摘要
目的研究盐酸槐定碱对DNA拓扑异构酶I和酶II(TOPO I、II)活性的影响。方法DNA超螺旋解旋法检测盐酸槐定碱注射液对拓扑异构酶I及酶II介导的PBR322 DNA解旋反应的影响。结果盐酸槐定碱注射液能明显抑制TOPOI介导的DNA解旋及断裂,在终浓度为6 250μg/m l和3 215μg/m l时对拓扑异构酶I均有抑制作用,且剂量--效应关系密切,但对拓扑异构酶II介导的DNA解旋反应无影响。结论结果提示盐酸槐定碱注射液的直接作用靶点是DNA拓扑异构酶I,该药为拓扑异构酶I抑制剂。
Objective The purpose of this study was to investigate the principle of activity of promoting DNA topoisomerase. Methods The effect of Sophoridine hydrochlorium on topoisomerase was measured by supereoiled DNA relaxation assay. Results Sophoridine hydrochlorium could markedly inhibit the activity of topoisomerase Ⅰ, by 6250μg/ml and 3215μg/ml respectively, could not prove that it inhibited the activity of topoisomerase Ⅱ Condusion It may be the fact that DNA topoisomerase Ⅰ is a direct target in antitumor activity of Sophoridine hydrochlorium.
出处
《时珍国医国药》
CAS
CSCD
北大核心
2006年第6期986-987,共2页
Lishizhen Medicine and Materia Medica Research
关键词
盐酸槐定碱
拓扑异构酶
活性作用
Sophoridine hydrochlorium
DNA topoisomerase
antitumor activity
