NB901对胃癌细胞DNA拓扑酶Ⅱ的活力及其对C─Ha─ras基因表达的影响  

EFFECT OF NB901 ON DNA TOPOISOMERASE Ⅱ ACTIVITY AND C-HA-RAS GENE EXPRESSION IN HUMAN GASTRIC CANCER CELLS

作　　者：杨定成[1] 徐文怀[1] 李通[1] 占洪生 李润昭 藏传兵 吕有勇 

机构地区：[1]北京医科大学第一医院外科,天然和仿生药物国家重点实验室,北京市肿瘤防治研究所

出　　处：《癌症》1994年第6期490-493,共4页Chinese Journal of Cancer

基　　金：国家重点实验室资助课题

摘　　要：本文从胃癌ＢＧＣ８２３细胞中分离出ＤＮＡ拓扑酶Ⅱ，应用ｐＢＲ３２２质粒ＤＮＡ作为底物测定酶的活力，发现５’脱氧－５＇醛基腺嘌呤核苷─ＮＢ９０１可以诱导拓扑酶Ⅱ对超螺旋ｐＢＲ３２２质粒ＤＮＡ的松散和裂解，并且可以抑制胃癌ＢＧＣ８２３细胞中Ｃ─Ｈａ─ｒａｓ基因的表达。结果提示抗癌化合物ＮＢ９０１是以癌细胞中ＤＮＡ拓扑酶Ⅱ为作用靶点，癌细胞中拓扑酶Ⅱ可能参与细胞增殖相关基因的转录调控，ＮＢ９０１能够干扰ｃ─Ｈａ─ｒａｓ基因的转录，从而抑制胃癌ＢＧＣ８２３细胞的增殖。DNA topoisomerase Ⅱ was isolated from gastric cancer BGC823 cellsand its activity was determined by using pBR322 DNA as the substrate. The experimentsshowed that the activity of DNA topoisomerase Ⅱ that catalyzed pBR322 DNA breakingand relaxing may be increased in the presence of the nucleotide derivative-NB901. At thesame time, NB901 may also inhibit the c-Ha-ras gene expressison of gastric cancer BGC-823 cells.This study suggested that DNA topoisomerase Ⅱ of the cancer cells may be thetarget of antitumor agent-NB901. Cellular topoisomerase Ⅱ might be involved in the tra-transcriptional regulation of genes required for cellular proliferation. NB901 have an effecton the cellular c-Ha-ras gene transcription and may effectively inhibit malignant prolife-ration of gastric cancer cells.

关 键 词：NB901 拓扑酶II 胃癌细胞 C-HA-RAS 基因 DNA 

分 类 号：R735.203[医药卫生—肿瘤] R730.3[医药卫生—临床医学]