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https://www.readbyqxmd.com/read/28768454/insight-into-the-structural-requirements-of-thiophene-3-carbonitriles-based-murf-inhibitors-by-3d-qsar-molecular-docking-and-molecular-dynamics-study
#1
Mohammed Afzal Azam, Srikanth Jupudi
The discovery of clinically relevant inhibitors against MurF enzyme has proven to be a challenging task. In order to get further insight into the structural features required for the MurF inhibitory activity, we performed pharmacophore and atom-based three-dimensional quantitative structure-activity relationship studies for novel thiophene-3-carbonitriles based MurF inhibitors. The five-feature pharmacophore model was generated using 48 inhibitors having IC50 values ranging from 0.18 to 663 μm. The best-fitted model showed a higher coefficient of determination (R(2) = 0...
October 2017: Journal of Receptor and Signal Transduction Research
https://www.readbyqxmd.com/read/28648042/-effects-of-lappaconitine-on-pain-and-inflammatory-response-of-severely-burned-rats-and-the-mechanism
#2
C L Yang, Z R Wei, T H Zhang, X Q Zeng, B H Wu
Objective: To explore the effects of lappaconitine (LA) on pain and inflammatory response of severely burned rats and the mechanism. Methods: Forty SD rats were divided into healthy+ normal saline group, sham injury+ normal saline group, pure burn group, burn+ LA group, and healthy+ LA group according to the random number table (the same dividing method below), with 8 rats in each group. Rats in pure burn and burn+ LA groups were inflicted with about 32% total body surface area deep partial-thickness scald (hereinafter referred to as burn) on the back and right hind...
June 20, 2017: Zhonghua Shao Shang za Zhi, Zhonghua Shaoshang Zazhi, Chinese Journal of Burns
https://www.readbyqxmd.com/read/28345929/utility-of-cyp3a4-and-pxr-car-cyp3a4-3a7-transgenic-mouse-models-to-assess-the-magnitude-of-cyp3a4-mediated-drug-drug-interactions
#3
Justin Q Ly, Kirsten Messick, Ann Qin, Ryan H Takahashi, Edna F Choo
Species differences in the expression, activity, regulation, and substrate specificity of metabolizing enzymes preclude the use of animal models to predict clinical drug-drug interactions (DDIs). The objective of this work is to determine if the transgenic (Tg) Cyp3a(-/-)Tg-3A4Hep/Int and Nr1i2/Nr1i3(-/-)-Cyp3a(-/-)Tg-PXR-CAR-3A4/3A7Hep/Int (PXR-CAR-CYP3A4/3A7) mouse models could be used to predict in vivo DDI of 10 drugs; alprazolam, bosutinib, crizotinib, dasatinib, gefitinib, ibrutinib, regorafenib, sorafenib, triazolam, and vandetinib (as victims); with varying magnitudes of reported CYP3A4 clinical DDI...
April 7, 2017: Molecular Pharmaceutics
https://www.readbyqxmd.com/read/28288398/characterization-of-extended-spectrum-%C3%AE-lactamases-esbls-producing-salmonella-in-retail-raw-chicken-carcasses
#4
Jing Qiao, Qiang Zhang, Walid Q Alali, Jiawei Wang, Lingyuan Meng, Yingping Xiao, Hua Yang, Sheng Chen, Shenghui Cui, Baowei Yang
Extended-spectrum β-lactamases (ESBLs)-producing Salmonella is considered a serious concern to public health worldwide. However, limited information is available on ESBLs-producing Salmonella in retail chicken products in China. The objective of this study was to characterize ESBLs-producing Salmonella isolates from retail chickens in China. A total of 890 Salmonella isolates from retail chicken carcasses collected from 4 provinces were firstly screened for ESBLs-production phenotype via the double-disk synergy test method...
May 2, 2017: International Journal of Food Microbiology
https://www.readbyqxmd.com/read/28177750/modulatory-role-of-co-enzyme-q10-on-methionine-and-choline-deficient-diet-induced-non-alcoholic-steatohepatitis-nash-in-albino-rats
#5
Dalia O Saleh, Rania F Ahmed, Mohamed M Amin
The present study aimed to evaluate the hepato-protective and neuro-protective activity of Co-enzyme Q10 (CoQ10) on non-alcoholic steatohepatitis (NASH) in albino rats induced by methionine and choline-deficient (MCD) diet. Rats were fed an MCD diet for 8 weeks to induce non-alcoholic steatohepatitis. CoQ10 (10 mg/(kg·day)(-1)) was orally administered for 2 consecutive weeks. Twenty-four hours after the last dose of the drug, the behavioral test, namely the activity cage test, was performed and the activity counts were recorded...
March 2017: Applied Physiology, Nutrition, and Metabolism, Physiologie Appliquée, Nutrition et Métabolisme
https://www.readbyqxmd.com/read/28051239/ex-vivo-expansion-of-antigen-specific-cd4-cd25-regulatory-t-cells-from-autologous-na%C3%A3-ve-cd4-t-cells-of-multiple-sclerosis-patients-as-a-potential-therapeutic-approach
#6
Y-J Xiang, M Ren, H Jiang, T-T Yang, Y He, D-H Ao, Y-Y Wang, Q Zhang, X-J He, X-G Gao, G-Z Liu
OBJECTIVE: CD4+CD25+ regulatory T cells (Tregs) have been found to have a decreased effector function in patients with multiple sclerosis (MS). In this study, we co-cultured naïve CD4+ T cells of MS patients with myelin basic protein (MBP)85-99 peptide as specific antigen and allogenic B cells as antigen-presenting cells, in an attempt to generate adequate antigen-specific CD4+CD25+ Tregs with normal or improved immune function. PATIENTS AND METHODS: Naïve CD4+ T cells were isolated from peripheral blood mononuclear cells (PBMCs) from patients with MS (n=5) and healthy controls (HC, n=5)...
December 2016: European Review for Medical and Pharmacological Sciences
https://www.readbyqxmd.com/read/28028033/interventions-for-preventing-cardiomyopathy-due-to-anthracyclines-a-bayesian-network-meta-analysis
#7
H Abdel-Qadir, G Ong, R Fazelzad, E Amir, D S Lee, P Thavendiranathan, G Tomlinson
Background: The relative efficacy of interventions for primary prevention of anthracycline-associated cardiotoxicity is unknown. Methods: We conducted a systematic review of randomized controlled trials for primary prevention of anthracycline-associated cardiotoxicity in adult cancer patients. We used hierarchal outcome definitions in the following order of priority: (1) composite of heart failure or decline in left ventricular ejection fraction, (2) decline in ejection fraction, or (3) heart failure...
March 1, 2017: Annals of Oncology: Official Journal of the European Society for Medical Oncology
https://www.readbyqxmd.com/read/28004656/co-delivery-of-indoleamine-2-3-dioxygenase-prevents-loss-of-expression-of-an-antigenic-transgene-in-dystrophic-mouse-muscles
#8
D Sharma, R Al-Khalidi, S Edgar, Q An, Y Wang, C Young, D Nowis, D C Gorecki
A significant problem affecting gene therapy approaches aiming at achieving long-term transgene expression is the immune response against the protein product of the therapeutic gene, which can reduce or eliminate the therapeutic effect. The problem is further exacerbated when therapy involves targeting an immunogenic tissue and/or one with a pre-existing inflammatory phenotype, such as dystrophic muscles. In this proof-of-principle study, we co-expressed a model antigen, bacterial β-galactosidase, with an immunosuppressive factor, indoleamine 2,3-dioxygenase 1 (IDO1), in muscles of the mdx mouse model of Duchenne muscular dystrophy...
February 2017: Gene Therapy
https://www.readbyqxmd.com/read/27666706/-experimental-study-on-substance-p-in-the-regulation-of-degranulation-of-cultured-murine-mast-cells
#9
F L Cheng, Q T Li, C Q Zhao, Y F An, X P Qi
Objective: To investigate the effect of interleukin-4 (IL-4) stimulation on the expression of FcεRⅠα and NK-1R on mature mast cells(MC) cultured and differentiated from mouse bone marrow stem cells, and then to study if these MC also respond to substance P (SP) both in FcεRⅠα and NK-1R dependent manners. Methods: Bone marrow cells were aseptically flushed from BALB/c mouse femurs into complete RPMI 1640, followed by culture with stem cell factor (SCF 100 μg/L), IL-3 (15 μg/L) and IL-4 (0, 10, 15, 20 and 25 μg/L, respectively)...
September 7, 2016: Zhonghua Er Bi Yan Hou Tou Jing Wai Ke za Zhi, Chinese Journal of Otorhinolaryngology Head and Neck Surgery
https://www.readbyqxmd.com/read/27593931/methyl-cpg-binding-protein-mbd2-plays-a-key-role-in-maintenance-and-spread-of-dna-methylation-at-cpg-islands-and-shores-in-cancer
#10
C Stirzaker, J Z Song, W Ng, Q Du, N J Armstrong, W J Locke, A L Statham, H French, R Pidsley, F Valdes-Mora, E Zotenko, S J Clark
Cancer is characterised by DNA hypermethylation and gene silencing of CpG island-associated promoters, including tumour-suppressor genes. The methyl-CpG-binding domain (MBD) family of proteins bind to methylated DNA and can aid in the mediation of gene silencing through interaction with histone deacetylases and histone methyltransferases. However, the mechanisms responsible for eliciting CpG island hypermethylation in cancer, and the potential role that MBD proteins play in modulation of the methylome remain unclear...
March 2017: Oncogene
https://www.readbyqxmd.com/read/27412900/monosialoganglioside-containing-nanoliposomes-restore-endothelial-function-impaired-by-al-amyloidosis-light-chain-proteins
#11
Daniel A Franco, Seth Truran, Volkmar Weissig, Diana Guzman-Villanueva, Nina Karamanova, Subhadip Senapati, Camelia Burciu, Marina Ramirez-Alvarado, Luis M Blancas-Mejia, Stuart Lindsay, Parameswaran Hari, Raymond Q Migrino
BACKGROUND: Light chain amyloidosis (AL) is associated with high mortality, especially in patients with advanced cardiovascular involvement. It is caused by toxicity of misfolded light chain proteins (LC) in vascular, cardiac, and other tissues. There is no treatment to reverse LC tissue toxicity. We tested the hypothesis that nanoliposomes composed of monosialoganglioside, phosphatidylcholine, and cholesterol (GM1 ganglioside-containing nanoliposomes [NLGM1]) can protect against LC-induced human microvascular dysfunction and assess mechanisms behind the protective effect...
June 13, 2016: Journal of the American Heart Association
https://www.readbyqxmd.com/read/27112133/cloning-purification-and-characterization-of-xylose-isomerase-from-thermotoga-naphthophila-rku-10
#12
Bilqees Fatima, Muhammad Nauman Aftab, Ikram-Ul Haq
A 1.3 kb xyl-A gene encoding xylose isomerase from a hyperthermophilic eubacterium Thermotoga naphthophila RKU-10 (TnapXI) was cloned and over-expressed in Escherichia coli to produce the enzyme in mesophilic conditions that work at high temperature. The enzyme was concentrated by lyophilization and purified by heat treatment, fractional precipitation, and UNOsphere Q anion-exchange column chromatography to homogeneity level. The apparent molecular mass was estimated by SDS-PAGE to be 49.5 kDa. The active enzyme showed a clear zone on Native-PAGE when stained with 2, 3, 5-triphenyltetrazolium chloride...
September 2016: Journal of Basic Microbiology
https://www.readbyqxmd.com/read/26927445/sodium-glucose-co-transporter-2-inhibitors-suppress-atrial-natriuretic-peptide-secretion-in-patients-with-newly-diagnosed-type-2-diabetes
#13
Y Wang, L Xu, L Yuan, D Li, Y Zhang, R Zheng, C Liu, X Feng, Q Li, Q Li, J Ma
AIMS: To observe changes in atrial natriuretic peptide levels after treatment with sodium-glucose co-transporter-2 inhibitors in patients with newly diagnosed type 2 diabetes. METHODS: A total of 28 patients with newly diagnosed Type 2 diabetes and HbA1c levels of 58 -91 mmol/mol (7.5-10.5%) were randomly selected to receive sodium-glucose co-transporter-2 inhibitor treatment (n = 18) or placebo (n = 10) for 24 weeks. We analysed atrial natriuretic peptide concentrations, using an enzyme-linked immunosorbent assay...
December 2016: Diabetic Medicine: a Journal of the British Diabetic Association
https://www.readbyqxmd.com/read/25783971/evidence-of-a-role-for-gtp-cyclohydrolase-1-in-visceral-pain
#14
D C Bulmer, C A Botha, A Wheeldon, K Grey, C A Mein, K Lee, C H Knowles, W J Winchester, Q Aziz
BACKGROUND: The enzyme guanosine triphosphate-cyclohydrolase-1 (GCH-1) is a rate limiting step in the de novo synthesis of tetrahydrobiopterin (BH4) a co-factor in monoamine synthesis and nitric oxide production. GCH-1 is strongly implicated in chronic pain based on data generated using the selective GCH-1 inhibitor 2,4-diamino-6-hydroxypyrimidine (DAHP), and studies which have identified a pain protective GCH-1 haplotype associated with lower BH4 production and reduced pain. METHODS: To investigate the role for GCH-1 in visceral pain we examined the effects of DAHP on pain behaviors elicited by colorectal injection of mustard oil in rats, and the pain protective GCH-1 haplotype in healthy volunteers characterized by esophageal pain sensitivity before and after acid injury, and assessed using depression and anxiety questionnaires...
May 2015: Neurogastroenterology and Motility: the Official Journal of the European Gastrointestinal Motility Society
https://www.readbyqxmd.com/read/25783038/metabolic-phenotype-microrna-data-fusion-analysis-of-the-systemic-consequences-of-roux-en-y-gastric-bypass-surgery
#15
Q Wu, J V Li, F Seyfried, C W le Roux, H Ashrafian, T Athanasiou, W Fenske, A Darzi, J K Nicholson, E Holmes, N J Gooderham
BACKGROUND/OBJECTIVES: Bariatric surgery offers sustained marked weight loss and often remission of type 2 diabetes, yet the mechanisms of establishment of these health benefits are not clear. SUBJECTS/METHODS: We mapped the coordinated systemic responses of gut hormones, the circulating miRNAome and the metabolome in a rat model of Roux-en-Y gastric bypass (RYGB) surgery. RESULTS: The response of circulating microRNAs (miRNAs) to RYGB was striking and selective...
July 2015: International Journal of Obesity: Journal of the International Association for the Study of Obesity
https://www.readbyqxmd.com/read/25510509/cortical-fast-spiking-parvalbumin-interneurons-enwrapped-in-the-perineuronal-net-express-the-metallopeptidases-adamts8-adamts15-and-neprilysin
#16
J Rossier, A Bernard, J-H Cabungcal, Q Perrenoud, A Savoye, T Gallopin, M Hawrylycz, M Cuénod, K Do, A Urban, Ed S Lein
The in situ hybridization Allen Mouse Brain Atlas was mined for proteases expressed in the somatosensory cerebral cortex. Among the 480 genes coding for protease/peptidases, only four were found enriched in cortical interneurons: Reln coding for reelin; Adamts8 and Adamts15 belonging to the class of metzincin proteases involved in reshaping the perineuronal net (PNN) and Mme encoding for Neprilysin, the enzyme degrading amyloid β-peptides. The pattern of expression of metalloproteases (MPs) was analyzed by single-cell reverse transcriptase multiplex PCR after patch clamp and was compared with the expression of 10 canonical interneurons markers and 12 additional genes from the Allen Atlas...
February 2015: Molecular Psychiatry
https://www.readbyqxmd.com/read/25273816/gene-cloning-and-enzymatic-characterization-of-alkali-tolerant-type-i-pullulanase-from-exiguobacterium-acetylicum
#17
Y Qiao, Q Peng, J Yan, H Wang, H Ding, B Shi
UNLABELLED: A pullulanase gene (Pul3YH5) of 2568 bp, which encodes a protein containing 855 amino acid residues, was cloned from the alkaliphilic bacterium Exiguobacterium acetylicum YH5. The pullulanase (Pul3YH5) contains the YNWGYDP motif of type I pullulanase as well as four conserved glycoside hydrolase sequences of the GH13 (α-amylase) family. When the pullulanase gene was cloned and expressed in Escherichia coli BL21 (DE3) plysS, the recombinant pullulanase had a molecular mass of ˜100·0 kDa...
January 2015: Letters in Applied Microbiology
https://www.readbyqxmd.com/read/24690287/purification-and-characterization-of-%C3%AE-amylase-from-miswak-salvadora-persica
#18
Saleh A Mohamed, Yaaser Q Almulaiky, Youssri M Ahmed, Omar A M Al-Bar, Ibrahim H Ibrahim
BACKGROUND: The miswak (Salvadora persica) is a natural toothbrush. It is well known that very little information has been reported on enzymes in miswak as medicinal plant. Recently, we study peroxidase in miswak. In the present study, the main goal of this work is to purify and characterize α-amylase from miswak. The second goal is to study the storage stability of α-amylase in toothpaste. METHOD: The purification method included chromatography of miswak α-amylase on DEAE-Sepharose column and Sephacryl S-200 column...
2014: BMC Complementary and Alternative Medicine
https://www.readbyqxmd.com/read/24489336/a8-31-characterisation-of-human-transitional-b-cells-though-their-regulatory-functions
#19
S Hillion, Q Simon, C Jamin, Y Renaudineau, J O Pers
Transitional B cells represent a cortical link between the initial B cell compartment in bone marrow and the mature peripheral B cell repertoire. The prior characterisation of human transitional B-cells has suggested that this population could be subdivised into two major subsets: the immature T1-Bcells CD19(+) CD10high CD24high CD38high IgMhigh IgDlow CD21low and tne intermediate cells mentionned as T2-B cells CD19(+) CD10 + CD24high CD38high IgMhigh IgDhigh CD21high. Recently B-cell regulation have been shed in light and a lot of evidences suggested that regulatory B cells (Bregs) are contained within the CD24high CD38high transitional B-cell subsets...
March 1, 2014: Annals of the Rheumatic Diseases
https://www.readbyqxmd.com/read/24426207/hematological-parameters-and-rbc-tbars-level-of-q-10-supplemented-tribal-sickle-cell-patients-a-hospital-based-study
#20
A S Thakur, G P Littaru, S Moesgaard, C Dan Sindberg, Y Khan, C M Singh
The study has been undertaken as number of sickle cell patients in Chhattisgarh tribal population is 23.7 %. The Co enzyme Q10 is a strong antioxidant and energy producing compound. The patients were divided into three groups group A homozygous (SS), group B heterozygous (AS) and group C controls for TBARS study. The age group is 10-55 years and 200 mg of CoQ10 was given to A and B groups. The hematological parameters, C reactive protein as well as RBC TBARS level were performed by usual and standard techniques...
April 2013: Indian Journal of Clinical Biochemistry: IJCB
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