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https://www.readbyqxmd.com/read/28646757/discovery-and-structure-activity-relationship-studies-of-2-benzylidene-2-3-dihydro-1h-inden-1-one-and-benzofuran-3-2h-one-derivatives-as-a-novel-class-of-potential-therapeutics-for-inflammatory-bowel-disease
#1
Tara Man Kadayat, Suhrid Banskota, Pallavi Gurung, Ganesh Bist, Til Bahadur Thapa Magar, Aarajana Shrestha, Jung-Ae Kim, Eung-Seok Lee
To develop effective therapeutics for inflammatory bowel disease (IBD), 2-benzylidene-2,3-dihydro-1H-inden-1-one and benzofuran-3(2H)-one derivatives, were designed and synthesized and their structure-activity relationships (SAR) were investigated. Compounds 7, 25, 26, 32, 39, 41, 52, 54, and 55 showed potent inhibitory effect (>70%) on the TNF-α-induced adhesion of monocytes to colon epithelial cells, which is one of the hallmark events leading to IBD. Such inhibitory activity of the compounds correlated with their suppressive activities against the TNF-α-induced production of ROS; ICAM-1 and MCP-1 expression, critical molecules involved in monocyte-epithelial adhesion; and NF-κB transcriptional activity...
June 10, 2017: European Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/28646448/purification-of-the-exopolysaccharide-produced-by-alteromonas-infernus-identification-of-endotoxins-and-effective-process-to-remove-them
#2
Alicia Grivaud-Le Du, Agata Zykwinska, Corinne Sinquin, Jacqueline Ratiskol, Pierre Weiss, Claire Vinatier, Jérôme Guicheux, Christine Delbarre-Ladrat, Sylvia Colliec-Jouault
Alteromonas infernus bacterium isolated from deep-sea hydrothermal vents can produce by fermentation a high molecular weight exopolysaccharide (EPS) called GY785. This EPS described as a new source of glycosaminoglycan-like molecule presents a great potential for pharmaceutical and biotechnological applications. However, this unusual EPS is secreted by a Gram-negative bacterium and can be therefore contaminated by endotoxins, in particular the lipopolysaccharides (LPS). Biochemical and chemical analyses of the LPS extracted from A...
June 23, 2017: Applied Microbiology and Biotechnology
https://www.readbyqxmd.com/read/28645584/effects-of-intranasal-treatment-with-slow-gyy4137-and-rapid-nahs-donors-of-hydrogen-sulfide-in-lipopolysaccharide-induced-airway-inflammation-in-mice
#3
Yesim Kaya-Yasar, Yasemin Karaman, Turgut Emrah Bozkurt, Sevgen Celik Onder, Inci Sahin-Erdemli
We have investigated the effects of slow (GYY4137) and rapid (NaHS) hydrogen sulfide (H2S) releasing donors in lipopolysaccharide (LPS)-induced airway inflammation in mice. LPS (0.1 mg/ml) in 60 μl PBS was administered by the intranasal (i.n.) route and control group received vehicle, whereas the subgroups of mice were treated with i.n. GYY4137 or NaHS. The tracheal reactivity, inflammatory cell count in bronchoalveolar lavage (BAL) fluid and lung histopathology were evaluated in all groups 48 h after LPS/PBS applications...
June 20, 2017: Pulmonary Pharmacology & Therapeutics
https://www.readbyqxmd.com/read/28645512/the-rna-seq-analysis-suggests-a-potential-multi-component-complement-system-in-oyster-crassostrea-gigas
#4
Lingling Wang, Huan Zhang, Leilei Wang, Daoxiang Zhang, Zhao Lv, Zhaoqun Liu, Weilin Wang, Zhi Zhou, Limei Qiu, Hao Wang, Jun Li, Linsheng Song
The complement system is one of the major effector mechanisms of immune system, playing essential roles in both the innate and adaptive immune responses. In the present study, the counterparts of vertebrate complement components were identified by screening the sequenced genome of Crassostrea gigas, resulting in the identification of 792 gene models containing complement-related domains. The transcriptome of haemocytes at 6, 12 and 24 h post lipopolysaccharides (LPS) stimulation showed differential expression of 77 C1q domain containing proteins, 53 C-type lectins and 42 fibrinogen-related proteins...
June 20, 2017: Developmental and Comparative Immunology
https://www.readbyqxmd.com/read/28645489/effects-of-hypnotic-bromovalerylurea-on-microglial-bv2-cells
#5
Shun Kawasaki, Naoki Abe, Fumito Ohtake, Afsana Islam, Mohammed Emamussalehin Choudhury, Ryo Utsunomiya, Satoshi Kikuchi, Tasuku Nishihara, Jun Kuwabara, Hajime Yano, Yuji Watanabe, Mayuki Aibiki, Toshihiro Yorozuya, Junya Tanaka
An old sedative and hypnotic bromovalerylurea (BU) has anti-inflammatory effects. BU suppressed nitric oxide (NO) release and proinflammatory cytokine expression by lipopolysaccharide (LPS)-treated BV2 cells, a murine microglial cell line. However, BU did not inhibit LPS-induced nuclear translocation of nuclear factor-κB and subsequent transcription. BU suppressed LPS-induced phosphorylation of signal transducer and activator of transcription 1 (STAT1) and expression of interferon regulatory factor 1 (IRF1)...
June 8, 2017: Journal of Pharmacological Sciences
https://www.readbyqxmd.com/read/28645263/microbiota-dependent-metabolite-and-cardiovascular-disease-marker-trimethylamine-n-oxide-tmao-is-associated-with-monocyte-activation-but-not-platelet-function-in-untreated-hiv-infection
#6
Judith M Haissman, Anna K Haugaard, Sisse R Ostrowski, Rolf K Berge, Johannes R Hov, Marius Trøseid, Susanne D Nielsen
BACKGROUND: HIV infection is associated with increased risk of cardiovascular disease beyond that explained by traditional risk factors. Altered gut microbiota, microbial translocation, and immune activation have been proposed as potential triggers. The microbiota-dependent metabolite trimethylamine-N-oxide (TMAO) predicts myocardial infarction (MI) in the general population and has recently been shown to induce platelet hyperreactivity. In the present study, we investigated if TMAO was associated with platelet function, microbial translocation, and immune activation in both untreated and combination anti-retroviral therapy (cART) HIV infection...
June 23, 2017: BMC Infectious Diseases
https://www.readbyqxmd.com/read/28645003/structure-and-gene-cluster-of-the-o-antigen-of-enterobacter-cloacae-c4115
#7
Andrei V Perepelov, Guangnan Xu, Andrei V Filatov, Xinjie Zhang, Alexander S Shashkov, Min Wang, Yuriy A Knirel
An O-polysaccharide was isolated by mild acid degradation of the lipopolysaccharide of Enterobacter cloacae C4115 and studied by sugar analysis along with 1D and 2D (1)H and (13)C NMR spectroscopy. The following structure of the linear pentasaccharide repeating unit of the O-polysaccharide was established: →2)-α-l-Rhap-(1 → 2)-α-l-Rhap-(1 → 2)-α-l-Rhap-(1 → 2)-α-d-Galp-(1 → 3)-α-d-FucpNAc-(1→ The O-antigen gene cluster of E. cloacae C4115 was sequenced. The gene functions were tentatively assigned by comparison with sequences in the available databases and found to be in consistence with the O-polysaccharide structure...
June 3, 2017: Carbohydrate Research
https://www.readbyqxmd.com/read/28644965/3-4-dihydroxybenzalacetone-attenuates-lipopolysaccharide-induced-inflammation-in-acute-lung-injury-via-down-regulation-of-mmp-2-and-mmp-9-activities-through-suppressing-ros-mediated-mapk-and-pi3k-akt-signaling-pathways
#8
Wei Chao, Jeng-Shyan Deng, Shyh-Shyun Huang, Pei-Ying Li, Yu-Chia Liang, Guan-Jhong Huang
3, 4-Dihydroxybenzalacetone (DBL) is a constituent of Phellinus linteus. This study demonstrated the protective effect of DBL on lipopolysaccharide (LPS)-induced acute lung injuries in mice. Pretreatment with DBL significantly improved LPS-induced histological alterations in lung tissues. In addition, DBL markedly reduced the total cell number, the leukocytes, the protein concentrations, and decreased the release of nitrite, tumor necrosis factor (TNF)-α, interleukin (IL)-1β, IL-6 and the activities of matrix metalloproteinase (MMP)-2 and -9 in the bronchoalveolar lavage fluid...
June 20, 2017: International Immunopharmacology
https://www.readbyqxmd.com/read/28644354/development-and-function-of-immune-cells-in-an-adolescent-patient-with-a-deficiency-in-the-interleukin-10-receptor
#9
Sharon Veenbergen, Marieke A van Leeuwen, Gertjan J Driessen, Rogier Kersseboom, Lilian F de Ruiter, Rolien H C Raatgeep, Dicky J Lindenbergh-Kortleve, Ytje Simons-Oosterhuis, Katharina Biermann, Dicky J J Halley, Lissy de Ridder, Johanna C Escher, Janneke N Samsom
OBJECTIVE: Monogenic defects in the interleukin-10 (IL-10) pathway are extremely rare and cause infantile-onset inflammatory bowel disease (IBD)-like pathology. Understanding how immune responses are dysregulated in monogenic IBD-like diseases can provide valuable insight in "classical" IBD pathogenesis. Here, we studied long-term immune cell development and function in an adolescent IL-10 receptor (IL10RA)-deficient patient who presented in infancy with severe colitis and fistulizing perianal disease and is currently treated with immune suppressants...
July 2017: Journal of Pediatric Gastroenterology and Nutrition
https://www.readbyqxmd.com/read/28644019/metabolomics-analysis-to-evaluate-the-anti-inflammatory-effects-of-polyphenols-glabridin-reversed-metabolism-change-caused-by-lps-in-raw-264-7-cells
#10
Kaiqin Liu, FuWei Pi, Hongxia Zhang, Jian Ji, Shuang Xia, Fangchao Cui, Jiadi Sun, Xiulan Sun
Inflammation has been shown to play a critical role in the development of many diseases. In this study, we used metabolomics to evaluate the inflammatory effect of lipopolysaccharide (LPS) and anti-inflammatory effect of glabridin (GB, a polyphenol from Glycurrhiza glabra L. roots) in RAW 264.7 cells. Multivariate statistical analysis showed that compared with the LPS group, the metabolic profile of the GB group was more similar to that of the control group. LPS impacted the amino acid, energy and lipid metabolisms in RAW 264...
June 23, 2017: Journal of Agricultural and Food Chemistry
https://www.readbyqxmd.com/read/28643674/microbiological-and-serological-control-of-escherichia-coli-o157-h7-in-kindergarten-staff-in-buenos-aires-city-and-suburban-areas
#11
Romina J Fernández-Brando, María Marta Amaral, Andrés E Ciocchini, Leticia V Bentancor, Jorge A Trelles, Marcelo Da Rocha, Martín Landriel, Mariana Ugarte, Gabriel Briones, Cristina Ibarra, Marina S Palermo
Shiga toxin (Stx)-producing Escherichia coli (STEC) infections are implicated in the development of the life-threatening hemolytic-uremic syndrome (HUS). Despite the magnitude of the social and economic problems caused by HUS, no licensed vaccine or effective therapy is currently available for human use. Prevention of STEC infections continues being the most important measure to reduce HUS incidence. This is especially true for Argentina where HUS incidence among children is extremely high and shows an endemic pattern...
2017: Medicina
https://www.readbyqxmd.com/read/28642745/structure-of-o-antigen-and-hybrid-biosynthetic-locus-in-burkholderia-cenocepacia-clonal-variants-recovered-from-a-cystic-fibrosis-patient
#12
A A Hassan, Rita F Maldonado, Sandra C Dos Santos, Flaviana Di Lorenzo, Alba Silipo, Carla P Coutinho, Vaughn S Cooper, Antonio Molinaro, Miguel A Valvano, Isabel Sá-Correia
Burkholderia cenocepacia is an opportunistic pathogen associated with chronic lung infections and increased risk of death in patients with cystic fibrosis (CF). In this work, we investigated the lipopolysaccharide (LPS) of clinical variants of B. cenocepacia that were collected from a CF patient over a period of 3.5 years, from the onset of infection until death by necrotizing pneumonia (cepacia syndrome). We report the chemical structure of the LPS molecule of various sequential isolates and the identification of a novel hybrid O-antigen (OAg) biosynthetic cluster...
2017: Frontiers in Microbiology
https://www.readbyqxmd.com/read/28642677/a-novel-workflow-combining-plaque-imaging-plaque-and-plasma-proteomics-identifies-biomarkers-of-human-coronary-atherosclerotic-plaque-disruption
#13
Regent Lee, Roman Fischer, Philip D Charles, David Adlam, Alessandro Valli, Katalin Di Gleria, Rajesh K Kharbanda, Robin P Choudhury, Charalambos Antoniades, Benedikt M Kessler, Keith M Channon
BACKGROUND: Atherosclerotic plaque rupture is the culprit event which underpins most acute vascular syndromes such as acute myocardial infarction. Novel biomarkers of plaque rupture could improve biological understanding and clinical management of patients presenting with possible acute vascular syndromes but such biomarker(s) remain elusive. Investigation of biomarkers in the context of de novo plaque rupture in humans is confounded by the inability to attribute the plaque rupture as the source of biomarker release, as plaque ruptures are typically associated with prompt down-stream events of myocardial necrosis and systemic inflammation...
2017: Clinical Proteomics
https://www.readbyqxmd.com/read/28642037/testosterone-regulates-3t3-l1pre-adipocyte-differentiation-and-epididymal-fat-accumulation-in-mice-through-modulating-macrophage-polarization
#14
Xiaojiao Ren, Xiaojian Fu, Xinhua Zhang, Shiqiang Chen, Shuguang Huang, Lun Yao, Guoquan Liu
Low testosterone levels are strongly related to obesity in males. The balance between the classically M1 and alternatively M2 polarized macrophages also plays a critical role in obesity. It is not clear whether testosterone regulates macrophage polarization and then affects adipocyte differentiation. In this report, we demonstrate that testosterone strengthens interleukin (IL) -4-induced M2 polarization and inhibits lipopolysaccharide (LPS) -induced M1 polarization, but has no direct effect on adipocyte differentiation...
June 19, 2017: Biochemical Pharmacology
https://www.readbyqxmd.com/read/28641987/food-deprivation-in-f0-generation-and-hypercaloric-diet-in-f1-generation-reduce-f2-generation-astrogliosis-in-several-brain-areas-after-immune-challenge
#15
T B Ogassawara, A Joaquim, C P Coelho, M M Bernardi, E Teodorov, M F M Martins, T B Kirsten, L V Bonamin, P D Dossa, L B Viebig, E F Bondan
AIMS: The effects of maternal food restriction during gestation in F0 generation followed by hypercaloric diet (HD) during puberty in F1 generation (F1HD) were investigated on astrocyte behavior of F2 generation. Also, the astrocyte behavior, after an immune challenge, was examined by the immunohistochemical expression of glial fibrillary acidic protein (GFAP) in several brain areas. METHODS: The body weight gain (BW) during development and in postnatal day (PND) 90-95, the retroperitoneal fat weight (RPF), and the size of larger and smaller adipocytes in the F1 generation were assessed to observe the effects of HD in female rats...
June 19, 2017: International Journal of Developmental Neuroscience
https://www.readbyqxmd.com/read/28641719/surfactant-protein-d-inhibits-interleukin-12p40-production-by-macrophages-through-the-sirp%C3%AE-rock-erk-signaling-pathway
#16
Rui Yamaguchi, Arisa Sakamoto, Takatoshi Yamamoto, Yasuji Ishimaru, Shinji Narahara, Hiroyuki Sugiuchi, Yasuo Yamaguchi
OBJECTIVE: Interleukin (IL)-12 has a pivotal profibrotic role in the development of idiopathic pulmonary fibrosis (IPF). Medical research trials based on IPF registry databases have actively recruited patients. Surfactant protein D (SP-D) is a useful biomarker in patients with IPF. SP-D binds to signal regulatory protein α (SIRPα), which acts as an inhibitory receptor, and this SP-D/SIRPα interaction may have an anti-inflammatory effect. Accordingly, the inhibitory effect of SP-D on IL-12p40 production by lipopolysaccharide (LPS)-stimulated macrophages was investigated...
June 2017: American Journal of the Medical Sciences
https://www.readbyqxmd.com/read/28641579/lps-alters-the-immuno-phenotype-of-glioma-and-glioma-stem-like-cells-and-induces-in-vivo-antitumor-immunity-via-tlr4
#17
Sheng Han, Chao Wang, Xiaofei Qin, Junzhe Xia, Anhua Wu
BACKGROUND: This study examined the ability of lipopolysaccharide (LPS) to affect glioma and glioma stem-like cells (GSCs) in vitro and to induce antitumor immunity in vivo and the role of TLR4 in these processes. METHODS: Using RT-PCR and immunohistochemistry, we examined the expression of TLR4 in 34 glioblastoma clinical samples. Using real time-PCR, western blot and ELISA analyses, the effect of LPS stimulation on the expression of immune related molecules was evaluated in RG2 and U87 GSCs...
June 22, 2017: Journal of Experimental & Clinical Cancer Research: CR
https://www.readbyqxmd.com/read/28641299/monocyte-subsets-are-differentially-lost-from-the-circulation-during-acute-inflammation-induced-by-human-experimental-endotoxemia
#18
Tamar Tak, Roger van Groenendael, Peter Pickkers, Leo Koenderman
Three human monocyte subsets are recognized with different functions in the immune system: CD14++/CD16- classical monocytes (CM), CD14++/CD16+ intermediate monocytes (IM) and CD14+/CD16++ non-classical monocytes (NCM). Increased IM and NCM percentages have been reported under inflammatory conditions, yet little is known about monocyte subsets at the onset of inflammation. The human endotoxemia model is uniquely capable of studying the first phases of acute inflammation induced by intravenous injection of 2 ng/kg bodyweight lipopolysaccharide (LPS) into healthy volunteers...
June 23, 2017: Journal of Innate Immunity
https://www.readbyqxmd.com/read/28641003/synthesis-and-anti-inflammatory-evaluation-of-2-aminobenzaldehydes-via-ir-iii-catalyzed-c-h-amidation-of-aldimines-with-acyl-azides
#19
Saegun Kim, Prashant Chakrasali, Hyo Sun Suh, Neeraj Kumar Mishra, Taeyoung Kim, Sang Hoon Han, Hyung Sik Kim, Byung-Moo Lee, Soo Bong Han, In Su Kim
The aldimine-directed C-H amidation of various arenes with N-acyl azides as amidation surrogates under cationic iridium(III) catalysis is described. This transformation efficiently provides a range of 2-aminobenzaldehydes derivatives with excellent site-selectivity and functional group compatibility. The resulting 2-aminobenzaldehyde framework provides facile access to a range of biologically interesting heterocycles. In addition, all synthetic compounds were screened for anti-inflammatory activity against interleukin-1β (IL-1β) and tumor necrosis factor alpha (TNF-α) with lipopolysaccharide (LPS)-induced RAW264...
June 22, 2017: Journal of Organic Chemistry
https://www.readbyqxmd.com/read/28640809/development-of-elisas-for-diagnosis-of-acute-typhoid-fever-in-nigerian-children
#20
Jiin Felgner, Aarti Jain, Rie Nakajima, Li Liang, Algis Jasinskas, Eduardo Gotuzzo, Joseph M Vinetz, Fabio Miyajima, Munir Pirmohamed, Fatimah Hassan-Hanga, Dominic Umoru, Binta Wudil Jibir, Safiya Gambo, Kudirat Olateju, Philip L Felgner, Stephen Obaro, D Huw Davies
Improved serodiagnostic tests for typhoid fever (TF) are needed for surveillance, to facilitate patient management, curb antibiotic resistance, and inform public health programs. To address this need, IgA, IgM and IgG ELISAs using Salmonella enterica serovar Typhi (S. Typhi) lipopolysaccharide (LPS) and hemolysin E (t1477) protein were conducted on 86 Nigerian pediatric TF and 29 non-typhoidal Salmonella (NTS) cases, 178 culture-negative febrile cases, 28 "other" (i.e., non-Salmonella) pediatric infections, and 48 healthy Nigerian children...
June 22, 2017: PLoS Neglected Tropical Diseases
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