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

Song, Shanshan; Cong, Peixu; Xu, Jie; Li, Guoyun; Liu, Xiaofang; Li, Zhaojie; Xue, Changhu; Xue, Yong; Wang, Yuming

doi:10.1016/j.jff.2016.05.002

Cited by 15 publications

(22 citation statements)

References 33 publications

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“…Although SCSs have structures similar to that of ginsenoside, there are still various differences between the saponins from the 2 different sources. Previous studies confirmed that SCSs can be absorbed in the body after oral administration in rats (Song and others ; Li and others ), and the pharmacokinetics and biodistribution of SCSs were investigated (Xiong and others ). The metabolism of SCSs in the gut and the absorption characteristics of the metabolites, however, were not clarified.…”

Section: Introductionmentioning

confidence: 89%

Characterization of Metabolic Pathways and Absorption of Sea Cucumber Saponins, Holothurin A and Echinoside A, in Vitro and in Vivo

Song

Zhang

Cao

et al. 2017

Journal of Food Science

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Sea cucumber saponins (SCSs) exhibit a wide spectrum of bioactivities, but their metabolic characteristics are not well elucidated. In this study, the metabolism of holothurin A (HA) and echinoside A (EA), 2 major saponins in sea cucumber, by gut microflora were investigated. First, we conducted an in vitro study, where in the SCSs were incubated with intestinal microflora and the metabolites were detected by high pressure liquid chromatography-high resolution mass spectrometry. We also conducted an in vivo study on rats, where in the intestinal contents, serum, urine, and feces were collected and evaluated after oral administration of SCSs. In the in vitro study, we identified 6 deglycosylated metabolites of HA and EA, assigned M1-M6. In the in vivo study, we found all the deglycosylated metabolites in the intestinal contents after oral administration, and both the metabolites and their prototype components could be absorbed. Four metabolites were identified in the serum, 6 in the urine, and 4 in the feces. The saponins with different structures showed different absorption characteristics in rats. According to our results, deglycosylation is the main intestinal microflora-mediated metabolic pathway for SCSs, and both the SCSs and deglycosylated metabolites can be absorbed by intestine. This study improves the understanding of the metabolism of HA and EA by gut flora, which will be useful for further analysis of the bioactivity mechanism of SCSs.

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Section: Introductionmentioning

confidence: 89%

Characterization of Metabolic Pathways and Absorption of Sea Cucumber Saponins, Holothurin A and Echinoside A, in Vitro and in Vivo

Song

Zhang

Cao

et al. 2017

Journal of Food Science

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“…The sample volume injected was 10 μL. ESI in the mass spectrometer was performed with the following parameters: ionization, negative ion mode; capillary voltage, 3.5 kV; atomizing voltage (N2), 40 psi; ion source temperature, 300 °C; drying gas (N2) flow rate, 10.0 L/min; drying gas temperature, 350 °C [16]. The mass range of FS mode was recorded from m/z 300 to 600.…”

Section: Methodsmentioning

confidence: 99%

Trimethylamine-N-oxide (TMAO)-induced atherosclerosis is associated with bile acid metabolism

et al. 2018

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BackgroundRecently, trimethylamine-N-oxide (TMAO) plasma levels have been proved to be associated with atherosclerosis development. Among the targets aimed to ameliorating atherosclerotic lesions, inducing bile acid synthesis to eliminate excess cholesterol in body is an effective way. Individual bile acid as endogenous ligands for the nuclear receptor has differential effects on regulating bile acid metabolism. It is unclear whether bile acid profiles are mechanistically linked to TMAO-induced development of atherosclerosis.MethodsMale apoE−/− mice were fed with control diet containing 0.3% TMAO for 8 weeks. Aortic lesion development and serum lipid profiles were determined. Bile acid profiles in bile, liver and serum were measured by liquid chromatographic separation and mass spectrometric detection (LC-MS). Real-time PCRs were performed to analyze mRNA expression of genes related to hepatic bile acid metabolism.ResultsThe total plaque areas in the aortas strongly increased 2-fold (P < 0.001) in TMAO administration mice. The levels of triglyceride (TG), total cholesterol (TC), low-density lipoprotein cholesterol (LDL-c) in TMAO group were also significantly increased by 25.5% (P = 0.044), 31.2% (P = 0.006), 28.3% (P = 0.032), respectively. TMAO notably changed bile acid profiles, especially in serum, the most prominent inductions were tauromuricholic acid (TMCA), deoxycholic acid (DCA) and cholic acid (CA). Mechanically, TMAO inhibited hepatic bile acid synthesis by specifically repressing the classical bile acid synthesis pathway, which might be mediated by activation of small heterodimer partner (SHP) and farnesoid X receptor (FXR).ConclusionsThese findings suggested that TMAO accelerated aortic lesion formation in apoE−/− mice by altering bile acid profiles, further activating nuclear receptor FXR and SHP to inhibit bile acid synthesis by reducing Cyp7a1 expression.

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“…The concentrations of EA and HA at 0.5 h reached 0.11 and 0.2 µg/mL, respectively. The first C max was 0.83 µg/mL (EA) and 0.34 µg/mL (HA) at a T max of 3 h and the second C max were 0.24 µg/mL (T max = 7 h) for EA and 0.27 µg/mL (T max = 9 h) for HA [ 39 ].…”

Section: Pharmacokinetics Studies In Animalsmentioning

confidence: 99%

Pharmacokinetics of Marine-Derived Drugs

et al. 2020

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Marine organisms represent an excellent source of innovative compounds that have the potential for the development of new drugs. The pharmacokinetics of marine drugs has attracted increasing interest in recent decades due to its effective and potential contribution to the selection of rational dosage recommendations and the optimal use of the therapeutic arsenal. In general, pharmacokinetics studies how drugs change after administration via the processes of absorption, distribution, metabolism, and excretion (ADME). This review provides a summary of the pharmacokinetics studies of marine-derived active compounds, with a particular focus on their ADME. The pharmacokinetics of compounds derived from algae, crustaceans, sea cucumber, fungus, sea urchins, sponges, mollusks, tunicate, and bryozoan is discussed, and the pharmacokinetics data in human experiments are analyzed. In-depth characterization using pharmacokinetics is useful for obtaining information for understanding the molecular basis of pharmacological activity, for correct doses and treatment schemes selection, and for more effective drug application. Thus, an increase in pharmacokinetic research on marine-derived compounds is expected in the near future.

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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

Cited by 15 publications

References 33 publications

Characterization of Metabolic Pathways and Absorption of Sea Cucumber Saponins, Holothurin A and Echinoside A, in Vitro and in Vivo

Characterization of Metabolic Pathways and Absorption of Sea Cucumber Saponins, Holothurin A and Echinoside A, in Vitro and in Vivo

Trimethylamine-N-oxide (TMAO)-induced atherosclerosis is associated with bile acid metabolism

Pharmacokinetics of Marine-Derived Drugs

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