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https://www.readbyqxmd.com/read/28445001/inhibition-properties-of-some-flavonoids-on-carbonic-anhydrase-i-and-ii-isoenzymes-purified-from-human-erythrocytes
#1
Zübeyir Huyut, Şükrü Beydemir, İlhami Gülçin
Carbonic anhydrases (CAs, E.C.4.2.1.1) play a critical role in many important physiological events and treatment of some diseases. Flavonoids or phenolic compounds have been discovered as novel CAs inhibitors instead of the traditional sulfonamides, with different binding to CAs, pro-drug activities, and new inhibition mechanisms. Here, we investigated the inhibition effects of some flavonoids including malvin, callistephin, oenin, pelargonin, silychristin, and 1-(4-methoxyphenyl)-2-methyl-3-nitro-1-H-indol-6-ol (ID-8) against hCA I and II, which purified from human erythrocytes by affinity column chromatography...
April 26, 2017: Journal of Biochemical and Molecular Toxicology
https://www.readbyqxmd.com/read/28443928/a-new-four-component-reaction-involving-the-michael-addition-and-the-gewald-reaction-leading-to-diverse-biologically-active-2-aminothiophenes
#2
Joice Thomas, Sampad Jana, Mahendra Sonawane, Bert Fiey, Jan Balzarini, Sandra Liekens, Wim Dehaen
The Gewald three-component reaction yielding highly substituted 2-aminothiophene heterocycles has been known for a long time and holds an extraordinary potential in the pharmaceutical industry. Herein, we describe a four-component reaction initiated by the conjugate addition of different indole derivatives to α,β-unsaturated carbonyl compounds. This is followed by an in situ Gewald three-component reaction which results in the formation of a compound containing an indole and a 2-aminothiophene moiety separated by a methylene spacer...
April 26, 2017: Organic & Biomolecular Chemistry
https://www.readbyqxmd.com/read/28443502/fe3o4-sio2-kit-6-as-an-efficient-and-reusable-catalyst-for-the-synthesis-of-novel-derivatives-of-3-3-aryl-1-phenyl-1h-pyrazol-4-yl-methylene-bis-1h-indole
#3
Mohammad Nikpassand, Leila Zare Fekri, Mozhdeh Nabatzadeh
Korea advanced institute of science and technology cubic ordered mesoporous silica (KIT-6 mesoporous) silica coated magnetite nanoparticles, is an effective, eco-benign and recyclable catalyst for the electrophilic substitution reactions of indoles with various synthetized aldehydes to afford the corresponding novel diindolylmethanes in high yields and short reaction times. The catalyst can be recovered and reused without loss of activity. The work-up of the reaction consists of a simple separation, followed by concentration of the crude product and purification...
April 25, 2017: Combinatorial Chemistry & High Throughput Screening
https://www.readbyqxmd.com/read/28443122/membrane-proteomics-of-arabidopsis-glucosinolate-mutants-cyp79b2-b3-and-myb28-29
#4
Islam Mostafa, Mi-Jeong Yoo, Ning Zhu, Sisi Geng, Craig Dufresne, Maged Abou-Hashem, Maher El-Domiaty, Sixue Chen
Glucosinolates (Gls) constitute a major group of natural metabolites represented by three major classes (aliphatic, indolic and aromatic) of more than 120 chemical structures. In our previous work, soluble proteins and metabolites in Arabidopsis mutants deficient of aliphatic (myb28/29) and indolic Gls (cyp79B2B3) were analyzed. Here we focus on investigating the changes at the level of membrane proteins in these mutants. Our LC/MS-MS analyses of tandem mass tag (TMT) labeled peptides derived from the cyp79B2/B3 and myb28/29 relative to wild type resulted in the identification of 4,673 proteins, from which 2,171 are membrane proteins...
2017: Frontiers in Plant Science
https://www.readbyqxmd.com/read/28442937/simultaneous-administration-of-fluoxetine-and-simvastatin-ameliorates-lipid-profile-improves-brain-level-of-neurotransmitters-and-increases-bioavailability-of-simvastatin
#5
Abdulrahman K Al-Asmari, Zabih Ullah, Aqeel Salman Al Masoudi, Ishtiaque Ahmad
Simvastatin (STT), a 3-hydroxy-3-methylglutaryl coenzyme A reductase inhibitor, is widely prescribed for dyslipidemia, whereas fluoxetine (FLX) is the first-choice drug for the treatment of depression and anxiety. A recent report suggests that selective serotonin reuptake inhibitors can interact with the cytochrome P450 3A4 substrate, and another one suggests that STT enhances the antidepressant activity of FLX. However, the data are inconclusive. The present study was designed to explore the pharmacokinetic and pharmacodynamic consequences of coadministration of STT and FLX in experimental animals...
2017: Journal of Experimental Pharmacology
https://www.readbyqxmd.com/read/28442131/multipoint-recognition-of-domoic-acid-from-seawater-by-dummy-template-molecularly-imprinted-solid-phase-extraction-coupled-with-high-performance-liquid-chromatography
#6
Xiuping He, Jianlei Chen, Jiangtao Wang, Liju Tan
Due to the high cost of domoic acid (DA), different carboxylic acid compounds including indole-3-acetic acid (IAA), pyrrole-2-formic acid (PFA), pyridine-2,3-dicarboxylic anhydride (PDA), trimesitinic acid (TA) and citric acid (CA) were investigated as dummy templates for the molecularly imprinted solid-phase extraction (MISPE) for selective isolation and pre-concentration of an amnesic shellfish poison (ASP), DA. The highest binding amount of the polymers towards DA was obtained when CA was used as dummy template owing to its high hydrophilicity...
April 13, 2017: Journal of Chromatography. A
https://www.readbyqxmd.com/read/28441581/design-combinatorial-synthesis-and-biological-evaluations-of-novel-3-amino-1-1-aryl-1h-1-2-3-triazol-5-yl-methyl-2-oxospiro-benzo-a-pyrano-2-3-c-phenazine-1-3-indoline-2-carbonitrile-antitumor-hybrid-molecules
#7
Yuanyuan Lu, Linlin Wang, Xiaobing Wang, Tao Xi, Jianmin Liao, Zhixiang Wang, Feng Jiang
A combinatorial chemical library of fifty-nine novel 3-amino-1'-((1-aryl-1H-1,2,3-triazol-5-yl)methyl)-2'-oxospiro[benzo[a]pyrano[2,3-c]phenazine-1,3'-indoline]-2-carbonitrile, designed as hybrid molecules of phenazine, pyran, indole and 1,2,3-triazole pharmacophores, were constructed in this study. Cytotoxic evaluation indicated that some compounds exhibited moderate cytotoxicity against HCT116, MCF7, HepG2 and A549 cancer cell lines in vitro, in which compound 36 was found to have best antiproliferative activity against the A549 cancer cell line with IC50 value of 5...
April 18, 2017: European Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/28441364/indole-derivatives-produced-by-the-metagenome-genes-of-the-escherichia-coli-harboring-marine-sponge-discodermia-calyx
#8
Feng-Lou Liu, Xiao-Long Yang
Three indole derivatives, a novel benzoxazine-indole hybrid (1) and two known indole trimers (2, 3), were isolated from the metagenomic library of the marine sponge Discodermia calyx based on functional screening. Their structures were elucidated by extensive spectroscopic analysis and comparison of their NMR data to that of known compounds. The antibacterial assay indicated that only compound 2 displayed significant antibacterial activity against Bacillus cereus, with approximately 20 mm diameter growth inhibition at 10 µg/paper...
April 25, 2017: Molecules: a Journal of Synthetic Chemistry and Natural Product Chemistry
https://www.readbyqxmd.com/read/28440700/selection-and-assessment-of-plant-growth-promoting-rhizobacteria-pgpr-for-biological-control-of-multiple-plant-diseases
#9
Ke Liu, Molli Newman, John A McInroy, Chia-Hui Hu, Joseph W Kloepper
A study was designed to screen individual strains of plant growth-promoting rhizobacteria (PGPR) for broad-spectrum disease suppression in vitro and in planta. In a preliminary screen, 28 of 196 strains inhibited eight different tested pathogens in vitro. In a secondary screen, these 28 strains showed broad spectrum antagonistic activity to six different genera of pathogens, and 24 of the 28 strains produced five traits reported to be related to plant growth promotion, including nitrogen fixation, phosphate solubilization, indole-3-acetic acid (IAA) production, siderophore production, and biofilm formation...
April 25, 2017: Phytopathology
https://www.readbyqxmd.com/read/28440656/heteroannulation-of-3-nitroindoles-and-3-nitrobenzo-b-thiophenes-a-multicomponent-approach-toward-pyrrole-fused-heterocycles
#10
P V Santhini, Sheba Ann Babu, Akhil Krishnan R, E Suresh, Jubi John
A simple, efficient, and general multicomponent reaction involving an enolizable ketone, a primary amine, and an N-protected 3-nitroindole was developed for the synthesis of a range of functionalized pyrrolo[3,2-b]indoles. The methodology was efficaciously utilized for the "pyrroloindoliztion" of natural products, the pyrrolization of 3-nitrobenzo[b]thiophene, and the gram-scale synthesis of pyrroloindole. Furthermore, a "one-pot" approach for accessing indolo[3,2-b]indoles was realized.
April 25, 2017: Organic Letters
https://www.readbyqxmd.com/read/28440569/toxicity-of-silver-nanoparticles-to-arabidopsis-inhibition-of-root-gravitropism-by-interfering-with-auxin-pathway
#11
Juzhi Sun, Likai Wang, Shuang Li, Liyan Yin, Jin Huang, Chunli Chen
Impacts of polyvinylpyrrolidine-coated silver nanoparticles (PVP-AgNPs) on root gravitropism in Arabidopsis thaliana were investigated at physiological, cellular and molecular level. Our results showed that AgNPs were taken up by the root and primarily localized at the cell wall and intercellular spaces. The root gravitropism was inhibited by exposure to AgNPs, and the inhibitions in root gravitropism caused by exposure to AgNPs exhibited a dose-response relationship. Auxin accumulation was reduced in the root tips due to exposure to AgNPs...
April 25, 2017: Environmental Toxicology and Chemistry
https://www.readbyqxmd.com/read/28440325/multiparametric-mri-ultrasound-fusion-guided-biopsy-decreases-detection-of-indolent-cancer-in-african-american-men
#12
M Kongnyuy, M M Siddiqui, A K George, A Muthigi, A Sidana, M Maruf, B Turkbey, P L Choyke, B J Wood, P A Pinto
BACKGROUND: Analysis of systematic 12-core biopsies (SBx) has shown that African-American (AA) men tend to harbor higher risk prostate cancer (PCa) at presentation relative to other races. Multiparametric magnetic resonance imaging (mpMRI) and MRI-ultrasound fusion-guided biopsy (FBx) have been shown to diagnose more intermediate- and high-risk PCa in the general population; however, the efficacy in AA remains largely uncharacterized. We aim to evaluate the utility of FBx in an AA patient cohort...
April 25, 2017: Prostate Cancer and Prostatic Diseases
https://www.readbyqxmd.com/read/28439797/desmoid-type-fibromatosis-who-when-and-how-to-treat
#13
REVIEW
Javier Martínez Trufero, Isabel Pajares Bernad, Irene Torres Ramón, Jorge Hernando Cubero, Roberto Pazo Cid
Desmoid-type fibromatosis is a sarcoma subtype that gathers some singular characteristics, making it a difficult challenge to face in clinical practice. Despite its excellent survival prognosis, these tumors may be unpredictable, ranging from an asymptomatic indolent course to persistent, local, and extended recurrences that significantly impair quality of life. Although surgery was initially considered the first elective treatment, collected published data during the past few years are now pointing to the "wait and see" approach as a reasonable initial strategy because many patients can live a long life with the disease without having symptoms...
May 2017: Current Treatment Options in Oncology
https://www.readbyqxmd.com/read/28439288/systemic-mastocytosis-with-kit-v560g-mutation-presenting-as-recurrent-episodes-of-vascular-collapse-response-to-disodium-cromoglycate-and-disease-outcome
#14
Iolanda Conde-Fernandes, Rita Sampaio, Filipa Moreno, José Palla-Garcia, Maria Dos Anjos Teixeira, Inês Freitas, Esmeralda Neves, Maria Jara-Acevedo, Luis Escribano, Margarida Lima
BACKGROUND: Mastocytosis are rare diseases characterized by an accumulation of clonal mast cells (MCs) in one or multiple organs or tissues. Patients with systemic mastocytosis (SM), whose MCs frequently arbor the activating D816V KIT mutation, may have indolent to aggressive diseases, and they may experience MC mediator related symptoms. Indolent SM with recurrent anaphylaxis or vascular collapse in the absence of skin lesions, ISMs(-), is a specific subtype indolent SM (ISM), and this clonal MC activation disorder represents a significant fraction of all MC activation syndromes...
2017: Allergy, Asthma, and Clinical Immunology
https://www.readbyqxmd.com/read/28438627/atypical-small-acinar-proliferation-and-high-grade-prostatic-intraepithelial-neoplasia-in-the-era-of-multi-parametric-mri-a-contemporary-review
#15
REVIEW
Todd G Manning, Ernest Cheung, Marlon Perera, Daniel Christidis, Jonathan S O'Brien, Catherine Mitchell, Damien M Bolton, Nathan Lawrentschuk
Multiparametric Magnetic Resonance Imaging (mpMRI) has added to the armamentarium for the diagnosis and surveillance for organ confined prostate cancer. Atypical small acinar proliferation (ASAP) and high-grade prostatic intraepithelial neoplasia (HGPIN) are premalignant prostatic lesions. The management of such lesions remains contentious, and the addition of mpMRI introduces further uncertainty given its ability to pick up indolent lesions and its use in targeted biopsy. We aimed to perform a comprehensive review of current evidence regarding ASAP, HGPIN and mpMRI to ascertain a consensus for a current management algorithm...
April 21, 2017: Urology
https://www.readbyqxmd.com/read/28438317/a-novel-chromatographic-approach-to-distinguish-gram-positive-from-gram-negative-bacteria-using-exogenous-volatile-organic-compound-metabolites
#16
Susana Ramírez-Guízar, Hannah Sykes, John D Perry, Edward C Schwalbe, Stephen P Stanforth, Ma Cristina I Perez-Perez, John R Dean
This paper utilized L-alanine aminopeptidase activity as a useful approach to distinguish between Gram-negative and Gram-positive bacteria. This was done using two enzyme substrates, specifically 2-amino-N-phenylpropanamide and 2-amino-N-(4-methylphenyl)propanamide which liberated the volatile compounds aniline and p-toluidine, respectively. Two complementary analytical techniques have been used to identify and quantify the VOCs, specifically static headspace multicapillary column gas chromatography ion mobility spectrometry (SHS-MCC-GC-IMS) and headspace solid phase microextraction gas chromatography mass spectrometry (HS-SPME-GC-MS)...
April 12, 2017: Journal of Chromatography. A
https://www.readbyqxmd.com/read/28438086/feline-leprosy-due-to-candidatus-mycobacterium-tarwinense
#17
Carolyn R O'Brien, Richard Malik, Maria Globan, George Reppas, Christina McCowan, Janet A Fyfe
OBJECTIVES: This paper, the first in a series of three on 'feline leprosy', provides a detailed description of disease referable to Candidatus 'Mycobacterium tarwinense', the most common cause of feline leprosy in Victoria, Australia. METHODS: Cases were sourced retrospectively and prospectively for this observational study, describing clinical, geographical and molecular microbiological data for cats definitively diagnosed with Candidatus 'M tarwinense' infection...
May 2017: Journal of Feline Medicine and Surgery
https://www.readbyqxmd.com/read/28437705/both-heavy-metal-amendment-of-soil-and-aphid-infestation-increase-cd-and-zn-concentrations-in-phloem-exudates-of-a-metal-hyperaccumulating-plant
#18
Clemens Stolpe, Franziska Giehren, Ute Krämer, Caroline Müller
Plants that are able to hyperaccumulate heavy metals show increased concentrations of these metals in their leaf tissue. However, little is known about the concentrations of heavy metals and of organic defence metabolites in the phloem sap of these plants in response to either heavy metal-amendment of the soil or biotic challenges such as aphid-infestation. In this study, we investigated the effects of heavy metal-exposure and of aphid-infestation on phloem exudate composition of the metal hyperaccumulator species Arabidopsis halleri L...
April 21, 2017: Phytochemistry
https://www.readbyqxmd.com/read/28437060/high-throughput-and-quantitative-measurement-of-microbial-metabolome-by-gas-chromatography-mass-spectrometry-using-automated-alkyl-chloroformate-derivatization
#19
Linjing Zhao, Yan Ni, Mingming Su, Hongsen Li, Fangcong Dong, Wenlian Chen, Runmin Wei, Lulu Zhang, Seu-Ping Guiraud, François-Pierre J Martin, Cynthia Rajani, Guoxiang Xie, Wei Jia
The ability to identify and quantify small molecule metabolites derived from gut microbial-mammalian co-metabolism is essential for the understanding of the distinct metabolic functions of the microbiome. To date, analytical protocols that quantitatively measure a complete panel of microbial metabolites in biological samples have not been established, but urgently needed by the microbiome research community. Here, we report an automated high-throughput quantitative method using a gas chromatography/time-of-flight mass spectrometry (GC/TOFMS) platform to simultaneously measure over one hundred microbial metabolites in human serum, urine, feces and Escherichia coli cell samples within 15 minutes per sample...
April 24, 2017: Analytical Chemistry
https://www.readbyqxmd.com/read/28436173/relationship-between-endobronchial-ultrasound-guided-ebus-transbronchial-needle-aspiration-utility-and-computed-tomography-staging-node-size-at-ebus-and-positron-emission-tomography-scan-node-standard-uptake-values-a-retrospective-analysis
#20
Clare Marchand, Andrew R L Medford
BACKGROUND: Endobronchial ultrasound-guided transbronchial needle aspiration (EBUS-TBNA) diagnoses and stages mediastinal lymph node pathology. This retrospective study determined the relationship between EBUS-TBNA utility and non-small cell lung cancer (NSCLC) stage, lymph node size, and positron emission tomography (PET) standard uptake values (SUV), and the utility of neck ultrasound in bulky mediastinal disease. METHODS: Data of 284 consecutive patients who had undergone EBUS-TBNA was collected...
April 24, 2017: Thoracic Cancer
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