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Characterization of the In Vivo and In Vitro Metabolites of Linarin in Rat Biosamples and Intestinal Flora Using Ultra-High Performance Liquid Chromatography Coupled with Quadrupole Time-of-Flight Tandem Mass Spectrometry

by 1,†, 1,2,†, 1,2, 1,2, 1,2, 1,2 and 1,2,*
1
School of Chinese Materia Medica, Tianjin University of Traditional Chinese Medicine, Tianjin 300193, China
2
Tianjin State Key Laboratory of Modern Chinese Medicine, Tianjin University of Traditional Chinese Medicine, Tianjin 300193, China
*
Author to whom correspondence should be addressed.
These authors contributed equally to this work.
Molecules 2018, 23(9), 2140; https://doi.org/10.3390/molecules23092140
Received: 30 July 2018 / Revised: 20 August 2018 / Accepted: 23 August 2018 / Published: 25 August 2018
(This article belongs to the Section Natural Products Chemistry)
Linarin, a flavone glycoside, is considered to be a promising natural product due to its diverse pharmacological activities, including analgesic, antipyretic, anti-inflammatory and hepatoprotective activities. In this research, the metabolites of linarin in rat intestinal flora and biosamples were characterized using ultra-high-performance liquid chromatography/quadrupole time-of-flight mass spectrometry (UPLC/Q-TOF-MS/MS). Three ring cleavage metabolites (4-hydroxybenzoic acid, 4-hydroxy benzaldehyde and phloroglucinol) were detected after linarin was incubated with rat intestinal flora. A total of 17 metabolites, including one ring cleavage metabolite (phloroglucinol), were identified in rat biosamples after oral administration of linarin. These results indicate that linarin was able to undergo ring fission metabolism in intestinal flora and that hydrolysis, demethylation, glucuronidation, sulfation, glycosylation, methylation and ring cleavage were the major metabolic pathways. This study provides scientific support for the understanding of the metabolism of linarin and contributes to the further development of linarin as a drug candidate. View Full-Text
Keywords: linarin; ring cleavage metabolites; UPLC/Q-TOF-MS/MS; rats; intestinal flora linarin; ring cleavage metabolites; UPLC/Q-TOF-MS/MS; rats; intestinal flora
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Feng, X.; Li, Y.; Guang, C.; Qiao, M.; Wang, T.; Chai, L.; Qiu, F. Characterization of the In Vivo and In Vitro Metabolites of Linarin in Rat Biosamples and Intestinal Flora Using Ultra-High Performance Liquid Chromatography Coupled with Quadrupole Time-of-Flight Tandem Mass Spectrometry. Molecules 2018, 23, 2140.

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