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目的采用新的合成路线制备姜黄素前体药物,评价其抗肿瘤活性。方法首先采用不同氨基酸与顺丁烯二酸酐进行酰化反应,然后将其分子内脱水环合形成重要中间体N-马来酰-氨基酸,接着在氯化亚砜作用下酰化,最后与姜黄素反应制备五种姜黄素前体药物;应用MTT法评价姜黄素前体药物对MGC-803肿瘤细胞增殖的作用。结果姜黄素前体药物5b~5e为新化合物,其结构经1HNMR,IR和元素分析表征;五种姜黄素前体药物均对MGC-803肿瘤细胞的生长有明显的抑制作用,且呈剂量依赖性。结论完成1种已知的和4种新的姜黄素前体药物的制备,其均对MGC-803肿瘤细胞有抑制作用。
Objective To prepare curcumin prodrugs by a new synthetic route and evaluate its antitumor activity. Methods Amino acids were first acylated with maleic anhydride, then dehydrated and cyclized to form N-maleyl-amino acid, which was then acylated by thionyl chloride. Finally, Five kinds of curcumin prodrugs were prepared by elemental reaction. The effect of curcumin prodrugs on the proliferation of MGC-803 tumor cells was evaluated by MTT assay. Results The curcumin prodrugs 5b ~ 5e were new compounds and their structures were characterized by 1HNMR, IR and elemental analysis. All five curcumin prodrugs inhibited the growth of MGC-803 tumor cells in a dose-dependent manner Sex. Conclusion One known and four new curcumin prodrugs were prepared, all of which have inhibitory effects on MGC-803 tumor cells.