Abstract：
BACKGROUND: Chlorins (dihydroporphyrins) are tetrapyrrole-based compounds that are more effective in photodynamic therapy than porphyrins. The instability of the compounds and their oxidation to porphyrin limits the use of these compounds. However, the design and synthesis of new stable chlorin-based cationic photosensitizers with the potential for use in cancer photodynamic therapy can be interesting.
METHODS: In this research, new tetracationic meso substituted chlorins were designed, synthesized, and characterized. After determining the chemical structure and spectroscopic properties of five new photosensitizers, their phototoxicity on breast cancer cell lines (MCF-7) was investigated under optimized conditions in terms of factors such as photosensitizer concentrations and light intensity.
RESULTS: The results of cytotoxicity assayed by the MTT method showed that the synthesized compounds, even up to the concentration of 50 μM had very low toxicity in the absence of light, which indicates their safety under dark conditions. Compounds A1 and A3 with the best physicochemical properties such as solubility, high absorption intensity in the effective range of photodynamic therapy, and the high quantum yield of singlet oxygen, had a good toxic effect (IC50 = 0.5 μM) on the cancer cells (MCF-7) in the presence of laser light.
CONCLUSIONS: According to the obtained results, compounds A1 and A3 have the potential to continue research on PDT for confirmation and use in treatment.
METHODS: In this research, new tetracationic meso substituted chlorins were designed, synthesized, and characterized. After determining the chemical structure and spectroscopic properties of five new photosensitizers, their phototoxicity on breast cancer cell lines (MCF-7) was investigated under optimized conditions in terms of factors such as photosensitizer concentrations and light intensity.
RESULTS: The results of cytotoxicity assayed by the MTT method showed that the synthesized compounds, even up to the concentration of 50 μM had very low toxicity in the absence of light, which indicates their safety under dark conditions. Compounds A1 and A3 with the best physicochemical properties such as solubility, high absorption intensity in the effective range of photodynamic therapy, and the high quantum yield of singlet oxygen, had a good toxic effect (IC50 = 0.5 μM) on the cancer cells (MCF-7) in the presence of laser light.
CONCLUSIONS: According to the obtained results, compounds A1 and A3 have the potential to continue research on PDT for confirmation and use in treatment.
摘要：
背景：氯（双氢卟啉）是基于四吡咯的化合物，在光动力疗法中比卟啉更有效。这些化合物的不稳定性及其对卟啉的氧化限制了这些化合物的使用。然而,具有用于癌症光动力治疗的潜力的新型稳定的基于氯的阳离子光敏剂的设计和合成可能是有趣的。
方法：在这项研究中，设计了新的四阳离子内消旋取代氯，合成，和特点。在确定了五种新型光敏剂的化学结构和光谱性质后，在优化条件下，根据光敏剂浓度和光强度等因素研究了它们对乳腺癌细胞系（MCF-7）的光毒性。
结果：MTT法测定细胞毒性的结果表明，合成的化合物，在没有光的情况下，即使浓度达到50μM也具有非常低的毒性，这表明他们在黑暗条件下的安全。化合物A1和A3具有最佳的理化性质，如溶解度，光动力疗法有效范围内的高吸收强度，和单线态氧的高量子产率，在激光存在下对癌细胞(MCF-7)具有良好的毒性作用(IC50=0.5μM)。
结论：根据获得的结果，化合物A1和A3有可能继续研究PDT以确认和用于治疗。
方法：在这项研究中，设计了新的四阳离子内消旋取代氯，合成，和特点。在确定了五种新型光敏剂的化学结构和光谱性质后，在优化条件下，根据光敏剂浓度和光强度等因素研究了它们对乳腺癌细胞系（MCF-7）的光毒性。
结果：MTT法测定细胞毒性的结果表明，合成的化合物，在没有光的情况下，即使浓度达到50μM也具有非常低的毒性，这表明他们在黑暗条件下的安全。化合物A1和A3具有最佳的理化性质，如溶解度，光动力疗法有效范围内的高吸收强度，和单线态氧的高量子产率，在激光存在下对癌细胞(MCF-7)具有良好的毒性作用(IC50=0.5μM)。
结论：根据获得的结果，化合物A1和A3有可能继续研究PDT以确认和用于治疗。
