【摘要】 本实验测定了19种黄酮类化合物对蛋白激酶C（PKC）活性的影响,并初步探讨了化学结构与活性之间的关系。其中从中药灯盏花中分离得到的野黄岑甙元和从黄芩中分离得到的黄芩素抑制PKC的IC₅₀分别为48μmol/L和76μmol/L,并观察到野黄芩甙元在Ca²⁺浓度10^-2至10^-7mol/L时都显示对PKC的抑制作用,这种作用也不因二油酰甘油酯或底物组蛋白的浓度增加而逆转,说明野黄芩甙元对PKC的作用属于非竞争性抑制。更多还原

【Abstract】 We studied the effects of 19 navonoids representing several different chemical classes on the activity of partially purified rat brain protein kinase C(PKC). Most of the navonoids were isolated from the Chinese hei’b drug Huang-Qin (Scuiellarw baicalensis) and Deng-Zhan-Hua (Erigeronbreviscapus). Scutellarin and baioalein have been shown to inhibit PKO with IC50 values of 48 and 76μmol/L respectively. Inhibition was observed at all cocentrations of Oa2+ between 10-s and 10-7mol/L. Inhibition of PKO activity could not be reversed by increasing the concentration of diacylglycerol or the substrate histone. Kinetic analyses revealed that the inhibition is noncompetitive.更多还原