School of Materials Science and Engineering, Wuhan Institute of Technology, Wuhan 430205, China.
Faculty of Science, University of Melbourne, Grattan Street, Parkville, Victoria 3010, Australia.
Bioorg Chem. 2022 Dec;129:106161. doi: 10.1016/j.bioorg.2022.106161. Epub 2022 Sep 17.
Dual-modal magnetic resonance/fluorescent imaging (MRI/FI) attracts moreandmoreattentions in diagnosis of tumors. A corresponding dual-modal imaging agent with sufficient tumor sensitivity and specificity should be matched to improve imaging quality. Tripeptide (RGD) and pentapeptide (YIGSR) were selected as the tumor-targeting groups and attached to gadolinium diethylenetriaminepentaacetic acid (Gd-DTPA) and rhodamine B (RhB), and then make two novel polypeptide-based derivatives (RGD-Gd-DTPA-RhB and YIGSR-Gd-DTPA-RhB), respectively. These derivatives were further characterized and their properties, such as cell uptake, cell cytotoxicity, MRI and FI assay, were measured. YIGSR-Gd-DTPA-RhB and RGD-Gd-DTPA-RhB had high relaxivity, good tumor-targeting property, low cell cytotoxicity and good red FI in B16F10 melanoma cells. Moreover, YIGSR-Gd-DTPA-RhB and RGD-Gd-DTPA-RhB possessed high uptake to B16F10 melanoma, and then achieve highly enhanced FI and MRI of tumors in mice for a prolonged time. Therefore, YIGSR-Gd-DTPA-RhB and RGD-Gd-DTPA-RhB can be applied as the potential agents for tumor targeted MRI/FI in vivo.
双模态磁共振/荧光成像（MRI/FI）在肿瘤诊断中越来越受到关注。应匹配相应的双模态成像剂，以提高成像质量，该成像剂应具有足够的肿瘤灵敏度和特异性。三肽（RGD）和五肽（YIGSR）被选为肿瘤靶向基团，并连接到钆二乙烯三胺五乙酸（Gd-DTPA）和若丹明 B（RhB）上，然后分别得到两种新型基于多肽的衍生物（RGD-Gd-DTPA-RhB 和 YIGSR-Gd-DTPA-RhB）。进一步对这些衍生物进行了表征，并测量了它们的性质，如细胞摄取、细胞毒性、MRI 和 FI 测定。YIGSR-Gd-DTPA-RhB 和 RGD-Gd-DTPA-RhB 具有高弛豫率、良好的肿瘤靶向性、低细胞毒性和良好的 B16F10 黑色素瘤细胞红色 FI。此外，YIGSR-Gd-DTPA-RhB 和 RGD-Gd-DTPA-RhB 对 B16F10 黑色素瘤具有高摄取率，从而在较长时间内实现了肿瘤的高增强 FI 和 MRI。因此，YIGSR-Gd-DTPA-RhB 和 RGD-Gd-DTPA-RhB 可以用作体内肿瘤靶向 MRI/FI 的潜在试剂。
