Bose Julie S, Gangan Vijay, Jain Swatantra Kumar, Manna Sunil K
Reliance Life Sciences Pvt. Ltd., Mumbai, India.
J Clin Immunol. 2009 Jan;29(1):90-8. doi: 10.1007/s10875-008-9230-3. Epub 2008 Sep 16.
Considering anti-tumorigenic activity of caffeic acid phenyl ester, synthesis of several esterified form of caffeic acid is a novel approach in designing for potent drugs.
Our study demonstrates that esterified caffeic acid with methyl vanillate, termed as caffeic acid methyl vanillate ester (CAMVE), blocked inflammatory stimuli-induced inflammatory responses. It decreased amounts of iNOS, Cox-2, and ICAM1 by inhibiting NF-kappaB through inhibition of IKK activity, I kappaB alpha degradation, and p65 nuclear translocation.
Overall, our data suggest that novel caffeic acid ester down-regulates inflammatory responses through inhibition of NF-kappaB and dependent several gene expressions, further suggesting its efficacy as a promising therapeutic agent.
鉴于咖啡酸苯酯的抗肿瘤活性,合成几种咖啡酸的酯化形式是设计强效药物的一种新方法。
我们的研究表明,与香草酸甲酯酯化的咖啡酸,即咖啡酸香草酸甲酯酯(CAMVE),可阻断炎症刺激诱导的炎症反应。它通过抑制IKK活性、IκBα降解和p65核转位来抑制NF-κB,从而减少诱导型一氧化氮合酶(iNOS)、环氧化酶-2(Cox-2)和细胞间黏附分子1(ICAM1)的量。
总体而言,我们的数据表明,新型咖啡酸酯通过抑制NF-κB和相关的几个基因表达来下调炎症反应,进一步表明其作为一种有前景的治疗剂的功效。