积雪草酸新型类似物的合成及体外抗肿瘤活性研究

Synthesis and in vitro Antitumor Activity of Asiatica Acid Analogues

设计合成积雪草酸类似物并对其进行体外抗肿瘤活性研究.以天然产物积雪草酸为母体,对C-2、C-3、C-23位羟基、C-28位羧基,以及C-12位双键进行改造,采用MTT法,选用人肝癌细胞(HepG2)和人肺癌细胞(A549)进行初步体外抗肿瘤活性测试.测试结果表明:目标化合物的抗肿瘤活性均优于母体积雪草酸,化合物Ⅰ_(4)、Ⅰ_(6)的活性与吉非替尼相当;积雪草酸新型类似物有较高的抗肿瘤活性,可对其进行进一步研究.

Asiatic acid analog were designed and synthesized,and their anti-tumor activities in vitro were studied.The natural product asiatic acid was used as the matrix to modify the hydroxyl group at C-2,C-3,C-23,C-28 carboxyl and C-12 double bonds.The antitumor activity of human liver cancer cells(HepG2)and human lung cancer cells(A549)were tested in vitro by MTT method.The antitumor activities of the target compounds were better than those of parent volume of snow oxalic acid,and the activities of compounds Ⅰ_(4) and Ⅰ_(6) were equivalent to gefitinib.The new analogues of asiatic acid have high antitumor activity which can be further studied.