Food and Drug Interactions: Effect of <i>Acanthopanax senticosus</i> Harms on CYP2C9 Activity (Part 2) / 日本補完代替医療学会誌
Japanese Journal of Complementary and Alternative Medicine
;
: 9-15, 2014.
Artigo
em Japonês
| WPRIM
| ID: wpr-376389
ABSTRACT
<b>Objective:
</b> <i>Acanthopanax senticosus</i> Harms extract (ASE) is an ingredient of functional foods, such as health supplements, in Japan. We investigated the effects of ASE on CYP2C9 activity.<br> <b>Methods andResults:
</b> CYP2C9-catalyzed diclofenac 4′-hydroxylase activities in human intestinal and liver microsomes (abbreviated as HIM and HLM, respectively) were significantly decreased by the addition of ASE in a concentration-dependent manner. Kinetic studies of diclofenac 4′-hydroxylase in HLM revealed that ASE addition significantly decreased <i>V</i><sub>max</sub> but had no effect on <i>K</i><sub>m</sub>. These results suggest that diclofenac 4′-hydroxylase activity is suppressed by ASE addition in a non-competitive manner. Then, we investigated the time courses of diclofenac 4′-hydroxylase activity in rat liver microsomes after ASE oral administration (50 to 400 mg/kg). Diclofenac 4′-hydroxylase activities were significantly lowered by the administration of 200 and 400 mg/kg ASE at 0.5 to 4 hr compared with control (0 hr). Furthermore, we investigated the effects of ASE oral administration on the pharmacokinetics of tolbutamide (substrate for CYP2C9) in rats. The area under the concentration-time curve of tolbutamide after ASE oral administration (400 mg/kg) was enhanced by approximately 1.6 times compared with that without ASE oral administration.<br> <b>Conclusion:
</b> These findings indicated that ASE inhibits human intestinal and hepatic CYP2C9 activities.<br>
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Índice:
WPRIM (Pacífico Ocidental)
Idioma:
Japonês
Revista:
Japanese Journal of Complementary and Alternative Medicine
Ano de publicação:
2014
Tipo de documento:
Artigo
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