AccScience Publishing / GPD / Volume 1 / Issue 1 / DOI: 10.36922/gpd.v1i1.87

Fluorescence imaging-guided photothermal therapy of asymmetric water-soluble pentamethine cyanine for colorectal cancer

Kun Tang1† Shuangshuang Jia1† Yaxin Zou1† Jiaheng Dong1 Fangyan Liu2 Kunli Cui1 Xiao Shi3 Lei Zhang1*
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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
Submitted: 8 May 2022 | Accepted: 16 June 2022 | Published: 29 June 2022
© 2022 by the Authors. This article is an open access article distributed under the terms and conditions of the Creative Commons Attribution 4.0 International License ( )

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 its potential applications as a NIR photosensitizer for the diagnosis and therapy of colorectal cancer (CRC). The results of fluorescence imaging analysis showed that CY5-664 preferentially accumulated in the tumor as time elapsed, and the maximum fluorescence intensity was obtained at 24 h. Cell viability and animal xenograft model experiments showed that CY5-664 significantly inhibited tumor growth in vivo with 0.8 W/cm2 of 660 nm red laser pointer for 2 min, and in vitro with 0.5 W/cm2 of 660 nm red laser pointer for 2 min. In vitro and in vivo photothermal conversion experiments showed that CY5-664 exhibited an anti-CRC activity mainly through the PTT effect. Therefore, this work provides experimental evidence that CY5-664 is a drug candidate for CRC treatment mainly through the PTT effect and an alternative treatment strategy to develop a pentamethine cyanine-based CRC theranostic photosensitizer for synergistic CRC targeting, imaging, and therapy.

Pentamethine cyanine
Photothermal therapy
Fluorescence imaging
Colorectal cancer
National Natural Science Foundation of China
China Postdoctoral Science Foundation
Key R&D and Promotion Projects in Henan Province

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Conflict of interest
The authors declare no conflict of interest.
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