Temoporfin (m-THPC) is a synthetic chlorin compound with light-activated actions that acts as a potent photosensitizer [1]. Temoporfin is activated at 652nm with a light penetration depth of 1cm, and exhibits a high tumor selectivity with residual photosensitivity for two weeks[2]. Temoporfin has been widely used in photodynamic therapy (PDT) to inhibit different cancer cell growth[3]. Temoporfin-based PDT can repolarize macrophages to the M1 phenotype, which can induce a phenotypic shift of tumor-associated macrophages[4].
In vitro, Temoporfin treatment for 24h followed by irradiation with a 500W halogen lamp at 5.5×10-2mW/cm2/nm light intensity and 39.6mJ/cm2/nm light energy significantly inhibited HCT116 cell viability with an IC50 value 36.4nM[5]. When exposed to 620-660nm light at a dose of 13.3J/cm2, Temoporfin treatment for 24h significantly inhibited the proliferation of HL60 and 4T1 cells with an IC50 value of 42nM and 117nM, respectively[6].
References:
[1] Senge M O. mTHPC–A drug on its way from second to third generation photosensitizer?[J]. Photodiagnosis and Photodynamic Therapy, 2012, 9(2): 170-179.
[2] Dragicevic-Curic N, Scheglmann D, Albrecht V, et al. Development of different temoporfin-loaded invasomes—novel nanocarriers of temoporfin: Characterization, stability and in vitro skin penetration studies[J]. Colloids and Surfaces B: Biointerfaces, 2009, 70(2): 198-206.
[3] Senge M O, Brandt J C. Temoporfin (Foscan®, 5, 10, 15, 20‐tetra (m‐hydroxyphenyl) chlorin)—a second‐generation photosensitizer[J]. Photochemistry and photobiology, 2011, 87(6): 1240-1296.
[4] Zhu Z, Scalfi-Happ C, Ryabova A, et al. Photodynamic activity of Temoporfin nanoparticles induces a shift to the M1-like phenotype in M2-polarized macrophages[J]. Journal of Photochemistry and Photobiology B: Biology, 2018, 185: 215-222.
[5] Banfi S, Caruso E, Caprioli S, et al. Photodynamic effects of porphyrin and chlorin photosensitizers in human colon adenocarcinoma cells[J]. Bioorganic & medicinal chemistry, 2004, 12(18): 4853-4860.
[6] Králová J, Briza T, Moserová I, et al. Glycol porphyrin derivatives as potent photodynamic inducers of apoptosis in tumor cells[J]. Journal of medicinal chemistry, 2008, 51(19): 5964-5973.
Temoporfin (m-THPC)是一种合成的chlorin化合物，具有光激活作用，可作为强效光敏剂[1]。Temoporfin在652nm波长下被激活，光穿透深度为1厘米，并具有高肿瘤选择性，残留光敏性可持续两周[2]。Temoporfin已被广泛用于光动力疗法（PDT）中以抑制不同癌细胞的生长[3]。基于Temoporfin的PDT可使巨噬细胞复极化为M1表型，从而诱导肿瘤相关巨噬细胞的表型转变[4]。
在体外，Temoporfin处理24小时后，以5.5×10-2mW/cm2/nm的光强度和39.6mJ/cm2/nm的光能量用500W卤素灯照射，显著抑制了HCT116细胞的活力，IC50值为36.4nM[5]。当暴露于620-660nm波长、剂量为13.3J/cm2的光照时，Temoporfin处理24小时显著抑制了HL60细胞和4T1细胞的增殖，IC50值分别为42nM和117nM[6]。