Gschwendt M, Horn F, Kittstein W, Marks F
Biochem Biophys Res Commun. 1983 Dec 16;117(2):444-7. doi: 10.1016/0006-291x(83)91220-2.
The flavonoid quercetin is a potent inhibitor of calcium- and phospholipid-dependent protein kinase (Ca, PL-PK) activity from mouse brain. Half-maximal inhibition of the kinase occurs at about 10 microM. If the tumor promoter 12-O-tetradecanoyl-phorbol-13-acetate (TPA) is used instead of calcium as a stimulating factor of the kinase enzyme activity is still inhibited by quercetin. The kinase inhibitor, however, does not interfere with the binding of TPA to its receptor.
类黄酮槲皮素是小鼠脑内钙和磷脂依赖性蛋白激酶(Ca,PL-PK)活性的强效抑制剂。该激酶活性被半最大抑制时槲皮素浓度约为10微摩尔。如果用肿瘤促进剂12-O-十四烷酰佛波醇-13-乙酸酯(TPA)替代钙作为激酶活性的刺激因子,其活性仍会被槲皮素抑制。然而,该激酶抑制剂并不干扰TPA与其受体的结合。