【摘要】 基质金属蛋白酶(Matrix metalloproteiriases,MMPs)是肿瘤细胞对正常组织的侵袭和转移过程中重要的调节因子,可以水解多种细胞内、细胞外及细胞膜上的底物,因而影响着多种细胞的行为.当MMPs表达异常时,很多种病理会改变甚至恶化,因此,MMPs已成为近年来备受关注的一类抗肿瘤药物靶标蛋白酶.选用MMPs的几种天然黄酮醇类药物小分子抑制剂,利用荧光滴定光谱和紫外-可见(UV-Vis)吸收光谱相结合,研究了它们与MMPs家族成员之一——MMP-16之间的分子识别和作用机理.研究结果表明,这几种黄酮醇化合物不但对MMP-16显示出了较强的结合能力,而且在结合模式、结合比和抗氧化性能等多方面都表现出了很强的结构-性能差异.更多还原

【Abstract】 Acting on a broad spectrum of extracellular,intracellular,and membrane-associated substrates,the matrix metalloproteinases(MMPs)are critical to the biological processes of organisms.And when aberrantly expressed,many pathological conditions may be born or exacerbated.Several natural flavonoids were used as the inhibitors of MMP-16,and the fluorometric titration and UV-Vis absorption spectra were performed to reveal the recognition and inhibition mechanism between them,large differences at binding model,stoichiometry and antioxidation were clarified between them.更多还原