Pharmacokinetics, Tissue Distribution and Excretion of Verticinone from F. hupehensis in Rats

Molecules

Xiao Wu¹  Jian-Guo Sun²  Ying Peng²  Yan Liang²  Guang-Ji Wang²  Hui Chen¹  Ji-Zhou Wu¹  Peng Zhang¹ 

[1]Hubei Key Laboratory of Natural Medicinal Chemistry and Resource Evaluation, School of Pharmacy of Tongji Medical College, Huazhong University of Science and Technology, 13# Hangkong Road, Wuhan 430030, China

[2] E-Mails:

[3]State Key Laboratory of Natural Medicines, Key Laboratory of Drug Metabolism and Pharmacokinetics, China Pharmaceutical University, 24# Tongjiaxiang, Nanjing 210009, China

[4] E-Mails:

关键词: verticinone;    pharmacokinetics;    tissue distribution;    excretion;    F. hupehensis;    Liliaceae;   

DOI  :  10.3390/molecules191220613

来源: mdpi

【 摘 要 】

Verticinone, the main active component in F. hupehensis, exhibits potent antitussive and expectorant effects. Here, a LC-MS method was developed and applied to study the pharmacokinetics, tissue distribution and excretion of verticinone in rats, and its plasma protein binding in vitro. A significant gender difference in the pharmacokinetics of verticinone in rats was observed, as its absolute oral bioavailability in male and female rats was 45.8% and 2.74%, respectively. The relative bioavailability of verticinone was significantly lower in female rats as compared to male, following intragastrical (i.g.) and intravenous (i.v.) administration. After successive i.g. administration of verticinone, accumulation was observed in female rats but not in the male ones. The tissue distribution study showed that verticinone had a good tissue penetrability and a high tissue affinity in most studied tissues, except brain. After a 2 mg/kg oral dose, less than 4% of the dose was excreted as unchanged parent compound in male rats, and less than 1% in female rats, which indicated that verticinone was metabolized more extensively in female rats than in male rats.

【 授权许可】

CC BY   
© 2014 by the authors; licensee MDPI, Basel, Switzerland.