Biotransformation of the naturally occurring lignan (-)-arctigenin in mammalian cell lines genetically engineered for expression of single cytochrome P450 isoforms.
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.
Kasper
R
R
Institut für Pharmazeutische Biologie, Freie Universität, Berlin-Dahlem, Federal Republic of Germany.
Gansser
D
D
Doehmer
J
J
D000818:Animals; D001711:Biotransformation; D002460:Cell Line; D006224:Cricetinae; D003412:Cricetulus; D003577:Cytochrome P-450 Enzyme System / Q000096:biosynthesis / Q000378:metabolism*; D005663:Furans / Q000378:metabolism*; D007527:Isoenzymes / Q000096:biosynthesis / Q000378:metabolism*; D017705:Lignans / Q000378:metabolism*; D015394:Molecular Structure; D051381:Rats; D011994:Recombinant Proteins / Q000096:biosynthesis / Q000378:metabolism; D014162:Transfection
D005663:Furans; D007527:Isoenzymes; D017705:Lignans; D011994:Recombinant Proteins; D003577:Cytochrome P-450 Enzyme System; C071942:arctigenin