雷公藤红素在不同血浆中的蛋白结合率测定  

Determination of protein binding rates of celastrol in different species of plasma by HPLC

作　　者：袁菱[1,2] 陈彦[1,2] 周蕾[1,2] 郑丽燕[1] 曹伟[1,2] 

机构地区：[1]江苏省中医药研究院国家中医药管理局中药释药系统重点研究室,江苏南京210028 [2]江苏大学药学院,江苏镇江212013

出　　处：《中国医院药学杂志》2013年第3期175-179,共5页Chinese Journal of Hospital Pharmacy

基　　金：江苏省自然科学基金项目(编号:SBK201022193);江苏省中医药领军人才项目(编号:LJ200913);江苏省"333高层次人才培养工程"(编号:2012)

摘　　要：目的:研究雷公藤红素与大鼠、比格犬和人的血浆蛋白结合率。方法:采用血浆平衡透析法,以高效液相色谱法对透析内液与外液中雷公藤红素的含量进行测定,计算雷公藤红素与大鼠、比格犬和人的血浆蛋白结合率。结果:雷公藤红素低中高(0.25,0.5,1.0μg.mL-1)3个浓度的大鼠血浆蛋白结合率分别为(78.5±1.6)%,(77.3±2.2)%,(76.4±2.9)%,比格犬血浆蛋白结合率分别为(69.6±4.7)%,(71.1±3.4)%,(68.0±2.1)%,人血浆蛋白结合率分别为(85.6±2.7)%,(84.0±4.7)%,(83.1±2.8)%。结论:雷公藤红素与血浆蛋白具有中等强度的结合,其中与人血浆中的蛋白结合较强,且人>大鼠>比格犬。OBJECTIVE To study the protein binding rate of celastrol in the plasma of rats, Beagle dogs and humans. METHODS Equilibrium dialysis method was carried out to determine the plasma protein binding rates in different species. HPLC was employed to determine the concentration of celastrol inside or outside of the dialysis membrane, and then protein binding rates were calculated. RESULTS The plasma protein binding rates of celastrol at low, middle and high concentrations in different species were as follows, the plasma protein binding rates were （78. 5± 1.6）%, （77. 3 ± 2. 2）%, （76. 4 ± 2. 9）% in rats, （69.6±4.7）%, （71.1± 3. 4） % , （68.0±2.1）% in Beagle dogs , and（85.6±2.7）%, （84.0±4.7）%, （83.1±2.8）% in humans, respectively. CONCLUSION The protein binding rates of celastrol were of middle strength, which in rats, Beagle dogs and humans plasma were decreased in the following order： humans plasma〉rats plasma〉Beagle dogs plasma.

关 键 词：雷公藤红素 血浆蛋白结合率 平衡透析法 

分 类 号：R969[医药卫生—药理学]