姜黄素类似物的合成及体外抗氧化活性研究

Synthesis and in vitro Antioxidant Activity of Curcumin Analogs

利用不同的芳香醛和乙酰丙酮缩合反应,合成了4种姜黄素类似物(A1～A4),化合物的结构经IR1、HNMR及MS等测试技术表征确证。采用邻苯三酚法研究化合物的体外抗氧化活性,台盼蓝细胞计数法研究体外抗肿瘤活性。结果表明,化合物A1、A2、A3的抗氧化活性和对K562细胞增殖的抑制活性均高于姜黄素,其活性与酚羟基密切相关。

Four curcumin analogs（A1-A4） were synthesized with various aromatic aldehyde and 2,4-pentanedione as raw materials via condensation reactions.The structures of all synthesized compounds were characterized by IR,1H NMR and mass spectra.Antioxidant activity in vitro of curcumin analogs were studied by the pyrogallol autoxidation method.Trypan blue staining assay was used to evaluate the in vitro antitumor activity of these derivatives.The results showed that antioxidant activity and the inhibitory activity of K562 cell proliferation of compounds A1,A3 and A4 was both higher than that of curcumin.The analysis of structure activity shows that the antioxidant and antitumor activities of curcumin analogs are related to-OH groups of Aromatic ring.