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Gene & Protein in Disease Cyanine and cancer therapy

anti-tumor effects in vitro. It influences the proliferation, Zhao et al. synthesized CYBF2, a cyanine photosensitizer
apoptosis, and ROS production of renal cancer cells, leading tailored for cancers PDT. Compared with traditional
to G2/M phase arrest, apoptosis, and mitochondrial damage anthocyanin photosensitizers (Figure 6B), CYBF2
in a ROS-dependent manner. These findings suggest that displays red light (660 nm) photosensitivity and enhanced
COS-Cy7 may emerge as a potential therapeutic agent for photostability. By producing ROS in cell mitochondria,
tumor therapy, particularly for renal cancer [197] . Therefore, CYBF2 effectively triggers cancer cell apoptosis through
COS-Cy7 can induce apoptosis in cancer cells through a mitochondrial damage [203] .
ROS-dependent mechanism, thereby exerting its anti-tumor The study conducted by Kulbacka et al. investigated the
effects. effects of four cyanine derivatives, namely KF-570, HM-118,
FBF-749, and ER-139, on malignant adenocarcinoma cells.
5.1.2. PTT activity Their findings revealed that HM-118 and KF-570 could
Phototherapy is a local treatment approach offering several induce apoptosis, necrosis, and autophagy in malignant
advantages, including minimal invasiveness, precise adenocarcinoma cells [204-206] . Specifically, HM-118 was
temporal and spatial control, and low susceptibility to drug observed to induce apoptosis and reduce clonogenic ability
resistance [198] . Among the primary phototherapy methods, in these cells, while ER-139 produced ROS upon irradiation,
PTT and PDT have gained significant attention in cancer causing oxidative damage in malignant adenocarcinoma
research. cells. This oxidative stress may induce cancer death through
apoptosis, necrosis, and autophagy [207] .
Photodynamic therapy involves the use of
Furthermore,
cyanine
photosensitizers and molecular oxygen under laser demonstrated anti-tumor derivative IR-775 has
Waszkiewicz
effects.
irradiation of specific wavelengths to produce ROS, which et al. investigated the impact of cyanine IR-775 and
exert substantial toxicity against tumor cells. In addition, 2-methoxyestradiol on ovarian and breast cancer cells
PDT can inhibit tumor angiogenesis and activate anti- (MDA-MB-231 and SK-OV-3). Their research revealed that
tumor immunity, thereby indirectly impeding tumor IR-775 and 2-methodestradiol induce cancer cell apoptosis
growth and metastasis [199-201] . through PDT, thus exhibiting anti-tumor properties [189] .
Liu et al. developed a novel cyanine photosensitizer, In addition, Krejcir et al. identified a novel anticancer
Cy-N-Rh, designed for PDT (Figure 6A). This molecule, a pentamethinium salt derivative (salt 1) (Figure 6C).
photosensitizer demonstrates excellent mitochondrial Their study demonstrated that PDT targeting the mitochondria
co-localization ability and can induce apoptosis by of tumor cells using salt 1 can disrupt mitochondrial structure,
producing intracellular ROS, exhibiting low dark toxicity, reduce cell metabolism, induce autophagy, and ultimately
elevated phototoxicity, and excellent biocompatibility [202] . trigger apoptosis in cancer cells [208,209] .

A B

C D E

Figure 5. (A-E) Various cyanine compounds. These cyanine compounds can induce cancer cell apoptosis through chemotherapy, thus exerting anti-tumor
activity.

Volume 2 Issue 4 (2023) 9 https://doi.org/10.36922/gpd.2486