Intestinal Glucuronidation, Prior to Hepatic Glucuronidation, Plays an Important Role in the Low Circulating Levels of Calycosin

Separations

article

Haodong Jiang¹  Huan Liu²  Pei Hu²  Shuoji Chen²  Yaqing Ye²  Chenggang Huang¹  Xiaoting Tian² 

[1] School of Chinese Materia Medica, Nanjing University of Chinese Medicine;Shanghai Institute of Materia Medica, Chinese Academy of Sciences;Guangxi Key Laboratory of Translational Medicine for Treating High-Incidence Infectious Diseases with Integrative Medicine, Guangxi University of Chinese Medicine

关键词: calycosin;    first-pass effect;    intestinal glucuronidation;    liver distribution;    metabolism;   

DOI  :  10.3390/separations9050115

学科分类：社会科学、人文和艺术（综合）

来源: mdpi

【 摘 要 】

Calycosin is a dietary flavonoid with favorable activities, which seems to be inconsistent with its low circulating levels in vivo. To address this issue, we developed a strategy to understand calycosin distribution by integrating qualitative and quantitative analyses of calycosin and its metabolites in portal vein plasma, the liver, and systemic plasma after oral administration to rats. Consequently, 21 metabolites were characterized in total, including the first report of a reductive biotransformation and 14 new metabolites. Compared with the low levels of calycosin, calycosin glucuronides were predominant in circulation, and both the hepatic and intestinal regions contributed to the high exposure of these calycosin glucuronides. However, intestinal glucuronidation, prior to hepatic glucuronidation, plays a key role in the low circulating levels of calycosin.

【 授权许可】

CC BY