[关键词]
[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(Cmax)、曲线下面积(AUC0~∞)均明显降低,半衰期(t1/2z)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。
[Key word]
[Abstract]
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 AUC0-∞ of rutin, quercetin, and isoquercitrin in the tumor-bearing rats were significantly decreased, t1/2z 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.
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[基金项目]
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)