Anemarrhena asphodeloides Non-Steroidal Saponin Components Alter the Pharmacokinetic Profile of Its Steroidal Saponins in Rat

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. OPEN ACCESSMolecules 2015, 20 11778These results indicate that SF in A. asphodeloides extracts could increase the absorption and improve the bioavailability of the steroidal saponins.

Absorption and pharmacokinetic study of two sulphated triterpenoid saponins in rat after oral and intravenous administration of saponin extracts of Pearsonothuria graeffei by HPLC-MS

“…Following oral dosing, two peaks in the concentrationtime curve of EA and HA in serum were observed. The double peak observed after oral administration of different saponins was also widely reported (Cai et al, 2008;Cai et al, 2010;Joo et al, 2010;Tang et al, 2015;Zhang, Zhang, Xu, Gu, & Zhao, 2007). However, Xu, Fang, and Chen (2003) showed that both Rb1 and Rg1 from Panax notoginseng could be absorbed through the rat GI tract after oral administration, and they both only had one peak time at 1.5 and 1 h, respectively (Li et al, 2004).…”

“…Many factors can affect the absorption process, including presystemic metabolism/efflux, the "absorption window" along the gastrointestinal tract, enterohepatic recirculation, variable gastric emptying and drug-drug interactions. Therefore, atypical drug absorption profiles such as double peaks are often encountered (Tang et al, 2015). Zhang et al (2007) reported that the plasma concentration-time curves of ginsenosides exhibited distinct double peaks after oral administration, and that this might involve enterohepatic recirculation.…”

Anemarsaponin BII inhibits the activity of CYP3A4, 2D6, and 2E1 with human liver microsomes

“…The C max of anemarsaponin BII was obtained as 271.22 ng/mL with the t 1/2 of 3.21 h (Tang et al. 2015 ). These values were far from the IC 50 values of CYP3A4, 2D6, and 2E1.…”

Pharmacological Activity, Pharmacokinetics, and Toxicity of Timosaponin AIII, a Natural Product Isolated From Anemarrhena asphodeloides Bunge: A Review

“…The total saponins, which are rich in rhizome, could be extracted by hot water under reflux and purified by EtOAc, n-BuOH, and H 2 O, and the content of saponins is more than 6% (Wang et al, 2014;Yang et al, 2016;Nian et al, 2017). Timo AIII, Timosaponin BII (Timo BII) and sarsasapogenin are three main active saponins isolated from A. asphodeloides Bunge (Figure 1), and they have been identified as quality control and pharmacokinetic markers of diverse A. asphodeloides Bungecontained Chinese herb formulas, such as TongGuanWan, Rhizoma Anemarrhenae-Phellodendron herb pair, guizhishaoyao-zhimu herb pair, zhimu-baihe herb pair, and so on (Tang et al, 2012;Wang et al, 2014;Tang et al, 2015;Yang et al, 2018). The biotransformation of Timo AIII from Timo BII could been mediated by b-D-glycosidase (Lu et al, 2016).…”