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Elisa Meroni, Nathalie Stakenborg, Pedro J Gomez-Pinilla, Gert De Hertogh, Gera Goverse, Gianluca Matteoli, Simon Verheijden, Guy E Boeckxstaens
BACKGROUND: Oxazolone-induced colitis has been frequently used in literature as a model of IBD, but insights into the underlying immune response and pathological features are surprisingly still very limited. Vagus nerve stimulation (VNS) has proven to be effective in innate and Th1/Th17 predominant inflammatory models, including pre-clinical models of colitis, however to what extent VNS is also effective in ameliorating Th2-driven colitis remains to be studied. In the present study, we therefore further characterized the immune response in oxazolone-induced colitis and investigated the potential therapeutic effect of VNS...
2018: PloS One
Gulsiye Ozturk Urut, Seher Aydin, Derya Topkaya, Elif Sahin, Serap Alp
New fluorescent thiophenyl group containing oxazol-5-one fluorophores of 3a (4-(3-thiophenylmethylene)-2-phenyloxazol-5-one), 3b (4-(3-thiophenylmethylene)-2-(4-tolyl)oxazol-5-one) and 3c (4-(3-thiophenylmethylene)-2-(4-nitrophenyl)oxazol-5-one) were synthesized and characterized. The newly synthesized oxazol-5-ones absorption and fluorescence characteristics were studied in some solvents of varying polarities. The heterocyclic chromophores were fluorescent, with two of them, 3a and 3b, emitting blue light, whilst the other one, 3c, emitting green light...
May 21, 2018: Journal of Fluorescence
Bora Kim, Hyun-Soo Kim
We synthesized and investigated the effects of a novel peptide B, RRFSLLRY as a novel PAR-2 antagonist. Peptide B decreased calcium levels in HaCat cells stimulated with trypsin and PAR-2 activator (SLIGKV) and cytokeratin 14 and PCNA was decreased by peptide B. Peptides B also reduced the expression of inflammatory cytokines such as TNF-α and interleukin-6. Significant increase of oxazolone-induced transepidermal water loss (TEWL) was decreased by the addition of peptide B in hairless mice. These findings suggest that the anti-inflammatory effect of peptide B is due to inhibition of PAR-2 signaling...
May 17, 2018: European Journal of Pharmacology
Ji-Hae Lee, Chang Soon Choi, Il-Hong Bae, Jin Kyu Choi, Young-Ho Park, Miyoung Park
BACKGROUND: Although it is established that epidermal barrier disturbance and immune dysfunction resulting in IgE sensitization are critical factors in the development of cutaneous inflammation, the pathogenesis and targeted therapy of atopic dermatitis (AD)-specific pathways have still been unknown. OBJECTIVE: Taking into account the fact that Th2 cytokines in AD have both unique and overlapping functions including increased epidermal thickening, inflammation, and decreased expressing of the barrier proteins keratinocyte differentiation, we sought to clarify our hypothesis that TRPV1 antagonist plays a critical role in skin barrier function and can be a therapeutic target for AD...
April 30, 2018: Journal of Dermatological Science
Martine Catharina Josephine Hofmann, Mike Schmidt, Olga Arne, Gerd Geisslinger, Michael John Parnham, Natasja Maria Wilhelmina Johanna de Bruin
BACKGROUND: Myeloperoxidase is used as a marker and diagnostic tool for inflammatory processes. Hypochlorous acid produced by myeloperoxidase oxidizes luminol to produce light. By injecting luminol into experimental animals, inflammatory processes can be tracked in real-time by bioluminescence imaging (BLI). OBJECTIVE: We aimed to establish BLI as a standardized assessment measure in three mouse models of dermal inflammation. METHODS: Oxazolone-induced delayed-type-hypersensitivity (DTH) (acute), a model for dermatitis, imiquimod (IMQ) (sub-chronic) model for psoriasis and the (chronic) bleomycin model for scleroderma were used...
April 23, 2018: Journal of Dermatological Science
Brock Matter, Christopher L Seiler, Kristopher Murphy, Xun Ming, Jianwei Zhao, Bruce Lindgren, Roger Jones, Natalia Tretyakova
Reactive oxygen and nitrogen species generated during respiration, inflammation, and immune response can damage cellular DNA, contributing to aging, cancer, and neurodegeneration. The ability of oxidized DNA bases to interfere with DNA replication and transcription is strongly influenced by their chemical structures and locations with the genome. In the present work, we examined the influence of local DNA sequence context, DNA secondary structure, and oxidant identity on the efficiency and the chemistry of guanine oxidation in the context of the Kras protooncogene...
April 24, 2018: Free Radical Biology & Medicine
Stephanie M Forget, Andrew W Robertson, Steven R Hall, Jeanna M MacLeod, David P Overy, Russell G Kerr, Kerry B Goralski, David L Jakeman
Herein, we report the characterization and antimicrobial activity of a previously unreported jadomycin (1) obtained from a culture of S. venezuelae ISP5230 with L-ornithine (Orn). 1 arises from the rearrangement of a putative five-membered ring containing jadomycin incorporating Orn, whereby intramolecular attack of the E-ring carbonyl from the δ-NH2 group of the Orn side chain results in collapse of the oxazolone ring and formation of a stable six-membered lactam. This rearrangement produces a jadomycin with a 3a hemiaminal position that is susceptible to solvolysis...
April 26, 2018: Journal of Antibiotics
Minmi Jo, Sun-Woo Won, Dong Guk Lee, Jungeon Yun, Sunhong Kim, Young-Shin Kwak
4,4-Dimethyloxazolones derived from N-protected aminoisobutyric acid (AIB) are particularly known as poor electrophiles due to the steric hindrance around the carbonyl and not employed as useful intermediates for amidation whereas numerous examples have been reported to support the utility of other oxazolones in amidation. AIB is an important and strategical synthon in medicinal chemistry but the peptide bond formation of the N-protected urethane derivatives of AIB is known to be often unproductive due to the rapid formation of the stable 4,4-dimethyloxazolone via an intramolecular cyclization...
May 2018: Archives of Pharmacal Research
Golnaz Parhizkar, Ahmad Reza Khosropour, Iraj Mohammadpoor-Baltork, Elahehnaz Parhizkar, Hadi Amiri Rudbari
A versatile and straightforward synthetic strategy for the construction of new tetrasubstituted 1,3-diazinones is described. The procedure is based on CsF-catalyzed, microwave-assisted, ring transformation reaction of arylidene azlactones with amidines. Moreover, this technique provides diversified trans- N-(6-oxo-1,4,5,6-tetrahydropyrimidin-5-yl)benzamides with a good antimicrobial activity.
June 11, 2018: ACS Combinatorial Science
Katja M Bendtsen, Peter Tougaard, Axel K Hansen
Inflammatory priming of immune cells in early life may optimize the response to a subsequent inflammatory challenge later in life. To prime the immune cells in the gut in vivo through a short inflammatory insult, we administered a low dose of dextran sulfate sodium (DSS) to 5-weeks-old BALB/c mice in the drinking water. We hypothesized that DSS-primed mice would show decreased inflammation and difference in immunological profiling, when subjected to presensitizing and oxazolone-induced colitis by rectal instillation at 9 weeks compared to non-DSS-primed control mice...
April 18, 2018: Inflammation
Gurpreet Kaur Sinhmar, Neel N Shah, Shruti U Rawal, Nimitt V Chokshi, Hiren N Khatri, Bhoomika M Patel, Mayur M Patel
The major challenge for the treatment of inflammatory bowel disease (IBD) is the incompetence to deliver the drug molecule selectively at the site of inflammation. Taking this into consideration, we proposed development of mannosylated nanostructured lipid carrier system (Mn-NLCs) for active targeting and site-specific delivery of budesonide to the inflamed tissues. The developed Mn-NLCs were characterized for particle size and size distribution, zeta potential, %entrapment efficiency, FTIR and TEM analysis...
April 16, 2018: Artificial Cells, Nanomedicine, and Biotechnology
Wei-Zhuo Tang, Zhong-Zhen Yang, Wei Wu, Jie Tang, Fan Sun, Shu-Ping Wang, Chun-Wei Cheng, Fan Yang, Hou-Wen Lin
Five new imidazole derivatives (1-5), together with eight related known alkaloids, were isolated from a calcareous marine sponge, Leucetta chagosensis, collected from the South China Sea. Their structures were fully characterized by spectroscopic methods. Structurally, 1 possesses an unusual skeleton featuring imidazole and oxazolone rings linked via a nitrogen atom, whereas 2 bears an intriguing guanylurea-substituted imidazole ring. Compounds 4 and 5 were identified as zinc complexes; they represent the metal complex analogues of naamidine J (6) and pyronaamidine (7), respectively...
April 27, 2018: Journal of Natural Products
Pankaj Kumar Singh, Om Silakari
O-Heterocycles have been explored in the field of medicinal chemistry for a long time, but their significance has not been duly recognised and they are often shunned in favour of N-heterocycles. The design of bioactive molecules for nearly every pathophysiological condition is primarily focused on novel N-heterocycles. The main reasons for such bias include the ease of synthesis and possible mimicking of physiological molecules by N-heterocycles. But considering only this criterion rarely provides breakthrough molecules for a given disease condition, and instead the risks of toxicity or side effects are increased with such molecules...
March 30, 2018: ChemMedChem
Grace E Kenney, Laura M K Dassama, Maria-Eirini Pandelia, Anthony S Gizzi, Ryan J Martinie, Peng Gao, Caroline J DeHart, Luis F Schachner, Owen S Skinner, Soo Y Ro, Xiao Zhu, Monica Sadek, Paul M Thomas, Steven C Almo, J Martin Bollinger, Carsten Krebs, Neil L Kelleher, Amy C Rosenzweig
Metal homeostasis poses a major challenge to microbes, which must acquire scarce elements for core metabolic processes. Methanobactin, an extensively modified copper-chelating peptide, was one of the earliest natural products shown to enable microbial acquisition of a metal other than iron. We describe the core biosynthetic machinery responsible for the characteristic posttranslational modifications that grant methanobactin its specificity and affinity for copper. A heterodimer comprising MbnB, a DUF692 family iron enzyme, and MbnC, a protein from a previously unknown family, performs a dioxygen-dependent four-electron oxidation of the precursor peptide (MbnA) to install an oxazolone and an adjacent thioamide, the characteristic methanobactin bidentate copper ligands...
March 23, 2018: Science
Phoebe F Lamie, John N Philoppes, Lucie Rárová
A new series of 1,2-diaryl-4-substituted-benzylidene-5(4H)-imidazolone derivatives 4a-l was synthesized. Their structures were confirmed by different spectroscopic techniques (IR, 1 H NMR, DEPT-Q NMR, and mass spectroscopy) and elemental analyses. Their cytotoxic activities in vitro were evaluated against breast, ovarian, and liver cancer cell lines and also normal human skin fibroblasts. Cyclooxygenase (COX)-1, COX-2 and lipoxygenase (LOX) inhibitory activities were measured. The synthesized compounds showed selectivity toward COX-2 rather than COX-1, and the IC50 values (0...
April 2018: Archiv der Pharmazie
Verónica Moner, Estibalitz Fernández, Ana Cristina Calpena, Adriana Garcia-Herrera, Mercedes Cócera, Olga López
BACKGROUND: Atopic dermatitis is a common skin disease characterized by a Th2 cell-dominant inflammatory infiltrate, elevated serum IgE levels and impaired epidermal barrier function. It is associated to abnormal epidermal lamellar body secretion, producing alteration in lipid composition and extracellular lamellar membrane organization. OBJECTIVES: The oxazolone-induced atopic dermatitis in hairless mice was used to evaluate in vivo the effect of the application of a lipid system that mimics the morphology, structure and composition of epidermal lamellar bodies...
January 31, 2018: Journal of Dermatological Science
Kranthikumar Yadav, J Laxmikanth Rao, R Srinivas, R Nagaraj, M V Jagannadham
The detection of post-translational modifications of proteins is an important comprehensive research area. Over the years, proteomic studies involving protein acetylation have attracted a great deal of attention. In the present study, we have focussed on the acetylation of histidine and the intrinsic stability of b1 -ion of oxazolone ring and/or with side chain imidazole bicyclic product. The formation of oxazolone structure may occur when an amino moiety undergoes acetylation reaction and when it is present in the vicinity of the side chain imidazole moiety...
January 1, 2018: European Journal of Mass Spectrometry
Jonghwan Jegal, No-June Park, Sang-A Park, Sim-Kyu Bong, Hyun Jegal, Su-Nam Kim, Min Hye Yang
Juniperus chinensis, commonly Chinese juniper, has been used for treating inflammatory diseases. This study aimed to investigate anti-atopic dermatitis (AD) effects of standardized J. chinensis fruits extract on murine oxazolone- and 2,4-dinitrochlorobenzene (DNCB)-induced models of AD. Ear swelling, epidermis thickening, and eosinophils infiltration in the oxazolone-mediated dermatitis of BALB/c mice were significantly reduced upon topical application of J. chinensis fruits 95% EtOH extract (JCE). Besides, transdermal administration of JCE to SKH-1 hairless mice inhibited the development of DNCB-induced AD-like skin lesions by suppressing transepidermal water loss and improving skin hydration...
2018: Biological & Pharmaceutical Bulletin
Arnaud Baslé, Abdelnasser El Ghazouani, Jaeick Lee, Christopher Dennison
Methanobactins (Mbns) are modified peptides that sequester copper (Cu) methanotrophs use to oxidize methane. Limited structural information is available for this class of natural products, as is an understanding of how cells are able to utilize Mbn-bound Cu. The crystal structure of Methylosinus sporium NR3K CuI -Mbn provides further information about the structural diversity of Mbns and the first insight into their Cu-release mechanism. Nitrogen ligands from oxazolone and pyrazinediol rings chelate CuI along with adjacent coordinating sulfurs from thioamides...
March 26, 2018: Chemistry: a European Journal
J B Wechsler, A Szabo, C L Hsu, R A Krier-Burris, H A Schroeder, M Y Wang, R G Carter, T E Velez, L M Aguiniga, J B Brown, M L Miller, B K Wershil, T A Barrett, P J Bryce
Ulcerative colitis (UC) patients exhibit elevated histamine, but how histamine exacerbates disease is unclear as targeting histamine 1 receptor (H1R) or H2R is clinically ineffective. We hypothesized that histamine functioned instead through the other colon-expressed histamine receptor, H4R. In humans, UC patient biopsies exhibited increased H4R RNA and protein expression over control tissue, and immunohistochemistry showed that H4R was in proximity to immunopathogenic myeloperoxidase-positive neutrophils. To characterize this association further, we employed both the oxazolone (Ox)- and dextran sulfate sodium (DSS)-induced experimental colitis mouse models and also found upregulated H4R expression...
January 24, 2018: Mucosal Immunology
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