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血小板中的前列腺素生物合成:前列腺素H2转化为E2异构酶的证明及其作用

Prostaglandin biosynthesis in platelets: demonstration and role of prostaglandin H2 leads to E2 isomerase.

作者信息

Raz A, Aharony D

出版信息

Res Commun Chem Pathol Pharmacol. 1978 Sep;21(3):507-15.

PMID:705027
Abstract

Double-labeled [3H/14C]-prostaglandin endoperoxide H2 was used to assess the presence in platelets of enzymatic activity for conversion of the endoperoxides to prostaglandin E2. This enzymatic activity (prostaglandin H2 leads to E2 isomerase) involves the selective removal of a hydrogen from the C-9 carbon atom of the endoperoxide molecule and is subject to an isotope discriminatory effect against tritium-labeled molecules. Rabbit washed platelet suspension was pre-incubated for 1 min, with imidazole (1 mM) to inhibit thromboxane A2 generation and [3H/14C]--prostaglandin H2 was added. Analysis of the [3H] and [14C] radioactive products in incubations with native vs. heat denatured platelets indicated that native platelets convert the endoperoxide enzymatically to mainly prostaglandin E2. Thus, although arachidonic acid released endogenously or added exogenously to platelets is converted mainly to thromboxane B2 and 120H-17:3 acid, platelets appear to possess prostaglandin H2 leads to E2 isomerase activity which becomes manifested when thromboxane synthetase activity is inhibited.

摘要

使用双标记的[3H/14C] - 前列腺素内过氧化物H2来评估血小板中存在将内过氧化物转化为前列腺素E2的酶活性。这种酶活性(前列腺素H2转化为E2异构酶)涉及从内过氧化物分子的C-9碳原子上选择性去除一个氢,并且对氚标记的分子存在同位素歧视效应。将兔洗涤血小板悬液用咪唑(1 mM)预孵育1分钟以抑制血栓素A2的生成,然后加入[3H/14C] - 前列腺素H2。对天然血小板与热变性血小板孵育中的[3H]和[14C]放射性产物的分析表明,天然血小板可将内过氧化物酶促转化为主要是前列腺素E2。因此,尽管内源性释放或外源性添加到血小板中的花生四烯酸主要转化为血栓素B2和12-羟基-17:3酸,但血小板似乎具有前列腺素H2转化为E2异构酶活性,当血栓素合成酶活性受到抑制时该活性会表现出来。

相似文献

1
Prostaglandin biosynthesis in platelets: demonstration and role of prostaglandin H2 leads to E2 isomerase.血小板中的前列腺素生物合成:前列腺素H2转化为E2异构酶的证明及其作用
Res Commun Chem Pathol Pharmacol. 1978 Sep;21(3):507-15.
2
Kinetic studies on the conversion of prostaglandin endoperoxide PGH2 by thromboxane synthase.血栓素合酶对前列腺素内过氧化物PGH2转化的动力学研究。
Prostaglandins. 1978 Oct;16(4):563-70. doi: 10.1016/0090-6980(78)90186-7.
3
Selective inhibition of prostaglandin endoperoxide thromboxane isomerase by 1-carboxyalkylimidazoles.1-羧基烷基咪唑对前列腺素内过氧化物血栓素异构酶的选择性抑制作用。
Prostaglandins. 1978 Oct;16(4):529-40. doi: 10.1016/0090-6980(78)90183-1.
4
[Kinetic mechanisms of enzyme activity of the thromboxane synthetase system. Thromboxane synthetase of human platelets].[血栓素合成酶系统的酶活性动力学机制。人血小板的血栓素合成酶]
Biokhimiia. 1984 Sep;49(9):1538-45.
5
Interactions of prostaglandin H2 and thromboxane A2 with human serum albumin.前列腺素H2和血栓素A2与人血清白蛋白的相互作用。
Eur J Biochem. 1980 Aug;109(2):561-6. doi: 10.1111/j.1432-1033.1980.tb04828.x.
6
Prostaglandin H2 in human platelet activation: coactivator and substitute for thromboxane A2.前列腺素H2在人血小板激活中的作用:协同激活剂及血栓素A2的替代物
Prog Clin Biol Res. 1989;301:315-9.
7
Platelet and blood vessel arachidonate metabolism and interactions.血小板与血管的花生四烯酸代谢及相互作用。
J Clin Invest. 1979 Feb;63(2):345-9. doi: 10.1172/JCI109309.
8
Transient concentrations and agonist potency of PGH2 in platelet activation by endogenous arachidonate.
Eicosanoids. 1989;2(4):241-8.
9
[Synthesis of thromboxane A2: limiting stages of primary thrombocyte aggregation in humans initiated by arachidonic acid and its metabolic products].[血栓素A2的合成:花生四烯酸及其代谢产物引发的人体原发性血小板聚集的限制阶段]
Biokhimiia. 1984 Dec;49(12):2035-40.
10
An antithrombotic agent, NQ301, inhibits thromboxane A2 receptor and synthase activity in rabbit platelets.一种抗血栓形成剂NQ301可抑制兔血小板中血栓素A2受体和合成酶的活性。
Basic Clin Pharmacol Toxicol. 2005 Sep;97(3):162-7. doi: 10.1111/j.1742-7843.2005.pto_973123.x.

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Inhibition of pulmonary thromboxane A2 synthase activity and airway responses by CGS 13080.CGS 13080对肺血栓素A2合酶活性及气道反应的抑制作用
Mol Cell Biochem. 1989 Jan 23;85(1):29-41. doi: 10.1007/BF00223511.