Takeda A, Hibino T, Hoshino A, Okumura H, Okada S
Department of Radiobiochemistry, School of Pharmaceutical Sciences, University of Shizuoka, Japan.
Int J Rad Appl Instrum B. 1991;18(5):499-502. doi: 10.1016/0883-2897(91)90110-7.
To elucidate a factor required for tumor-imaging 99mTc-labeled radiopharmaceuticals, in vivo behaviors of 99mTc-L-cysteine (99mTc-Cys) and 99mTc-2-mercaptoethylamine (99mTc-ME) were compared with that of 99mTc-DL-homocysteine (99mTc-Hcy) which had been found to accumulate in several experimental tumors. When these three complexes were intravenously injected into mice bearing Ehrlich solid tumor, their tumor affinity was found to depend on their binding ability to serum albumin; 99mTc-Hcy, the albumin-binding ability of which was highest of the three, was the most tumor-tropic. When the albumin-bound complexes of these three were injected, their tumor distributions were enlarged. These results suggest the importance of serum albumin in serving as a carrier for the transport of 99mTc-Hcy-related compounds to tumor tissue.
为阐明肿瘤显像用99mTc标记放射性药物所需的一个因素,将99mTc-L-半胱氨酸(99mTc-Cys)和99mTc-2-巯基乙胺(99mTc-ME)的体内行为与已发现可在几种实验性肿瘤中蓄积的99mTc-DL-高半胱氨酸(99mTc-Hcy)的体内行为进行了比较。当将这三种配合物静脉注射到荷艾氏实体瘤小鼠体内时,发现它们的肿瘤亲和力取决于它们与血清白蛋白的结合能力;99mTc-Hcy在三者中与白蛋白的结合能力最强,对肿瘤的趋向性也最高。当注射这三种物质与白蛋白结合的配合物时,它们在肿瘤中的分布增加。这些结果表明血清白蛋白作为载体将99mTc-Hcy相关化合物转运至肿瘤组织的重要性。