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Liposomal formulations of magnesium sulfanyl tribenzoporphyrazines for the photodynamic therapy of cancer
Journal of Inorganic Biochemistry ( IF 3.8 ) Pub Date : 2018-04-09
Jaroslaw Piskorz, Dariusz T. Mlynarczyk, Wojciech Szczolko, Krystyna Konopka, Nejat Düzgüneş, Jadwiga Mielcarek

Photodynamic therapy of cancer comprises the activation of photosensitizer molecules delivered to cancer cells, to generate reactive oxygen species that mediate cytotoxicity. In this study, previously synthesized dendritic magnesium tribenzoporphyrazines were incorporated into four types of liposomes containing either 1-palmitoyl-2-oleoyl-sn-glycero-3-phosphocholine (POPC) or 1,2-dioleoyl-sn-glycero-3-phosphoethanolamine (DOPE) as the zwitterionic lipids. The addition of either l-α-phosphatidyl-dl-glycerol (PG) or 1,2-dioleoyl-3-trimethylammoniumpropane (DOTAP) imparted a negative or positive charge, respectively. Novel formulations were tested in oral squamous cell carcinoma cell lines (CAL 27, HSC-3) as well as cervical adenocarcinoma cells (HeLa). Positively charged DOTAP:POPC liposomes were the most effective carriers for all tested tribenzoporphyrazines. Calculated IC50 values for DOTAP:POPC liposomes indicated that the incorporation of tribenzoporphyrazines into these liposomes can improve photocytotoxicity up to 50-fold compared to the free forms of macrocycles. Oral cancer cells (CAL 27 and HSC-3) were more sensitive to liposomal photodynamic treatment than HeLa cells.



中文翻译:

硫烷基三苯并卟啉镁的脂质体制剂用于癌症的光动力治疗

癌症的光动力疗法包括激活传递给癌细胞的光敏剂分子,以产生介导细胞毒性的活性氧。在这项研究中,先前合成的树突状三苯并卟啉镁被掺入四种包含1-棕榈酰基-2-油酰基-sn-甘油-3-磷酸胆碱(POPC)或1,2-二醇基-sn-甘油-3-磷酸乙醇胺的脂质体中(DOPE)为两性离子脂质。加入任一-α-磷脂酰DL-甘油(PG)或1,2-二油酰基-3-三甲基铵丙烷(DOTAP)分别带负电或正电。在口腔鳞状细胞癌细胞系(CAL 27,HSC-3)以及宫颈腺癌细胞(HeLa)中测试了新型制剂。带正电荷的DOTAP:POPC脂质体是所有测试的三苯并卟啉类药物中最有效的载体。计算得出的DOTAP:POPC脂质体的IC 50值表明,与游离形式的大环化合物相比,将三苯并卟啉类药物掺入这些脂质体可将光细胞毒性提高多达50倍。口腔癌细胞(CAL 27和HSC-3)比HeLa细胞对脂质体的光动力治疗更敏感。

更新日期:2018-04-10
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