Pharmacokinetic parameters of three active ingredients hederacoside C, hederacoside D, and alpha-hederin in Hedera helix in rats

Abstract

In Hedera helix hederacoside C, hederacoside D, and ɑ-hederin are three major bioactive saponins and play pivotal roles in the overall biological activity. In this study, a specific and sensitive ultra-high performance liquid chromatography with tandem mass spectrometry method has been developed and validated for the quantification of three major bioactive saponins in rat plasma. Chromatographic separation was performed on a reversed-phase Thermo Hypersil GOLD C18 column (2.1 mm × 50 mm, 1.9 μm) using a gradient mobile phase system of acetonitrile-water containing 0.1% formic acid. The assay was successfully applied to study the pharmacokinetic behavior of the three analytes in rats after oral and intravenous administration of a mixture of saponins (hederacoside C, hederacoside D, and ɑ-hederin). Further research was performed to compare the pharmacokinetic behavior of the three analytes after the oral administration of a mixture of saponins and an extract of saponins from Hedera helix, and results showed that double peaks were evident on concentration-time profile for each of the three saponins. The difference in the pharmacokinetic characteristics of three saponins between a mixture of saponins and an extract of saponins from Hedera helix was found in rat, which would be beneficial for the preclinical research and clinical use of Hedera helix.