National Institute of Health and Nutrition, 1-23-1 Toyama, Shinjuku-ku, Tokyo 162-8636, Japan.
Food Chem Toxicol. 2012 Mar;50(3-4):750-5. doi: 10.1016/j.fct.2011.11.054. Epub 2011 Dec 8.
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 2-3 weeks. 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 1 week 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.
毛喉鞘蕊花根提取物（CFE）作为一种减肥膳食补充剂而广受欢迎。在这项研究中，通过其药物相互作用潜力来评估安全性，研究了含有 10％活性成分毛喉素的标准化 CFE 对肝药物代谢系统的影响。雄性 ICR 小鼠喂食含有 0-5％CFE 或 0.05％纯毛喉素的基于 AIN93G 的饮食 2-3 周。摄入两种不同来源的 0.5％CFE 可显著增加相对肝重，肝细胞色素 P450（CYP）的总含量，并诱导 CYP（特别是 2B、2C、3A 型）和谷胱甘肽 S-转移酶（GST）活性。CFE 可显著增加 CYP 和 GST 的 mRNA 表达，呈剂量相关反应。然而，与 CFE 不同，摄入 0.05％纯毛喉素与 CYP3A 和 GST 活性的弱诱导相关，相对肝重、总肝含量或其他 CYP 活性无明显增加。CFE 对 CYP 和 GST 的诱导作用在喂食 1 周时即可观察到，并在停止喂食 CFE 后迅速恢复。这些结果表明 CFE 对 CYP 的诱导潜力，并且这种作用主要归因于 CFE 中其他尚未确定的成分，而不是毛喉素。
