Ho Chung-Li, Liu I-Hsiang, Wu Yu-Hsien, Chen Liang-Cheng, Chen Chun-Lin, Lee Wan-Chi, Chuang Cheng-Hui, Lee Te-Wei, Lin Wuu-Jyh, Shen Lie-Hang, Chang Chih-Hsien
Isotope Application Division, Institute of Nuclear Energy Research, Taoyuan 32546, Taiwan.
J Biomed Biotechnol. 2011;2011:101497. doi: 10.1155/2011/101497. Epub 2011 May 24.
Molecular imaging with promise of personalized medicine can provide patient-specific information noninvasively, thus enabling treatment to be tailored to the specific biological attributes of both the disease and the patient. This study was to investigate the characterization of DO3A-CH(2)CO-G-4-aminobenzoyl-Q-W-A-V-G-H-L-M-NH(2) (AMBA) in vitro, MicroSPECT/CT imaging, and biological activities of (111)In-AMBA in PC-3 prostate tumor-bearing SCID mice. The uptake of (111)In-AMBA reached highest with 3.87 ± 0.65% ID/g at 8 h. MicroSPECT/CT imaging studies suggested that the uptake of (111)In-AMBA was clearly visualized between 8 and 48 h postinjection. The distribution half-life (t(1/2α)) and the elimination half-life (t(1/2β)) of (111)In-AMBA in mice were 1.53 h and 30.7 h, respectively. The C(max) and AUC of (111)In-AMBA were 7.57% ID/g and 66.39 h % ID/g, respectively. The effective dose appeared to be 0.11 mSv/MBq(-1). We demonstrated a good uptake of (111)In-AMBA in the GRPR-overexpressed PC-3 tumor-bearing SCID mice. (111)In-AMBA is a safe, potential molecular image-guided diagnostic agent for human GRPR-positive tumors, ranging from simple and straightforward biodistribution studies to improve the efficacy of combined modality anticancer therapy.
具有个性化医疗前景的分子成像能够以非侵入性方式提供患者特异性信息，从而使治疗能够根据疾病和患者的特定生物学特性进行定制。本研究旨在调查DO3A-CH(2)CO-G-4-氨基苯甲酰基-Q-W-A-V-G-H-L-M-NH(2)（AMBA）的体外特性、MicroSPECT/CT成像以及（111）In-AMBA在荷PC-3前列腺肿瘤的SCID小鼠中的生物学活性。（111）In-AMBA在8小时时摄取量最高，为3.87±0.65% ID/g。MicroSPECT/CT成像研究表明，注射后8至48小时之间（111）In-AMBA的摄取情况清晰可见。（111）In-AMBA在小鼠体内的分布半衰期（t(1/2α)）和消除半衰期（t(1/2β)）分别为1.53小时和30.7小时。（111）In-AMBA的C(max)和AUC分别为7.57% ID/g和66.39 h % ID/g。有效剂量似乎为0.11 mSv/MBq(-1)。我们证明了（111）In-AMBA在过表达GRPR的荷PC-3肿瘤的SCID小鼠中有良好的摄取。（111）In-AMBA是一种安全的、潜在的分子影像引导诊断剂，可用于人类GRPR阳性肿瘤，从简单直接的生物分布研究到提高联合抗癌治疗的疗效。
