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在经过基因工程改造以表达单一细胞色素P450同工型的哺乳动物细胞系中天然存在的木脂素(-)-牛蒡子苷元的生物转化。

Biotransformation of the naturally occurring lignan (-)-arctigenin in mammalian cell lines genetically engineered for expression of single cytochrome P450 isoforms.

作者信息

Kasper R, Gansser D, Doehmer J

机构信息

Institut für Pharmazeutische Biologie, Freie Universität, Berlin-Dahlem, Federal Republic of Germany.

出版信息

Planta Med. 1994 Oct;60(5):441-4. doi: 10.1055/s-2006-959528.

Abstract

V79 Chinese hamster cells genetically engineered for stable expression of single forms of rat cytochromes P450 1A1, P450 1A2, and P450 2B1, and human P450 1A2 were used to analyse the metabolism of (-)-arctigenin. Concentrations of metabolites formed in the medium were determined by TLC, HPLC, GC, and GC-MS. Only in the cell line expressing rat P450 2B1 was (-)-arctigenin metabolized to a significant extent. The lignan was converted by O-demethylation to (-)-3'-O-demethylarctigenin.

摘要

V79中国仓鼠细胞经基因工程改造,可稳定表达单一形式的大鼠细胞色素P450 1A1、P450 1A2和P450 2B1,以及人细胞色素P450 1A2,用于分析(-)牛蒡子苷元的代谢。通过薄层色谱法(TLC)、高效液相色谱法(HPLC)、气相色谱法(GC)和气相色谱-质谱联用法(GC-MS)测定培养基中形成的代谢物浓度。只有在表达大鼠P450 2B1的细胞系中,(-)牛蒡子苷元才会有显著程度的代谢。该木脂素通过O-去甲基化转化为(-)-3'-O-去甲基牛蒡子苷元。

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