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https://www.readbyqxmd.com/read/28068430/molecular-mimics-of-classic-p-glycoprotein-inhibitors-as-multidrug-resistance-suppressors-and-their-synergistic-effect-on-paclitaxel
#1
Moustafa E El-Araby, Abdelsattar M Omar, Maan T Khayat, Hanan A Assiri, Ahmed M Al-Abd
P-glycoprotein (Pgp) is a membrane bound efflux pump spread in a variety of tumor cells and considered as a main component of multidrug resistance (MDR) to chemotherapies. In this work, three groups of compounds (imidazolone, oxazolone and vinyl dipeptide derivatives) were synthesized aiming to develop a molecular framework that effectively suppresses MDR. When tested for their influence on Pgp activity, four compounds coded Cur1-01, Cur1-12V, Curox-1 and Curox-3 significantly decreased remaining ATP concentration indicating Pgp substrate site blocking...
2017: PloS One
https://www.readbyqxmd.com/read/28063053/oxazolone-induced-intestinal-inflammation-in-adult-zebrafish
#2
Sylvia Brugman, Edward E S Nieuwenhuis
Zebrafish are an excellent model for the study of intestinal immunity. The availability of several transgenic reporter fish for different innate and adaptive immune cells and the high homology in terms of gut function and morphology enables in depth analysis of the process of intestinal inflammation. Here, we describe a method to induce intestinal inflammation by intra-rectal injection of the hapten oxazolone in adult zebrafish.
2017: Methods in Molecular Biology
https://www.readbyqxmd.com/read/28053892/anti-inflammatory-activity-of-bartogenic-acid-containing-fraction-of-fruits-of-barringtonia-racemosa-roxb-in-acute-and-chronic-animal-models-of-inflammation
#3
Kalpesh R Patil, Chandragouda R Patil
The fruits of Barringtonia racemosa are traditionally used in Indian medicine for the treatment of pain and inflammatory conditions. In this study, a fraction of ethyl acetate extract of fruits of B. racemosa (BREAF) was investigated for anti-inflammatory activity in experimental models of acute and chronic inflammation. Activity against acute inflammation was evaluated in inflammogens induced rat paw edema models. Whereas, effect in chronic inflammation was evaluated in cotton pellet granuloma and oxazolone induced delayed type hypersensitivity (DTH) model in mice...
January 2017: Journal of Traditional and Complementary Medicine
https://www.readbyqxmd.com/read/28026941/cobalt-catalyzed-carbozincation-of-ynamides
#4
Romain Sallio, Martin Corpet, Loic Habert, Muriel Durandetti, Corinne Gosmini, Isabelle Gillaizeau
An original cobalt-catalyzed ynamide carbozincation leading mainly to diverse 3-aryl enamides with mild reaction conditions and good functional-group tolerance has been developed. This reaction displays an excellent regio- and total stereoselectivity and opens the way to appealing synthetic applications. Moreover, this approach allows the selective synthesis of biologically relevant 3,5-disubstituted oxazolone frameworks.
December 27, 2016: Journal of Organic Chemistry
https://www.readbyqxmd.com/read/27981377/myrrh-exerts-barrier-stabilising-and-protective-effects-in-ht-29-b6-and-caco-2-intestinal-epithelial-cells
#5
Rita Rosenthal, Julia Luettig, Nina A Hering, Susanne M Krug, Uwe Albrecht, Michael Fromm, Jörg-Dieter Schulzke
PURPOSE: Myrrh, the oleo-gum resin of Commiphora molmol, is well known for its anti-inflammatory properties. In different animal models, it protected against DSS-, TNBS- and oxazolone-induced colitis. To date, no information concerning the effect of myrrh on barrier properties are available. Thus, this study investigates the effect of myrrh on paracellular barrier function in the absence or presence of the pro-inflammatory cytokine TNFα. METHODS: Monolayers of human colon cell lines HT-29/B6 and Caco-2 were incubated with myrrh under control conditions or after challenge with the pro-inflammatory cytokine TNFα...
December 15, 2016: International Journal of Colorectal Disease
https://www.readbyqxmd.com/read/27966619/nlrp3-inflammasome-has-a-protective-effect-against-oxazolone-induced-colitis-a-possible-role-in-ulcerative-colitis
#6
Shigehiro Itani, Toshio Watanabe, Yuji Nadatani, Naoki Sugimura, Sunao Shimada, Shogo Takeda, Koji Otani, Shuhei Hosomi, Yasuaki Nagami, Fumio Tanaka, Noriko Kamata, Hirokazu Yamagami, Tetsuya Tanigawa, Masatsugu Shiba, Kazunari Tominaga, Yasuhiro Fujiwara, Tetsuo Arakawa
The inflammasomes induce maturation of pro-interleukin-1β (IL-1β) and pro-IL-18. We investigated roles of the NLRP3 inflammasome in the pathogenesis of ulcerative colitis (UC). After induction of oxazolone-induced colitis, a mouse UC model, colonic tissues were assayed for inflammatory mediators. Histological studies were performed on inflamed colonic tissue from mice and UC patients. Histological severity of murine colitis peaked on day 1, accompanied by an increase in the expression of Th2 cytokines including IL-4 and IL-13...
December 14, 2016: Scientific Reports
https://www.readbyqxmd.com/read/27942772/interleukin-19-contributes-as-a-protective-factor-in-experimental-th2-mediated-colitis
#7
Yasuyuki Fujimoto, Yasu-Taka Azuma, Yukiko Matsuo, Mitsuru Kuwamura, Nobuyuki Kuramoto, Mariko Miki, Naoki Azuma, Midori Teramoto, Kazuhiro Nishiyama, Takeshi Izawa, Hidemitsu Nakajima, Tadayoshi Takeuchi
Inflammatory bowel disease results from chronic dysregulation of the mucosal immune system and aberrant activation of both the innate and adaptive immune responses. IL-19 is a member of the IL-10 family, and IL-10 plays an important role in inflammatory bowel disease. We have previously shown that IL-19 knockout mice are more susceptible to innate-mediated colitis. Next, we ask whether IL-19 contributes to T cells-mediated colitis. Here, we investigated the role of IL-19 in a mouse model of Th2 cell-mediated colitis...
December 9, 2016: Naunyn-Schmiedeberg's Archives of Pharmacology
https://www.readbyqxmd.com/read/27917708/synthesis-spectroscopic-characterization-and-antimicrobial-activities-of-benzoxazolone-derivatives
#8
Nida Iqbal Siddiqui, Muhammad Ali Versiani, Khurshid Jawaid, Maryam Shafique, Abdul Hameed, Nida Ambreen, Aneela Karim, Khalid Mohammed Khan
: : Background: Pathogenic microbial diseases are now the key virulence in our daily life. Significant research has been carried out in order to trigger the bacterial infections. Amongst the organic molecules, oxazolone and derivatives were found to have excellent bioactivities including antimicrobial activities. METHODS: By keeping in mind the considerable antimicrobial activities of class benzoxazolones, a series of benzoxazolone derivatives 3-16 have been synthesized...
December 5, 2016: Medicinal Chemistry
https://www.readbyqxmd.com/read/27913732/a-hydantoin-isoform-of-cyclic-n6-threonylcarbamoyladenosine-ct6a-is-present-in-trnas
#9
Michal Matuszewski, Jakub Wojciechowski, Kenjyo Miyauchi, Zofia Gdaniec, Wojciech M Wolf, Tsutomu Suzuki, Elzbieta Sochacka
N(6)-Threonylcarbamoyladenosine (t(6)A) and its derivatives are universally conserved modified nucleosides found at position 37, 3' adjacent to the anticodon in tRNAs responsible for ANN codons. These modifications have pleiotropic functions of tRNAs in decoding and protein synthesis. In certain species of bacteria, fungi, plants and protists, t(6)A is further modified to the cyclic t(6)A (ct(6)A) via dehydration catalyzed by TcdA. This additional modification is involved in efficient decoding of tRNA(Lys) Previous work indicated that the chemical structure of ct(6)A is a cyclic active ester with an oxazolone ring...
December 2, 2016: Nucleic Acids Research
https://www.readbyqxmd.com/read/27904267/application-of-topical-acids-improves-atopic-dermatitis-in-murine-model-by-enhancement-of-skin-barrier-functions-regardless-of-the-origin-of-acids
#10
Noo Ri Lee, Hae-Jin Lee, Na Young Yoon, Donghye Kim, Minyoung Jung, Eung Ho Choi
BACKGROUND: The acidic pH of the stratum corneum (SC) is important for epidermal permeability barrier homeostasis. Acidification of the skin surface has been suggested as a therapeutic strategy for skin disorders such as atopic dermatitis (AD). OBJECTIVE: We performed an animal study to evaluate the usefulness of acidification of SC for inhibition of AD lesions and to find out if the therapeutic effect of vinegar is attributable to its herbal contents, rather than its acidity...
December 2016: Annals of Dermatology
https://www.readbyqxmd.com/read/27882883/electrospray-ionization-tandem-mass-spectrometric-study-of-protonated-and-alkali-cationized-%C3%AE-%C3%AE%C2%B5-hybrid-peptides-differentiation-of-a-pair-of-dipeptide-positional-isomers
#11
A Ramesh Babu, G Raju, C Purna Chander, B Shoban Babu, R Srinivas, G V M Sharma
A new class of Boc-N-protected hybrid peptides derived from L- Ala and ε(6)-Caa (L-Ala = L-Alanine, Caa = C-linked carboamino acid derived from D-xylose) have been studied by positive ion electrospray ionization (ESI) ion-trap tandem mass spectrometry (MS/MS). MS(n) spectra of protonated and alkali-cationized hybrid peptides produce characteristic fragmentation involving the peptide backbone, the tert-butyloxycarbonyl (Boc) group, and the side chain. The dipeptide positional isomers are differentiated by the collision-induced dissociation (CID) of the protonated and alkali-cationized peptides...
2016: European Journal of Mass Spectrometry
https://www.readbyqxmd.com/read/27866317/spectrofluorimetric-and-potentiometric-determination-of-acidity-constants-of-4-4-acetyloxy-3-methoxybenzylidene-5-oxazolone-derivatives
#12
Derya Topkaya Taskiran, Gulsiye Ozturk Urut, Sevda Ayata, Serap Alp
4-(4'-acetyloxy-3'-methoxybenzylidene)-5-oxazolone fluorescent molecules bearing four different aryl groups attached to the 2-position of 5-oxazolone ring have been investigated by spectrophotometric and potentiometric techniques in solution media. The acidity constants (pKa) of the fluorescent molecules were precisely determined in acetone, acetonitrile, dimethylformamide and in 1:1 mixture of toluene-isopropanol. The studied derivatives were titrated with tetrabutylammonium hydroxide and non-aqueous perchloric acid by scanning the basic and acidic region of the pH scale...
November 19, 2016: Journal of Fluorescence
https://www.readbyqxmd.com/read/27807191/mast-cells-limit-the-exacerbation-of-chronic-allergic-contact-dermatitis-in-response-to-repeated-allergen-exposure
#13
Vladimir-Andrey Gimenez-Rivera, Frank Siebenhaar, Carolin Zimmermann, Hanna Siiskonen, Martin Metz, Marcus Maurer
Allergic contact dermatitis is a chronic T cell-driven inflammatory skin disease that is caused by repeated exposure to contact allergens. Based on murine studies of acute contact hypersensitivity, mast cells (MCs) are believed to play a role in its pathogenesis. The role of MCs in chronic allergic contact dermatitis has not been investigated, in part because of the lack of murine models for chronic contact hypersensitivity. We developed and used a chronic contact hypersensitivity model in wild-type and MC-deficient mice and assessed skin inflammatory responses to identify and characterize the role of MCs in chronic allergic contact dermatitis...
November 2, 2016: Journal of Immunology: Official Journal of the American Association of Immunologists
https://www.readbyqxmd.com/read/27795312/an-aminotransferase-is-responsible-for-the-deamination-of-the-n-terminal-leucine-and-required-for-formation-of-oxazolone-ring-a-in-methanobactin-of-methylosinus-trichosporium-ob3b
#14
Wenyu Gu, Bipin S Baral, Alan A DiSpirito, Jeremy D Semrau
: Gene expression in methanotrophs has been shown to be affected by the availability of a variety of metals, most notably copper-regulating expression of alternative forms of methane monooxygenase. A copper-binding compound, or chalkophore, called methanobactin plays a key role in copper uptake in methanotrophs. Methanobactin is a ribosomally synthesized and posttranslationally modified peptide (RiPP) with two heterocyclic rings with an associated thioamide for each ring, formed from X-Cys dipeptide sequences that bind copper...
January 1, 2017: Applied and Environmental Microbiology
https://www.readbyqxmd.com/read/27776738/bone-marrow-derived-innate-macrophages-attenuate-oxazolone-induced-colitis
#15
Zhao Cheng, Hong-Ling Peng, Rong Zhang, Xian-Ming Fu, Guang-Sen Zhang
Previous studies have shown that a subpopulation of granulocyte macrophage colony-stimulating factor (GM-CSF)-dependent F4/80(high) CD11b(high) innate macrophages could be derived from bone marrow cells by continuous in vitro culturing. These cells could be induced to differentiate into M1 or M2 macrophages in vitro. In the current study, we sought to determine whether bone marrow cell-derived innate macrophages (BMIMs) could be used to fulfill an anti-inflammatory purpose by intravenous transplantation in vivo after being stimulated to differentiate into M2 macrophages...
January 2017: Cellular Immunology
https://www.readbyqxmd.com/read/27702671/major-differences-between-human-atopic-dermatitis-and-murine-models-as-determined-by-global-transcriptomic-profiling
#16
David A Ewald, Shinji Noda, Margeaux Oliva, Thomas Litman, Saeko Nakajima, Xuan Li, Hui Xu, Peter Scheipers, Naila Svitacheva, Tord Labuda, James G Krueger, Mayte Suárez-Fariñas, Kenji Kabashima, Emma Guttman-Yassky
BACKGROUND: Atopic dermatitis (AD) is caused by a complex interplay between immune and barrier abnormalities. Murine models of AD are essential for preclinical assessments of new treatments. While many models have been used to simulate AD, their transcriptomic profiles are not fully understood, and a comparison of these models with the human AD transcriptomic fingerprint is lacking. OBJECTIVE: We sought to evaluate the transcriptomic profiles of six common murine models and determine how they relate to human AD skin...
October 1, 2016: Journal of Allergy and Clinical Immunology
https://www.readbyqxmd.com/read/27639807/rectal-delivery-of-a-dnazyme-that-specifically-blocks-the%C3%A2-transcription-factor-gata3-and-reduces-colitis-in-mice
#17
Vanessa Popp, Katharina Gerlach, Stefanie Mott, Agnieszka Turowska, Holger Garn, Raja Atreya, Hans-Anton Lehr, I-Cheng Ho, Harald Renz, Benno Weigmann, Markus F Neurath
BACKGROUND & AIMS: GATA3 is a transcription factor that regulates T-cell production of cytokines. We investigated the role of GATA3 in development of colitis in mice. METHODS: We performed quantitative polymerase chain reaction and immunofluorescence analyses of colon tissues from patients with Crohn's disease (n = 61) or ulcerative colitis (UC, n = 74) or from patients without inflammatory bowel diseases (n = 22), to measure levels of GATA3. Colitis was induced by administration of oxazolone or 2,4,6-trinitrobenzenesulfonic acid to control mice, mice with T-cell-specific deletion of GATA3, and mice with deletion of tumor necrosis factor receptor (TNFR) 1 and TNFR2 (TNFR double knockouts); some mice were given a GATA3-specific DNAzyme (hgd40) or a control DNAzyme via intrarectal administration, or systemic injections of an antibody to TNF before or during sensitization and challenge phase of colitis induction...
January 2017: Gastroenterology
https://www.readbyqxmd.com/read/27620138/vitamin-d-treatment-attenuates-2-4-6-trinitrobenzene-sulphonic-acid-tnbs-induced-colitis-but-not-oxazolone-induced-colitis
#18
Tianjing Liu, Yongyan Shi, Jie Du, Xin Ge, Xu Teng, Lu Liu, Enbo Wang, Qun Zhao
Crohn's disease (CD) and ulcerative colitis (UC) have different immunological mechanisms, while both of them are potential targets of vitamin D treatment. In this study, we have tried to address the role of vitamin D in CD and UC using two mouse models. Mice of C57B6L were given vitamin D before the induction of colitis. Our results showed that vitamin D attenuated 2,4,6-trinitrobenzene sulphonic acid (TNBS)-induced colitis but not oxazolone-induced colitis. Vitamin D could preserve the local histology, alleviate inflammation, suppress apoptosis, maintain tight junction function and decrease permeability...
2016: Scientific Reports
https://www.readbyqxmd.com/read/27614265/sema4d-is-required-in-both-the-adaptive-and-innate-immune-responses-of-contact-hypersensitivity
#19
Zhenlai Zhu, Yang Luo, Jinlei Yu, Jixin Gao, Yueqiang Zhang, Chunying Xiao, Chen Zhang, Gang Wang, Yufeng Liu, Meng Fu, Xu Yao, Wei Li
Originally recognized as a regulator of axon guidance in the nervous system, Semaphorin 4D (Sema4D, CD100) also participates in various immune responses and many immune-related diseases. However, whether Sema4D is involved in the pathogenesis of contact hypersensitivity (CHS) remains unclear. In this study, we explored the role of Sema4D in oxazolone-induced CHS using Sema4D knockout (KO) mice. We found that Sema4D KO mice developed attenuated CHS responses, as indicated by milder ear-swelling, lower expression of IL-1β, IL-6, CXCL2 and CXCL5, and decreased recruitment of neutrophils, CD8(+) T cells and CD4(+) T cells...
October 2016: Molecular Immunology
https://www.readbyqxmd.com/read/27610159/potent-anti-inflammatory-activity-of-tetramethylpyrazine-is-mediated-through-suppression-of-nf-k
#20
Wei Chen, Weixiong Chen, Jinshui Zhu, Niwei Chen, Yunmin Lu
The purpose of the current study was to evaluate the anti-inflammatory activity of tetramethlpyrazine on oxazolone-induced colitis mice. Spleen mononuclear cells (SMC), lamina propria mononuclear cells (LPMC) and peripheral blood mononuclear cells (PBMC) were isolated from oxazolone-induced colitis and normal mice. The colitis cells treated by oxazolone were randomly divided into model, low dose, middle dose and high dose groups treated with 0, 0.5, 1.0 and 2.0 g/L tetramethlpyrazine, respectively. The apoptotic rate of SMC and LPMC in the oxazolone-induced group was lower than that in the normal group...
2016: Iranian Journal of Pharmaceutical Research: IJPR
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