Metabolic Pharmacokinetics of Isoflavones in the Roots of Pueraria lobata in Rats

葛根異黃酮於鼠體內之代謝動力學

江秀梅(Hsiu-Mei Chiang) ； 葉怡柔(Yi-Rou Yeh) ； 李珮端(Pei-Dawn Lee Chao) ； 徐素蘭(Su-Lan Hsiu) ； 侯鈺琪(Yu-Chi Hou) ； 姬盈璋(Ying-Chang Chi) ； 溫國慶(Kuo-Ching Wen)

《Mid-Taiwan Journal of Medicine》 10卷2期 (2005/06) Pp. 57-64

https://doi.org/10.6558/MTJM.2005.10(2).1

摘要

目的　葛根爲臨床上廣泛使用之中藥，含豐富之異黃酮成分包括葛根素、大豆苷及大豆苷元，本研究探討大鼠口服葛根後，異黃酮之代謝動力學。
方法　利用HPLC梯度沖提法同時定量葛根濃縮散劑中葛根系、大豆苷及大豆苷元之含量。七雙大鼠口服葛根濃縮散劑後對於特定時間點採血，血清檢品分別以β-葡萄糖醛酸酶及硫酸酶水解。水解前後之血清檢品分別以HPLC定量，並利用WINNONLIN之非室體模式計算動力學參數。
結果　葛根濃縮散劑中之葛根素、大豆苷及大豆苷元之含量分別爲33.9、1.3及0.9毫克／克。口服葛根後血清未檢出原型之葛根素、大豆苷及大豆苷元，而以大豆苷元之葡萄糖醛酸及硫酸結合態代謝物存在於血流，且主要爲硫酸結合態代謝物。
結論　此等結合態代謝物於葛根異黃酮之活性上可能扮演重要的角色，值得進一步研究。

關鍵字

大豆苷元 ； 大豆苷 ； 黃異酮 ； 藥物動力學 ； 葛根 ； 葛根素

並列摘要

Purpose. Puerariae radix, the root of Pueraria lobata, is widely used in clinical Chinese medicine. It is abundant in isoflavones including puerarin, daidzin, and daidzein. This study investigated the metabolic pharmacokinetics of isoflavones after orally administrating Puerariae radix to Spraque-Dawley rats.
Methods. The concentrations of puerarin, daidzin and daidzein in commercial extract of Puerariae radix were simultaneously quantified by a gradient high performance liquid chromatographic method (HPLC). Seven rats were orally given the commercial extract of Puerariae radix and blood samples were withdrawn at specific time points. Serum samples were assayed by HPLC prior to and after enzymatic hydrolysis with β-glucuronidase and sulfatase. Pharmacokinetic parameters were calculated using noncompartment model of WINNONLIN.
Result. The contents of puerarin, daidzin and daidzein in the commercial extract of Puerariae radix were 33.9, 1.3 and 0.9 mg/g, respectively. After oral administration of Puerariae radix, the parent forms of puerarin, daidzin and daidzein were not detected in serum; however, the sulfates and glucuronides of daidzein were found in the blood, predominantly as daidzein sulfates.
Conclusions. Daidzein sulfates and glucuronides ma play important roles in the biological activities of isoflavones in Puerariae radix and are worthy of further investigation.

並列關鍵字

daidzein ； daidzin ； isoflavone ； pharmacokinetics ； Pueraria lobata ； puerarin