【摘要】 目的制备心肌保护药物35S-炔丙基半胱氨酸(35S-propargyl-cysteine,35S-SPRC)并以其为示踪剂研究SPRC在SD大鼠体内的生物学分布。方法以半胱氨酸为起始原料合成非标记的SPRC,通过冷试验确定合成路线、反应条件及分析鉴定方法。在此基础上,以35 S-L-半胱氨酸为原料合成35 S-SPRC,35 S-SPRC的鉴定采用TLC法及放射自显影法。按实验要求,将35S-SPRC配制成一定比活度的放射性溶液。取SD大鼠18只,随机分成3组,按15mg/kg的剂量通过灌胃给药35S-SPRC。在不同时相将大鼠处死,取各脏器,称重、匀浆、消化,用液体闪烁计数器测定各样本的放射性活度。结果最终产物35S-SPRC的TLC结果与SPRC完全一致,35S-SPRC的放化纯度大于95%。大鼠体内的生物学分布表明,35S-SPRC在大部分器官内0.5h达到峰值。结论运用35S-SPRC能准确地测定SPRC在大鼠体内的生物分布。更多还原

【Abstract】 Objective To prepare 35S-propargyl-cysteine(35S-SPRC) and through the isotopic tracer method to measure the biodistribution of SPRC in vivo of SD rats.Methods Non-radioactive labelled SPRC was synthesized by the starting material of cysteine and the synthetic route,reaction conditions and analytical identification were determined by the acquiration.On this basis,35S-L-cysteine was used to make 35S-SPRC,whose identification involved methods of TLC and phosphorus screen device autoradiography.To meet the experimental requirements,35S-SPRC was prepared in certain specific activity and radioactive concentration.Eighteen SD rats were randomly divided into 3 groups.35S-SPRC of 15 mg/kg was given intragastrically.The rats were killed at different time points with viscera organs first taken out,then homogenized,solubilized,and the liquid scintillation gauge was used to determine the radioactivity of each sample.Results TLC behavior of 35S-SPRC was completely as same as SPRC,with its radiochemical purity being higher than 95%.The biological distribution in rats showed that,within half an hour,35S-SPRC could reach its peak concentration in most organs.Conclusions The use of 35S-SPRC can accurately determine the SPRC biodistribution in rats.更多还原