单羰基姜黄素类似物的结构改造及药理作用研究进展

Research Progress of Structural Modification and Pharmacological Action of Monocarbonyl Curcumin Analogues

关键词:  姜黄素  单羰基姜黄素类似物  抗肿瘤  结构改造  构效关系

Key words:  curcumin  monocarbonyl curcumin analogues  anti-tumor  structural modification  structure-activity relationship

摘要:

姜黄素是中药姜黄的主要活性成分，具有抗肿瘤、抗炎、抗氧化等多种药理活性。临床前研究发现，姜黄素具有体内代谢速度快、溶解度不高、生物利用度低等缺陷，因此，其临床应用受到了限制。近年来国内外科学家以姜黄素为先导化合物，设计合成了大量的单羰基姜黄素类似物，并对其药理活性进行了评价，以解决姜黄素存在的缺陷。本文从单羰基姜黄素类似物连接链的角度进行分类，分别对1，4-戊二烯-3-酮类、环酮类和查尔酮类姜黄素类似物的设计合成、活性测试和构效关系等方面进行综述，并对未来姜黄素类似物的设计合成进行展望，为开发更为高效的姜黄素类新药提供参考。

Abstract:

Curcumin is the main active ingredient of Curcuma longa, which has been reported to possess many pharmacological activities, such as anti-tumor, anti-inflammatory and anti-oxidation. Unfortunately, curcumin has a weak pharmacokinetic profile in vivo, which significantly inhibits its clinical application. In recent years, with curcumin as the lead compound, a large number of monocarbonyl curcumin analogues have been synthesized, and the pharmacological activities were evaluated. This article briefly outlines the synthetic method, activity test and structure-activity relationship of three kinds of curcumin analogues from the perspective of spacers, respectively. At last, the design and synthesis of novel curcumin analogues are prospected, which was expected to develop many efficient curcumin analogues.