小儿豉翘清热颗粒黄酮组分在模拟婴儿胃肠道环境中的消化特性  

Digestive properties of flavonoid components in Xiaoer Chiqiao Qingre Granules in simulated infant gastrointestinal environment

作　　者：周滨滨 杨艳君 朱毛毛 杨冰 马维坤 朱向珺 刘俊 赵菁 封亮 贾晓斌 ZHOU Bin-bin;YANG Yan-jun;ZHU Mao-mao;YANG Bing;MA Wei-kun;ZHU Xiang-jun;LIU Jun;ZHAO Jing;FENG Liang;JIA Xiao-bin(Stale Key Laboratory of Natural Medicine Active Components and Pharmacodynarmics,School of Traditional Chinese Pharmacy,China Pharmaceutical Uniersiry,Nanjing 11198,China;Jiangsu Health Derelopment Research Center,National Health and Family Planning Commission Contraceptives Adrerse Reaction Sureillance Center,Nanjing 210036,China;Jiangsu Key Laboratory of Chinese Medicine and Characteristic Preparations for Paediatries,Jumpcan Pharmaceutical Co.,Ltd.,Taixing 225400,Chuna)

机构地区：[1]中国药科大学中药学院天然药物活性组分与药效国家重点实验室,江苏南京211198 [2]国家卫生健康委计划生育药具不良反应监测中心江苏省卫生健康发展研究中心,江苏南京210036 [3]济川药业集团有限公司江苏省儿科中药与特色制剂重点实验室,江苏泰兴225400

出　　处：《中国中药杂志》2022年第21期5735-5745,共11页China Journal of Chinese Materia Medica

基　　金：江苏省科技成果转化专项(BA2020077);江苏省卫生健康发展研究中心开放课题(JSHD2021040);中国药科大学双一流创新团队项目(CPU2018GY11);天然药物活性组分与药效国家重点实验室项目(SKLNMZZ202025)。

摘　　要：为阐明小儿豉翘清热颗粒黄酮组分在婴儿胃肠道环境中的消化特性,该研究通过建立体外模拟婴儿胃、肠环境模型,采用UPLC对小儿豉翘清热颗粒黄酮组分消化过程的含量变化进行分析,并经质量权重系数法整合黄酮组分整体含量,借助UPLC-Q-TOF-MS技术,探究黄酮组分胃肠液消化产物并推测其代谢途径。结果表明,在胃肠液消化过程中,黄酮组分发生氧化、还原、脱糖基、甲基化等Ⅰ相代谢反应,产生共11种消化产物。由黄酮组分含量与成分变化结果可知,小儿豉翘清热颗粒黄酮组分在胃液中较稳定,在肠液中其含量呈先上升后保持稳定的趋势,主要原因为在胃肠消化时黄酮组分从蛋白质、多糖等大分子物质中释放,使其含量有所上升,同时发生了Ⅰ相代谢反应,但代谢速率相对较小,致使其含量趋于稳定。该研究初步探究了小儿豉翘清热颗粒黄酮组分在婴儿胃肠道环境中的消化特征,为进一步研究小儿豉翘清热颗粒药效组分在婴儿体内吸收、转运、代谢等过程奠定基础,同时为儿科中药的生物药剂学性质研究提供参考依据。This study aimed to elucidate the digestive characteristics of flavonoid components in Xiaoer Chiqiao Qingre Granules(XECQ) in the gastrointestinal environment of infants. An in vitro model was established to simulate the gastric and intestinal environment of infants. UPLC was used to analyze the content change of flavonoid components in XECQ, and their overall content was integrated through the mass fraction weight coefficient method. UPLC-Q-TOF-MS was employed to determine the digestive products of flavonoid components in gastrointestinal fluids and their metabolic pathways. The results showed that in the process of digestion, 11 digestion products were generated by oxidation, reduction, deglycosylation, methylation and other phase Ⅰ metabolism. From flavonoid content and component changes, it was found that the flavonoid components in XECQ were relatively stable in the gastric fluid, while their content in the intestinal fluid was first increased and then maintained stable. This was mainly because flavonoid components were released from proteins, polysaccharides and other macromolecular substances during gastrointestinal digestion. In addition, phase Ⅰ metabolism occurred, but with relatively low metabolic rate, resulting in their stable content. This study preliminarily explored the digestive characteristics of flavonoid components in XECQ in the infant gastrointestinal environment, which laid a foundation for further studying the absorption, transport and metabolism of pharmacodynamics components in XECQ, and facilitated the study of the biopharmaceutical pro-perties of pediatric Chinese medicine.

关 键 词：小儿豉翘清热颗粒 黄酮组分 UPLC-Q-TOF-MS技术 婴儿 消化特性 

分 类 号：R272[医药卫生—中医儿科学]