PDF(Pubmed)
Abstract：
Although the wide variety of bioactivities of curcumin has been reported by researchers, the clinical application of curcumin is still limited due to its poor aqueous solubility. In view of this, a series of dimethylaminomethyl-substituted curcumin derivatives were designed and synthesized (compounds 1-15). Acetate of these derivatives were prepared (compounds 1a-15a). The Mannich reaction and aldol condensation reaction are the main reactions involved in this study. Compounds 6, 10, 12, 3a, 5a, 6a, 7a, 8a, 10a, 11a, 12a, 13a, 14a, and 15a exhibited better in vitro anti-inflammatory activity compared to curcumin in the RAW264.7 cell line. Compounds 5, 1a, 5a, 8a, and 12a exhibited better in vitro antioxidant activity compared to curcumin in the PC 12 cell line. Compounds 11, 13, 5a, 7a, and 13a exhibited better in vitro radiation protection compared to curcumin in the PC 12 cell line. The aqueous solubilities of all the curcumin derivative acetates were greatly improved compared to curcumin.
摘要：
尽管研究人员已经报道了姜黄素的多种生物活性，由于姜黄素水溶性差，其临床应用仍受到限制。鉴于此,设计并合成了一系列二甲基氨基甲基取代的姜黄素衍生物（化合物1-15）。制备这些衍生物的乙酸盐(化合物1a-15a)。曼尼希反应和羟醛缩合反应是本研究涉及的主要反应。化合物6,10,12,3a,5a,a.7a,8a,10a,11a,12a,13a,14a,和15a在RAW264.7细胞系中表现出与姜黄素相比更好的体外抗炎活性。化合物5,1a,5a,8a,和12a在PC12细胞系中与姜黄素相比表现出更好的体外抗氧化活性。化合物11、13、5a、7a,和13a在PC12细胞系中与姜黄素相比表现出更好的体外辐射防护。与姜黄素相比,所有姜黄素衍生物乙酸酯的水溶解度都有很大改善。
