类姜黄素化合物的合成及对蛋白质非酶糖基化抑制活性的研究

Synthesis and Non-enzymatic Glycation Inhibition Activities of Curcumin Analogs

通过芳香醛和环己酮及丙酮在乙酸-HC l催化缩合制备了两个系列(A、C)类姜黄素化合物,多酚羟基类姜黄素不需经过羟基保护一步直接缩合制得。对所合成的类姜黄素化合物对牛血清白蛋白非酶糖基化的抑制活性进行了研究,结果表明带酚羟基的类姜黄素均表现出一定的非酶糖基化的抑制活性,四羟基类姜黄素A2及C2表现出极强的非酶糖基化的抑制活性,IC50分别为5.1μmol/L和9.4μmol/L。

Two classes of curcumin analogs （A, C ） were synthesized by coupling the appropriate aromatic aldehyde with cyclohexanon or acetone under the catalysis of gacial acetic acid saturated with anhydrous HCl. The polyhydroxyl curcumin analogs were synthesized by one step without protection of the phenolic hydroxyl groups of aromatic aldehyde. The non-enzymatic glycation inhibition activities of synthetic curcumin analogs were evaluated in vitro. Results indicated that curcumin analogs with phenolic group showed potent activities, curcurmin analogs with tetrahydroxyl groups, A： and C2 , showed much higher non-enzymatic glycation inhibition activities with IC50 of 5.1μmol/L and 9.4μmol/L, respectively.