雷公藤红素新型衍生物体外抗肿瘤活性

目的探讨几种雷公藤红素新型衍生物的体外抗肿瘤活性。方法取对数生长期的大鼠肾上腺髓质嗜铬瘤分化细胞株PC12细胞以及大鼠神经胶质瘤C6细胞,加入雷公藤红素、雷公藤红素衍生物(Cel-1～Cel-13)及阳性对照药顺铂,48 h后,通过四甲基偶氮唑盐比色法,测定各化合物半数抑制浓度(IC50),用以观察雷公藤红素各衍生物对PC12细胞以及C6两种细胞株增殖的影响。结果雷公藤红素衍生物Cel-1、Cel-3、Cel-6和Cel-13对PC12细胞的IC50值分别为(1.6±0.3)、(2.2±0.3)、(1.3±0.3)和(2.4±0.1)μmol.L-1,明显小于母核雷公藤红素(3.2±0.4)μmol.L-1(P<0.05,P<0.01);Cel-1对C6细胞的IC50值为(0.6±0.2)μmol.L-1,明显小于母核雷公藤红素(1.5±0.3)μmol.L-1(P<0.05);而且Cel-1、Cel-3、Cel-6和Cel-13明显小于顺铂对PC12和C6的IC50(11.6±0.8)、(59.0±4.0)μmol.L-1](P<0.01)。结论雷公藤红素新型衍生物中4个化合物有较好的体外抗肿瘤活性,比母体雷公藤红素活性强。

Antitumor effect of novel celastrol analogues in vitro

AIM To study the antitumor activity of novel celastrol analogues in vitro.METHODS PC12 cells and C6 cells in log phase growth were added into the 96-well plate respectively.celastrol and its analogues(Cel-1-Cel-13)as well as the positive control medicine cisplatin were added,48 h later,MTT method was used to determine the half inhibitory concentration(IC50)of cells,and to observe the anticancer activity of celastrol analogues on the proliferation of PC12 cells and C6 cells.RESULTS The IC50 values of Cel-1,Cel-3,Cel-6 and Cel-13 were(1.6 ± 0.3),(2.2 ± 0.3),(1.3 ± 0.3)and(2.4 ± 0.1)μmol·L-1 in PC12 cells respectively,which were significantly lower than that of celastrol(3.2 ± 0.4)μmol·L-1](P < 0.05,P < 0.01),and the IC50 values of Cel-1 in C6 cells(0.6 ± 0.2)μmol·L-1] were significantly lower than that of celastrol(1.5 ± 0.3)μmol·L-1](P < 0.05).Their IC50 values were significantly lower than those of cisplatin(11.6 ± 0.8),(59.0 ± 4.0)μmol·L-1(P < 0.01)].CONCLUSION Four novel celastrol analogues have better antitumoractivity than the parent celastrol.