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.
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.
G xu, LP zhang, LF Chen , CO Hu, . INHIBITION OFPROTEIN KINASE C BY STILBENOIDSJ. Acta Pharmaceutica Sinica, 1994, 29(11): 818-822.
Citation: G xu, LP zhang, LF Chen , CO Hu, . INHIBITION OFPROTEIN KINASE C BY STILBENOIDSJ. Acta Pharmaceutica Sinica, 1994, 29(11): 818-822.

二苯乙烯类化合物对蛋白激酶C的抑制作用

INHIBITION OFPROTEIN KINASE C BY STILBENOIDS

  • 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。

     

    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.

     

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