Lee P C, Dasmahaptra A K
Department of Pediatrics, Medical College of Wisconsin, Milwaukee 53226.
Chem Biol Interact. 1994 Oct;93(1):1-10. doi: 10.1016/0009-2797(94)90081-7.
1-Ethynylpyrene (EP) inhibits microsomal 7-ethoxyresorufin O-deethylase (EROD) activities from the liver of both trout and rat. Trout hepatocytes treated with EP had increased microsomal EROD activity and a concomitant increase in CYPIA1 protein as measured by Western blot analysis. EP at 10(-9)-10(-6) M did not interfere with beta-naphthoflavone (BNF) induction of CYPIA1 in trout hepatocytes. In contrast, treatment with alpha-naphthoflavone (ANF), another inhibitor of CYPIA1, resulted in a significant inhibition of the basal (at 10(-6) M ANF) and BNF induced (at 10(-8) M and higher concentrations of ANF) level of EROD activity. ANF also did not significantly induce CYPIA1 protein but led to attenuation of the induction of CYPIA1 proteins by BNF in trout hepatocyte cultures. Thus, in trout hepatocytes, EP acts differently from ANF in the modulation of CYPIA1.
1-乙炔基芘（EP）抑制虹鳟鱼和大鼠肝脏微粒体7-乙氧基异吩恶唑酮O-脱乙基酶（EROD）的活性。用EP处理的虹鳟鱼肝细胞微粒体EROD活性增加，同时通过蛋白质印迹分析测得CYPIA1蛋白也相应增加。10^(-9)-10^(-6) M的EP不干扰β-萘黄酮（BNF）对虹鳟鱼肝细胞中CYPIA1的诱导作用。相反，用另一种CYPIA1抑制剂α-萘黄酮（ANF）处理，会显著抑制基础水平（10^(-6) M ANF时）以及BNF诱导水平（10^(-8) M及更高浓度的ANF时）的EROD活性。ANF也不会显著诱导CYPIA1蛋白，但会导致虹鳟鱼肝细胞培养物中BNF对CYPIA1蛋白的诱导作用减弱。因此，在虹鳟鱼肝细胞中，EP在调节CYPIA1方面的作用与ANF不同。
