School of Materials Science and Engineering, Wuhan Institute of Technology, Wuhan, 430205, China; School of Chemistry, Physics & Mechanical Engineering, Science and Engineering Faculty, Queensland University of Technology, Brisbane, QLD, 4001, Australia.
School of Materials Science and Engineering, Wuhan Institute of Technology, Wuhan, 430205, China.
Talanta. 2020 May 15;212:120718. doi: 10.1016/j.talanta.2020.120718. Epub 2020 Jan 14.
Currently, fluorescent imaging is one of the most promising diagnostic approaches for facile detection of cancers in situ in thanks to a fluorescent probe. Two novel polypeptide-based fluorescent probes for different biomarkers to cancers are reported here. These probes focused on tyrosine-isoleucine-glycine-serine-arginine (YIGSR) and arginine-glycine-aspartic (RGD), which receptors play an important role in the extracellular matrix and are overexpressed in tumor cells and then can be used as tumor-targeting groups in fluorescent imaging. In this work, the pentpeptide-rhodamine B derivative (YIGSR-RhB) and tripeptide-rhodamine B derivative (RGD-RhB) were synthesized respectively by using the solid phase synthesis methods. These derivatives were further characterized by HNMR, MS, UV and IR, etc. Their fluorescent and biocompatibility properties, such as the cell cytotoxicity, cell uptake and fluorescent imaging of tumor cells, and fluorescent imaging in BALB/c female mice with 4T1 tumors and C57 mice with B16F10 tumor in vivo, were also measured. Experiment results demonstrated that YIGSR-RhB and RGD-RhB possessed the low cell cytotoxicity, good tumor-targeting property and fluorescent properties similar to rhodamine B. Moreover, YIGSR-RhB and RGD-RhB can be taken up highly by the B16F10 melanoma cells and 4T1 breast cancer cells, and then achieve the good fluorescent imaging in these tumor cells in vitro and tumors of mice in vivo. Therefore, YIGSR-RhB and RGD-RhB can be used as the potential tumor-targeting probes for fluorescent imaging. They can directly attach the cell membrane and specifically target to the tumor cells.
目前，荧光成像是一种最有前途的诊断方法之一，用于原位检测癌症，这要归功于荧光探针。本文报道了两种新型基于多肽的荧光探针，用于检测不同的癌症生物标志物。这些探针集中在酪氨酸-异亮氨酸-甘氨酸-丝氨酸-精氨酸（YIGSR）和精氨酸-甘氨酸-天冬氨酸（RGD）上，这些受体在细胞外基质中起着重要作用，在肿瘤细胞中过度表达，然后可以作为荧光成像中的肿瘤靶向基团。在这项工作中，通过固相合成方法分别合成了五肽-罗丹明 B 衍生物（YIGSR-RhB）和三肽-罗丹明 B 衍生物（RGD-RhB）。通过 1H NMR、MS、UV 和 IR 等方法对这些衍生物进行了进一步的表征。还测量了它们的荧光和生物相容性特性，如细胞毒性、细胞摄取和肿瘤细胞的荧光成像，以及体内 BALB/c 雌性小鼠 4T1 肿瘤和 C57 小鼠 B16F10 肿瘤的荧光成像。实验结果表明，YIGSR-RhB 和 RGD-RhB 具有低细胞毒性、良好的肿瘤靶向性和与罗丹明 B 相似的荧光特性。此外，YIGSR-RhB 和 RGD-RhB 可以被 B16F10 黑色素瘤细胞和 4T1 乳腺癌细胞高度摄取，然后在这些肿瘤细胞中实现良好的体外荧光成像和体内小鼠肿瘤的荧光成像。因此，YIGSR-RhB 和 RGD-RhB 可用作荧光成像的潜在肿瘤靶向探针。它们可以直接附着在细胞膜上，特异性地靶向肿瘤细胞。
