左旋千金藤啶碱在活体大鼠体内代谢过程的可视化PET/CT显像研究

Study on visualization of metabolic process of L-stepholidine in living rats by PET/CT in vivo

目的探索通过PET/CT显像将中药有效成分在体内的代谢过程变成可视的图像,并通过图像对其进行定量分析的可行性。方法以延胡索的有效成分左旋千金藤啶碱(L-SPD)作为研究对象。使用正电子核素11碳(11C)标记L-SPD,在热室内化学合成11C-L-SPD。SD大鼠戊巴比妥钠麻醉后固定于木板上,尾iv 37 MBq 11C-L-SPD。分别于注射后5、15、30、45、60、90 min行PET/CT显像。使用工作站获得脑、心脏、肺脏、肝脏、肾脏、肠腔、膀胱的放射性容积分布比值(distribution volume ratios,DVR)。结果 PET/CT显像显示在5 min时11C-L-SPD在肝脏、肾脏分布最多,心脏、肺、脑可见放射性分布。肝、肾是11C-L-SPD的主要代谢及排泄器官,肝、肾、肠腔、膀胱在5 min DVR分别为(1.37±0.42)%、(1.10±0.19)%、(0.89±0.18)%、(0.97±0.11)%,90 min分别为(0.65±0.11)%、(0.54±0.05)%、(5.49±1.44)%、(9.86±1.88)%。结论 PET/CT显像可以直观、动态地观察L-SPD在活体内的分布及代谢特点,有望用于其他中药有效成分的活体显像研究。

Objective To exolpre the feasibility to transform the metabolic process of active constituents of Chinese herbal medicine in vivo into images by PET/CT and to make quantitative analysis. Methods The l-stepholidine was used as study object, and chemical synthesis of HC-L-SPD was performed in hot room. PET/CT scan was performed in different time, 5, 15, 30, 45, 60, and 90 min after injecting 11C-L-SPD by vail in rats, and the information of brain, heart, lung, liver, kidney, intestine, and bladder was transferred to the Workststion. The distribution volume ratios （DVR） of the above tissues were obtained. Results 11C-L-SPD was keeping in a relative higher level in liver and kidney at 5 rain. metabolism through the liver, kidney was the main eccrisis organ. The distribution of 11C-L-SPD in liver, kidney, intestine, and bladder was （1.37 ± 0.42）%, （1.10 ± 0.19）%, （0.89 ±0.18）%, and （0.97 ±0.111）% respectively at 5 rain and was （0.65 ± 0.11）%, （0.54 ±0.05）%, （5.49 ± 1.44）%, and （9.86 ±1.88）% respectively at 90 min. Conclusion PET/CT imaging could observe the distribution and metabolism of 11c-L-SPD dynamically and directly. It could be used in the research of other Chinese medicines.