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Molecules 2015, 20(3), 4225-4237; doi:10.3390/molecules20034225

Pharmacokinetics and Tissue Distribution Study of Caudatin in Normal and Diethylnitrosamine-Induced Hepatocellular Carcinoma Model Rats

Department of Pharmacology and Toxicology, Jiangsu Provincial Institute of Traditional Chinese Medicine, 100 Shizi Street, Nanjing 210028, China
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Academic Editor: Jean Jacques Vanden Eynde
Received: 17 November 2014 / Revised: 15 February 2015 / Accepted: 26 February 2015 / Published: 5 March 2015
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Abstract

Caudatin is a potential antitumor agent isolated from the traditional Chinese medicine “baishouwu”, which was the root tuber of Cynanchum auriculatum Royle ex Wight. In our previous studies, caudatin showed selectivity on human hepatoma cell line SMMC7721 among several different tumor cell lines, and further in vivo tests validated the inhibitory action of caudatin against hepatic cancer using an H22 solid tumor model in mice, but to our knowledge, the biopharmaceutical properties of caudatin are largely unknown. In this study, a simple, rapid and sensitive ultra-performance liquid chromatography-tandem mass spectrometry (UPLC-MS/MS) method for the determination of caudatin in rat plasma and tissues, which kept the run time to detect one sample within 4 min, was developed and validated. Pharmacokinetics and tissue distribution studies of caudatin in conventional rats and hepatocellular carcinoma (HCC) model rats were then conducted for the first time. Statistically significant differences were observed between conventional rats and diethylnitrosamine (DEN)-induced HCC rats with respect to pharmacokinetic parameters, including maximum concentration (Cmax), time to reach Cmax (Tmax), half-life (t1/2), area under the concentration-time curve (AUC0-t, AUC0-∞), mean residence time (MRT0-t and MRT0-∞), and oral clearance (CL/F). Increased exposures of caudatin were found in the plasma and livers of HCC model rats, which would be helpful for a better understanding of pharmacological effect of caudatin in treating HCC disease. View Full-Text
Keywords: pharmacokinetics; C-21 steroidal glycoside; Cynanchum auriculatum Royle ex wight; caudatin; hepatocellular carcinoma pharmacokinetics; C-21 steroidal glycoside; Cynanchum auriculatum Royle ex wight; caudatin; hepatocellular carcinoma
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This is an open access article distributed under the Creative Commons Attribution License which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited. (CC BY 4.0).

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Peng, Y.; Ding, Y. Pharmacokinetics and Tissue Distribution Study of Caudatin in Normal and Diethylnitrosamine-Induced Hepatocellular Carcinoma Model Rats. Molecules 2015, 20, 4225-4237.

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