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核心技术专利：CN118964589B侵权必究

核心技术专利：CN118964589B侵权必究

Lee H S, Jin C B, Chong H S, Yun C H, Park J S, Kim D H

Doping Control Center, Korea Institute of Science and Technology, Seoul.

Xenobiotica. 1994 Nov;24(11):1053-62. doi: 10.3109/00498259409038665.

The metabolism of 7,8-benzoflavone (ANF) was studied in human liver microsomal fractions. Five metabolites were generated and tentatively identified as ANF 5,6-oxide, 5,6-dihydrodiol, 7,8-dihydrodiol, 6-hydroxy ANF, and 7-hydroxy ANF based on UV and mass spectral analysis. 2. The involvement of P4503A in the metabolism of ANF was confirmed by the following observations: (1) correlation of ANF 5,6-oxide formation was noted with testosterone 6 beta-hydroxylation, an indicator of P4503A, in human liver microsomal fractions; (2) metabolism of ANF was inhibited by various selective P4503A enzyme inhibitors; (3) rabbit antibody raised against P4503A4 inhibited the ANF metabolism by > 80%; and (4) microsomal fractions that specifically expressed P4503A4 metabolized ANF to oxidized metabolites. 3. These results indicate that P4503A isoform(s) mainly metabolize ANF to oxidized derivatives in human liver microsomal fractions.

在人肝微粒体组分中研究了7,8-苯并黄酮（ANF）的代谢。生成了五种代谢产物，并根据紫外光谱和质谱分析初步鉴定为ANF 5,6-氧化物、5,6-二氢二醇、7,8-二氢二醇、6-羟基ANF和7-羟基ANF。2. 通过以下观察结果证实了P4503A参与ANF的代谢：（1）在人肝微粒体组分中，观察到ANF 5,6-氧化物的形成与睾酮6β-羟基化（P4503A的一个指标）相关；（2）ANF的代谢受到各种选择性P4503A酶抑制剂的抑制；（3）针对P4503A4产生的兔抗体抑制ANF代谢超过80%；（4）特异性表达P4503A4的微粒体组分将ANF代谢为氧化代谢产物。3. 这些结果表明，在人肝微粒体组分中，P4503A同工型主要将ANF代谢为氧化衍生物。

Lee H S, Jin C B, Chong H S, Yun C H, Park J S, Kim D H

Doping Control Center, Korea Institute of Science and Technology, Seoul.

Xenobiotica. 1994 Nov;24(11):1053-62. doi: 10.3109/00498259409038665.

The metabolism of 7,8-benzoflavone (ANF) was studied in human liver microsomal fractions. Five metabolites were generated and tentatively identified as ANF 5,6-oxide, 5,6-dihydrodiol, 7,8-dihydrodiol, 6-hydroxy ANF, and 7-hydroxy ANF based on UV and mass spectral analysis. 2. The involvement of P4503A in the metabolism of ANF was confirmed by the following observations: (1) correlation of ANF 5,6-oxide formation was noted with testosterone 6 beta-hydroxylation, an indicator of P4503A, in human liver microsomal fractions; (2) metabolism of ANF was inhibited by various selective P4503A enzyme inhibitors; (3) rabbit antibody raised against P4503A4 inhibited the ANF metabolism by > 80%; and (4) microsomal fractions that specifically expressed P4503A4 metabolized ANF to oxidized metabolites. 3. These results indicate that P4503A isoform(s) mainly metabolize ANF to oxidized derivatives in human liver microsomal fractions.

在人肝微粒体组分中研究了7,8-苯并黄酮（ANF）的代谢。生成了五种代谢产物，并根据紫外光谱和质谱分析初步鉴定为ANF 5,6-氧化物、5,6-二氢二醇、7,8-二氢二醇、6-羟基ANF和7-羟基ANF。2. 通过以下观察结果证实了P4503A参与ANF的代谢：（1）在人肝微粒体组分中，观察到ANF 5,6-氧化物的形成与睾酮6β-羟基化（P4503A的一个指标）相关；（2）ANF的代谢受到各种选择性P4503A酶抑制剂的抑制；（3）针对P4503A4产生的兔抗体抑制ANF代谢超过80%；（4）特异性表达P4503A4的微粒体组分将ANF代谢为氧化代谢产物。3. 这些结果表明，在人肝微粒体组分中，P4503A同工型主要将ANF代谢为氧化衍生物。