| 二苯乙烯类化合物对蛋白激酶C的抑制作用 |
| |
| 引用本文： | 徐光,张礼萍,陈力芳,胡昌奇.二苯乙烯类化合物对蛋白激酶C的抑制作用[J].药学学报,1994,29(11):818-822. |
| |
| 作者姓名： | 徐光 张礼萍 陈力芳 胡昌奇 |
| |
| 作者单位： | 上海医科大学基础医学院生物化学教研室，上海药学院天然药物化学教研室 |
| |
| 摘 要： | 报道15种二苯乙烯类化合物对蛋白激酶C(PKC)活性的影响。其中从中药金雀根中分得的3种二苯乙烯类低聚体α-viniferin,kobophenol A 和 miyabenolC,它们抑制PKC的IC50分别为62.5,52.0和27.5μmol·L-1。另外6种含酚羟基的二苯乙烯化合物对PKC也显示不同程度的抑制作用,但当酚羟基全甲基化或全乙酰化后其抑制作用大大降低甚至消失。酶动力学研究证明miyabenolC对PKC的抑制作用属于非竞争性抑制。
|
| 关 键 词： | 二苯乙烯类 蛋白激酶C 金雀根 |
| 收稿时间： | 1994-03-29 |
INHIBITION OFPROTEIN KINASE C BY STILBENOIDS |
| |
| G xu,LP zhang,LF Chen and CO Hu.INHIBITION OFPROTEIN KINASE C BY STILBENOIDS[J].Acta Pharmaceutica Sinica,1994,29(11):818-822. |
| |
| Authors: | G xu LP zhang LF Chen and CO Hu |
| |
| Abstract: | The effect of 15stilbenolus on protein kinase C(PKC)was studied in order tosearch for naturally occurring PKC inhibitors.All these compounds were isolated from Chinesemedicines. Three oligomeric stilbenes from Caragana sinica,α-viniferin ,kobophenol A and miyabenolC,were shown to intensely inhibit the activity of patially purified rat brain PKC with IC50 values of62.5 ,52.0 ,and 27.5 μmol.L-1 ,respectivel Kinetic analyses revealed that the inhibition wasnoncompetitive. The other compounds also showed the effect.Monomer stilbenes exhibited PKCinhibitory activity at higher μmol·L-1 concentrations than oligomeric stilbenes.Whenever they aremethylated or acetylated perfectly , the inhibition weekens or disappears. |
| |
| Keywords: | Stilbenoids Protein kinase C Caragana sinica |
| 本文献已被 CNKI 维普 等数据库收录！ |
| 点击此处可从《药学学报》浏览原始摘要信息 |
| 点击此处可从《药学学报》下载免费的PDF全文 |
|
