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从海洋腔肠动物中分离出的岩沙海葵毒素。对(钠,钾)-ATP酶的抑制作用。

Palytoxin isolated from marine coelenterates. The inhibitory action on (Na,K)-ATPase.

作者信息

Ishida Y, Takagi K, Takahashi M, Satake N, Shibata S

出版信息

J Biol Chem. 1983 Jul 10;258(13):7900-2.

PMID:6134726
Abstract

Palytoxin (PTX), C129H223N3O54, a highly toxic substance isolated from zoanthids of Palythoa tuberculosa, inhibited (Na,K)-ATPase (ATP phosphohydrolase, EC 3.6.1.3) prepared from guinea pig heart and hog cerebral cortex in a dose-dependent manner at concentrations greater than 10(-8) M. In the presence of Na (100 mM) and K (20 mM), PTX showed potency nearly equal to that of ouabain. When the ATPase was activated by the various Na concentrations at a constant K concentration, both PTX and ouabain inhibited the ATPase activity noncompetitively. On the other hand, when K concentration was changed at a constant Na concentration, PTX caused a competitive inhibition in all ranges of K concentrations employed, whereas ouabain caused a competitive inhibition at low concentrations and a noncompetitive inhibition at high concentrations.

摘要

岩沙海葵毒素(PTX),化学式为C129H223N3O54,是一种从瘤海葵属的海葵中分离出的剧毒物质,在浓度高于10^(-8) M时,它能以剂量依赖的方式抑制豚鼠心脏和猪脑皮层制备的(钠,钾)-ATP酶(ATP磷酸水解酶,EC 3.6.1.3)。在存在100 mM钠和20 mM钾的情况下,PTX的效力几乎与哇巴因相当。当ATP酶在恒定的钾浓度下被不同的钠浓度激活时,PTX和哇巴因均非竞争性地抑制ATP酶活性。另一方面,当在恒定的钠浓度下改变钾浓度时,PTX在所使用的所有钾浓度范围内均引起竞争性抑制,而哇巴因在低浓度时引起竞争性抑制,在高浓度时引起非竞争性抑制。

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