ACTIVATION OF PROTEIN-KINASE-C FROM GUINEA-PIG AND RAT VENTRICULAR MUSCLES BY MUSCLIDE-A1 AND ITS (2R,5S)-DIASTEREOMER

被引:6
|
作者
KIMURA, I [1 ]
TAKAMURA, Y [1 ]
UWANO, T [1 ]
HATA, Y [1 ]
KIMURA, M [1 ]
KIKUCHI, T [1 ]
机构
[1] TOYAMA MED & PHARMACEUT UNIV,RES INST WAKAN YAKU ORIENTAL MED,TOYAMA 93001,JAPAN
关键词
VENTRICULAR PROTEIN KINASE C; MUSCLIDE-A1; (2R; 5S)-DIASTEREOMER; 1,2-DIOCTANOYL GLYCEROL;
D O I
10.1002/ptr.2650090105
中图分类号
R914 [药物化学];
学科分类号
100701 ;
摘要
The activating effects of musclide-A1, 6-methyl-2,5-heptanediol 5-(hydrogen sulphate) (la), and its (2R, 5S)- and (2R, SR)-diastereomers on ventricular protein kinase C from guinea-pig and rat were compared with other natural compounds derived from musk and non-natural related compounds, The (2R, 5S)-diastereomer was most potent among musk-derived compounds and its related non-natural compounds. The activation by la (20 mu M) was produced in the presence of low [Ca2+](0) and phosphatidylserine like 1,2-dioctanoylglycerol (2 mu M). The activation pattern for peaks eluted by a hydroxyapatite column demonstrated that la activates ventricular-specific protein kinase C peak II, suggesting one mechanism for the beta-adrenergic cardiotonic potentiation by 1a.
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页码:16 / 20
页数:5
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