熊果酸的结构修饰物及其抗肿瘤活性

The modificated compounds from ursolic acid and their antitumor activities

目的 结构修饰熊果酸 ,制备其衍生物以观察抗肿瘤活性。方法 对熊果酸的 1、2位和 3位进行氧化 ,制备其衍生物 ,并以Hela和HL - 6 0为模型进行了生物活性测试。结果 制备了 6个衍生物 ,其中 4个化合物为新化合物 ;熊果酸结构修饰物的活性均较熊果酸弱。结论 熊果酸经过结构修饰、改造后 ,生物活性受到影响。

OBJECTIVE To develop the modification of ursolic acid for preparing its derivatives and observing their antitumour activities. METHODS Oxidation of ursolic acid on its 1,2 and 3-position was carried out and the models of Hela and HL-60 cells were used for bioactive screenings. RESULTS Six derivatives were obtained and four of them were new compounds. Their antitumor values on the model of Hela and HL-60 were less than that of ursolic acid. CONCLUSION The antitumour activity of ursolic acid may decrease after its structure modification.