芫花酯甲是蛋白激酶C Phorbol esters受体的特异性拮抗剂

本文用DE-52离子交换、Sephadex G-200凝胶过滤和phenyl-Sepharose亲和层析等柱层析,从大鼠脑中分离和纯化蛋白激酶C,并应用~3H-phorbol-12,13-dibutyrate(~3H-PdBu)结合蛋白激酶C的试验方法,研究了芫花酯甲对蛋白激酶C的结合特性。芫花酯甲对Ca~(2+),PS激活蛋白激酶C催化组蛋白Ⅲ-s磷酸化无任何影响,但它可以完全拮抗在同样测试系统中PdBu对蛋白激酶C的激动作用,结果提示芫花酯甲与PdBu作用在蛋白激酶C的相同部位,是后者的特异性拮抗剂。     

Yuanhuacin A Is a Selective Antagonist of Phorbol Ester Receptor in Protein Kinase C

Protein kinase C with a molecular weight of 82 kD has been purified to electrophoresis homogenous from rat brain through a series of chromatography columns including DE-52, Sepharose G-200 and phenyl-Sepharose. The enzyme possessed autophosphorylation activity. Yuanhuacin A inhibited the ~3H-phorbol-12, 13-dibutyrate (~3H-PdBu) binding of PKC with an IC_(50) value of 1.48±0.28×10~(-8) mol/L when the concentration of ~3H-PdBu was 1.5×10~(-9) mol/L (K_i=1.2×10~(-8) mol/L). Yuanhuacin A inhibited the PdBu-stimulated PKC activity in the catalysis of the phosphorylation of Histone Ⅲ-S with an IC_(50) of 2.82±0.37×10~(-9) mol/L (PdBu=10~(-6) mol/L), while it had no effect on the basal and Ca~(2+)-stimulated PKC activity in the same assay system. This result suggests that Yuanhuacin A is a selective antagonist of the phorbol ester receptor in protein kinase C.     

车辆点火脉冲对短波电磁环境影响的数值模拟与试验研究

为评估车辆点火脉冲对短波接收站电磁环境的影响，首先分析了车辆点火原理模型，并测试了小轿车、卡车两种典型车辆的点火脉冲生成的频域噪声；其次利用基于距量法的电磁计算软件对小轿车、卡车的点火脉冲等效天线与10 m单极子接收天线之间的传输效应进行了数值模拟与分析，获得传输损耗波动曲线。最后通过3辆汽车点火实测对乡村短波接收站的电磁环境影响进行了对比分析。仿真与实测结果表明:卡车点火脉冲辐射功率高于小轿车辐射功率14 dB；车辆点火脉冲等效天线相对于10 m单极子接收天线，在7.5 MHz传输损耗最小，相距30，100 m时传输损耗分别为24，32.2 dB；试验中，在30 m距离处，3辆小汽车点火脉冲对短波电磁环境的影响为抬高了低频段底噪1～2 dB，当距离增加到100 m以上时，已无明显影响。