AI Article Synopsis
- Five new cationic sulfonamide-substituted dibenzothiazole squaraines (SQ-D1 to SQ-D5) were synthesized based on zwitterionic dibenzothiazole squaraine SQ.
- Among them, SQ-D2 emerged as the most effective photosensitizer due to its rigid structure and strong electron-withdrawing -CN group, demonstrating superior ROS generation, photostability, and photo-cytotoxicity.
- In animal studies, SQ-D2 showed effective tumor retention, easy removal, and impressive PDT efficacy at low doses, outperforming some clinically approved photosensitizers for treating human breast cancer, indicating its potential for future cancer therapies.
Article Abstract
On the base of the zwiterionic dibenzothiazole squaraine SQ, five cationic aromatics sulfonamide substituted dibenzothiazole squaraines SQ-D1 ∼ 5 have been designed and synthesized. Through the formation of the cationic compound, a higher rigid structure and the addition of the strong electron-withdrawing group (-CN), an ideal photosensitizer SQ-D2 has been gotten. In all the sulfonaminosquaraines, compound SQ-D2 exhibited the highest ROS generation efficacy and photostability. It also showed the highest photo-cytotoxicity (IC = 0.25 ± 0.08 μM), very low dark-cytotoxicity and the excellent cell uptake. In animal study, it not only showed the effective tumor retention and the easy removal from the body, but also exhibited the effective PDT efficacy at low drug dose (0.15 mg/kg) and the good biocompatibility. Furthermore, photosensitizer SQ-D2 as a single component exhibited greater potential than clinically approved photosensitizer m-THPC and some nanomaterials with photosensitizers in PDT therapy towards human breast cancer. This work provides a new perspective to develop the ideal photosensitizer of the squaraine dyes.
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| http://dx.doi.org/10.1016/j.jphotobiol.2023.112653 | DOI Listing |
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