上海中医药杂志2026，Vol.60Issue(1)：73-81,9.DOI:10.16305/j.1007-1334.2026.z20250513006
基于黄芪皂苷类成分药代动力学特征解析黄芪皂苷Ⅰ的质控合理性
Analysis of rationality of quality control for astragaloside Ⅰ based on pharmacokinetic characteristics of Astragalus saponins
摘要
Abstract
Objective Given that cycloastragenol is the primary active in vivo metabolite of astragaloside compounds,this study aimed to evaluate the suitability of quality control markers for Astragalus saponins.Methods High-performance liquid chromatography(HPLC)was used to quantify the main components in Astragalus aqueous extract and total Astragalus saponins.Pharmacokinetic studies were conducted in male C57BL/6J mice,which were randomly divided into five groups:total Astragalus saponins group,astragaloside Ⅰ group,astragalosideⅣ group,cycloastragenol group,and control group.Each treatment group was administered 50 mg·kg-1 body weight of the corresponding agent via gavage,while the control group received physiological saline.Serum,liver tissue,and intestinal contents were collected at 10,30,90,180,300,480,960,and 1 440 minutes post-administration.Concentrations of astragalosides Ⅰ-Ⅳ,isoastragalosides Ⅰ-Ⅱ,and cycloastragenol were determined using UHPLC-Q-Exactive Orbitrap high-resolution mass spectrometry(HRMS),and pharmacokinetic parameters were subsequently calculated.Additionally,in vitro fecal microbiota incubation assays were performed with astragalosides Ⅰ andⅣ;concentrations of cycloastragenol and the major saponins were measured at 0,1,3,8,and 24 hours using UHPLC-Q-Exactive Orbitrap HRMS.Results In both Astragalus aqueous extract and total Astragalus saponins,the content of astragaloside Ⅰ was significantly higher than that of astragaloside Ⅳ.After oral administration,the exposure of cycloastragenol in serum and liver tissue in the total Astragalus saponins group was 2.6-fold and 10.4-fold higher,respectively,compared with that in the astragaloside Ⅳ group.Astragaloside Ⅰ exhibited a higher metabolic efficiency to cycloastragenol than astragaloside Ⅳ:in vitro,its metabolic efficiency was 7.3-fold higher,and in vivo,its total conversion rate was 5.9-fold greater.Conclusion Compared with astragaloside Ⅳ,astragaloside Ⅰ is a more appropriate quality control marker for Astragalus saponins.关键词
黄芪皂苷类成分/黄芪皂苷Ⅰ/黄芪皂苷Ⅳ/环黄芪醇/中药/质量控制Key words
Astragalus saponins/astragaloside Ⅰ/astragaloside Ⅳ/cycloastragenol/Chinese materia medica/quality control引用本文复制引用
LIU Wei,LI Chunhui,ZHANG Linzhang,CHEN Jiamei,LIU Ping..基于黄芪皂苷类成分药代动力学特征解析黄芪皂苷Ⅰ的质控合理性[J].上海中医药杂志,2026,60(1):73-81,9.基金项目
上海市科委科技启明星项目(24QA2709200) （24QA2709200）
上海市东方英才计划青年项目(QNWS2024054) （QNWS2024054）
上海市"科技创新行动计划"自然科学基金项目(24ZR1467100) （24ZR1467100）
上海市超级博士后激励计划(2024530) （2024530）
上海市自然科学基金青年基金项目(25ZR1402483) （25ZR1402483）
中国博士后基金面上项目(2025M773981) （2025M773981）
国家资助博士后研究人员计划C档资助项目(GZC20252641) （GZC20252641）
