Investigation of SP94 Peptide as a Specific Probe for Hepatocellular Carcinoma Imaging and Therapy

  • Sci Rep. 2016 Sep 21:6:33511. doi: 10.1038/srep33511.
Yanli Li  1  2  3  4 Yan Hu  1  2  3 Jie Xiao  1  2  3 Guobing Liu  1  2  3 Xiao Li  1  2  3 Yanzhao Zhao  1  2  3 Hui Tan  1  2  3 Hongcheng Shi  1  2  3 Dengfeng Cheng  1  2  3
Affiliations
  • 1. Department of Nuclear Medicine, Zhongshan Hospital, Fudan University, Shanghai 200032, China.
  • 2. Shanghai Institute of Medical Imaging, Shanghai 200032, China.
  • 3. Institute of Nuclear Medicine, Fudan University, Shanghai 200032, China.
  • 4. Jining NO.1 People's Hospital, Jining, Shandong 272000, China.
Abstract

SP94 (SFSIIHTPILPL), a novel peptide, has shown specific binding to hepatocellular carcinoma (HCC) cells. We aimed to investigate the capability of SP94 as a targeting probe for HCC imaging and therapy following labeling with technetium-99m ((99m)Tc) and rhenium-188 ((188)Re). HYNIC-SP94 was prepared by solid phase synthesis and then labeled with (99m)Tc. Cell competitive binding, internalization assay, in vitro and in vivo stability, biodistribution and micro-single photon emission computed tomography /computed tomography (SPECT/CT) imaging studies were performed to investigate the capability of (99m)Tc tricine-EDDA/HYNIC-SP94 as a specific HCC imaging probe. Initial promising targeting results inspired evaluation of its therapeutic effect when labeled by (188)Re. HYNIC-SP94 was then labeled again with (188)Re to perform cell Apoptosis, microSPECT/CT imaging evaluation and immunohistochemistry. Huh-7 cells exhibited typical apoptotic changes after (188)Re irradiation. According to (99m)Tc tricine-EDDA/HYNIC-SP94 microSPECT/CT imaging, tumor uptake was significantly decreased compared with that of pre-treatment with (188)Re-HYNIC-SP94. The immunohistochemistry also displayed obvious necrosis and Apoptosis as well as inhibition of proliferation in the (188)Re-HYNIC-SP94 treatment group. The results supported that (99m)Tc tricine-EDDA/HYNIC-SP94 is able to target HCC cells and (188)Re-HYNIC- SP94 holds potential as a therapeutic agent for HCC, making (99m)Tc/(188)Re-HYNIC-SP94 a promising targeting probe for HCC imaging and therapy.

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