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https://www.readbyqxmd.com/read/29236214/neural-network-modeling-of-ache-inhibition-by-new-carbazole-bearing-oxazolones
#1
Levent Cavas, Gamze Topcam, Cevher Gundogdu-Hizliates, Yavuz Ergun
Acetylcholine esterase (AChE) is one of the targeted enzymes in the therapy of important neurodegenerative diseases such as Alzheimer's disease. Many studies on carbazole- and oxazolone-based compounds have been conducted in the last decade due to the importance of these compounds. New carbazole-bearing oxazolones were synthesized from several carbazole aldehydes and p-nitrobenzoyl glycine as AChE inhibitors by the Erlenmeyer reaction in the present study. The inhibitory effects of three carbazole-bearing oxazolone derivatives on AChE were studied in vitro and the experimental results were modeled using artificial neural network (ANN)...
December 13, 2017: Interdisciplinary Sciences, Computational Life Sciences
https://www.readbyqxmd.com/read/29225517/intestinally-restricted-janus-kinase-inhibition-a-potential-approach-to-maximize-the-therapeutic-index-in-inflammatory-bowel-disease-therapy
#2
David T Beattie, M Teresa Pulido-Rios, Fei Shen, Melissa Ho, Eva Situ, Pam R Tsuruda, Patrick Brassil, Melanie Kleinschek, Sharath Hegde
Background: An unmet need remains for safe and effective treatments to induce and maintain remission in inflammatory bowel disease (IBD) patients. The Janus kinase (JAK) inhibitor, tofacitinib, has demonstrated robust efficacy in ulcerative colitis patients although, like other systemic immunosuppressants, there may be safety concerns associated with its use. This preclinical study evaluated whether modulating intestinal inflammation via local JAK inhibition can provide efficacy without systemic immunosuppression...
2017: Journal of Inflammation
https://www.readbyqxmd.com/read/29206209/dioscorea-quinqueloba-ameliorates-oxazolone-and-2-4-dinitrochlorobenzene-induced-atopic-dermatitis-symptoms-in-murine-models
#3
Jonghwan Jegal, No-June Park, Sim-Kyu Bong, Hyun Jegal, Su-Nam Kim, Min Hye Yang
Dioscorea quinqueloba has been used for food substances, as well as in herbal medicines for allergic diseases such as asthma. This study aimed to investigate the anti-atopic dermatitis (AD) effects of the total extract of D. quinqueloba rhizomes and active fractionson murine oxazolone- and 2,4-dinitrochlorobenzene-induced models of AD. Specific AD symptoms, such as erythema, ear swelling, and epidermis thickening, were significantly reduced in the oxazolone-mediated AD BALB/c mice upon topical application of D...
December 5, 2017: Nutrients
https://www.readbyqxmd.com/read/29205369/regulatory-b-cells-induced-by-ultraviolet-b-through-toll-like-receptor-4-signalling-contribute-to-the-suppression-of-contact-hypersensitivity-responses-in-mice
#4
Xiaoming Liu, Haiyan Huang, Hongbin Gao, Xia Wu, Wei Zhang, Bo Yu, Xia Dou
BACKGROUND: Ultraviolet (UV) B irradiation is known to suppress contact hypersensitivity (CHS) responses in mouse models by suppressing immune responses. However, the cellular mechanisms responsible for UVB-induced systemic suppression remain unclear. Regulatory B cells have been reported to play an inhibitory role during CHS. It is presently unknown whether regulatory B cells contribute to the effect of UVB phototherapy. OBJECTIVE: To investigate the inductive effect of UVB on regulatory B cells and the underlying mechanisms by using a CHS mouse model...
December 5, 2017: Contact Dermatitis
https://www.readbyqxmd.com/read/29156380/structure-based-design-of-herg-neutral-antihypertensive-oxazalone-and-imidazolone-derivatives
#5
Busecan Aksoydan, Isik Kantarcioglu, Ismail Erol, Ramin Ekhteiari Salmas, Serdar Durdagi
Angiotensin II receptor type 1 (AT1) antagonists are the most recent drug class against hypertension. Recently first crystal structure of AT1 receptor is deposited to the protein data bank (PDB ID: 4YAY). In this work, several molecular screening methods such as molecular docking and de novo design studies were performed and it is found that oxazolone and imidazolone derivatives reveal similar/better interaction energy profiles compared to the FDA approved sartan molecules at the binding site of the AT1 receptor...
October 18, 2017: Journal of Molecular Graphics & Modelling
https://www.readbyqxmd.com/read/29116551/anti-inflammatory-effect-of-a-novel-locally-acting-a2a-receptor-agonist-in-a-rat-model-of-oxazolone-induced-colitis
#6
L Antonioli, A El-Tayeb, C Pellegrini, M Fornai, O Awwad, G Giustarini, G Natale, L Ryskalin, Z H Németh, C E Müller, C Blandizzi, R Colucci
Adenosine represents a powerful modulating factor, which has been shown to orchestrate the scope, duration, and remission of the inflammatory response through the activation of four specific receptors, classified as A1, A2A, A2B, and A3, all being widely expressed in a variety of immune cells. Several selective A2A receptor agonists have displayed anti-inflammatory effects, through the suppression of IL-12, TNF, and IFN-γ production by monocytes and lymphocytes, in the setting of chronic intestinal inflammation...
November 8, 2017: Purinergic Signalling
https://www.readbyqxmd.com/read/29057517/the-indane-diastereoisomers-ph2-and-ph5-divergence-between-their-effects-in-delayed-type-hypersensitivity-models-and-a-model-of-colitis
#7
Neil H Frankish, Brendan McHale, Helen Sheridan
OBJECTIVES: Compounds PH2 and PH5 are distereoisomers of novel indane compounds, synthesised as analogues of secondary metabolites of the fern, Onychium. In this study, we compare their effects on a variety of inflammatory models. METHODS: In an effort to extend our knowledge of their anti-inflammatory profile, we have investigated their activity in two models of delayed-type hypersensitivity (DTH); the methylated bovine serum albumin model (mBSA) and the oxazolone contact hypersensitivity (CHS) model, on IL2 release from Jurkat cells and in the dextran sulphate sodium (DSS) murine model of inflammatory bowel disease...
October 23, 2017: Journal of Pharmacy and Pharmacology
https://www.readbyqxmd.com/read/29049008/exogenous-murine-antimicrobial-peptide-cramp-significantly-exacerbates-ovalbumin-induced-airway-inflammation-but-ameliorates-oxazolone-induced-intestinal-colitis-in-balb-c-mice
#8
Yang Li, Xiaojie Chu, Cunbao Liu, Weiwei Huang, Yufeng Yao, Ye Xia, Pengyan Sun, Qiong Long, Xuejun Feng, Kui Li, Xu Yang, Hongmei Bai, Wenjia Sun, Yanbing Ma
Cathelicidin has been reported to be multifunctional. The current study aimed to investigate the influences of exogenous cathelicidin-related antimicrobial peptide (CRAMP) on inflammatory responses in different disease models. In OVA-induced allergic airway inflammation, CRAMP significantly enhanced the infiltration of inflammatory cells and accumulation of proinflammatory Th2 cytokine IL-13 and IL-33 in bronchial alveolar lavage fluid (BALF), exacerbated lung tissue inflammation and airway goblet cell hyperplasia, and elevated OVA-specific IgE level in serum...
October 19, 2017: Human Vaccines & Immunotherapeutics
https://www.readbyqxmd.com/read/29043360/synthesis-photophysical-and-biological-properties-of-a-new-oxazolone-fluorescent-probe-for-bioimaging-an-experimental-and-theoretical-study
#9
Przemysław Krawczyk, Beata Jędrzejewska, Piotr Cysewski, Tomasz Janek
In this study, a new oxazolone derivative 4-{N,N-bis[2-phenyl-4-benzylidene-1,3-oxazol-5(4H)-one]amino}benzaldehyde (PB3) was synthesized and investigated as a fluorescent dye. The spectroscopic properties in different solvents were thoroughly studied. The experimental data were supported by quantum-chemical calculations using density functional theory. Measurements and theoretical calculations showed that the PB3 dye is characterized by non-monotonic solvatochromism, a strongly polar charge transfer excited state, a large Stokes' shift, a high fluorescence quantum yield and a high fluorescence lifetime...
October 31, 2017: Organic & Biomolecular Chemistry
https://www.readbyqxmd.com/read/28962179/evaluation-of-hyaluronic-acid-p40-conjugated-cream-in-a-mouse-model-of-dermatitis-induced-by-oxazolone
#10
Katia Mangano, Franca Vergalito, Santa Mammana, Andrea Mariano, Rocco De Pasquale, Antonia Meloscia, Silvia Bartollino, Germano Guerra, Ferdinando Nicoletti, Roberto Di Marco
P40 is a particulate fraction or fragment isolated from Corynebacterium granulosum, which exhibits a wide spectrum of pharmacological functions including antitumor, antibacterial, phagocytic, antiviral and cytokine induction effects. In the present study, the immunomodulatory potential of P40-conjugated with hyaluronic acid was assessed in a mouse model of dermatitis induced by oxazolone. Oxazolone-induced allergic contact dermatitis is a T cell-mediated Th2-like hypersensitivity reaction, which mimics the corresponding reaction in humans...
September 2017: Experimental and Therapeutic Medicine
https://www.readbyqxmd.com/read/28957753/structure-based-design-of-herg-neutral-antihypertensive-oxazalone-and-imidazolone-derivatives
#11
Busecan Aksoydan, Isik Kantarcioglu, Ismail Erol, Ramin Ekhteiari Salmas, Serdar Durdagi
Angiotensin II receptor type 1 (AT1) antagonists are the most recent drug class against hypertension. Recently first crystal structure of AT1 receptor is deposited to the protein data bank (PDB ID: 4YAY). In this work, several molecular screening methods such as molecular docking and de novo design studies were performed and it is found that oxazolone and imidazolone derivatives reveal similar/better interaction energy profiles compared to the FDA approved sartan molecules at the binding site of the AT1 receptor...
August 12, 2017: Journal of Molecular Graphics & Modelling
https://www.readbyqxmd.com/read/28912045/sulfate-reducing-bacteria-stimulate-gut-immune-responses-and-contribute-to-inflammation-in-experimental-colitis
#12
Vanessa Ribeiro Figliuolo, Liliane Martins Dos Santos, Alessandra Abalo, Hayandra Nanini, Angela Santos, Nilda M Brittes, Claudio Bernardazzi, Heitor Siffert Pereira de Souza, Leda Quercia Vieira, Robson Coutinho-Silva, Claudia Mara Lara Melo Coutinho
The intestinal microbiota is critical for mammalian immune system development and homeostasis. Sulfate-reducing bacteria (SRB) are part of the normal gut microbiota, but their increased levels may contribute to colitis development, likely in association with hydrogen sulfide (H2S) production. Here, we investigated the effects of SRB in the gut immune response in germ-free mice, and in experimental colitis. After 7days of colonization with Desulfovibrio indonesiensis or with a human SRB consortium (from patients with colitis), germ-free mice exhibited alterations in the colonic architecture, with increased cell infiltration in the lamina propria...
November 15, 2017: Life Sciences
https://www.readbyqxmd.com/read/28892206/il-33-and-ige-stimulate-mast-cell-production-of-il-2-and-regulatory-t-cell-expansion-in-allergic-dermatitis
#13
P Salamon, I Shefler, I Moshkovits, A Munitz, D Horwitz Klotzman, Y A Mekori, A Y Hershko
BACKGROUND: We have previously shown that mast cells (MCs) suppress chronic allergic dermatitis in mice. The underlying mechanism involves MC-derived IL-2, which supports regulatory T cell (Treg) response at the site of inflammation. However, it is not clear what are the factors that drive MCs to produce IL-2. OBJECTIVE: To understand the mechanisms that lead to IL-2 production from MCs in chronic allergic dermatitis. METHODS: Isolated murine bone marrow-derived MCs (BMMCs) were incubated with various stimulators, and IL-2 production was assessed by RT-PCR and ELISA...
November 2017: Clinical and Experimental Allergy: Journal of the British Society for Allergy and Clinical Immunology
https://www.readbyqxmd.com/read/28862441/reaction-of-ynamides-with-iminoiodinane-derived-nitrenes-formation-of-oxazolones-and-polyfunctionalized-oxazolidinones
#14
Romain Rey-Rodriguez, Gwendal Grelier, Loïc Habert, Pascal Retailleau, Benjamin Darses, Isabelle Gillaizeau, Philippe Dauban
This article describes the reaction of ynamides with metallanitrenes generated in the presence of an iodine(III) oxidant. N-(Boc)-Ynamides are converted to oxazolones via a cyclization reaction. The reaction is mediated by a catalytic dirhodium-bound nitrene species that first behaves as a Lewis acid. The oxazolones can be converted in a one pot manner to functionalized oxazolidinones following a regio- and stereoselective oxyamination reaction with the same nitrene reagent generated in stoichiometric amounts...
September 1, 2017: Journal of Organic Chemistry
https://www.readbyqxmd.com/read/28842393/e6130-a-novel-cx3c-chemokine-receptor-1-cx3cr1-modulator-attenuates-mucosal-inflammation-and-reduces-cx3cr1-leukocyte-trafficking-in-mice-with-colitis
#15
Hisashi Wakita, Tatsuya Yanagawa, Yoshikazu Kuboi, Toshio Imai
The chemokine fractalkine (CX3C chemokine ligand 1; CX3CL1) and its receptor CX3CR1 are involved in the pathogenesis of several diseases, including inflammatory bowel diseases such as Crohn's disease and ulcerative colitis, rheumatoid arthritis, hepatitis, myositis, multiple sclerosis, renal ischemia, and atherosclerosis. There are no orally available agents that modulate the fractalkine/CX3CR1 axis. [(3S,4R)-1-[2-Chloro-6-(trifluoromethyl)benzyl]-3-{[1-(cyclohex-1-en-1-ylmethyl)piperidin-4-yl]carbamoyl}-4-methylpyrrolidin-3-yl]acetic acid (2S)-hydroxy(phenyl)acetate (E6130) is an orally available highly selective modulator of CX3CR1 that may be effective for treatment of inflammatory bowel disease...
November 2017: Molecular Pharmacology
https://www.readbyqxmd.com/read/28826779/gene-expression-profiles-in-auricle-skin-as-a-possible-additional-endpoint-for-determination-of-sensitizers-a-multi-endpoint-evaluation-of-the-local-lymph-node-assay
#16
Hiromi Tsuchiyama, Akihisa Maeda, Mayumi Nakajima, Mika Kitsukawa, Kei Takahashi, Tomoya Miyoshi, Mayu Mutsuga, Yoshiji Asaoka, Yohei Miyamoto, Keiyu Oshida
The murine local lymph node assay (LLNA) is widely used to test chemicals to induce skin sensitization. Exposure of mouse auricle skin to a sensitizer results in proliferation of local lymph node T cells, which has been measured by in vivo incorporation of H(3)-methyl thymidine or 5-bromo-2'-deoxyuridine (BrdU). The stimulation index (SI), the ratio of the mean proliferation in each treated group to that in the concurrent vehicle control group, is frequently used as a regulatory-authorized endpoint for LLNA...
October 5, 2017: Toxicology Letters
https://www.readbyqxmd.com/read/28818461/discovery-and-process-development-of-a-novel-tace-inhibitor-for-the-topical-treatment-of-psoriasis
#17
Jean-Guy Boiteau, Gilles Ouvry, Jean-Marie Arlabosse, Stéphanie Astri, Audrey Beillard, Yushma Bhurruth-Alcor, Laetitia Bonnary, Claire Bouix-Peter, Karine Bouquet, Marilyne Bourotte, Isabelle Cardinaud, Catherine Comino, Benoît Deprez, Denis Duvert, Angélique Féret, Feriel Hacini-Rachinel, Craig S Harris, Anne-Pascale Luzy, Arnaud Mathieu, Corinne Millois, Nicolas Orsini, Jonathan Pascau, Artur Pinto, David Piwnica, Gaëlle Polge, Arnaud Reitz, Kevin Reversé, Nicolas Rodeville, Patricia Rossio, Delphine Spiesse, Samuel Tabet, Nathalie Taquet, Loïc Tomas, Emmanuel Vial, Laurent F Hennequin
Targeting the TNFα pathway is a validated approach to the treatment of psoriasis. In this pathway, TACE stands out as a druggable target and has been the focus of in-house research programs. In this article, we present the discovery of clinical candidate 26a. Starting from hits plagued with poor solubility or genotoxicity, 26a was identified through thorough multiparameter optimisation. Showing robust in vivo activity in an oxazolone-mediated inflammation model, the compound was selected for development. Following a polymorph screen, the hydrochloride salt was selected and the synthesis was efficiently developed to yield the API in 47% overall yield...
August 2, 2017: Bioorganic & Medicinal Chemistry
https://www.readbyqxmd.com/read/28807557/the-role-of-toll-like-receptor-3-in-chronic-contact-hypersensitivity-induced-by-repeated-elicitation
#18
Risa Yasuike, Risa Tamagawa-Mineoka, Mayumi Ueta, Naomi Nakamura, Shigeru Kinoshita, Norito Katoh
BACKGROUND: Accumulating evidence suggests that Toll-like receptor (TLR)-3 signaling is involved in non-infectious immune and inflammatory reactions as well as in viral infections. The skin of patients with atopic dermatitis (AD) is often infected with virus and bacteria, leading to the aggravation of atopic symptoms. These findings suggest TLR3 signaling may be involved in the pathogenesis of AD, but the exact role of TLR3 in AD remains to be defined. OBJECTIVE: The purpose of this study was to investigate the role of TLR3 in chronic contact hypersensitivity reactions induced by repeated elicitation, resembling the features of AD...
August 4, 2017: Journal of Dermatological Science
https://www.readbyqxmd.com/read/28781714/generation-repair-and-replication-of-guanine-oxidation-products
#19
REVIEW
Katsuhito Kino, Masayo Hirao-Suzuki, Masayuki Morikawa, Akane Sakaga, Hiroshi Miyazawa
Guanine is the most readily oxidized of the four DNA bases, and guanine oxidation products cause G:C-T:A and G:C-C:G transversions through DNA replication. 8-Oxo-7,8-dihydroguanine (8-oxoG) causes G:C-T:A transversions but not G:C-C:G transversions, and is more readily oxidized than guanine. This review covers four major findings. (i) 2,2,4-Triamino-5(2H)-oxazolone (Oz) is produced from guanine and 8-oxoG under various oxidative conditions. Guanine is incorporated opposite Oz by DNA polymerases, except REV1...
2017: Genes and Environment: the Official Journal of the Japanese Environmental Mutagen Society
https://www.readbyqxmd.com/read/28748525/topically-applied-azaphenothiazines-inhibit-contact-sensitivity-to-oxazolone-in-mice
#20
Jolanta Artym, Maja Kocięba, Ewa Zaczyńska, Michał Zimecki, Małgorzata Jeleń, Beata Morak-Młodawska, Krystian Pluta, Katarzyna Kaleta-Kuratewicz, Jan P Madej, Piotr Kuropka, Jan Kuryszko
In this work we investigated the efficacy of two topically applied azaphenothiazine derivatives, 9-chloro-6-acetylaminobutylquinobenzo[3,2-b][1,4]thiazine (compound 4) and 6-chloroethylureidoethyldiquino[3,2-b;2';3'-e][1,4]thiazine (compound 5), in the amelioration of inflammatory symptoms of contact sensitivity (CS) to oxazolone in mice, in relation to the commercial ointment Protopic® (tacrolimus), the reference drug. The compounds were administered 24 h following elicitation of CS and, 24 h later, the parameters of inflammation, such as ear edema, blood composition, leukocyte level, numbers of cells in the draining lymph nodes, histological picture of the inflamed tissue, and the morphometric analysis, were analyzed...
July 27, 2017: Histology and Histopathology
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