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

Xinchi Feng¹  Feng Qiu¹  Yang Li¹  Chenxi Guang¹  Miao Qiao¹  Tong Wang¹  Liwei Chai¹ 

[1] School of Chinese Materia Medica, Tianjin University of Traditional Chinese Medicine, Tianjin 300193, China;

关键词: linarin;    ring cleavage metabolites;    UPLC/Q-TOF-MS/MS;    rats;    intestinal flora;   

DOI  :  10.3390/molecules23092140

来源: DOAJ

【 摘 要 】

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.

【 授权许可】

Unknown