Faculty of Medicine, Department of Biophysics, Karadeniz Technical University, Trabzon, Turkey.
Faculty of Science, Department of Chemistry, Karadeniz Technical University, Trabzon, Turkey.
Photodiagnosis Photodyn Ther. 2021 Dec;36:102615. doi: 10.1016/j.pdpdt.2021.102615. Epub 2021 Nov 2.
Protoporphyrin IX (PpIX), which is an efficient photosensitive agent, cannot be used directly in photodynamic therapy due to its aggregation in physiological environment. If PpIX is made water-soluble without losing its photosensitive properties, it can be used in many medical fields, including cancer treatment. Here we report synthesis of PpIX homologue with mPEG550 (Porfipeg) and its photodynamic effects on both in-vitro and in-vivo environment. Porfipeg is synthesized to give PpIX the ability to dissolve in water. Spectrometric (FT-IR, NMR, MS, UV-vis and Fluorescence) measurements were performed. Porfipeg can penetrate into the cells and indicates no cytotoxicity in the dark whereas cell viability significantly reduced with light irradiation. The cells can be visualized by fluorescence microscope. In-vivo experiment revealed that intravenous injection of Porfipeg is more efficient than intraperitoneal injection for the acute photodynamic effects within 30 min. Moreover it is excreted by the kidneys. In conclusion, Porfipeg has remarkable potentials to be used in both fluorescence guidance in surgeries and photodynamic therapy for cancer treatment.
原卟啉 IX（PpIX）是一种有效的光敏剂，但由于其在生理环境中聚集，不能直接用于光动力疗法。如果 PpIX 在不丧失光敏特性的情况下变成水溶性的，就可以用于许多医学领域，包括癌症治疗。在这里，我们报告了一种具有 mPEG550 的 PpIX 同系物（Porfipeg）的合成及其在体外和体内环境中的光动力效应。Porfipeg 的合成使 PpIX 能够溶解在水中。进行了光谱学（FT-IR、NMR、MS、UV-vis 和荧光）测量。Porfipeg 可以穿透细胞，在黑暗中没有细胞毒性，而光照会显著降低细胞活力。可以通过荧光显微镜观察到细胞。体内实验表明，在 30 分钟内，Porfipeg 的静脉注射比腹腔注射对急性光动力效应更有效。此外，它还可以通过肾脏排泄。总之，Porfipeg 具有在手术中的荧光引导和癌症光动力治疗方面的显著应用潜力。
