熊果酸衍生物的合成及其对肺癌细胞活性抑制的研究

目的：探讨合成的熊果酸衍生物对肺癌LTEP-α-2肿瘤细胞增殖的抑制作用。方法：熊果酸经氧化、肟化和腙化合成为3-氧代熊果酸、3-肟基熊果酸和3-（2＇,4＇-二硝基）-苯腙熊果酸。采用MTT法检测熊果酸及其衍生物对肺癌LTEP-α-2细胞的体外抗肿瘤活性。结果：熊果酸及其衍生物对肺癌LTEP-α-2细胞有抑制作用,且3-肟基熊果酸对肺癌LTEP-α-2细胞抑制作用高于其他化合物,其抑制率为90.0%,IC50为7.4μg/m L。结论：熊果酸衍生物3-肟基熊果酸抗肺癌LTEP-α-2肿瘤细胞活性高于熊果酸的活性。

Synthesis and Inhibitory Activity on Lung Cancer of Ursolic Acid Derivatives

Objective： To investigate the inhibitory effect of ursolic acid derivatives on proliferation of Lung LTEP-α-2tumor cells. Methods： 3-oxo-ursolic acid,3-oximino ursolic acid and 3-（2,4-dinitrophenyl）-hydrazone ursolic acid were synthesized by oxidation,oximation and hydrazonation from ursolic acid. The antitumor activities of oleanolic acid and its derivatives on lung adenoma cell line LTEP-α-2 were investigated by MTT colorimetric assay. Results： All compounds had significant antitumor activity. 3-Oximino ursolic acid had the highest activity on lung adenoma cell line LTEP-α-2,which was more effective than other ursolic acid derivatives,and the inhibition rate was 90%,IC50 was7. 4 μg / m L. Conclusion： The inhibitory activity of 3-oximino ursolic acid on Lung LTEP-α-2 tumor cells was more effective than ursolic acid.