【摘要】 本文建立了一个微量、简便、快速的醛糖还原酶抑制剂筛选方法,对32个黄酮类化合物进行了筛选。其中黄芩甙元和异金丝桃甙乙酸盐作用较强,IC₅₀分别为3.5×10^-6M及2.2×10^-6M。此外,还对其抑制酶的动力学进行了分析。更多还原

【Abstract】 Thirty two flavonoid compounds were screened for inhibition of rat lens aldose reductase activity, among which baiclein and lsohyperoside acetate were found to exhibit markedly enzyme-inhibitary activities with IC₅₀ values of 3.5×10^-6 M and 2.2×10^-6 M, respectively. Baiclein displayed a mixed noncompetitive and competitive inhibition, while isohyperoside acetate a mixed noncompetitive and uncompetitive type of inhibition.Increased aldose reductase activity has been implicated in pathogenesis of diabetic complications so that treatment of these diabetic complications with aldose reductase inhibitors may be a valid approach.更多还原