中国药理学与毒理学杂志
中國藥理學與毒理學雜誌
중국약이학여독이학잡지
CHINESE JOURNAL OF PHARMACOLOGY AND TOXICOLOGY
2001年
1期
76-78
,共3页
卢大用%沈祖铭%陈恩鸿%周建军%胥彬%堀江清史%曹静懿
盧大用%瀋祖銘%陳恩鴻%週建軍%胥彬%堀江清史%曹靜懿
로대용%침조명%진은홍%주건군%서빈%굴강청사%조정의
钙调蛋白%吗丙嗪%雷佐生%抗肿瘤药物%唾液酸
鈣調蛋白%嗎丙嗪%雷佐生%抗腫瘤藥物%唾液痠
개조단백%마병진%뢰좌생%항종류약물%타액산
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(0.02~0.1mmol.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)有关.
比較瞭抗癌結構類似物嗎丙嗪和雷佐生對紅細胞膜鈣調蛋白(CaM)活性的影響.觀察兔紅細胞膜Ca2+,Mg2+-ATP酶(CaM的靶酶)活性反映膜CaM激活ATP酶的活性.結果顯示嗎丙嗪(0.1~1mmol.L-1)濃度依賴性抑製CaM激活ATP酶活性(下降11%~32%).雷佐生在高濃度(0.5mmol.L-1)仍未顯示抑製CaM激活ATP酶活性的作用.嗎丙嗪在低濃度(0.02~0.1mmol.L-1)能增加N-乙酰神經氨痠(0.2mmol.L-1)抑製CaM激活ATP酶活性的作用.結果錶明嗎丙嗪對CaM活性的抑製作用彊于雷佐生,因而可能在CaM介導的抑瘤途徑的作用較雷佐生彊,且其作用可能與神經氨痠(唾液痠)有關.
비교료항암결구유사물마병진화뢰좌생대홍세포막개조단백(CaM)활성적영향.관찰토홍세포막Ca2+,Mg2+-ATP매(CaM적파매)활성반영막CaM격활ATP매적활성.결과현시마병진(0.1~1mmol.L-1)농도의뢰성억제CaM격활ATP매활성(하강11%~32%).뢰좌생재고농도(0.5mmol.L-1)잉미현시억제CaM격활ATP매활성적작용.마병진재저농도(0.02~0.1mmol.L-1)능증가N-을선신경안산(0.2mmol.L-1)억제CaM격활ATP매활성적작용.결과표명마병진대CaM활성적억제작용강우뢰좌생,인이가능재CaM개도적억류도경적작용교뢰좌생강,차기작용가능여신경안산(타액산)유관.
To compare the effects of antitumor derivatives probimane andrazoxane on calmodulin(CaM) in rabbit erythrocytes by observing CaM activated Ca2+,Mg2+-ATPase activity of rabbit erythrocyte membranes. It was showed that probimane (0.1-1.0 mmol.L-1) inhibited cell CaM activated Ca2+,Mg2+-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 Ca2+,Mg2+-ATPase activity. Probimane at low concentrations (0.02-0.1 mmol.L-1) enhanced the inhibitory effect of N-acetylneuraminic acid on CaM activated Ca2+,Mg2+-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).