白花蛇舌草中芦丁、槲皮苷、异槲皮苷在正常大鼠与荷瘤大鼠体内药动学研究  

Pharmacokinetics of rutin,quercitrin,and isoquercitrin in Hedyotis diffusa in normal and tumor-bearing rats

作　　者：孟莹[1] 逯双 陈明月[1] 王少平[1] 曹广尚[3] 杨培民[3] MENG Ying1, LU Shuang2, CHEN Ming-yue1, WANG Shao-ping1, CAO Guang-shang3, YANG Pei-min3(1. Shandong University of Traditional Chinese Medicine, Ji＇nan 250355, China 2. Beijing Harmony Health Medical Diagnostics Co., Ltd., Ji＇nan 250000, China 3. Affiliated Hospital of Shandong University of Traditional Chinese Medicine, Ji＇nan 250011, Chin)

机构地区：[1]山东中医药大学,山东济南250355 [2]北京和合医学诊断技术股份有限公司,山东济南250000 [3]山东中医药大学附属医院,山东济南250011

出　　处：《中草药》2018年第6期1345-1350,共6页Chinese Traditional and Herbal Drugs

基　　金：国家自然科学基金资助项目(81773950;81274052);山东省自然科学基金资助项目(ZR2015HL116;ZR2011HL043)

摘　　要：目的以白花蛇舌草中黄酮苷类成分芦丁、槲皮苷、异槲皮苷为研究对象,基于荷瘤大鼠模型,研究黄酮苷类成分在病理状态下的药动学特征。方法 SD大鼠Walker-256皮下肿瘤模型,采用HPLC-MS/MS方法,分析比较白花蛇舌草中黄酮苷在荷瘤状态及正常机体状态的药动学特征。结果与正常大鼠黄酮苷药动学参数比较,荷瘤大鼠体内黄酮苷类成分芦丁、槲皮苷、异槲皮苷的最大浓度(C_(max))、曲线下面积(AUC_(0~∞))均明显降低,半衰期(t_(1/2z))延长,且3种成分在24 h后仍能检测到,代谢时间延长,揭示病理状态对黄酮苷药动学特征造成影响。结论 HPLC-MS/MS法操作简便、分析速度快、灵敏,适用于黄酮苷在大鼠体内的药动学研究,白花蛇舌草黄酮苷类成分在正常大鼠和荷瘤大鼠体内药动学特征有所差异。Objective Based on the tumor-bearing rat model, using rutin, quercitrin, and isoquercitrin from Hedyotis diffusa as the research object, the pharmacokinetics of those three flavonoid glycosides in the pathological state was studied. Methods Establishing a method for the comparison of the pharmacokinetics of flavonoid extracts in normal rats and tumor-bearing rats, which was analyzed by HPLC-MS/MS in subcutaneous tumor models of SD rat made with tumour cell of Walker-256. Results Compared with the pharmacokinetics parameters of flavonoid glycosides in normal rats, the Cmax and AUC（0-∞） of rutin, quercetin, and isoquercitrin in the tumor-bearing rats were significantly decreased, t（1/2z） was prolonged, and the metabolic time of three components was prolonged to 24 h, which revealed the effect of pathological condition on the pharmacokinetic characteristics of flavonoid glycosides. Conclusion The method established in this study is simple, fast, sensitive, and suitable for the pharmacokinetic study of flavonoid glycosides in rats in vivo. The pharmacokinetic characteristics of flavonoids in normal and tumor-bearing rats are different.

关 键 词：白花蛇舌草 黄酮苷 荷瘤大鼠 药动学 芦丁 槲皮苷 异槲皮苷 

分 类 号：R285.5[医药卫生—中药学]