A sensitive liquid chromatography-electrospray tandem mass spectrometric method for lancemaside A and its metabolites in plasma and a pharmacokinetic study in mice

作者：Joh Eun Ha; Kim Dong Hyun^*

来源：Journal of Chromatography B-Analytical Technologies in the Biomedical and Life Sciences, 2010, 878(21): 1875-1880.

DOI：10.1016/j.jchromb.2010.05.003

• Codonopsis lanceolata
• Lancemaside A
• Echinocystic acid
• Metabolism
• LC-MS/MS
• Pharmacokinetic study

A high-performance liquid chromatography tandem mass spectrometry (HPLC-MS/MS) method employing electrospray ionization (ESI) has been developed for simultaneous determination of lancemaside A (3-O-beta-D-glucuronopyranosyl-3 beta, 16 alpha-dihydroxyolean-12-en-28-oic acid 28-O-beta-D-xylopyranosyl(1 -> 3)-beta-D-xylopyranosyl-(1 -> 4)-alpha-L-rhamnopyranosyl-(1 -> 2)-alpha-L-arabinopyranosyl ester) and its metabolites in mouse plasma. When lancemaside A (60 mg/kg) was orally administered to mice, echinocystic acid was detected in the blood. T(max) and C(max) of the echinocystic acid were 6.5 +/- 1.9 h and 56.7 +/- 29.1 ppb. Orally administered lancemaside A was metabolized to lancemaside X (3 beta, 16 alpha-dihydroxyolean-12-en-28-oic acid 28-O-beta-D-xylopyranosyl(1 -> 3)-beta-D-xylopyranosyl-(1 -> 4)-alpha-L-rhamnopyranosyl-(1 -> 2)-alpha-L-arabinopyranosyl ester) by intestinal microflora in mice, which was metabolized to echinocystic acid by intestinal microflora and/or intestinal tissues. Human intestinal microflora also metabolized lancemaside A to echinocystic acid via lancemaside X. These results suggest that the metabolism by intestinal microflora may play an important role in pharmacological effects of orally administered lancemaside A.

• 出版日期2010-7-1