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NR4A1 agonist cytosporone B attenuates neuroinflammation in a mouse model of multiple sclerosis
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作者 Hai-Zhen Yu Bing-Qing Zhu +2 位作者 Lin Zhu Shuo Li Li-Mei Wang 《Neural Regeneration Research》 SCIE CAS CSCD 2022年第12期2765-2770,共6页
Nuclear receptor subfamily 4 group A1(NR4A1)is an orphan nuclear receptor,which is expressed in the majority of cells.NR4A1 expression in peripheral blood mononuclear cells is low during the preclinical stage of multi... Nuclear receptor subfamily 4 group A1(NR4A1)is an orphan nuclear receptor,which is expressed in the majority of cells.NR4A1 expression in peripheral blood mononuclear cells is low during the preclinical stage of multiple sclerosis.Knockout of the Nr4a1 gene in mice can aggravate the symptoms of experimental autoimmune encephalomyelitis(EAE),which is an animal model of multiple sclerosis.In this study,we intragastrically administered the NR4A1 agonist cytosporone B(Csn-B)to mice after inducing EAE.After treatment with Csn-B,the clinical symptoms in the EAE mice were substantially attenuated compared with that in PBS-treated control mice.The percentages of CD4+T cells and F4/80+cells in the central nervous system were decreased.In addition,interferon-γand interleukin-17 production by proinflammatory Th1/Th17 cells in the central nervous system and interferon-γlevels in splenocytes were decreased after Csn-B treatment.These findings suggest that the NR4A1 agonist Csn-B can alleviate nerve injury after EAE induction,and,therefore,may be useful as a potential treatment for multiple sclerosis. 展开更多
关键词 cytosporone B(Csn-B) experimental autoimmune encephalomyelitis MACROPHAGES MICROGLIA multiple sclerosis NR4A1 agonist NR4A1 TH1 TH17 treatment
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Cytosporone B的高效合成
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作者 吕超 李剑芳 +1 位作者 徐洪蛟 沈月毛 《有机化学》 SCIE CAS CSCD 北大核心 2015年第9期2013-2018,共6页
真菌聚酮(cytosporone B,Csn-B)具有多种生物活性,是研究生物过程的重要小分子探针,其高效合成备受关注.本研究以商品3,5-二羟基苯乙酮为原料,苄基保护羟基得到3,5-二苄氧基苯乙酮,然后与硫粉和吗啡啉进行Willgerodt-Kindler反应得到3,5... 真菌聚酮(cytosporone B,Csn-B)具有多种生物活性,是研究生物过程的重要小分子探针,其高效合成备受关注.本研究以商品3,5-二羟基苯乙酮为原料,苄基保护羟基得到3,5-二苄氧基苯乙酮,然后与硫粉和吗啡啉进行Willgerodt-Kindler反应得到3,5-二苄氧基苯乙硫酰胺,一锅煮水解该酰胺得到关键中间体3,5-二苄氧基苯乙酸;然后经酯化、傅克酰基化和脱除苄基,分别以5步反应得到Csn-B(总产率68.8%)或secocurvularin(总收率67.3%);Csn-B经水解得到cytosporone A(Csn-A),总产率65.3%;Csn-B经还原环合得到cytosporone C(Csn-C),总产率64.0%.该合成方法步骤少、产率高,原料廉价,适合Csn-B的大量制备. 展开更多
关键词 聚酮 cytosporone B 小分子探针 Willgerodt-Kindler反应
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Metabolites from mangrove endophytic fungus Dothiorella sp. 被引量:3
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作者 XUQingyan WANGJianfeng +4 位作者 HUANGYaojian ZHENGZhonghui SONGSiyang ZHANGYongmin SUWenjin 《Acta Oceanologica Sinica》 SCIE CAS CSCD 2004年第3期541-547,共7页
Mangroves are special woody plant communities in the intertidal zone of tropical and subtropical coasts. They prove to be a natural microorganisms and new metabolites storage. In the study of mangrove endophytic fungi... Mangroves are special woody plant communities in the intertidal zone of tropical and subtropical coasts. They prove to be a natural microorganisms and new metabolites storage. In the study of mangrove endophytic fungi metabolites, four new compounds, Compounds 1, 2, 3 and 4, as well as a known octaketide, oytosporone B (5), are isolated from an endophytic fungus, Dothiorella sp., HTF3. They all show cytotoxic activities. The elucidation of these structures is mainly based on 1D/ 2D NMR and ESI-MS spectral analyses. 展开更多
关键词 Dothiorella sp. MANGROVE endophytic fungus dothiorelones cytosporone B
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Nur77对前列腺癌细胞生长的影响
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作者 吴剑平 张光远 +2 位作者 许斌 陈恕求 陈明 《中华男科学杂志》 CAS CSCD 北大核心 2021年第7期589-594,共6页
目的:本研究试图揭示Nur77对前列腺癌细胞生长的影响,并探索其用于治疗前列腺癌的价值。方法:采用Western印迹技术检测Nur77蛋白在前列腺癌组织及细胞中的表达情况,并且采用流式细胞仪等检测Nur77对前列腺癌细胞的生长和凋亡的影响。结... 目的:本研究试图揭示Nur77对前列腺癌细胞生长的影响,并探索其用于治疗前列腺癌的价值。方法:采用Western印迹技术检测Nur77蛋白在前列腺癌组织及细胞中的表达情况,并且采用流式细胞仪等检测Nur77对前列腺癌细胞的生长和凋亡的影响。结果:人前列腺癌组织和细胞中存在Nur77和雄激素受体(AR)的表达,过表达的Nur77能抑制前列腺癌LNCaP细胞的生长和细胞周期的进展,使用Nur77的小分子受体激动剂Cytosporone B和DIMC能显著抑制前列腺癌LNCaP细胞的生长,并诱导细胞凋亡。结论:Nur77能抑制前列腺癌细胞的生长,诱导细胞凋亡,有望成为治疗前列腺癌潜在的新的分子靶点。 展开更多
关键词 Nur77 前列腺癌 雄激素 cytosporone B DIMC
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