Systematic characterization of the metabolites of echinacoside and acteoside from Cistanche tubulosa in rat plasma, bile, urine and feces based on UPLC‐ESI‐Q‐TOF‐MS

Abstract

Echinacoside (ECH) and acteoside (ACT), as the most and major active components of Cistanche tubulosa, were reported to possess cardioactive, neuroprotective and hepatocyte protective effects, as well as antibacterial, antioxidative effects. Recently, more studies have focused on their pharmacological activities. However, their metabolic profiles in vivo have not been sufficiently investigated. This study proposes an approach for rapidly identifying the complicated and unpredictable metabolites of ECH and ACT in rat plasma, bile, urine and feces, and systematically and comprehensively revealing their major metabolic pathways, based on powerful ultra-high performance liquid chromatography coupled with quadrupole time-of-flight tandem mass spectrometry. Plasma, bile, urine and feces were collected from rats after a single 200 mg/kg oral dose. A total of 49 metabolites were detected in rat biological samples. Through analyzing metabolites in bile samples, it was found that ECH and ACT were subjected to a marked hepatic first-pass effect in liver. Copyright © 2016 John Wiley & Sons, Ltd.

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

“…S2, Supporting Information). On the basis of the retention time (RT), accurate mass, mass spectral fragmentation patterns and the previous investigation of credible MS and MS/MS fragmentation behaviors of phenylethanoid glycosides such as acteoside and echinacoside, a total of 45 potential active metabolites of ISAT including the parent compound and structural isomers were tentatively identified in vivo (rat plasma, bile, urine and feces) in the present study. According to the structures of metabolites, it was apparent that dehydroxylation, hydrolyzation, methylation, reduction, sulfation, and glucuronidation were the main metabolic pathways of ISAT in vivo .…”

“…Metabolites M14 (RT = 4.67 min, pseudomolecular ion 181.0506) and M7 (RT = 6.42 min, pseudomolecular ion 181.0506) with the same elemental composition of C 9 H 9 O 4 were identified as dihydroxycaffeic acid and homovanillic acid, respectively, according to a previous report …”

“…The metabolites M8 and M9 with [M–H] – ions at m/z 357.0830 and 261.0076, which were 176 Da and 80 Da more than that of m/z 181.0506, suggesting that they were glucuronide and sulfated conjugates of homovanillic acid …”

Comparison of the Chemical Profiles and Antioxidant Activities of Different Parts of Cultivated Cistanche deserticola Using Ultra Performance Liquid Chromatography-Quadrupole Time-of-Flight Mass Spectrometry and a 1,1-Diphenyl-2-picrylhydrazyl-Based Assay

“…Thus, the peak was determined as cistanoside A, as its retention time and mass spectra correspond to those of the authentic reference standard. Finally, the antioxidants were identified by their mass spectra and fragmentation patterns with the aid of standard references and literature reports [ 24 , 25 , 26 , 27 , 28 , 29 , 30 , 31 , 32 ].…”

Therapeutic potential of phenylethanoid glycosides: A systematic review

“…After ig administration of 200 mg/kg verbascoside and 200 mg/kg echinacoside in rats, their relative content in plasma, feces, urineand bile was calculated. Only 1.54% of echinacoside and no verbascoside was detected in plasma 205. Sibirioside A (200 mg/kg) and angoroside C (200 mg/kg) from S. radix were widely distributed in heart, lung, liver, stomach, kidney, and small intestine in…”