Abstract
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-β- d-glucuronopyranosyl-3β, 16α-dihydroxyolean-12-en-28-oic acid 28- O-β- d-xylopyranosyl(1→3)-β- d-xylopyranosyl-(1→4)-α- l-rhamnopyranosyl-(1→2)-α- 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 (3β, 16α-dihydroxyolean-12-en-28-oic acid 28- O-β- d-xylopyranosyl(1→3)-β- d-xylopyranosyl-(1→4)-α- l-rhamnopyranosyl-(1→2)-α- 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.
Published Version
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