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丹参酮ⅡA磺酸钠对大鼠心,脑微粒体Na~+,K~+-ATP酶的抑制作用
引用本文:王幼林,陈念航,丁建花.丹参酮ⅡA磺酸钠对大鼠心,脑微粒体Na~+,K~+-ATP酶的抑制作用[J].中国药理学与毒理学杂志,1994(1).
作者姓名:王幼林  陈念航  丁建花
作者单位:南京医科大学药理教研室
摘    要:丹参酮ⅡA磺酸钠(DS-201)体外可逆性抑制大鼠心,脑微粒体Na+,K+ATP酶。并具有浓度依赖性,且对心微粒体Na+,K+-ATP酶的抑制作用较扯降低Na+或ATP浓度则增强或减弱其抑酶作用,动力学分析表明DS-201对脑微粒体Na+,K+-ATP酶的作用近似Na+的竞争性拮抗剂,ATP的反竞争性拮抗剂,有K+及Mg2+存在时则表现为非竞争性或混合型抑制,但对心肌微粒体Na+,K+-ATP酶的作用则略有差别。

关 键 词:磺酸类  丹参酮    钾腺苷三磷酸酶  心脏    微粒体

Inhibitory effects of sodium tanshinone Ⅱ A sulphonate onmicrosomal Na+, K+-ATPase in rat heart and brain
WANG You-Lin,CHEN Nian-Hang, DINGJian-Hua.Inhibitory effects of sodium tanshinone Ⅱ A sulphonate onmicrosomal Na+, K+-ATPase in rat heart and brain[J].Chinese Journal of Pharmacology and Toxicology,1994(1).
Authors:WANG You-Lin  CHEN Nian-Hang  DINGJian-Hua
Abstract:The effects of sodium tanshinoneⅡ A sulphonate (DS-201) on the microsomal Na+,K+-ATPase from hearts and brains of rats were investi-gated in vilro. DS-201 inhibited the enzyme quicklyand reversibly. The inhibition was in a concentration-dependent manner and stronger on heart enzyme thanon that of brain. The DS-201 inhibition was enhancedat low Na+, but weakened at low ATP. Kinetic ana-lyses indicated the competitive nature of theinteraction between Na+ and DS-201 on the enzymeof brain. The DS-201 inhibition was uncompetitive forATP, noncompetitive or mixed type in the presence ofK+ and Mg2+ for the brain enzyme. However, thereare some differences in the action of DS-201 on theheart microsomal Na+. K+-ATPase.
Keywords:sulfonic acids  tanshinone  sodium  potassium adenosine triphosphatase  heart  brain  microsomes
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