Quantitative LC/MS/MS method and pharmacokinetic studies of columbin, an anti-inflammation furanoditerpen isolated from Radix Tinosporae.

Abstract

Columbin is an important component isolated from Radix Tinosporae. It has been demonstrated to possess many pharmacological activities, including anti-inflammation, antitumor and inhibition of enzyme activity in vivo. The purpose of the present study was to examine in vivo pharmacokinetics and bioavailability of columbin in rats using a high-performance liquid chromatography coupled with tandem mass spectrometry quantitative detection method. The columbin was extracted from rat plasma samples by methyl tert-butyl ether, evaporated and reconstituted in 100 microL methanol prior to analysis. The separation was performed using a Luna reversed-phase analytical column (5 microm, 100 x 2.0 mm) and an SB-C18 guard column (5 microm, 20 x 4.0 mm). The mobile phase was a mixture of methanol and water containing 25 mmoL/L NH(4)Ac (80:20, v/v). The method was validated within the concentration range of 5-5000 ng/mL, and the calibration curves were linear with correlation coefficients (r) >0.999. It was further applied to assess pharmacokinetics and oral bioavailability of columbin after i.v. and oral administration to rats. The oral bioavailability of columbin was only 3.18%, which indicated that columbin had poor absorption or underwent extensive first-pass metabolism.

• Authors: Qirong Shi, Mingjin Liang, Weidong Zhang, Chuan Zhang, Runhui Liu, Yunheng Shen, Huiliang Li, Xiaolin Wang, Xiangwei Wang, Qiongqun Pan, Chunlin Chen
• Journal: Biomedical chromatography : BMC (Biomed Chromatogr) Vol. 21 Issue 6 Pg. 642-8 (Jun 2007) ISSN: 0269-3879 [Print] England
• PMID: 17345572 (Publication Type: Evaluation Study, Journal Article, Research Support, Non-U.S. Gov't)
• Copyright: Copyright 2007 John Wiley & Sons, Ltd.

Chemical References

• Anti-Inflammatory Agents
• Diterpenes
• Lactones
• Plant Extracts
• columbin

Topics

• Administration, Oral
• Animals
• Anti-Inflammatory Agents (blood, chemistry, pharmacokinetics)
• Biological Availability
• Chromatography, High Pressure Liquid (methods)
• Diterpenes (blood, chemistry, pharmacokinetics)
• Injections, Intravenous
• Lactones (blood, chemistry, pharmacokinetics)
• Male
• Molecular Structure
• Plant Extracts (chemistry, metabolism)
• Plant Roots (chemistry, metabolism)
• Rats
• Rats, Sprague-Dawley
• Reproducibility of Results
• Sensitivity and Specificity
• Spectrometry, Mass, Electrospray Ionization (methods)
• Spectrophotometry, Ultraviolet (methods)
• Tandem Mass Spectrometry (methods)
• Tinospora (chemistry, metabolism)