半边旗有效化合物对肺癌细胞DNA拓扑异构酶、TPK及c-myc基因的影响  

Effect of active compounds isolated from Pteris Semipinnata L on DNA topoisomerases and tyrosine protein kinase and expression c myc of in lung adenocarcinoma cells

作　　者：李金华[1] 梁念慈[1] 莫丽儿[2] 张晓[1] 何承伟[1] 

机构地区：[1]广东医学院医用生化研究所,广东湛江524023 [2]广东医学院化学教研室,广东湛江524023

出　　处：《癌症》2000年第8期763-767,共5页Chinese Journal of Cancer

基　　金：广东省科委重大科技攻关项目!(N09622007 -002);国家自然科学基金!(批准号 :39870900)

摘　　要：研究半边旗有效化合物6F和A对肺癌细胞DNA拓扑异构酶(TOPO)Ⅰ和Ⅱ活性的影响;化合物A对细胞胞浆和胞膜酪氨酸蛋白激酶(TPK)活性及癌基因c -myc蛋白表达的影响。方法 :通过电泳法测定化合物6F和A对肺癌细胞DNA拓扑异构酶(TOPO)Ⅰ、Ⅱ活性的影响;用液体闪烁计数法测定化合物A对酪氨酸蛋白激酶(TPK)活性的影响;流式细胞仪间接荧光检测法测定化合物A对c -myc基因蛋白表达的影响。结果 :化合物6F和A可抑制细胞DNA拓扑异构酶Ⅰ、Ⅱ的活性,1 0mg/L的6F和A即开始抑制TOPOⅠ的活性,随浓度升高抑制作用增强 ;0 01mg/L的6F和10 0mg/L的A对TOPOⅡ的活性有强烈的抑制作用;化合物A对细胞中胞膜TPK活性有一定的抑制作用,但对胞浆TPK的活性几乎没有影响;化合物A对c -myc基因的蛋白表达有抑制作用。结论 :DNA拓扑异构酶是化合物6F和A抑制细胞生长的靶点之一,化合物A对TPK活性有一定的抑制作用,对cObjective: To investigate the effect of active compounds6F and A from Pteris Semipinnata L (PsL)on the activites of DNA topoisomerase(TOPO)Ⅰand Ⅱ, activities of cytosolic and membrane TPK, and expression of oncogene c myc in lung adenocarcinoma cells Methods: The effect of compounds6F and A on activities of TOPOⅠand Ⅱwere assayed by electrophoresis;the effect of compound A on activities of cytosolic and membrane TPK was measureed byscintillation counting;the effect of compound A on expression of oncogene c myc was determined by flow cytomertry indirect fluorimetry Results: Compounds 6F and A inhibited the activities of DNA TOPOⅠand Ⅱ, 1 0 mg/L of 6F or A strongly inhibited the activities of TOPOⅠ, while their strongly inhibition to TOPO Ⅱoccured with the concentration of 0 01 mg/L and 1 0 mg/L respectively Compound A mildly inhibited the activities of membrane TPK,but almost did not inhibite the activities of cytosolic TPK Compound A also inhibited the expression of oncogene c myc Conclusion: Topoisomerases are target of compound 6F and Awhich inhibiting the growth of tumor cells Compound A could slightly inhibit the activities of TPK, and exhibis a inhibitory effect on the expression of oncogene c myc

关 键 词：DNA拓扑异构酶 TPK 肺癌 半边旗有效化合物 

分 类 号：R734.2[医药卫生—肿瘤] R979.1[医药卫生—临床医学]