目的研究五加皮Age蛋白的药动学特征。方法采用氯胺T法用125I标记Age蛋白,形成125I-Age复合物。S180荷瘤小鼠iv给药后,采用同位素示踪法结合SDS-PAGE电泳测定血浆中Age蛋白质量浓度。用3P87药动学软件分析血浆中Age蛋白的药动学参数。结果小鼠iv125I-Age后,Age蛋白在体内的代谢符合二房室分布模型。按剂量50、100、200μg/kgiv后,测得Age蛋白分布相半衰期(t1/2α)分别为0.34、0.45、0.26h,消除相半衰期(t1/2β)为14.13、16.49、17.42h,全身清除率(CLs)为0.0454、0.0491、0.0533mL/(h·kg)。结论Age蛋白在荷瘤小鼠体内药动学行为符合线性二室模型,在体内的分布和消除均较慢。

Objective To study the pharmacokinetic characteristics of Age protein in Cortex Acanthopanax.Methods Age protein was labeled using 1251 with chloramine-T method.the concentrationof Age protein in mouse plasma was determined by radioisotope tracer labeling method combined withSDS-PAGE.The pharmacokinetic parameters of Age protein in plasma were evaluated by a pharmacokinetic3P87 software.Results The Results showed that concentration-time curves after iV 125I-Age tOmice were fitted to a two-co.mpartment model.Following iv 125I-Age to mice in threedoses of 50,100,and200g/kg ,the (t1/2α) were 0.34,0.45,and 0.26 h,and(t1/2β) were 14.13,16.49,and 17.42 h.The systemicclearances(CLs)were 0.045 4,0.049 1,and 0.053 3 mL/(h·kg).Conclusion Pharmacokinetics ofAge protein conforms tO linear tWO-compartment model and it 7S distribution and elimination are both slowin tumor-bearing mice in vivo.

国家自然科学基金资助项目(3037153);河北省自然科学基金资助项目(C2004000610)