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7.4 μg/mL。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。

Objective: To investigate the inhibitory effect of ursolic acid derivatives on proliferation of Lung LTEP-α-2 tumor 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 was 7.4 μg/mL. Conclusion: The inhibitory activity of 3-oximino ursolic acid on Lung LTEP-α-2 tumor cells was more effective than ursolic acid.