吗丙嗪和雷佐生抑制兔红细胞膜钙调蛋白活力的比较  

Comparison between probimane and razoxane on inhibiting calmodulin activity of rabbit erythrocyte membrane

作　　者：卢大用[1] 陈恩鸿[2] 曹静懿 周建军[2] 沈祖铭[1] 胥彬[2] 堀江清史 

机构地区：[1]上海大学生命科学学院,上海200436 [2]中国科学院上海药物研究所,上海200031 [3]日本旭化成工业株式会社,东京1018481

出　　处：《中国药理学与毒理学杂志》2001年第1期76-78,共3页Chinese Journal of Pharmacology and Toxicology

基　　金：上海市高等教育科学技术发展基金资助项目!(97A49)&&

摘　　要：比较了抗癌结构类似物吗丙嗪和雷佐生对红细胞膜钙调蛋白 (CaM)活性的影响 .观察兔红细胞膜Ca2 +,Mg2 + ATP酶 (CaM的靶酶 )活性反映膜CaM激活ATP酶的活性 .结果显示吗丙嗪 ( 0 .1～ 1mmol·L- 1)浓度依赖性抑制CaM激活ATP酶活性 (下降11%～ 32 % ) .雷佐生在高浓度 ( 0 .5mmol·L- 1)仍未显示抑制CaM激活ATP酶活性的作用 .吗丙嗪在低浓度 ( 0 .0 2～ 0 .1mmol·L- 1)能增加N 乙酰神经氨酸( 0 .2mmol·L- 1)抑制CaM激活ATP酶活性的作用 .结果表明吗丙嗪对CaM活性的抑制作用强于雷佐生 ,因而可能在CaM介导的抑瘤途径的作用较雷佐生强 ,且其作用可能与神经氨酸 (唾液酸 )To compare the effects of antitumor derivatives probimane and razoxane on calmodulin(CaM) in rabbit erythrocytes by observing CaM activated Ca 2+ ,Mg 2+ ATPase activity of rabbit erythrocyte membranes. It was showed that probimane (0.1-1.0 mmol·L -1 ) inhibited cell CaM activated Ca 2+ ,Mg 2+ ATPase activity (decreasing 11%-32%) in a dose dependent manner. Razoxane at a concentration of 0.5 mmol·L -1 did not inhibit CaM activated Ca 2+ ,Mg 2+ ATPase activity. Probimane at low concentrations (0.02-0.1 mmol·L -1 ) enhanced the inhibitory effect of N acetylneuraminic acid on CaM activated Ca 2+ ,Mg 2+ ATPase activity. The results manifest that probimane may be more potent to CaM pathways of tumor than razoxane does and its effect might be correlated with neuraminic acids(sialic acids).

关 键 词：钙调蛋白 吗丙嗪 雷佐生 抗肿瘤药物 唾液酸 红细胞膜 

分 类 号：R965[医药卫生—药理学]