Wen Ling, Zhu Mao-Mao, Yang Yan-Jun, Zhu Xiang-Jun, Liu Jun, Zhao Jing, Feng Liang, Jia Xiao-Bin
State Key Laboratory of Natural Medicine Active Components and Pharmacodynamics, School of Traditional Chinese Pharmacy,China Pharmaceutical University Nanjing 211198, China.
Jiangsu Health Development Research Center, National Health and Family Planning Commission Contraceptives Adverse Reaction Surveillance Center Nanjing 210036, China.
Zhongguo Zhong Yao Za Zhi. 2022 Nov;47(21):5775-5788. doi: 10.19540/j.cnki.cjcmm.20220513.501.
To clarify the metabolic transformation mechanism of phenylethanoid glycosides in Xiaoer Chiqiao Qingre Granules in vivo, this study extracted and separated the phenylethanoid glycosides in Xiaoer Chiqiao Qingre Granules. Based on UPLC-Q-TOF-MS/MS technology, the retention time and primary and secondary mass spectrometry information were analyzed by UNIFI software, and 11 phenylethanoid glycosides in Xiaoer Chiqiao Qingre Granules were preliminarily identified. Sixty-nine metabolites related to phenylethanoid glycosides were identified from the plasma samples of juvenile rats after administration of Xiaoer Chiqiao Qingre Granules. In addition, this study simulated the transformation system of intestinal flora in children, and discussed the metabolic effects of intestinal flora on the representative components forsythoside A, forsythoside E, and salidroside of phenylethanoid glycosides. The model of gastrointestinal heat retention in children with food accumulation was established to study the differential metabolites of phenylethanoid glycosides. Through the comparative analysis of the representative components absorbed in blood and the intestinal floral transformation products, it was found that the main metabolic pathways of phenylethanoid glycosides were dehydrogenation, oxidation, acetylation, sulfation, and glucuronidation. The findings of this study revealed the transformation law of phenylethanoid glycosides in the gastrointestinal tract. Through the preliminary discussion of the pharmacological mechanism, this study provides references for further clarifying the pharmacodynamic material basis of Xiaoer Chiqiao Qingre Granules and exploring the pediatric Chinese medicine compound.
为阐明小儿豉翘清热颗粒中苯乙醇苷类成分在体内的代谢转化机制,本研究对小儿豉翘清热颗粒中的苯乙醇苷类成分进行了提取分离。基于超高效液相色谱-四极杆飞行时间串联质谱(UPLC-Q-TOF-MS/MS)技术,通过UNIFI软件分析保留时间及一级、二级质谱信息,初步鉴定出小儿豉翘清热颗粒中的11种苯乙醇苷类成分。从小儿豉翘清热颗粒给药后幼年大鼠的血浆样本中鉴定出69种与苯乙醇苷类相关的代谢产物。此外,本研究模拟儿童肠道菌群转化体系,探讨了肠道菌群对苯乙醇苷类代表性成分连翘酯苷A、连翘酯苷E和红景天苷的代谢作用。建立食积化热型小儿胃肠积热模型,研究苯乙醇苷类的差异代谢产物。通过对吸收入血的代表性成分与肠道菌群转化产物的比较分析,发现苯乙醇苷类的主要代谢途径为脱氢、氧化、乙酰化、硫酸化和葡萄糖醛酸化。本研究结果揭示了苯乙醇苷类在胃肠道的转化规律。通过对药理机制的初步探讨,为进一步阐明小儿豉翘清热颗粒的药效物质基础及探索儿科复方中药提供参考。