首页> 外文期刊>Journal of Cellular Physiology >Novel caffeic acid ester derivative induces apoptosis by expressing FasL and downregulating NF-KappaB: Potentiation of cell death mediated by chemotherapeutic agents.
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Novel caffeic acid ester derivative induces apoptosis by expressing FasL and downregulating NF-KappaB: Potentiation of cell death mediated by chemotherapeutic agents.

机译:小说中咖啡酸酯衍生物诱导细胞凋亡表达FasL表达下调由NF-KappaB:增强作用的细胞死亡化疗药物。

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摘要

In the present study, we demonstrate the biological activity of esterified caffeic acid with methyl vanillate also termed as caffeic acid methyl vanillate ester (CAMVE). CAMVE potentiates TNF-induced cell death as analyzed by cell viability assay and blocks inflammatory stimuli-induced nuclear transcription factor kappaB (NF-kappaB) activation and NF-kappaB-dependent genes expression. CAMVE-mediated inhibition of NF-kappaB or induction of cell death is not cell type specific. CAMVE inhibits cell proliferation by inhibiting G1 to S phase progression. It suppresses TNF-induced Bcl-2 expression and potentiates chemotherapeutic agents-mediated cell death. CAMVE enhances intracellular free Ca(2+) and thereby activates calcineurin. Calcineurin, in turns, activates nuclear transcription factor NF-AT and its dependent genes such as FasL, which induces cell death. The data demonstrate that CAMVE is one of the combinatorial products, which is able to inhibit NF-kappaB regulated genes and cell proliferation. The combinatorial synthesis of novel caffeic ester derivatives can be a useful approach to generate potent chemotherapeutic agents and designing CAMVE as potent therapeutic agent for combination therapy may be useful to treat tumors.
机译:在目前的研究中,我们将演示生物活性的酯化咖啡酸香子兰酸盐也称为咖啡酸甲酯香子兰酸盐酯甲酯(CAMVE)。TNF-induced细胞死亡,细胞分析可行性分析和炎症stimuli-induced核转录因子kappaB (NF-kappaB)激活和NF-kappaB-dependent基因表达。CAMVE-mediated NF-kappaB或抑制诱导细胞死亡的细胞类型具体。抑制G1 S期进展。抑制TNF-induced bcl - 2表达和强化化疗agents-mediated细胞死亡。从而激活钙调磷酸酶。轮流,核转录因子激活NF-AT FasL等及其相关的基因诱导细胞死亡。CAMVE是组合产品能够抑制NF-kappaB调节基因和细胞增殖。金融衍生品可以是一项新型咖啡酯有用的方法来生成的化疗药物和设计CAMVE强效治疗代理进行联合治疗可能是有用的治疗肿瘤。

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