Xiao D M, Zhou W H, Zhang Y H, Wang X L, Zhu B, Zhang J B, Yang G D, Chen H C
Institute of Basic Medical Sciences, Chinese Academy of Medical Sciences, Beijing.
Yao Xue Xue Bao. 1993;28(7):494-8.
Protein kinase C(PKC) and protein kinase A(PKA) purified from rat liver were incubated with (-)- and (+)-gossypol. The activity of PKC was significantly inhibited in a concentration-dependent manner by both (-)-gossypol and (+)-gossypol. (-)-gossypol was found to inhibit type I PKA, whereas the inhibitory action of (+)-gossypol for type I PKA was less potent. Both (-)-gossypol and (+)-gossypol showed inhibition for type II PKA only at high concentration. These results suggest that administration of gossypol might impair cellular signal transduction.
从大鼠肝脏中纯化得到的蛋白激酶C(PKC)和蛋白激酶A(PKA)与(-)-和(+)-棉酚一起孵育。(-)-棉酚和(+)-棉酚均以浓度依赖性方式显著抑制PKC的活性。发现(-)-棉酚抑制I型PKA,而(+)-棉酚对I型PKA的抑制作用较弱。(-)-棉酚和(+)-棉酚仅在高浓度时才对II型PKA表现出抑制作用。这些结果表明,棉酚的给药可能会损害细胞信号转导。