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Gene & Protein in Disease





                                        ORIGINAL RESEARCH ARTICLE
                                        Fluorescence imaging-guided photothermal

                                        therapy of asymmetric water-soluble
                                        pentamethine cyanine for colorectal cancer



                                                                  1†
                                                1†
                                        Kun Tang , Shuangshuang Jia , Yaxin Zou , Jiaheng Dong , Fangyan Liu ,
                                                                                            1
                                                                                                        2
                                                                             1†
                                        Kunli Cui , Xiao Shi , and Lei Zhang *
                                                                      1
                                                        3
                                                1
                                        1 Henan International Joint Laboratory for Nuclear Protein Regulation, School of Basic Medical
                                        Sciences, Henan University, Kaifeng 475004, P. R. China
                                        2 Department of  Academician Shengshou Hu  Workstation, Fuwai Central China Cardiovascular
                                        Hospital, Zhengzhou 450046, P. R. China
                                        3 Department of Pharmacy,  The First  Affiliated Hospital of Henan University, Henan University,
                                        Kaifeng 475004, P. R. China
                                        Abstract
                                        The  combination of  advanced  optical  technology  and tumor  treatment  has
                                        developed into a selectively targeted tumor therapy strategy. Near-infrared (NIR)
                                        cyanine derivative has recently received increasing attention in photothermal
                                        therapy (PTT) because of its excellent biocompatibility, non-immunogenicity, high
                                        fluorescence  and photothermal conversion  efficiency, photostability,  and tumor-
                                        homing. In this study, an asymmetric and water-soluble pentamethine cyanine was
                                        designed and synthesized to investigate the photosensitive activity and to explore
            † These authors contributed equally   its potential applications as a NIR photosensitizer for the diagnosis and therapy of
            to this work
                                        colorectal cancer (CRC). The results of fluorescence imaging analysis showed that
            *Corresponding author:      CY5-664 preferentially accumulated in the tumor as time elapsed, and the maximum
            Lei Zhang                   fluorescence intensity was obtained at 24 h. Cell viability and animal xenograft model
            (zhlei@henu.edu.cn)
                                        experiments showed that CY5-664 significantly inhibited tumor growth in vivo with
            Citation: Tang K, Jia S, Zou Y,   0.8 W/cm  of 660 nm red laser pointer for 2 min, and in vitro with 0.5 W/cm  of 660 nm
                                               2
                                                                                                    2
            et al. Fluorescence imaging-guided
            photothermal therapy of asymmetric   red laser pointer for 2 min. In vitro and in vivo photothermal conversion experiments
            water-soluble pentamethine cyanine   showed that CY5-664 exhibited an anti-CRC activity mainly through the PTT effect.
            for colorectal cancer. Gene Protein   Therefore, this work provides experimental evidence that CY5-664 is a drug candidate
            Dis, 1(1):87.
            https://doi.org/10.36922/gpd.v1i1.87   for CRC treatment mainly through the PTT effect and an alternative treatment
                                        strategy to develop a pentamethine cyanine-based CRC theranostic photosensitizer
            Received: May 8, 2022
            Accepted: June 16, 2022     for synergistic CRC targeting, imaging, and therapy.
            Published Online: June 29, 2022
            Copyright: © 2022 Author(s).   Keywords: Pentamethine cyanine; Photothermal therapy; Fluorescence imaging; Near-
            This is an Open Access article   infrared; Colorectal cancer
            distributed under the terms of the
            Creative Commons Attribution
            License, permitting distribution,
            and reproduction in any medium,
            provided the original work is   1. Introduction
            properly cited.
            Publisher’s Note: AccScience   Colorectal cancer (CRC), a common clinical malignant tumor of the digestive tract,
            Publishing remains neutral with   is seriously threatening human health due to the high incidence and mortality rates .
                                                                                                           [1]
            regard to jurisdictional claims in
            published maps and institutional   The occurrence and development of CRC are usually related to diet changes and
                                                         [2]
            affiliations.               environmental factors . According to the statistics on cancer in 185 countries in 2018,
            Volume 1 Issue 1 (2022)                         1                       https://doi.org/10.36922/gpd.v1i1.87
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