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Caffeine biotransformation was demonstrated in three novel human hepatocyte cell lines established from normal liver tissue and cultured continuously for 19 to 30 months. Caffeine and its metabolites were identified and quantified by high performance liquid chromatography. Without induction, caffeine was metabolized to the four primary metabolites [theobromine (37X), paraxanthine (17X), theophylline (13X), 1,3,7-trimethylurate (137U)]. Under these basal conditions 137U was the predominant metabolite. The actual pattern of metabolite production was a reproducible characteristic of each line. After induction with dibenz(a,h)anthracene, the formation of 17X was increased 4-17 fold. Induction with phenobarbital did not change the metabolic profile. These human hepatocyte lines can reproduce in vitro metabolism of caffeine observed in man in vivo.
E A Roberts, and
K N Furuya, and
B K Tang, and
W Kalow
June 1994,
Hepatology (Baltimore, Md.),
E A Roberts, and
K N Furuya, and
B K Tang, and
W Kalow
December 1997,
Virus research,
E A Roberts, and
K N Furuya, and
B K Tang, and
W Kalow
April 1987,
Biochemical pharmacology,
E A Roberts, and
K N Furuya, and
B K Tang, and
W Kalow
May 1994,
British journal of clinical pharmacology,
E A Roberts, and
K N Furuya, and
B K Tang, and
W Kalow
January 1993,
Drug metabolism and disposition: the biological fate of chemicals,
E A Roberts, and
K N Furuya, and
B K Tang, and
W Kalow
June 1994,
Human & experimental toxicology,
E A Roberts, and
K N Furuya, and
B K Tang, and
W Kalow
June 1976,
Journal of the National Cancer Institute,
E A Roberts, and
K N Furuya, and
B K Tang, and
W Kalow
June 1987,
Gynecologic oncology,
E A Roberts, and
K N Furuya, and
B K Tang, and
W Kalow
December 1990,
Cell biology international reports,
E A Roberts, and
K N Furuya, and
B K Tang, and
W Kalow
April 1989,
Xenobiotica; the fate of foreign compounds in biological systems,
