一种9,11-偶氮前列腺素的合成及生物学特性：前列腺素内过氧化物的高活性生化模拟物
Synthesis and biological properties of a 9,11-azo-prostanoid: highly active biochemical mimic of prostaglandin endoperoxides.
作者信息
Corey E J, Nicolaou K C, Machida Y, Malmsten C L, Samuelsson B
出版信息
Proc Natl Acad Sci U S A. 1975 Sep;72(9):3355-8. doi: 10.1073/pnas.72.9.3355.
Abstract
The 9,11-azo-prostanoid III [(5Z, 9alpha, 11alpha, 13E, 15S)-9, 11-azo-15-hydroxyprosta-5,13-dienoic acid] has been obtained by synthesis and tested for biological activity in systems which are responsive to the prostaglandin endoperoxides PGH2 (I) and PGG2 (II). The azo analog III is a powerful mimic of these endoperoxides with reference to platelet aggregation and release of serotonin when added to human platelet-rich plasma. The analog III is substantially more active (about 7 fold) than PGG2 in stimulating muscle contraction in the isolated rabbit aorta strip. The very great stability of III relative to PGH2 and PGG2 and its potency as a mimic of these important substances suggest that this azo analog will be of considerable value in future studies of the prostaglandin endoperoxides.
摘要
9,11-偶氮前列腺素III [（5Z,9α,11α,13E,15S）-9,11-偶氮-15-羟基前列腺-5,13-二烯酸] 已通过合成获得，并在对前列腺素内过氧化物PGH2（I）和PGG2（II）有反应的系统中测试了其生物活性。当添加到富含人血小板的血浆中时，偶氮类似物III在血小板聚集和血清素释放方面是这些内过氧化物的有力模拟物。在刺激离体兔主动脉条肌肉收缩方面，类似物III比PGG2活性强得多（约7倍）。III相对于PGH2和PGG2具有非常高的稳定性，并且作为这些重要物质的模拟物具有效力，这表明这种偶氮类似物在未来前列腺素内过氧化物的研究中将具有相当大的价值。
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Synthesis and biological properties of a 9,11-azo-prostanoid: highly active biochemical mimic of prostaglandin endoperoxides.一种9,11-偶氮前列腺素的合成及生物学特性：前列腺素内过氧化物的高活性生化模拟物
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