通过碘-131标记白藜芦醇探讨白藜芦醇在小鼠体内的分布代谢。采用过氧化物酶法对白藜芦醇进行131^I标记;经乙酸乙酯萃取纯化,以聚酰胺薄膜为支持介质,V(三氯甲烷):V(丙酮):V(乙醇):V(水)=4:4:0.5:0.4为展开剂,测定标记物的标记率和放化纯;KM小鼠尾静脉注射131^I-白藜芦醇(每只0.185MBq,n=5)。131^I-白藜芦醇标记率达69.3%,萃取分离后其放化纯为95.9%,3、7和15d后分别为92.0%、90.4%、90.1%;动物实验显示,131^I-白藜芦醇在小鼠体内广泛分布,主要经肝和肾进行代谢,5min时每克组织百分注射剂量率(%ID·g^-1)分别为16.35、13.05,在肠中也有较高分布,10min时%ID·g^-1为11.70;甲状腺的摄取率随时间的延长而增加。碘标白藜芦醇标记物较稳定,可用于进一步的微量示踪研究。
In order to investigate the preparation of radioiodinated resveratrol and its biodistribution in mice, resveratrol was labeled with 131^I using lactoperoxidase methods and purified by ethyl acetate. The radiolabeled compound was characterized by polyamide TLC, in which the substratum of Vtrichoromethane: Vaacetone: Vetbanol : VAdam's ale : 4 : 4 : 0. 5 : 0. 4 was used as the developing agent. Biodistribution studies were accomplished on KM mice. At different time after radiopharmaceutical i. v. administration (0. 185 MBq 131^I-tetrahydropalmatine/mouse), the animals were sacrificed (n=5 animals for each time). Blood and the interested tissues were collected, washed, weighted and counted. The percent injected dose per gram (%ID · g^-1) was calculated for each sample. The labeling yield of 131^I-resveratrol is 69.3% and its RCPs are 95.9%, 92.0%, 90.4%, and 90. 1% after 1, 3, 7 and 15 d, respectively. Biodistribution in mice demonstrates that131^Iresveratrol is distributed into broad organs and tissues. However, it reveals higher levels in liver, kidney and intestine than in other tissues. In liver and kidney, the % ID · g ^-1are 16. 35% and 13. 05% at 5 min, respectively. 131^I-resveratrol is metabolized mainly through liver and kidney. Simultaneously, its high distribution is also found in intestine. The %ID · g^-1of 131^I-resveratrol is 11. 700% at 10 min; the activity in thyroid increases with time. Therefore, the 131^ I-resveratrol is worthy of further investigation to trace the compound in vivo and ex vivo.