高良姜素结构修饰及对K562细胞的抑制活性

Structural modification of galangin and the study of inhibition activity on K562 cells

对高良姜素进行结构修饰,期望得到活性更好的抑制K562细胞增殖的衍生物,并初步总结构效关系。通过化学法以高良姜素为母核进行结构修饰得到了12个衍生物,经MTT法测定了高良姜素及其衍生物在5种不同浓度下培养48 h对K562细胞的抑制活性。12个衍生物中有10个为新化合物。化合物A-1、A-6、A-7、A-8、A-9、A-11和高良姜素活性良好,在浓度为100μmol/L时,对K562细胞的抑制率均大于50%,其中A-1,A-6,A-7这3个衍生物的活性较高良姜素活性好,且A-1活性最强,其IC50为16.7μmol/L。通过本研究发现了活性较强的高良姜素衍生物,并发现在高良姜素3位羟基进行适当的结构修饰可以大大增强对K562细胞的抑制活性,但因所做衍生物数目有限,深入的构效关系总结还有待进一步研究。

To obtain some galangin derivatives with better inhibitory proliferation activity on K562 cells,and make preliminary summary of the structure-effect relationship. Use chemical methods to gain 12 derivatives from galangin,and by MTT assay measure galangin and its derivatives＇ proliferation inhibition effect in five different concentrations on K562 cells. There were 10 new compounds form the 12 derivatives. A-1,A-6,A-7,A-8 and A-9,A-11 and galangin showed good activities with more than 50% inhibition rate in the concentration of 100μmol / L on K562 cells. Three derivatives A-1,A-6 and A-7 showed better activity than galangin,and A-1 had the strongest activity with the IC5016. 7μmol / L. Through this study,strong active derivatives were found,and it can greatly enhance the inhibitory activities on K562 cells if appropriate structural modification is made through 3-hydroxyl on the mother nucleus of galangin. But due to the limited number of the derivatives,deep structure-effect relationship summary is still in need of further study.