Murugesan S, Banerji A P, Noronha O P, Samuel A M, Fernandes A O
Radiation Medicine Centre, Bhabha Atomic Research Centre, Tata Memorial Hospital Annexe, Parel, Mumbai, India.
Indian J Exp Biol. 2001 Aug;39(8):742-7.
Purified field bean protease inhibitor (FBPI) was labeled with 99mTcO4- to ascertain its ability to locate tumors in tumor-bearing rat models. The labeling was done with Sn2+ as a reducing agent and the yield was 95%. It was stable for 2 hr at ambient temperature. The biodistribution study of the intravenously injected radiolabeled FBPI in normal Wistar rats at various time intervals showed a rapid blood clearance from the systemic circulation (approximately 5hr). The complex was predominantly excreted through the renal and the hepatobiliary systems. In vivo distribution and scintiimaging of 99mTc-FBPI were carried out in rats bearing carcinogen-induced mammary tumor or transplanted C6-gliomas. The results obtained were compared with conventional tumor-seeking radiopharmaceuticals such as 99mTc-(V)dimercaptosuccinic acid (DMSA), 201Thallous chloride (TICI) and 99mTc-Citrate. The tumor to muscle (T/M) ratios obtained with 99mTc-FBPI in rat C6 glioma was nearly 2 to 5-fold higher than obtained with all the three conventional tumor-seeking agents. The T/M ratio obtained with 99mTc-FBPI in rat mammary tumor on the other hand appeared to be 2-3-fold higher than noted with 99mTc(V)-DMSA and 201TlCl. The ratio was however comparable with that obtained with 99mTc-Citrate. The study indicated that 99mTc-FBPI has the specific potentials for imaging gliomas and possibly other tumors as well.
纯化的蚕豆蛋白酶抑制剂（FBPI）用99mTcO4-进行标记，以确定其在荷瘤大鼠模型中定位肿瘤的能力。标记以Sn2+作为还原剂进行，产率为95%。它在室温下稳定2小时。对正常Wistar大鼠在不同时间间隔静脉注射放射性标记的FBPI后的生物分布研究表明，其从体循环中快速清除（约5小时）。该复合物主要通过肾和肝胆系统排泄。对携带致癌物诱导的乳腺肿瘤或移植C6胶质瘤的大鼠进行了99mTc-FBPI的体内分布和闪烁成像。将获得的结果与传统的肿瘤靶向放射性药物如99mTc-(V)二巯基丁二酸（DMSA）、氯化铊（201Tl）和99mTc-柠檬酸盐进行比较。在大鼠C6胶质瘤中，99mTc-FBPI获得的肿瘤与肌肉（T/M）比值比所有三种传统肿瘤靶向剂获得的比值高近2至5倍。另一方面，在大鼠乳腺肿瘤中，99mTc-FBPI获得的T/M比值似乎比99mTc(V)-DMSA和201TlCl高2至3倍。然而，该比值与99mTc-柠檬酸盐获得的比值相当。该研究表明，99mTc-FBPI具有对胶质瘤以及可能其他肿瘤进行成像的特定潜力。
