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Gene & Protein in Disease Cyanine and cancer therapy
A B D
C
E
F G H
Figure 6. (A-H) Different small molecule cyanine compounds. These compounds can induce cancer cell apoptosis through PDT, thus exerting anti-tumor activity.
Wezgowiec et al. proposed the discovery of two cyanine G0/G1 phase cell cycle arrest and reducing ATP levels.
compounds, namely IR-775 (Figure 6D) and IR-786 These findings indicate that IR-783 holds promise as a
(Figure 6E), which have been demonstrated to act on potential new drug for breast cancer treatment [214] . On the
MCF-7/WT cells through PDT without inducing any side other hand, Tang et al. and Hou et al. observed that IR-783
effects on these cells. These compounds hold promise as reduces the activity of MDA-MB-231 cells and facilitates
antitumor agents capable of inducing cancer cell apoptosis apoptosis in breast cancer cells by inducing mitochondrial
through PDT [210] . In addition, IR-786 demonstrates potential fragmentation [215,216] . In addition, certain studies have
as a molecular probe for fluorescent biological imaging [211] . demonstrated that IR-783 exhibits cancel cell uptake and
accumulation, targeting brain, prostate, and colon tumors,
Cai et al. designed and synthesized three lysosome- with minimal toxicity to normal tissues [217-219] . Furthermore,
targeted fluorescent probes, namely, HCL 1 (Figure 6F), IR-783 can reduce the activity of cancer cells through both
HCL 2 (Figure 6G), and HCL 3 (Figure 6H), based on PTT and PDT [220,221] . With its broad-spectrum anticancer
the structure of Cy7. Lysosomes play a critical role in activity and specificity for prostate, bladder, and breast
cell survival and apoptosis. On irradiation, both HCL 1 cancer, IR-783 holds promise as a promising NIRF dye [222,223] .
and HCL 3 are capable of producing ROS and inducing
cell apoptosis. Meanwhile, HCL 2 exhibits effective tumor Cao et al. modified the indocyanine green derivative
targeting and demonstrates a PDT effect in vivo [212] . Cy7 with a heavy atom iodine to form a new NIR dye
called CyI. Through PPT and PDT, CyI can rapidly and
PTT, which incorporates both PDT and PTT, has emerged simultaneously generate ROS and heat, inducing increased
as a tumor ablation method for treating various types of cancer cell apoptosis and a higher inhibition rate in deep
cancer. PDT can enhance the sensitivity of tumor cells to PTT tumors. Importantly, while maintaining its fluorescence
by modulating the tumor microenvironment. In contrast, characteristics, CyI can be used for non-invasive in vivo
the heat produced by PTT can increase blood flow, enhance imaging [188] .
oxygen supply, and increase the therapeutic efficacy of PDT.
Therefore, the combined therapy of PDT and PTT can induce Sun et al. synthesized the near-infrared fluorescent
apoptosis of cancer cells by producing high temperature or small molecule compound IR-817 through the oxidation-
ROS, thereby exerting an anti-tumor effect [213] . reduction reaction of IR-808 and choline, providing
an integrated approach to diagnosis and treatment
IR-783, a NIF heptamethine cyanine dye with cancer- (Figure 7B). IR-817 exhibits maximum absorption and
targeting properties, exhibits anticancer effects (Figure 7A). emission peaks at 764 nm and 790 – 820 nm, respectively,
On one hand, as reported by Li et al., IR-783 inhibits within the NIR region (700 – 900 nm). The anti-tumor
the proliferation and migration of breast cancer cells. mechanism of IR-817 involves promoting the expression of
It exerts a dose- and time-dependent inhibitory effect BAX and inhibiting the expression of Bcl-2 protein, thereby
on MDA-MB-231 and MCF-7 cancer cells by inducing increasing the BAX/Bcl-2 ratio and further triggering the
Volume 2 Issue 4 (2023) 10 https://doi.org/10.36922/gpd.2486

