生物活性 | |||
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描述 | G protein-coupled receptor (GPCR) agonists through their receptors can transactivate protein tyrosine kinase receptors such as epidermal growth factor receptor and serine/threonine kinase receptors most notably transforming growth factor (TGF)-β receptor (TβRI). Several GPCR agonists such as Ang II, thrombin, ET‐1 can mediate the transactivation of a multitude of protein tyrosine kinase receptors[3]. Sodium ferulate (SF), a sodium salt of ferulic acid (3-methoxy-4-hydroxy-cinnamate sodium), acts as a potent antioxidant by scavenging ROS and enhancing the cell stress response through the upregulation of cytoprotective systems, such as heme oxygenase-1, superoxide dismutase, catalase, and Hsp70[4]. SF inhibits the expression and/or activity of enzymes, including inducible nitric oxide synthase, caspases, and cyclooxygenase-2, as well as the activation of JNK. In a vitro study, with treatments of 250, 500 and 1,000 μmol/l SF, the apoptotic percentage of OA chondrocytes was attenuated in a concentration-dependent manner[5]. The MCF-7 cells were treated with ferulic acid at 1 µM, 10 µM and 100 µM along with 100 ng EGF/ml from 24 to 96 h. Ferulic acid gave 14 to 30% inhibition from 24 to 96 h at 10 µM and 20 to 35% inhibition from 24 to 96 h at 100 µM[6]. In a vivo experiment, oral administration of taurine and SF (40 and 30 mg/kg/day, respectively) significantly attenuated the developed liver damage induced by administration of iron, resulting in decreases of liver weight/body weight and serum ALT and AST levels[7]. |
临床研究 | |||||
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NCT号 | 适应症或疾病 | 临床期 | 招募状态 | 预计完成时间 | 地点 |
NCT03092076 | Healthy | Phase 1 | Completed | - | - |
NCT01982734 | Pharmacokinetics of New Curcum... 展开 >>in Formulations Safety of New Curcumin Formulations 收起 << | Early Phase 1 | Completed | - | Germany ... 展开 >> University of Hohenheim Stuttgart, Baden-Württemberg, Germany, 70599 收起 << |
NCT02150356 | Glucose and Lipid Metabolism ... 展开 >> Incretin Hormones Plasma Levels Inflammation, Oxidative Stress and Endothelial Function 收起 << | Not Applicable | Completed | - | Italy ... 展开 >> Dept. Clinical Medicine and Surgery, Federico II University Naples, Italy, 80131 收起 << |
实验方案 | |||
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1mg | 5mg | 10mg | |
1 mM 5 mM 10 mM |
4.63mL 0.93mL 0.46mL |
23.13mL 4.63mL 2.31mL |
46.26mL 9.25mL 4.63mL |
参考文献 |
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