摘要
5′-碘靛玉红是靛玉红苯环5′位碘取代的衍生物。对大、小鼠急性毒性试验表明,未见与靛玉红有明显差异。对大鼠W256的实验治疗表明,二药等克分子剂量(2mM/kg)或等剂量(800mg/kg)灌胃,本品的抑瘤率为57～72％(P<0.01),靛玉红为30～34％(P<0.05),二者有显著差异。本品的ID_(50)为490±32.9mg/kg,CI大于10;而靛玉红的抑瘤率低于50％。本品还能明显延长L7212小鼠的存活时间41～73％(P<0.01);而靛玉红无活性。P388瘤细胞体外试验表明,二药均能抑制~3H-TdR参入瘤细胞的DNA,但本品的IC_(50)明显低于靛玉红,分别为6.4和17.0μg/ml。以上结果证明了,5′-碘靛玉红的抗癌活性比靛玉红高。
5′-iodoinirubin, a chemically synthesized new drug, is one of the derivatives of indirubin used in treating chronic granuloeytic leukemia. Assay of antitumor activity showed that 5'-iodoindirubin was active against trans-plantable tumors; Such as Walker carcinosarcoma256,lymphocytic leuekmia L7212, L7712, L759, and Lewis lung car-cinoma.When the rats were treated with intragastric administration 400-1000 mg/kg daily for 7 consecutive days,the growth of W256 was inhibited by 48％-83％.Its ID50 was 490±32.9 mg/kg; CI was more than 10. The antitumor activ- ity of 5'-iodoindirubin on W256 was significantly higher than that of indirubin at the same dosage.The survival time of L7212-bearing 615 mice also was signific-antly prolonged by 5'-iodoindirubin.The therapeutic effect of 5'-iodoindirubin on L7212 at the same dosage was higher than that of indirubin, N'-methylindirubin,and N'-ethylindirubin. In vitro, IC50 and IC10 of 5'-iodoindirubin on^3H-TdR incorporation into DNA of P388 cells were 6.4 and 0.72 Mg/ml respectivelly, but that of indirubin were 17.0 and 6.2 Mg/ml respectivelly.
出处
《华西药学杂志》
CAS
CSCD
北大核心
1991年第2期63-68,共6页
West China Journal of Pharmaceutical Sciences
关键词
5`-碘靛玉红
靛玉红
抗肿瘤活性
5′-iodoindirubin Indirubin Activity of antitumor Walker carcinosarcoma 258 Lymphocytic leukemia P_333 3~H-TdR DNA
