摘要
DNA拓扑异构酶是某些抗癌,抗菌药物的靶酶。马来酸酐类聚阴离子化合物具有抗菌、抗病毒、抗瘤活性。普遍认为其作用机理是调节机体免疫功能。作者对20个马来酸酐类聚阴离子化合物,包括:①马来酸酐和呋喃的1:1交替共聚物半铵盐(MFN),②二乙烯基醚和马来酸酐的1:2交替共聚物MVE),③马来酸和呋哺的1:1交替共聚物(MF)。经反复试验,发现其中6个化合物在30μg/ml浓度下对小鼠艾氏腹水癌细胞的DNA拓扑异构酶Ⅱ的性有确定抑制作用。其中MVE_1的最低抑制浓度为5μg/ml。实验提示马来酸酐类聚阴离子化合物对拓扑酶Ⅱ的抑制可能是其抗癌作用机制之一。
It was Known that DNA Topoisomerase is a kind of enzyme which catalyzes the stereoisomery change of DNA and plays important role in the replication of DNA. It was recognized to be the target enzyme of some kinds of antitumor or antibacterial drugs. Maleic anhydride copolymers possess antibacterial, antivirals and antitumor activities in vivo, they have been classified as biological response modifiers (BRM).( In this paper 20 maleic anhydride copolymers including three groups of com pounds:1)semi-ammonium-salt of 1 : 1 re-gulary alternating copolymers of maleic anhydride and furane (MFN);2)the 1 : 2 regulary alternating copolymers of divinyl ether and maleic anhydride (MVE);3) the 1 : 1 regulary alternating copolymers of maleic anhydride and furane (MF)were studied. It was found that 6 of this 20 compounds showed inhibitory effect on the Topoisomerase II extracted from mice bearing Ehrlich ascitic tumor. According to their molecular weights the active agents are denominated as followinsMVE1, MVE2, MVE4, MF1; MF2, MVE6. The inhibitory effect on TOPO II was shown under the concentration of 30μg/ml. Among them MVE1 was the most active one with minimal inhibition concentration of 5μg/ml. Above results may provide new supplementary evidence to the antitumor mechanism of maleic copolymers.
出处
《癌症》
SCIE
CAS
CSCD
北大核心
1991年第4期271-274,共4页
Chinese Journal of Cancer
基金
国家自然科学基金
关键词
马来酸酐
拓扑异构酶Ⅱ
抑制作用
inhibitory effect, maleic anhydride copolymers, Topoisomerase Ⅱ
