto Ratmoyo, Florian Bittner, Fumihiko Sato, Dirk Selmar
The most prominent alkaloid of Chelidonium majus is dihydrocoptisine, revealing the characteristical benzophenanthridine skeleton. Up to now, any information about the enzymes responsible for its biosynthesis in C. majus and the related genes respectively, is lacking. Based on sequence similarities to the corresponding methylenedioxy bridge-forming cytochrome P450-enzymes involved in the isoquinoline alkaloid biosynthesis in Eschscholzia californica, genes for a cheilanthifoline synthase and a stylopine synthase from C...
June 19, 2017: Plant & Cell Physiology
https://www.readbyqxmd.com/read/28633128/involvement-of-udp-glucuronosyltransferases-in-higenamine-glucuronidation-and-the-gender-and-species-differences-in-liver
#11
Zhi Liang, Chang Xu, Lingna Dong, Yile Fu, Qiong Wu, Jie Zhao, Ling Ye, Zheng Cai, Menghua Liu, Bijun Xia, Lan Tang, Zhongqiu Liu
OBJECTIVES: Higenamine (HG), an active ingredient of Aconite root in Chinese herbal medicine, is mainly metabolized by UDP-glucuronosyltransferases (UGT). However, the systematic glucuronidation of HG in humans remains unclear. The purpose of this study was to investigate the glucuronidation of HG. METHODS: 12 recombinant human UGT (rUGT) isozymes were used to characterize the HG glucuronidation. Liver microsomes from male and female mice, rats, guinea pigs, dogs, and humans were used to determine the species and gender differences using liquid chromatography-mass spectrometry...
June 17, 2017: Biomedicine & Pharmacotherapy, Biomédecine & Pharmacothérapie
https://www.readbyqxmd.com/read/28631076/effects-of-glycyrrhizic-acid-on-the-pharmacokinetics-of-pristimerin-in-rats-and-its-potential-mechanism
#12
Xiufen Zhao, Yan Wu, Dongmei Wang
BACKGROUND AND OBJECTIVES: Pristimerin has been reported to possess a wide range of pharmacological activities. This study investigates the effects of glycyrrhizic acid on the pharmacokinetics of pristimerin in rats. METHODS: The pharmacokinetics of orally administered pristimerin (2 mg/kg) with or without glycyrrhizic acid pretreatment (at a dose of 100 mg/kg/day for 7 days) were investigated. The plasma concentration of pristimerin was determined using a sensitive and reliable LC-MS/MS method, and the pharmacokinetics profiles were calculated and compared...
June 19, 2017: European Journal of Drug Metabolism and Pharmacokinetics
https://www.readbyqxmd.com/read/28629535/enhanced-absorption-and-inhibited-metabolism-of-emodin-by-2-3-5-4-tetrahydroxystilbene-2-o-%C3%AE-d-glucopyranoside-possible-mechanisms-for-polygoni-multiflori-radix-induced-liver-injury
#13
Qiong Yu, Li-Long Jiang, Na Luo, Ya-Xi Fan, Jiang Ma, Ping Li, Hui-Jun Li
Polygoni Multiflori Radix (PMR) has been commonly used as a tonic in China for centuries. However, PMR-associated hepatotoxicity is becoming a safety issue. In our previous in vivo study, an interaction between stilbenes and anthraquinones has been discovered and a hypothesis is proposed that the interaction between stilbene glucoside-enriching fraction and emodin may contribute to the side effects of PMR. To further support our previous in vivo results in rats, the present in vitro study was designed to evaluate the effects of 2, 3, 5, 4'-tetrahydroxystilbene-2-O-β-D-glucopyranoside (TSG) on the cellular absorption and human liver microsome metabolism of emodin...
June 2017: Chinese Journal of Natural Medicines
https://www.readbyqxmd.com/read/28629077/effects-of-the-surface-modification-of-polyurethane-substrates-on-genotoxicity-and-blood-activation-processes
#14
Roman Major, Hanna Plutecka, Anna Gruszczynska, Juergen M Lackner, Boguslaw Major
The aim of this study was to determine the mutagenic and thrombogenic potential of a material composed of a thin coating deposited on a polymeric substrate. In this work, a surface was modified in a manner that would mimic the function of cellular niches. Finally, the surfaces should actively capture and differentiate progenitor cells from the blood stream. Thin films with 10 to 500nm thicknesses were deposited by unbalanced, pulsed DC magnetron sputtering on smooth polyurethane. Such high energy conditions led to a stiffening of the polymer surface layers by pseudodiffusion during the initial stages of film growth...
October 1, 2017: Materials Science & Engineering. C, Materials for Biological Applications
https://www.readbyqxmd.com/read/28628921/activation-of-cox-2-mpges-1-pge2-cascade-via-nlrp3-inflammasome-contributes-to-albumin-induced-proximal-tubule-cell-injury
#15
Yibo Zhuang, Fei Zhao, Jing Liang, Xu Deng, Yue Zhang, Guixia Ding, Aihua Zhang, Zhanjun Jia, Songming Huang
BACKGROUND/AIMS: The activation of NOD-like receptor family, pyrin domain containing3 (NLRP3) inflammasome has been shown to be positively correlated with the severity of proteinuria in chronic kidney disease (CKD) patients. Prostaglandin E2 (PGE2), an important inflammatory mediator, is also involved in various kidney injuries. The aim of the present study was to investigate the involvement of NLRP3 inflammasome and PGE2 synthetic pathway in albumin-induced renal tubular injury. METHODS: Murine proximal tubular cells (mPTCs) were treated with albumin to induce cell injury...
June 19, 2017: Cellular Physiology and Biochemistry
https://www.readbyqxmd.com/read/28627961/microsomal-prostaglandin-e2-synthase-1-inhibitors-a-patent-review
#16
Anastasia Psarra, Aikaterini Nikolaou, Maroula G Kokotou, Dimitris Limnios, George Kokotos
Microsomal prostaglandin E2 synthase-1 (mPGES-1) catalyzes the terminal step of prostaglandin E2 (PGE2) generation. It is strongly upregulated in inflamed tissues and overexpressed in tumors and it has been recognized as a key enzyme in inflammatory diseases such as arthritis, atherosclerosis, stroke and cancer. Thus, a great effort has been devoted in developing synthetic mPGES-1 inhibitors as novel anti-inflammatory agents. Areas covered: This review article summarizes the mPGES-1 inhibitors presented in patent literature from 2000 to August 2016 and their biological evaluation, discussing their activities in vitro and in vivo...
June 19, 2017: Expert Opinion on Therapeutic Patents
https://www.readbyqxmd.com/read/28624999/in-vitro-biotransformation-safety-and-chemopreventive-action-of-novel-8-methoxy-purine-2-6-dione-derivatives
#17
Małgorzata Anna Marć, Enrique Domínguez-Álvarez, Karolina Słoczyńska, Paweł Żmudzki, Grażyna Chłoń-Rzepa, Elżbieta Pękala
Metabolic stability, mutagenicity, antimutagenicity, and the ability to scavenge free radicals of four novel 8-methoxy-purine-2,6-dione derivatives (compounds 1-4) demonstrating analgesic and anti-inflammatory properties were determined. Metabolic stability was evaluated in Cunninghamella and microsomal models, mutagenic and antimutagenic properties were assessed using the Ames and the Vibrio harveyi tests, and free radical scavenging activity was evaluated with 2,2-diphenyl-1-picrylhydrazyl radical scavenging assay...
June 17, 2017: Applied Biochemistry and Biotechnology
https://www.readbyqxmd.com/read/28623772/development-and-validation-of-a-highly-sensitive-lc-esi-ms-ms-method-for-estimation-of-iiim-mcd-211-a-novel-nitrofuranyl-methyl-piperazine-derivative-with-potential-activity-against-tuberculosis-application-to-drug-development
#18
Asmita Magotra, Anjna Sharma, Ajai Prakash Gupta, Priya Wazir, Shweta Sharma, Parvinder Pal Singh, Manoj Kumar Tikoo, Ram A Vishwakarma, Gurdarshan Singh, Utpal Nandi
In the present study, a simple, sensitive, specific and rapid liquid chromatography (LC) tandem mass spectrometry (MS/MS) method was developed and validated according to the Food and Drug Administration (FDA) guidelines for estimation of IIIM-MCD-211 (a potent oral candidate with promising action against tuberculosis) in mice plasma using carbamazepine as internal standard (IS). Bioanalytical method consisted of one step protein precipitation for sample preparation followed by quantitation in LC-MS/MS using positive electrospray ionization technique (ESI) operating in multiple reaction monitoring (MRM) mode...
June 8, 2017: Journal of Chromatography. B, Analytical Technologies in the Biomedical and Life Sciences
https://www.readbyqxmd.com/read/28623690/candidate-cytochrome-p450-genes-for-ethoxyresorufin-o-deethylase-activity-in-oyster-crassostrea-gigas
#19
Marília Nardelli Siebert, Jacó Joaquim Mattos, Guilherme Toledo-Silva, Guilherme Razzera, Afonso Celso Dias Bainy
Vertebrate cytochrome P450 1 (CYP1) enzymes metabolize endogenous and xenobiotic compounds and usually demonstrate a substrate-inducible response. Ethoxyresorufin O-deethylase activity (EROD) is a common method to quantify CYP1 enzymes activity in these organisms. Despite the absence of this gene family in protostomes, CYP1-like genes were identified in several species, even though no evolutionary relationship has been established with the vertebrate CYP1 family. In the present study, EROD activity was evaluated in microsomal fraction of gills, digestive gland and mantle of Crassostrea gigas...
June 9, 2017: Aquatic Toxicology
https://www.readbyqxmd.com/read/28623260/qualifying-a-eukaryotic-cell-free-system-for-fluorescence-based-gpcr-analyses
#20
Anne Zemella, Solveig Grossmann, Rita Sachse, Andrei Sonnabend, Michael Schaefer, Stefan Kubick
Membrane proteins are key elements in cell-mediated processes. In particular, G protein-coupled receptors (GPCRs) have attracted increasing interest since they affect cellular signaling. Furthermore, mutations in GPCRs can cause acquired and inheritable diseases. Up to date, there still exist a number of GPCRs that has not been structurally and functionally analyzed due to difficulties in cell-based membrane protein production. A promising approach for membrane protein synthesis and analysis has emerged during the last years and is known as cell-free protein synthesis (CFPS)...
June 16, 2017: Scientific Reports
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