Department of Cellular and Molecular Medicine, University of Ottawa, Ottawa, ON, Canada.
J Ethnopharmacol. 2009 Oct 29;126(1):119-26. doi: 10.1016/j.jep.2009.07.036. Epub 2009 Aug 7.
Cree traditional medicine is commonly used concomitantly with prescribed drugs to treat health problems related to type II diabetes (T2D) that is endemic in the Cree population. However, the safety of traditional Cree medicines with respect to drug metabolism is unknown.
Seventeen anti-diabetic plant extracts were screened for their potential inhibition of 11 isoforms of the drug-metabolizing cytochrome P450s (CYPs), and flavin-containing monooxygenase 3 (FMO3) in fluorometric plate reader assays. Comparative analyses were conducted to determine if particular extracts were more inhibitory, or if particular enzymes were more inhibited.
Many anti-diabetic plant extracts inhibited the CYPs, with CYP2C and 3A isoforms being most prone to inhibition. The order of inhibition for the enzymes by the Cree plant extracts was: 2C19>3A7>3A5>3A4>2C9>2C8>FMO3>1A2>2E1>19>2D6>2B6. Extracts from Rhododendron groenlandicum, Sorbus decora, and Kalmia angustifolia were identified as having strong inhibition towards many CYP isoforms.
These findings demonstrate that extracts from most plant species examined have the potential to affect CYP2C- and 3A4-mediated metabolism, and have the potential to affect the bioavailability and pharmacokinetics of conventional and traditional medicines during concomitant use.
克里传统医学常与处方药联合使用，以治疗克里人群中流行的 II 型糖尿病（T2D）相关的健康问题。然而，传统克里药物在药物代谢方面的安全性尚不清楚。
使用荧光板读数测定法筛选了 17 种抗糖尿病植物提取物，以评估它们对 11 种同工型药物代谢细胞色素 P450（CYPs）和黄素单加氧酶 3（FMO3）的潜在抑制作用。进行了比较分析，以确定特定提取物的抑制作用更强，或者特定酶的抑制作用更强。
许多抗糖尿病植物提取物抑制了 CYPs，其中 CYP2C 和 3A 同工型最容易受到抑制。克里植物提取物对酶的抑制顺序为：2C19>3A7>3A5>3A4>2C9>2C8>FMO3>1A2>2E1>19>2D6>2B6。从格陵兰杜鹃、花楸和狭叶杜香中提取的物质被鉴定为对许多 CYP 同工型具有强烈的抑制作用。
这些发现表明，大多数被检查的植物物种的提取物具有影响 CYP2C-和 3A4 介导的代谢的潜力，并可能影响传统药物和传统药物在同时使用时的生物利用度和药代动力学。
