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首页> 外文期刊>Life sciences >THE RELAXANT ACTION OF JATROPHONE IN RAT PORTAL VEIN - A COMPARISON WITH PROTEIN KINASE C INHIBITORS
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THE RELAXANT ACTION OF JATROPHONE IN RAT PORTAL VEIN - A COMPARISON WITH PROTEIN KINASE C INHIBITORS

机译：葛根酮对大鼠门静脉的放松作用-与蛋白质激酶C抑制剂的比较。

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Jatrophone, staurosporine and H-7, caused graded inhibition of rat portal vein contractions induced by phorbol 12-myristate 13-acetate (PMA), noradrenaline, endotllelin-1 or KCl, with IC(50)s of 86 nM, 13 mu M, 11 mu M and 9 mu M, respectively. Jatrophone was equipotent to H-7, but 100 to 500 fold less potent than staurosporine. Jatrophone, H-7 and staurosporine, also dose-dependently inhibited rhythmic contractions of tile rat portal-mesenteric vein with IC(50)s of 15 mu M, 9 mu M and 75 nM, respectively. Jatrophone, H-7 and staurosporine caused graded relaxations of preparations contracted with endothelin-1 or PMA with IC(50)s of 12 and > 1000 mu M, 8 and 13 mu M and 7 and 12 nM, respectively. All three compounds caused graded inhibition of caffeine-induced contractions in Ca2+-free solution containing EGTA. The similarity between the vasorelaxant actions of jatrophone, staurosporine and H-7 in rat portal vein suggests that jatrophone acts, at least in part, through inhibition of PKC-dependent mechanisms. Moreover, like the PKC inhibitors, its vasorelaxant action may also involve other mechanisms unrelated to protein kinase C inhibition. [References: 33]
机译：麻风树菌，星形孢菌素和H-7导致大鼠佛波醇12-肉豆蔻酸酯13-乙酸酯（PMA），去甲肾上腺素，内皮素-1或KCl诱导的大鼠门静脉收缩的分级抑制，IC（50）s为86 nM，13μM分别为11微米和9微米。麻风车对H-7具有同等效力，但效力比十字孢菌素低100至500倍。 Jatrophone，H-7和星形孢菌素也剂量依赖性地抑制瓦特大鼠门-肠系膜静脉的节律性收缩，其IC（50）分别为15μM，9μM和75 nM。 Jatrophone，H-7和星形孢菌素引起与内皮素-1或PMA收缩的制剂的分级松弛，IC（50）分别为12和> 1000μM，8和13μM，7和12 nM。在含有EGTA的无Ca2 +溶液中，所有这三种化合物均导致咖啡因诱导的收缩的分级抑制。麻疯树，星形孢菌素和H-7在大鼠门静脉中的血管舒张作用之间的相似性表明，麻疯树的作用至少部分是通过抑制PKC依赖性机制来实现的。此外，像PKC抑制剂一样，其血管舒张作用也可能涉及其他与蛋白激酶C抑制无关的机制。 [参考：33]

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