摘要
部分纯化的大鼠肝脏蛋白激酶C和蛋白激酶A,在体外与棉酚的旋光异构体分别温育,结果(--)棉酚和(+)棉酚对蛋白激酶C活力均有剂量依赖性的抑制作用;(-)棉酚对Ⅰ型蛋白激酶A活力的抑制作用明显比(+)棉酚强,而(-)棉酚和(+)棉酚在高浓度时对Ⅱ型蛋白激酶A才显示抑制作用。结果提示棉酚在体内可能干扰细胞信息的传递过程。
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.
出处
《药学学报》
CAS
CSCD
北大核心
1993年第7期494-498,共5页
Acta Pharmaceutica Sinica
基金
国家自然科学基金
关键词
棉酚
蛋白激酶C
蛋白激酶A
Gossypol
Protein kinase C
Protein kinase A
