摘要
目的研究类黄酮的α-葡萄糖苷酶、晚期糖基化产物(AGEs)的抑制活性,并探讨抑制活性与其性质间的相关性。方法采用紫外分光光度法和荧光法分别测定类黄酮对酶、AGEs的抑制率并计算出IC50值,推出抑制活性必需基团及数目,用HPLC法测得蛋白结合率,计算Pearson相关性。结果酶抑制活性必需基团为B环邻二酚羟基和C环α,β-不饱和酮基,AGEs抑制活性必需基团为B环邻二酚羟基;两者抑制率与必需基团数的r分别为0.820、0.767。人血清白蛋白(HSA)、糖化人血清白蛋白(G-HSA)的结合率分别与AGEs抑制率(r=0.759)和Xlog P(r=0.905)高度相关。结论α-葡萄糖苷酶和AGEs的抑制率与必需基团数高度相关,AGEs的抑制活性还与HSA的结合率高度相关,G-HSA的结合率与酯水分配系数高度相关。
OBJECTIVE To investigate the inhibition of flavonoids on α - glucosidase,AGEs formation and the correlation with their properties. METHODS UV and fluorescence method were applied to detect the inhibition and IC50 of flavonoids on α - glucosidase and AGEs formation, and their essential groups for inhibition were derived. Protein binding rate was obtained by HPLC method. Pearson similarity computation was then performed to calculate their correlations. RESULTS The adjacent phenolic hydroxyl in B ring and α, β - unsaturated ketone in C ring were the essential groups for α - glucosidase inhibition and adjacent phenolic hydroxylwas essential for AGEs inhibition, the inhibition rate was highly correlated to essential group numbers （r = 0. 820 and 0. 767 respectively）. HSA and glycared HSA binding rate was highly correlated to AGEs inhibition rate （ r = 0.759 ） and XlogP（ r = 0.905 ）. CONCLUSION The α - glucosidase and AGEs inhibition rate is highly correlated with essential group numbers. HSA binding rate is highly correlated with AGEs inhibition rate, and the glycated ABR is highly correlated with XlogP.
出处
《华西药学杂志》
CAS
CSCD
2015年第4期430-432,共3页
West China Journal of Pharmaceutical Sciences
