Effect of a novel synthesized sulfonamido-based gallate-SZNTC on chondrocytes metabolism in vitro
作者:Qin Liu、Mu-Yan Li、Xiao Lin、Cui-Wu Lin、Bu-Ming Liu、Li Zheng、Jin-Min Zhao
DOI:10.1016/j.cbi.2014.08.002
日期:2014.9
osteoarthritis (OA) should have not only potent anti-inflammatory effect but also favorable biological properties to restore cartilage function. Gallic acid (GA) and its derivatives are anti-inflammatory agents reported to have an effect on OA (Singh et al., 2003) [1]. However, GA has much weaker antioxidant effects and inferior bioactivity compared with its derivatives. We modified GA with the introduction
治疗骨关节炎(OA)的理想治疗剂不仅应具有有效的抗炎作用,而且还应具有良好的生物学特性以恢复软骨功能。没食子酸(GA)及其衍生物是抗炎药,据报道对OA有影响(Singh等,2003)[1]。然而,与它的衍生物相比,GA具有更弱的抗氧化作用和较差的生物活性。我们通过引入磺酰胺修饰了GA,以合成一种新型的基于磺酰胺基的没食子酸酯,命名为3,4,5-三羟基-N- [4-(噻唑-2-基氨磺酰基)-苯基]-苯甲酰胺钠盐(SZNTC),并进行了分析其软骨保护和药理作用。还进行了SZNTC与GA和磺胺噻唑钠(ST-Na)的比较。结果显示,SZNTC可以有效抑制白介素-1(IL-1)介导的金属蛋白酶-1(MMP-1)和MMP-3的诱导,并且可以诱导金属蛋白酶-1(TIMP-1)的组织表达,证明了减少OA进展的能力。SZNTC还可以通过促进细胞增殖和维持关节软骨细胞表型来发挥软骨保护作用,这可以通过改善细胞