Prostaglandin endoperoxides and thromboxanes: role in platelets and in vascular and respiratory smooth muscle.

Prostaglandin endoperoxides and thromboxanes: role in platelets and in vascular and respiratory smooth muscle.
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前列腺素内过氧化物和血栓素:在血小板以及血管和呼吸平滑肌中的作用。

DOI:
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发表时间:
1976
期刊:
Acta biologica et medica Germanica
影响因子:
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通讯作者:
B. Samuelsson
B. Samuelsson
中科院分区:
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文献类型:
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作者:
B. Samuelsson

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1. 两组不稳定的(1/2 = 5分钟)内过氧化物,PGG和PGH化合物,已经被分离出来,并被证明是前列腺素的前体。2. 从内过氧化物中衍生出了一类新的化合物(血栓烷)。迄今为止,已在血小板、白细胞、肺组织、脾脏、肾脏和脐动脉中发现了血栓烷。在血小板中,血栓烷是内过氧化物的主要产物。3. 在内过氧化物和凝血素B2之间检测到一种高度不稳定(t1 /2 = 30-40 s)的中间体血栓素A2。结构分析表明它具有双环氧环辛烷结构。4. 血栓素A2诱导血小板聚集,引起离体兔主动脉收缩。PIPER和VANE发现的兔主动脉收缩物质(RCS)主要由血栓素A2和一定程度的内过氧化物PGG2和PGH2组成。5. 内过氧化物和凝血烷是血小板聚集所必需的。血小板环加氧酶缺乏症由于释放机制异常而引起止血缺陷。6. 内过氧化物对血管和气道平滑肌有独特的作用。这种效果不是由于转化为稳定的前列腺素(PGE, PGF等)。7. 多不饱和脂肪酸经环加氧酶催化途径形成的生物活性化合物根据其稳定性可分为三大类,即稳定的前列腺素(PGE等)、内过氧化物(PGG和PGH)和凝血酶。
1. Two groups of unstable (t 1/2 = 5 min) endoperoxides, PGG and PGH compounds, have been isolated and shown to be precursors of the prostaglandins. 2. A new group of compounds (thromboxanes) derived from the endoperoxides has been discovered. Thromboxanes have so far been found in platelets, leucocytes, lung tissue, spleen, kidney and umbilical artery. In platelets the thromboxane constitute the major products derived from the endoperoxides. 3. A highly unstable (t 1/2 = 30-40 s) intermediate, thromboxane A2, between the endoperoxides and thromboxane B2 has been detected. Structural work indicates that it has a bicyclic oxaneoxetane structure. 4. Thromboxane A2 induces platelet aggregation and causes contraction of the isolated rabbit aorta. Rabbit aorta contracting substance (RCS) discovered by PIPER and VANE consists mainly of thromboxane A2 and to some extent of the endoperoxides PGG2 and PGH2. 5. Endoperoxides and thromboxanes are essential for platelet aggregation. Platelet cyclo-oxygenase deficiency gives rise to a hemostatic defect due to an abnormal release mechanism. 6. The endoperoxides have unique actions on vascular and air-way smooth muscle. The effects are not due to conversion to the stable prostaglandins (PGE, PGF etc). 7. The biologically active compounds formed from polyunsaturated fatty acids via the cyclo-oxygenase catalyzed pathway can be divided into three groups depending on the stability, viz. the stable prostaglandins (PGE etc.), the endoperoxides (PGG and PGH) and the thromboxanes.