碘标白藜芦醇及其小鼠体内分布

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¹³¹I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¹³¹I白藜芦醇（每只0.185MBq，n=5）。¹³¹I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，¹³¹I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。

Radioiodine Labeling of Resveratrol and Its Biodistribution in Mice

In order to investigate the preparation of radioiodinated resveratrol and its biodistribution in mice, resveratrol was labeled with ¹³¹I using lactoperoxidase methods and purified by ethyl acetate. The radiolabeled compound was characterized by polyamide TLC, in which the substratum of V_{trichoromethane}∶ Vacetone∶Vethanol∶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 ¹³¹I 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 ¹³¹I 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 that ¹³¹I resveratrol 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. ¹³¹I resveratrol is metabolized mainly through liver and kidney. Simultaneously, its high distribution is also found in intestine. The %ID?g^-1 of ¹³¹I resveratrol is 11.70% at 10 min; the activity in thyroid increases with time. Therefore, the ¹³¹I resveratrol is worthy of further investigation to trace the compound in vivo and ex vivo.