Goto R, Unno K, Takeda A, Okada S, Tamemasa O
Department of Radiobiochemistry, Shizuoka College of Pharmacy, Japan.
J Pharmacobiodyn. 1987 Sep;10(9):456-61. doi: 10.1248/bpb1978.10.456.
The radioactivity distribution of 75Se-labeled D-selenomethionine (D-SeMet-75Se) was investigated in tumor-bearing mice in order to develop a new radioactive diagnostic agent. D-SeMet-75Se was enzymatically prepared from commercially available L-selenomethionine-75Se (L-SeMet-75Se) by using amino acid racemase and immobilized L-amino acid oxidase. No difference between D- and L-SeMet-75Se was found in the excretion rate into urine and feces in normal mice within 48 h after administration. The in vivo uptake of D-SeMet-75Se in both Ehrlich solid tumor and sarcoma-180 solid tumor was several times higher than that of L-SeMet-75Se but the uptake of D- and L-SeMet-75Se were similar in the pancreas. These results indicated that D-SeMet-75Se might be useful as a tumor-imaging agent. In vitro experiments on Ehrlich ascites tumor cells showed that D-SeMet-75Se was incorporated into the tumor cells by a Na+-dependent active transport system similar to L-SeMet-75Se and that a transport mechanism specific for D-SeMet-75Se might be present in tumor cells in addition to a transport system common to both D- and L-forms.
为开发一种新型放射性诊断剂,研究了75Se标记的D-硒代蛋氨酸(D-SeMet-75Se)在荷瘤小鼠体内的放射性分布。通过使用氨基酸消旋酶和固定化L-氨基酸氧化酶,从市售的L-硒代蛋氨酸-75Se(L-SeMet-75Se)酶法制备D-SeMet-75Se。给药后48小时内,正常小鼠尿液和粪便排泄率在D-和L-SeMet-75Se之间未发现差异。Ehrlich实体瘤和肉瘤-180实体瘤中D-SeMet-75Se的体内摄取量比L-SeMet-75Se高几倍,但胰腺中D-和L-SeMet-75Se的摄取量相似。这些结果表明,D-SeMet-75Se可能作为一种肿瘤显像剂有用。对Ehrlich腹水肿瘤细胞的体外实验表明,D-SeMet-75Se通过与L-SeMet-75Se相似的Na+依赖性主动转运系统被肿瘤细胞摄取,并且除了D-和L-形式共有的转运系统外,肿瘤细胞中可能存在对D-SeMet-75Se特异的转运机制。