摘要
研究藤茶总黄酮口服给药后大鼠肠道代谢的产物及其体外抗肝癌活性。采用超高效液相色谱-高分辨质谱(UPLC-HRMS)联用技术分析总黄酮在大鼠肠道中的代谢产物,并以MTT法检测代谢产物对肝癌细胞HepG2增殖的抑制活性。通过UPLC-HRMS测定,总黄酮在大鼠粪便中检测到6个代谢产物。其主成分二氢杨梅素主要通过硫酸化、去羟基化、甲基化、还原去羟基化等反应发生代谢转化;其他成分杨梅苷、杨梅素则分别发生水解、去羟基化反应生成相应的代谢产物;这些代谢产物对HepG2细胞增殖有较好抑制作用,在不同作用时间点(48 h、72 h),其IC50分别是179.58、103.24μg/mL。藤茶总黄酮口服后在大鼠肠道中可发生多种代谢反应,其代谢产物具有体外抗肝癌活性。
To investigate the intestinal metabolites of Ampelopsis grossedentala total flavonoids after oral administration and anti-hepatoma activity in vitro.The metabolites of total flavonoids in the intestinal tract of rats were analyzed by ultra-high performance liquid chromatography-high resolution mass spectrometry(UPLCHRMS),and their inhibitory activities on the proliferation of hepatocellular carcinoma cells HepG2 were detected by MTT assay.Six metabolites of total flavonoids were detected in rat feces by UPLC-HRMS.The main component dihydromyricetin was metabolically transformed through sulfation,dehydroxylation,methylation,reduction dehydroxylation reactions,and the other components,myricitrin and myricetin,were hydrolyzed and dehydroxylated to produce the corresponding metabolites.These metabolites could inhibit the proliferation of HepG2 cells,and the IC50 was 179.58 and 103.24μg/mL at different time points(48 h and 72 h),respectively.After oral administration of A.grossedentala total flavonoids,a variety of metabolic reactions can occur in the rat gut,and its metabolites have anti-hepatoma activity in vitro.
作者
林珠灿
苗航
罗花彩
刘冬雪
陈达炜
郭素华
LIN Zhu-can;MIAO Hang;LUO Hua-cai;LIU Dong-xue;CHEN Da-wei;GUO Su-hua(College of Pharmacy,Fujian University of Traditional Chinese Medicine,Fuzhou,Fujian 350122,China;People's Hospital Affiliated to Fujian University of traditional Chinese Medicine,Fuzhou,Fujian 350004,China;NHC Key Laboratory of Food Safety Risk Assessment,China National Center for Food Safety Risk Assessment,Beijing 100021,China)
出处
《井冈山大学学报（自然科学版）》
2023年第5期73-78,共6页
Journal of Jinggangshan University (Natural Science)
基金
福建省自然科学基金面上项目(2021J01919)。
关键词
藤茶总黄酮
肠道代谢产物
体外抗肝癌
Ampelopsis grossedentala total flavonoids
intestinal metabolites
anti-hepatoma activity in vitro
