白芍总苷对小鼠单核巨噬细胞作用时-效曲线研究  

Study on Time-Effect Curve of Total Glucosides of Paeony on Mouse Mononuclear Macrophages

作　　者：王帅[1,2,3] 包永睿[1,2,3] 杨欣欣[1,2,3] 李天娇[1,2,3] 孟宪生[1,2,3] 

机构地区：[1]辽宁中医药大学药学院,辽宁大连116600 [2]辽宁省组分中药工程技术研究中心,辽宁大连116600 [3]辽宁省现代中药研究工程实验室,辽宁大连116600

出　　处：《时珍国医国药》2017年第3期541-544,共4页Lishizhen Medicine and Materia Medica Research

基　　金：国家自然科学基金(No.81241111);辽宁省高等学校优秀人才支持计划项目(No.LR2013044)

摘　　要：目的利用药动参数结合药效综合指标开展白芍总苷体外抗炎时效相关性评价研究,为探讨其临床合理利用提供前期实验基础。方法取SD大鼠灌服白芍总苷提取液(290mg·kg^(-1))后,以HPLC-TOF-MS法测定不同采血时间点血浆中芍药内酯苷、芍药苷浓度,根据药时曲线计算药动学参数;以TNF-α、IL-6和NO的综合指标为考察对象,开展不同时间点含药血浆体外药效评价研究;将体内药动与体外药效相结合开展时效相关性分析,评价白芍总苷作用规律及特点。结果白芍总苷中芍药苷和芍药内酯苷的T_(max)分别为60、30min,C_(max)为1860.7、895.8μg·ml^(-1);白芍总苷含药血浆浓度(尤其是芍药苷)与小鼠单核巨噬细胞体外炎症模型抑制率之间呈良好的相关性。结论实验明确了白芍总苷体内代谢与药效的变化规律,为其临床合理使用及新药开发提供基础。Objective Using pharmacokinetic parameter combined with comprehensive indexes of efficacy to carry out the anti - inflammatory time- effect correlation evaluation study of total glucosides of paeony（TGP） in vitro, which provides preliminary ex- perimental basis for its reasonable clinical use. Methods After orally administrated TGP extract（290mg·kg-1 ）, HPLC -TOF - MS method was used to detect the content of peony lactone glycosides and paeoniflorin at different blood sampling time point in plasma of SD rat. Pharmacokinetic parameters were calculated according to drug - time curve ; taking TNF -α, IL - 6 and NO comprehensive index as investigation object to promote efficacy evaluation research at different time points in vitro; combining the pharmacokinetics in vivo with efficacy in vitro to carry out time - effect correlation analysis and evaluate functional rules and char- acteristics of TGP. Results The Tin= of peony lactone glycosides and paeoniflorin in TGP were 60 and 30min, Cmax were 1860.7 and 895.8μg·mL-1. There is good correlation between drug plasma concentration of TGP （especially paeoniflorin） and its inhibition rate on mononuclear macrophage. Conclusion This experiment has revealed the metabolism of TGP in vivo and the efficacy change rules, which provides the basis for the reasonable clinical use and new drug development of TGP.

关 键 词：白芍总苷 小鼠单核巨噬细胞 TNF-Α IL-6 NO 时-效曲线 

分 类 号：R285.5[医药卫生—中药学]