柯里拉京抗肿瘤和致突变作用实验研究

Studies on Antitumor Activity,Mutagenicity Action by Corilagin

目的 :观察柯里拉京药效和对人肿瘤细胞株的抑制生长作用。方法 :对柯里拉京 (Corilagin)进行了Ames试验、中国仓鼠肺细胞 (CHL)染色体畸变试验、小鼠骨髓多染红细胞微核试验和体外对人癌细胞株抗肿瘤活性试验。结果 :柯里拉京 (312 5～ 5 0 0 0 μg 皿 )对鼠伤寒沙门氏菌的诱发回变菌落数均未超过自发回变菌落数的 2倍 ;对CHL细胞 (14～ 2 2 0 μg mL)分别作用 6～ 4 8h的最高畸变率为 4 % ;对昆明小鼠 (112～ 11 2mg kg ,ip× 1)的微核细胞率测定最高 <3‰ ;体外对人卵巢癌细胞 (A2 780 )、鼻咽癌细胞 (KB)、骨肉瘤细胞 (OS 732 )、人肺腺癌 (A5 4 9)和人结肠癌细胞 (HCT 8)IC50 值分别为 0 2 5、1 2、7 4 2、8 2 5及 9 0 8μg kg。结论 :Corilagin对A2 780、KB、OS 732、A5 4 9和HCT 8细胞具有明显的抑制作用 。

Objective To study the antitumor activity and mutagenicity test of Corilagin in vitro and in vivo.Methods The genotoxicity tests were used to investigate the possible harmful effects on genetic material (DNA).Three tests were porformed,they were:1)A test for gene mutation in sulmonella typhimurium (Ames test);2)An in vitro test for chromosomal aberration in Chinese hamster lung cells (CHL);3)An in vivo test for chromosomal damage using mice bone marrow micronucleus assay.Results The dose at 312 5-5 000 μg/plate in vitro by Ames test (with and without activation) were negative,and 14-220 μg/mL for 6-48 h in vitro,respectively,the maximum aberration rate on CHL was 4%.The micronuclei rate of bone marrow micronucleus assay (112-11 2 mg/kg,ip×1) was <3 0‰.The test results of antitumor effect showed corilagin had obvious activities on A2780,KB,OS 732,A549 and HCT 8,the IC 50 value were 0 25,1 2,7 42,8 25 and 9 08 μg/mL,one by one.Conclusions Corilagin is safe and no evidence of mutagenic action,and corilagin has strong antitumor activities on human tumor cell lines such as A2780,KB,OS 732, A549 and HCT 8 in vitro. China J Cancer Prev Treat,2003,10(5):469-472