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从电鳗的电器官中寻找一种“哇巴因样”物质,结果发现了花生四烯酸及相关脂肪酸。

A search for an 'ouabain-like' substance from the electric organ of Electrophorus electricus which led to arachidonic acid and related fatty acids.

作者信息

Bidard J N, Rossi B, Renaud J F, Lazdunski M

出版信息

Biochim Biophys Acta. 1984 Jan 11;769(1):245-52. doi: 10.1016/0005-2736(84)90029-4.

DOI:10.1016/0005-2736(84)90029-4
PMID:6318825
Abstract

The electric organ of Electrophorus electricus contains substances which inhibit (Na+ + K+)-ATPase activity, the specific binding of [3H]ouabain to purified (Na+ + K+)-ATPase and 86Rb+ uptake by chick cardiac cells in culture. The active organic material was extracted from microsomal membranes. Its purification was carried out by chromatography on Sep-Pak C-18 and thin-layer chromatography. Reverse-phase liquid chromatography and mass spectrometry identified the active material as a mixture of unsaturated fatty acids. Linoleic (18:2), arachidonic (20:4), linolenic (18:3) and docosahexaenoic acids (22:6) contributed to about 60% of the total activity of the active material. The other active substances could be arachidonic analogs, since they have both a lipophilic and carboxylic character. Pure unsaturated fatty acids have been shown to be active in the different biological assays used to analyze the endogenous 'ouabain-like' activity. Linolenic, arachidonic and docosahexaenoic acids were the most active, whereas saturated fatty acids and glyceryl esters or methyl esters of unsaturated fatty acids were inactive. It is possible that in pathological situations in which the level of unsaturated fatty acids increases, these molecules may then act as physiological inhibitors of the sodium pump.

摘要

电鳗的电器官含有抑制(Na⁺ + K⁺)-ATP酶活性、[³H]哇巴因与纯化的(Na⁺ + K⁺)-ATP酶特异性结合以及培养的鸡心肌细胞对⁸⁶Rb⁺摄取的物质。活性有机物质是从微粒体膜中提取的。通过Sep-Pak C-18柱色谱和薄层色谱进行纯化。反相液相色谱和质谱鉴定活性物质为不饱和脂肪酸混合物。亚油酸(18:2)、花生四烯酸(20:4)、亚麻酸(18:3)和二十二碳六烯酸(22:6)约占活性物质总活性的60%。其他活性物质可能是花生四烯酸类似物,因为它们兼具亲脂性和羧基特性。已表明纯不饱和脂肪酸在用于分析内源性“类哇巴因”活性的不同生物学测定中具有活性。亚麻酸、花生四烯酸和二十二碳六烯酸活性最强,而饱和脂肪酸以及不饱和脂肪酸的甘油酯或甲酯则无活性。在不饱和脂肪酸水平升高的病理情况下,这些分子可能会作为钠泵的生理抑制剂发挥作用。

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1
A search for an 'ouabain-like' substance from the electric organ of Electrophorus electricus which led to arachidonic acid and related fatty acids.从电鳗的电器官中寻找一种“哇巴因样”物质,结果发现了花生四烯酸及相关脂肪酸。
Biochim Biophys Acta. 1984 Jan 11;769(1):245-52. doi: 10.1016/0005-2736(84)90029-4.
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Binding of unsaturated fatty acids to Na+, K(+)-ATPase leading to inhibition and inactivation.不饱和脂肪酸与钠钾ATP酶结合,导致抑制和失活。
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Affinity labeling of the digitalis receptor with p-nitrophenyltriazene-ouabain, a highly specific alkylating agent.用地高辛受体与对硝基苯基三氮烯哇巴因(一种高度特异性烷基化剂)进行亲和标记。
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Identification of Na+/K+-ATPase inhibitors in bovine plasma as fatty acids and hydrocarbons.牛血浆中作为脂肪酸和碳氢化合物的钠钾ATP酶抑制剂的鉴定。
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J Neurochem. 1980 Sep;35(3):753-5. doi: 10.1111/j.1471-4159.1980.tb03719.x.

引用本文的文献

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Interactions of K+ATP channel blockers with Na+/K+-ATPase.钾离子ATP通道阻滞剂与钠钾ATP酶的相互作用。
Mol Cell Biochem. 2007 Dec;306(1-2):231-7. doi: 10.1007/s11010-007-9574-7. Epub 2007 Aug 25.
2
Inhibition of human colonic (Na+ + K+)-ATPase by arachidonic and linoleic acid.花生四烯酸和亚油酸对人结肠(钠+钾)-ATP酶的抑制作用。
Naunyn Schmiedebergs Arch Pharmacol. 1986 Apr;332(4):398-402. doi: 10.1007/BF00500094.
3
The receptor function of the Na+, K+-activated adenosine triphosphatase system.钠钾激活的三磷酸腺苷酶系统的受体功能。
Biochem J. 1985 Apr 1;227(1):1-11. doi: 10.1042/bj2270001.