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Poonsit Hiransai Suvina Ratanachaiyavong Arunporn Itharat Potchanapond Graidist Prasit Ruengrairatanaroj Juntipa Purintrapiban 《Journal of cellular biochemistry》2010,109(5):1057-1063
Dioscorealide B (DB), a naphthofuranoxepin has been purified from an ethanolic extract of the rhizome of Dioscorea membranacea Pierre ex Prain & Burkill which has been used to treat inflammation and cancer in Thai Traditional Medicine. Previously, DB has been reported to have anti‐inflammatory activities through reducing nitric oxide (NO) and tumor necrosis factor‐α (TNF‐α) production in lipopolysaccharides (LPS)‐induced RAW 264.7 macrophage cells. In this study, the mechanisms of DB on LPS‐induced NO production and cytokine expression through the activation of nuclear factor‐κB (NF‐κB) and ERK1/2 are demonstrated in RAW 264.7 cells. Through measurement with Griess's reagent, DB reduced NO level with an IC50 value of 2.85 ± 0.62 µM that was due to the significant suppression of LPS‐induced iNOS mRNA expression as well as IL‐1β, IL‐6, and IL‐10 mRNA at a concentration of 6 µM. At the signal transduction level, DB significantly inhibited NF‐κB binding activity, as determined using pNFκB‐Luciferase reporter system, which action resulted from the prevention of IκBα degradation. In addition, DB in the range of 1.5–6 µM significantly suppressed the activation of the ERK1/2 protein. In conclusion, the molecular mechanisms of DB on the inhibition of NO production and mRNA expression of iNOS, IL‐1β, IL‐6, and IL‐10 were due to the inhibition of the upstream kinases activation, which further alleviated the NF‐κB and MAPK/ERK signaling pathway in LPS‐induced RAW264.7 macrophage cells. J. Cell. Biochem. 109: 1057–1063, 2010. © 2010 Wiley‐Liss, Inc. 相似文献
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Ganglioside GM3 suppresses lipopolysaccharide‐induced inflammatory responses in rAW 264.7 macrophage cells through NF‐κB,AP‐1, and MAPKs signaling 下载免费PDF全文
Junyoung Park Choong‐Hwan Kwak Sun‐Hyung Ha Kyung‐Min Kwon Fukushi Abekura Seung‐Hak Cho Young‐Chae Chang Young‐Choon Lee Ki‐Tae Ha Tae‐Wook Chung Cheorl‐Ho Kim 《Journal of cellular biochemistry》2018,119(1):1173-1182
Gangliosides are known to specifically inhibit vascular leukocyte recruitment and consequent interaction with the injured endothelium, the basic inflammatory process. In this study, we have found that the production of nitric oxide (NO), a main regulator of inflammation, is suppressed by GM3 on murine macrophage RAW 264.7 cells, when induced by LPS. In addition, GM3 attenuated the increase in cyclooxyenase‐2 (COX‐2) protein and mRNA levels in lipopolysaccharide (LPS)‐activated RAW 264.7 cells in a dose‐dependent manner. Moreover, GM3 inhibited the expression and release of pro‐inflammatory cytokines of tumor necrosis factor‐alpha (TNF‐α), interleukin‐6 (IL‐6), and interleukin‐1β (IL‐1β) in RAW 264.7 macrophages. At the intracellular level, GM3 inhibited LPS‐induced nuclear translocation of nuclear factor kappa‐light‐chain‐enhancer of activated B cells (NF‐κB) and activator protein (AP)‐1 in RAW 264.7 macrophages. We, therefore, investigated whether GM3 affects mitogen‐activated protein kinase (MAPK) phosphorylation, a process known as the upstream signaling regulator. GM3 dramatically reduced the expression levels of the phosphorylated forms of ERK, JNK, and p38 in LPS‐activated RAW 264.7 cells. These results indicate that GM3 is a promising suppressor of the vascular inflammatory responses and ganglioside GM3 suppresses the LPS‐induced inflammatory response in RAW 264.7 macrophages by suppression of NF‐κB, AP‐1, and MAPKs signaling. Accordingly, GM3 is suggested as a beneficial agent for the treatment of diseases that are associated with inflammation. 相似文献
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K313, a novel benzoxazole derivative,exhibits anti‐inflammatory properties via inhibiting GSK3β activity in LPS‐induced RAW264.7 macrophages 下载免费PDF全文
Bo‐Bo Zhao Hui‐Jie Guo Yang Liu Xing‐Yan Luo Shu‐Xia Yang Yan‐Tang Wang Xiao Leng Chun‐Fen Mo Qiang Zou 《Journal of cellular biochemistry》2018,119(7):5382-5390
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Diterpenes from the Roots of Oryza sativa L. and Their Inhibition Activity on NO Production in LPS‐Stimulated RAW264.7 Macrophages 下载免费PDF全文
Jin‐Gyeong Cho Byeong‐Ju Cha Sang Min Lee Sabina Shrestha Rak‐Hun Jeong Dong Sung Lee Youn‐Chul Kim Dong‐Geol Lee Hee‐Cheol Kang Jiyoung Kim Nam‐In Baek 《化学与生物多样性》2015,12(9):1356-1364
Two new pimarane diterpenoids, momilactone D ( 3 ) and momilactone E ( 5 ), along with three known diterpenoids, momilactone A ( 1 ), sandaracopimaradien‐3‐one ( 2 ), and oryzalexin A ( 4 ) were isolated from Oryza sativa roots. The chemical structures of the compounds were determined by spectroscopic data analysis. The isolated diterpenoids were evaluated for their ability to inhibit NO production and iNOS mRNA and protein expression in LPS‐stimulated RAW264.7 macrophages. Compound 4 showed strong inhibition activity on NO production, and compounds 1 and 4 decreased the expression of iNOS mRNA and protein levels. 相似文献
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Seulah Lee Dahae Lee Joo Chan Lee Ki Sung Kang Rhim Ryoo Hyun‐Ju Park Ki Hyun Kim 《化学与生物多样性》2018,15(9)
Calvatia species, generally known as puffball mushrooms, are used both as sources of food and as traditional medicine. Among the Calvatia genus, Calvatia nipponica (Agaricaceae) is one of the rarest species. Using bioassay‐guided fractionation based on anti‐inflammatory effects, five alkaloids ( 1 – 5 ), two phenolics ( 6 and 7 ), and a fatty acid methyl ester ( 8 ) were isolated from the fruiting bodies of C. nipponica. Compound 8 was identified from C. nipponica for the first time, and all isolates ( 1 – 8 ) were tested for inhibition of nitric oxide (NO) production in lipopolysaccharide (LPS)‐stimulated RAW264.7 macrophages. Compound 7 showed mild inhibition while compound 8 significantly inhibited NO production with an IC50 value of 27.50 ± 0.08 μm . The mechanism of NO inhibition of compound 7 was simulated by molecular docking analysis against nitric oxide synthase (iNOS), which revealed the interactions of 7 with the key amino acid residue and the heme in the active site. With the most potent inhibition against LPS‐induced inflammation, compound 8 was further investigated with respect to its mechanism of action, and the activity was found to be mediated through the inhibition of iNOS and COX‐2 expression. 相似文献
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Aminothiazoles inhibit RANKL‐ and LPS‐mediated osteoclastogenesis and PGE2 production in RAW 264.7 cells 下载免费PDF全文
Anna Kats Maria Norgård Zenebech Wondimu Catalin Koro Hernán Concha Quezada Göran Andersson Tülay Yucel‐Lindberg 《Journal of cellular and molecular medicine》2016,20(6):1128-1138
Periodontitis is characterized by chronic inflammation and osteoclast‐mediated bone loss regulated by the receptor activator of nuclear factor‐κB (RANK), RANK ligand (RANKL) and osteoprotegerin (OPG). The aim of this study was to investigate the effect of aminothiazoles targeting prostaglandin E synthase‐1 (mPGES‐1) on RANKL‐ and lipopolysaccharide (LPS)‐mediated osteoclastogenesis and prostaglandin E2 (PGE2) production in vitro using the osteoclast precursor RAW 264.7 cells. RAW 264.7 cells were treated with RANKL or LPS alone or in combination with the aminothiazoles 4‐([4‐(2‐naphthyl)‐1,3‐thiazol‐2‐yl]amino)phenol (TH‐848) or 4‐(3‐fluoro‐4‐methoxyphenyl)‐N‐(4‐phenoxyphenyl)‐1,3‐thiazol‐2‐amine (TH‐644). Aminothiazoles significantly decreased the number of multinucleated tartrate‐resistant acid phosphatase (TRAP)‐positive osteoclast‐like cells in cultures of RANKL‐ and LPS‐stimulated RAW 264.7 cells, as well as reduced the production of PGE2 in culture supernatants. LPS‐treatment induced mPGES‐1 mRNA expression at 16 hrs and the subsequent PGE2 production at 72 hrs. Conversely, RANKL did not affect PGE2 secretion but markedly reduced mPGES‐1 at mRNA level. Furthermore, mRNA expression of TRAP and cathepsin K (CTSK) was reduced by aminothiazoles in RAW 264.7 cells activated by LPS, whereas RANK, OPG or tumour necrosis factor α mRNA expression was not significantly affected. In RANKL‐activated RAW 264.7 cells, TH‐848 and TH‐644 down‐regulated CTSK but not TRAP mRNA expression. Moreover, the inhibitory effect of aminothiazoles on PGE2 production was also confirmed in LPS‐stimulated human peripheral blood mononuclear cell cultures. In conclusion, the aminothiazoles reduced both LPS‐ and RANKL‐mediated osteoclastogenesis and PGE2 production in RAW 264.7 cells, suggesting these compounds as potential inhibitors for treatment of chronic inflammatory bone resorption, such as periodontitis. 相似文献
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A series of novel 7‐substituted coumarin derivatives were synthesized and evaluated. Biological screening results obtained by the evaluation of the compounds’ inhibition against LPS‐induced IL‐6 and TNF‐α release in RAW 264.7 cells indicated that most compounds exhibited potent anti‐inflammatory activity. Among them, N‐(3‐methoxybenzyl)‐2‐[(2‐oxo‐2H‐chromen‐7‐yl)oxy]acetamide ( 2d ) showed the best activity. The potential targets of title compound 2d were reversely screened with the molecular modeling software, Discovery Studio 2017 R2. Screening and molecule docking results showed that 2d could bind to the active site (NLS Polypeptide) of NF‐κB p65, and this binding affinity was confirmed by surface plasmon resonance (SPR) analysis. Furthermore, Western blot assay showed that 2d remarkably blocked the NF‐κB signaling pathway in vitro. Collectively, all these findings suggested that compound 2d might be a promising lead compound worthy of further pursuit. 相似文献
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Anna Kats Natalija Gerasimcik Tuomas Nreoja Jonas Nederberg Simon Grenlv Ekaterina Lagnhed Suchita Desai Gran Andersson Tülay Yucel‐Lindberg 《Journal of cellular and molecular medicine》2019,23(2):1152-1163
Inflammatory mediator prostaglandin E2 (PGE2) contributes to bone resorption in several inflammatory conditions including periodontitis. The terminal enzyme, microsomal prostaglandin E synthase‐1 (mPGES‐1) regulating PGE2 synthesis is a promising therapeutic target to reduce inflammatory bone loss. The aim of this study was to investigate effects of mPGES‐1 inhibitors, aminothiazoles TH‐848 and TH‐644, on PGE2 production and osteoclastogenesis in co‐cultures of periodontal ligament (PDL) and osteoclast progenitor cells RAW 264.7, stimulated by lipopolysaccharide (LPS), and bone resorption in RANKL‐mediated peripheral blood mononuclear cells (PBMCs). PDL and RAW 264.7 cells were cultured separately or co‐cultured and treated with LPS alone or in combination with aminothiazoles. Multinucleated cells stained positively for tartrate‐resistant acid phosphatase (TRAP) were scored as osteoclast‐like cells. Levels of PGE2, osteoprotegerin (OPG) and interleukin‐6, as well as mRNA expression of mPGES‐1, OPG and RANKL were analysed in PDL cells. PBMCs were treated with RANKL alone or in combination with aminothiazoles. TRAP‐positive multinucleated cells were analysed and bone resorption was measured by the CTX‐I assay. Aminothiazoles reduced LPS‐stimulated osteoclast‐like cell formation both in co‐cultures and in RAW 264.7 cells. Additionally, aminothiazoles inhibited PGE2 production in LPS‐stimulated cultures, but did not affect LPS‐induced mPGES‐1, OPG or RANKL mRNA expression in PDL cells. In PBMCs, inhibitors decreased both osteoclast differentiation and bone resorption. In conclusion, aminothiazoles reduced the formation of osteoclast‐like cells and decreased the production of PGE2 in co‐cultures as well as single‐cell cultures. Furthermore, these compounds inhibited RANKL‐induced bone resorption and differentiation of PBMCs, suggesting these inhibitors for future treatment of inflammatory bone loss such as periodontitis. 相似文献
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α‐Solanine Isolated From Solanum Tuberosum L. cv Jayoung Abrogates LPS‐Induced Inflammatory Responses Via NF‐κB Inactivation in RAW 264.7 Macrophages and Endotoxin‐Induced Shock Model in Mice 下载免费PDF全文
Ji‐Sun Shin Kyoung‐Goo Lee Hwi‐Ho Lee Hae Jun Lee Hyo‐Jin An Jung‐Hwan Nam Dae Sik Jang Kyung‐Tae Lee 《Journal of cellular biochemistry》2016,117(10):2327-2339
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Anti‐Neuroinflammatory Effect of MC13, a Novel Coumarin Compound From Condiment Murraya,Through Inhibiting Lipopolysaccharide‐Induced TRAF6‐TAK1‐NF‐κB,P38/ERK MAPKS and Jak2‐Stat1/Stat3 Pathways 下载免费PDF全文
Ke‐Wu Zeng Qian Yu Li‐Xi Liao Fang‐Jiao Song Hai‐Ning Lv Yong Jiang Peng‐Fei Tu 《Journal of cellular biochemistry》2015,116(7):1286-1299
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7‐Methoxy‐(9H‐β‐Carbolin‐1‐il)‐(E)‐1‐Propenoic Acid,a β‐Carboline Alkaloid From Eurycoma longifolia,Exhibits Anti‐Inflammatory Effects by Activating the Nrf2/Heme Oxygenase‐1 Pathway 下载免费PDF全文
Nguyen Hai Dang Young‐Yeon Choo Nguyen Tien Dat Nguyen Hoai Nam Chau Van Minh Jeong‐Hyung Lee 《Journal of cellular biochemistry》2016,117(3):659-670