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姜黄素类吡唑作为炎症性肠病新治疗药物的合成与生物学评价:对基质金属蛋白酶的影响

Synthesis and biological evaluation of curcuminoid pyrazoles as new therapeutic agents in inflammatory bowel disease: effect on matrix metalloproteinases.

作者信息

Claramunt R M, Bouissane L, Cabildo M P, Cornago M P, Elguero J, Radziwon A, Medina C

机构信息

Departamento de Química Orgánica y Bio-Orgánica, Facultad de Ciencias, UNED, Senda del Rey 9, E-28040 Madrid, Spain.

出版信息

Bioorg Med Chem. 2009 Feb 1;17(3):1290-6. doi: 10.1016/j.bmc.2008.12.029. Epub 2009 Jan 6.

Abstract

Seven N-unsubstituted curcuminoid pyrazoles have been synthesized from the corresponding beta-diketones (including curcumin). We evaluated the possibility of curcuminoid pyrazoles regulating the activity of matrix metalloproteinases (MMPs) by human intestinal epithelial cells in vitro. Zymographic analysis revealed that three compounds significantly down-regulated MMP-9 activity on inflammation-induced intestinal epithelial cells, making them original candidates for the treatment of inflammatory bowel disease (IBD).

摘要

已从相应的β-二酮(包括姜黄素)合成了七种N-未取代的姜黄素类吡唑。我们在体外通过人肠上皮细胞评估了姜黄素类吡唑调节基质金属蛋白酶(MMPs)活性的可能性。酶谱分析表明,三种化合物可显著下调炎症诱导的肠上皮细胞中MMP-9的活性,使其成为治疗炎症性肠病(IBD)的原始候选药物。

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