State Key Laboratory of Molecular Oncology, Department of Urology, National Cancer Center/National Clinical Research Center for Cancer/Cancer Hospital, Chinese Academy of Medical Sciences and Peking Union Medical College, Beijing 100021, China.
State Key Laboratory of Bioactive Substance and Function of Natural Medicines, Institute of Materia Medica, Chinese Academy of Medical Sciences/Peking Union Medical College, Beijing 100050, China.
Molecules. 2022 May 10;27(10):3057. doi: 10.3390/molecules27103057.
The bioavailability of flavonoids is generally low after oral administration. The metabolic transformation of flavonoids by the gut microbiota may be one of the main reasons for this, although these metabolites have potential pharmacological activities. Liquiritigenin is an important dihydroflavonoid compound found in that has a wide range of pharmacological properties, such as antitumor, antiulcer, anti-inflammatory, and anti-AIDS effects, but its mechanism of action remains unclear. This study explored the metabolites of liquiritigenin by examining gut microbiota metabolism and hepatic metabolism in vitro. Using LC-MS/MS and LC/MS-IT-TOF techniques, three possible metabolites of liquiritigenin metabolized by the gut microbiota were identified: phloretic acid (M3), resorcinol (M4), and M5. M5 is speculated to be davidigenin, which has antitumor activity. By comparing these two metabolic pathways of liquiritigenin (the gut microbiota and liver microsomes), this study revealed that there are three main metabolites of liquiritigenin generated by intestinal bacteria, which provides a theoretical basis for the study of pharmacologically active substances in vivo.
黄酮类化合物经口服给药后通常生物利用度较低。肠道微生物群对黄酮类化合物的代谢转化可能是其中的主要原因之一，尽管这些代谢物具有潜在的药理活性。甘草素是在甘草中发现的一种重要的二氢黄酮类化合物，具有广泛的药理作用，如抗肿瘤、抗溃疡、抗炎和抗艾滋病作用，但作用机制尚不清楚。本研究通过体外考察肠道微生物群代谢和肝代谢，探讨了甘草素的代谢产物。利用 LC-MS/MS 和 LC/MS-IT-TOF 技术，鉴定出甘草素经肠道菌群代谢的三种可能的代谢产物：对羟基苯甲酸（M3）、间苯二酚（M4）和 M5。推测 M5 为具有抗肿瘤活性的大卫定。通过比较甘草素的这两种代谢途径（肠道菌群和肝微粒体），本研究揭示了肠道细菌产生的甘草素的三种主要代谢产物，为体内研究药理活性物质提供了理论依据。
