Abstract
A rapid, selective and sensitive UPLC-MS/MS assay was established to determine the plasma concentrations of four steroidal saponins. Sprague-Dawley rats were allocated to four groups which were orally administered Anemarrhena asphodeloides extracts (ASE), ASE combined with macromolecular fraction (ASE-MF), ASE combined with small molecule fraction (ASE-SF) and ASE combined with small molecule and macromolecular fraction (ASE-SF-MF) containing approximately the same dose of ASE. At different time points, the concentration of timosaponin BII, anemarsaponin BIII, timosaponin AIII and timosaponin E1 in rat plasma were determined and main pharmacokinetic parameters including Cmax, Tmax, T1/2, AUC were calculated using the DAS 3.2 software package. The statistical analysis was performed using the Student’s t-test with p < 0.05 as the level of significance. MF had no effect on the pharmacokinetic behaviors and parameters of four steroidal saponins. It was found that Cmax and AUC of four steroidal saponins in group ASE-SF and ASE-SF-MF, were significantly increased compared with those in group ASE. These results indicate that SF in A. asphodeloides extracts could increase the absorption and improve the bioavailability of the steroidal saponins.
Highlights
Anemarrhena asphodeloides, the dried rhizome of A. asphodeloides Bunge
A rapid, selective and specific LC-MS/MS method for the simultaneous analysis of four components of A. asphodeloides in rat plasma in a simple 4.2 min chromatographic run was developed for the first time
The results obtained from this study implied that after combination with different fractions extracted from A. asphodeloides extract, the pharmacokinetic behaviors of the four steroidal saponins showed differences their pure forms or from other extracts
Summary
Anemarrhena asphodeloides, the dried rhizome of A. asphodeloides Bunge (Fam. Liliaceae), is mainly distributed in China, Mongolia and other eastern Asian countries. A. asphodeloides has been commonly used in traditional medicine in China, Japan, and Korea for thousands of years [1]. As the decoction of the entire rhizome extract is taken orally, the pharmacological activity observed in humans is attributed to the entire rhizome extract, which includes steroidal saponins, flavonoids, pigments, polysaccharides, etc. The main active components of A. asphodeloides are steroidal saponins, with extremely diverse structures such as timosaponin BII (1), anemarsaponin BIII (2), timosaponin AIII (3) and timosaponin E1 (4) (Figure 1), which have been shown to improve senile dementia and have anti-blood coagulation, anti-oxidant, anti-tumor, anti-osteoporosis, anti-inflammation, and blood sugar and blood pressure lowering effects [7,8,9,10,11,12,13]. Non-steroidal saponin small molecule ingredients such as flavonoids [14,15], organic acids [16,17], amino acids, nucleosides, oligosaccharides and a non-steroidal saponin macromolecule fraction comprising pigments and polysaccharides exist in
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