Ikeda Atsushi, Satake Shuhei, Mae Tomoya, Ueda Masafumi, Sugikawa Kouta, Shigeto Hajime, Funabashi Hisakage, Kuroda Akio
Department of Applied Chemistry, Graduate School of Engineering, Hiroshima University, 1-4-1 Kagamiyama, Higashi-Hiroshima, Hiroshima 739-8527, Japan.
Department of Molecular Biotechnology, Graduate School of Advanced Sciences of Matter, Hiroshima University, 1-3-1 Kagamiyama, Higashi-Hiroshima, Hiroshima 739-8530, Japan.
ACS Med Chem Lett. 2017 Apr 19;8(5):555-559. doi: 10.1021/acsmedchemlett.7b00098. eCollection 2017 May 11.
Water-soluble cyclodextrin (CyD) complexed with porphyrin derivatives with different substituents in the -positions showed different photodynamic activities toward cancer cells under illumination at wavelengths over 600 nm, the most suitable wavelengths for photodynamic therapy (PDT). In particular, aniline- and phenol-substituted derivatives had high photodynamic activity because of the efficient intracellular uptake of the complexes by tumor cells. These complexes showed greater photodynamic activity than photofrin, currently the main drug in clinical use as a photosensitizer. These results represent a significant step toward the optimization of porphyrin derivatives as photosensitizers.
在600nm以上波长光照下,与在β-位带有不同取代基的卟啉衍生物复合的水溶性环糊精(CyD)对癌细胞表现出不同的光动力活性,这是光动力疗法(PDT)最合适的波长。特别是,苯胺和苯酚取代的衍生物具有高光动力活性,这是因为肿瘤细胞对复合物有高效的细胞内摄取。这些复合物比目前临床上用作光敏剂的主要药物卟吩姆钠表现出更大的光动力活性。这些结果代表了卟啉衍生物作为光敏剂优化方面的重要一步。