Jun-Jun Wang, Xiao-Lei Miao, Jing-Ya Chen, Yong Chen
Hubei Province Key Laboratory of Biotechnology of Chinese Traditional Medicine, Hubei Collaborative Innovation Center for Green Transformation of Bio-resources, Hubei University, Wuhan, 430062, China.
Eur J Drug Metab Pharmacokinet. 2016 Oct;41(5):587-94. doi: 10.1007/s13318-015-0281-6.
Honokiol (HK) is the main bioactive compound isolated from the bark of Magnolia officinalis. The present work is the first to report the pharmacokinetics and distribution of HK and its two metabolites of hydroxylated HK conjugated with glucuronic and sulfuric acid (M1) and HK monoglucuronide (M2) in plasma, liver, kidney and brain following oral administration of HK (40 mg/kg) to healthy Wistar rats. The results showed that only HK but not M1 or M2 was found in brain. Additionally, our work indicated that M2 not HK was the major compound in liver and plasma. The elimination of HK in liver, kidney and brain, and M2 in liver and kidney was more rapid than in plasma. The finding suggested that some of the pharmacological activity of HK might be generated by M2 but not HK.
厚朴酚(HK)是从厚朴树皮中分离出的主要生物活性化合物。本研究首次报道了在健康Wistar大鼠口服给予HK(40mg/kg)后,HK及其与葡萄糖醛酸和硫酸结合的两种羟基化HK代谢物(M1)和HK单葡萄糖醛酸苷(M2)在血浆、肝脏、肾脏和大脑中的药代动力学及分布情况。结果显示,在大脑中仅发现了HK,而未发现M1或M2。此外,我们的研究表明,肝脏和血浆中的主要化合物是M2而非HK。HK在肝脏、肾脏和大脑中的消除,以及M2在肝脏和肾脏中的消除比在血浆中更快。这一发现表明,HK的某些药理活性可能是由M2而非HK产生的。