姜黄素衍生物的合成方法研究进展

Research progress in the synthesis of curcumin derivatives

姜黄素是姜科和天南星科植物中广泛存在的一种色素,具有抗肿瘤、抗炎、抗氧化等活性,毒性低,但其临床应用因稳定性差、生物利用度低而受到限制。近年来,对姜黄素衍生物的合成方法主要分为两类,一是改变姜黄素的β-二酮结构或苯环结构,设计合成其类似物;二是在姜黄素结构中引入其他活性小分子。通过以上结构改造,能够有效改善姜黄素的稳定性、溶解度及生物活性,为其临床应用创造了良好的前景。

Curcumin is a kind of pigment that widely exists in Zingiberaceae plants and Araceae plants, with anti-tumor, anti-inflammatory and antioxidative activities and low toxicity. However,its application is restricted due to its poor stability and low bioavailability. In recent years,the synthesis of curcumin derivatives could be divided into 2 kinds：one is to design and syn- thesize curcumin analogues by adding substituents to the 13-biketone or the benzene rings;the other is to bond the original struc- ture of eurcumin with other active micromolecular substances. The structure modification could effectively improve the stability, solubility and biological activities of curcumin,and subsequently,create a good prospect for its future clinical applications.