Coleus forskohlii extract induces hepatic cytochrome P450 enzymes in mice

• Published in: Food and chemical toxicology Vol. 50; no. 3-4; pp. 750 - 755
• Main Authors: Virgona, Nantiga, Yokotani, Kaori, Yamazaki, Yuko, Shimura, Fumio, Chiba, Tsuyoshi, Taki, Yuko, Yamada, Shizuo, Shinozuka, Kazumasa, Murata, Masatsune, Umegaki, Keizo
• Format: Journal Article
• Language: English
• Published: Oxford Elsevier Ltd 01.03.2012; Elsevier
• Subjects: Animals; Base Sequence; Biological and medical sciences; Coleus - chemistry; Coleus forskohlii; cytochrome P-450; Cytochrome P-450 Enzyme System - biosynthesis; Cytochrome P450; Dietary supplement; dietary supplements; DNA Primers; drugs; Drug–herb interaction; Enzyme Induction; Forskolin; gene expression; glutathione transferase; Glutathione Transferase - metabolism; liver; Liver - drug effects; Male; Medical sciences; messenger RNA; Mice; Mice, Inbred ICR; Microsomes, Liver - enzymology; Organ Size - drug effects; Plant Extracts - pharmacology; Plant Roots - chemistry; Plectranthus barbatus; Real-Time Polymerase Chain Reaction; Toxicology; weight loss; Dietary supplement; CFE; Cytochrome P450; Forskolin; Cyclo; GST; CYP; PXR; cAMP; Coleus forskohlii; Drug–herb interaction; Digestive system; Enzyme; Biochemical compound; Liver; Rodentia; Extract; Vertebrata; Plant; Drug-herb interaction; Mammalia; Mouse; EC 1.14.14.1; Animal; Plant origin; Drug interaction; Supplementation; Food supplement
• ISSN: 0278-6915; 1873-6351
• DOI: 10.1016/j.fct.2011.11.054

► Coleus forskohlii root extract (CFE) induced activities of hepatic drug metabolizing enzymes (CYPs and GST) in mice. ► CFE increased mRNA expression of CYPs and GST with dose related responses. ► Intake of two different sources of CFE showed similar response toward inductions of CYPs. ► Induction of CYPs by CFE was detected at 1week of feeding and rapidly recovered after discontinuation. ► Forskolin was not involved in the marked induction of CYPs by CFE. Coleus forskohlii root extract (CFE) is popular for use as a weight loss dietary supplement. In this study, the influence of standardized CFE containing 10% active component forskolin on the hepatic drug metabolizing system was investigated to evaluate the safety through its drug interaction potential. Male ICR mice were fed AIN93G-based diets containing 0–5% CFE or 0.05% pure forskolin for 2–3weeks. Intake of two different sources of 0.5% CFE significantly increased the relative liver weight, total content of hepatic cytochrome P450 (CYP) and induced CYPs (especially 2B, 2C, 3A types) and glutathione S-transferase (GST) activities. CFE significantly increased mRNA expression of CYPs and GST with dose related responses. However, unlike the CFE, intake of 0.05% pure forskolin was found to be associated with only weak induction in CYP3A and GST activities with no significant increases in relative liver weight, total hepatic content or other CYPs activities. The inductions of CYPs and GST by CFE were observed at 1week of feeding and rapidly recovered by discontinuation of CFE. These results indicated the induction potential of CFE on CYPs, and that this effect was predominantly due to other, as yet unidentified constituents, and not forskolin contained in CFE.