In vivo pharmacokinetics, distribution, and excretion of an anticancer agent isolated from red ginseng, in rat

Abstract

1. The compound 20(S),25-epoxydammarane-3β,12β,24α-triol (24-hydroxy-panaxadiol or 24-OH-PD), isolated from the red Panax ginseng CA Meyer possesses anticancer activity. Our aim was to study the pharmacokinetic characteristics of 24-OH-PD, which is essential for pre-clinical research during the development of new drugs.

2. In this study, a simple and sensitive ultra-performance liquid chromatography-mass spectrometry (LC-MS/MS) method was established and used for studying the pharmacokinetics, in vitro protein binding, tissue distribution, and elimination profiles of 24-OH-PD in rats.

3. 24-OH-PD was characterized by linear pharmacokinetics in the dose range of 2.5–10 mg/kg and had relatively longer half-life (4.82–5.45 h) than the other ginsenosides. It had a wide tissue distribution profile in rats and was primarily distributed in the lung. Within 96 h of intravenous administration, 13.84% of 24-OH-PD was excreted out via feces and 0.02% via urine in its unchanged form.

4. In conclusion, a simple LC-MS/MS method with high sensitivity and selectivity was established for the quantification of 24-OH-PD.

Keywords:

• 24-OH-panaxadiol
• pharmacokinetics
• LC-MS/MS
• plasma protein binding
• ginsenoside
• distribution
• elimination

Disclosure statement

The authors declare that they have no conflicts of interest with the contents of this article.

Author contributions

Q. Z. established the analytical method, analyzed data, calculated PK parameters and prepared the manuscript. N. Z. and C. W. performed the animal experiment and revised the manuscript. Q. Z. and P. L. designed the whole research and interpreted the results of experiments. R. W. analyzed PK parameters. P. L. reviewed the final manuscript, and all the authors have read and approved the final version.

Additional information

Funding

This work was supported by the Natural Science Foundation of Shanxi Province, China [No. 201801D221272], China Postdoctoral Science Foundation [No. 2018M641678], Higher school science and technology innovation project of Shanxi Province, China [No. 2019L0413], Scientific Research Foundation of Shanxi Medical University, China [No. BS201730].