A metabolic way to investigate related hurdles causing poor bioavailability in oral delivery of isoacteoside in rats employing ultrahigh‐performance liquid chromatography/quadrupole time‐of‐flight tandem mass spectrometry

Cui, Qingling; Pan, Yingni; Yan, Xiaowei; Bao, Qu; Liu, Xiaoqiu; Xiao, Wei

doi:10.1002/rcm.7795

Cited by 6 publications

(2 citation statements)

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“…There are eight possible metabolic pathways that led to the generation of these metabolites, including deglycosylation, the removal of rhamnose and the removal of hydroxytyrosol. Cui et al [ 41 ] showed that isoacteoside (ISAT) was metabolized in the gastrointestinal tract before entering the bloodstream, which reveals the reason for its poor bioavailability. The biotransformation process of oral ISAT in vivo is as follows.…”

Section: The Bioavailability Of Phgsmentioning

confidence: 99%

Research Progress and Trends of Phenylethanoid Glycoside Delivery Systems

Huang

Zhao

Cui

et al. 2022

Foods

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Background: Phenylethanoid glycosides (PhGs) are obtained from a wide range of sources and show strong biological and pharmacological activities, such as antioxidant, antibacterial and neuroprotective effects. However, intestinal malabsorption and the low bioavailability of PhGs seriously affect their application. Delivery systems are an effective method to improve the bioavailability of active substances. Scope and approach: In this article, the biological activities of and delivery systems for PhGs are introduced. The application statuses of delivery systems for echinacoside, acteoside and salidroside are reviewed. Finally, the problems of the lack of uniform standards for delivery systems and the poor targeted delivery accuracy of PhGs in the current research are proposed and suggestions for future research are put forward based on those problems. Key findings and conclusions: Although there are still some problems in the delivery system of phenylethanoside, such as inconsistent standards and inaccurate delivery, phenylethanoside itself has been proven to have a variety of physiological activities. Therefore, the action mechanism and application of phenylethanoside and its delivery system should be studied further.

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Section: The Bioavailability Of Phgsmentioning

confidence: 99%

Research Progress and Trends of Phenylethanoid Glycoside Delivery Systems

Huang

Zhao

Cui

et al. 2022

Foods

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“…Most herbal medicines are administered orally, and the components are inevitably metabolized before absorption from the gastrointestinal tract; however, poor oral absorption of PhGs was observed in a Caco-2 cell monolayer model, suggesting poor intestinal permeability (Gao et al, 2015; Zhou et al, 2018). A low blood drug concentration and relatively rapid metabolism of PhGs were observed after dosing in previous pharmacokinetic studies (Qi et al, 2013; Deng et al, 2014; Li et al, 2015a; Cui et al, 2016a; Li et al, 2016a; Su et al, 2016; Cui et al, 2017; Feng et al, 2018; Qian et al, 2018); however, these existing results are inadequate to fully understand the metabolic process and the mechanism underlying the pharmacologic activities. An in vitro digestion model provides a useful platform for fast and reproducible assessment of herbal medicine metabolism (Payne et al, 2012; Kang et al, 2013; Xu et al, 2017; Cui et al, 2018; Zhang et al, 2018; Feng et al, 2019).…”

Section: Introductionmentioning

confidence: 97%

An Integrated Approach to Characterize Intestinal Metabolites of Four Phenylethanoid Glycosides and Intestinal Microbe-Mediated Antioxidant Activity Evaluation In Vitro Using UHPLC-Q-Exactive High-Resolution Mass Spectrometry and a 1,1-Diphenyl-2-picrylhydrazyl-Based Assay

et al. 2019

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Intestinal bacteria have a significant role in metabolism and the pharmacologic actions of traditional Chinese medicine active ingredients. Phenylethanoid glycosides (PhGs), as typical phenolic natural products, possess wide bioactivities, but low oral bioavailability. The aim of this work was to elucidate the metabolic mechanism underlying PhGs in the intestinal tract and screen for more active metabolites. In this study, a rapid and reliable method using an effective post-acquisition approach based on advanced ultra-high-performance liquid chromatography (UHPLC) coupled with hybrid Quadrupole-Orbitrap high resolution mass spectrometry (Q-Exactive-HRMS) provided full MS and HCD MS 2 data. Thermo Scientific™ Compound Discoverer™ software with a Fragment Ion Search (FISh) function in one single workflow was developed to investigate the intestinal microbial metabolism of four typical PhGs. Furthermore, antioxidant activity evaluation of PhGs and their related metabolites was simultaneously carried out in combination with a 1,1-diphenyl-2-picrylhydrazyl (DPPH) assay to understand how intestinal microbiota transformations modulate biological activity and explore structure–activity relationships (SARs). As a result, 26 metabolites of poliumoside, 42 metabolites of echinacoside, 42 metabolites of tubuloside, and 46 metabolites of 2′-acetylacteoside were identified. Degradation, reduction, hydroxylation, acetylation, hydration, methylation, and sulfate conjugation were the major metabolic pathways of PhGs. Furthermore, the degraded metabolites with better bioavailability had potent antioxidant activity that could be attributed to the phenolic hydroxyl groups. These findings may enhance our understanding of the metabolism, pharmacologic actions, and real active forms of PhGs.

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