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Comparing a thioglycosylated chlorin and phthalocyanine as potential theranostic agents.
Bioorganic & Medicinal Chemistry ( IF 3.5 ) Pub Date : 2019-12-30 , DOI: 10.1016/j.bmc.2019.115259
Sunaina Singh 1 , Amit Aggarwal 1 , N V S Dinesh K Bhupathiraju 2 , Ivana Radivojevic Jovanovic 3 , Michael Landress 1 , Michelle Paola Tuz 1 , Ruomei Gao 4 , Charles M Drain 2
Affiliation  

Herein we describe the design, efficient synthesis, and photophysical properties of two macrocycle dyes for cancer theranostics. This study compares a glycosylated chlorin with a glycosylated phthalocyanine designed to specifically target cancer, wherein the photophysical properties enable both fluorescence imaging and the sensitization of the formation of reactive oxygen species (ROS) for photodynamic therapy. Both the compounds show low darktoxicity (IC50 > 100 μM). The glycosylated phthalocyanine showed low phototoxicity (IC50 > 100 μM) while glycosylated chlorin showed high phototoxicity (IC50 = 1-2 μM). ZnPcGlc8 has low solubility and also form aggregates in aqueous media, thus resulting in minimal uptake in two different human breast cancer cell lines: MDA-MB-231 and MCF-7. The glycosylated chlorin however was efficiently taken up by these two cell lines, thus allows fluorescence imaging in cells and in xenograft tumor model in mice. In this study, we find that the chlorin conjugate is the more promising theranostic agent.

中文翻译:

比较硫代糖基化的二氢卟酚和酞菁作为潜在的治疗药物。

在这里,我们描述了两种用于癌症治疗的大环染料的设计,有效合成和光物理性质。这项研究将糖基化的二氢卟酚与专门针对癌症的糖基化的酞菁进行了比较,其中光物理特性使荧光成像和对光动力学治疗的活性氧(ROS)形成的敏化成为可能。两种化合物均显示出低的暗毒性(IC50> 100μM)。糖基化酞菁显示出低光毒性(IC50> 100μM),而糖基化二氢卟酚显示出高光毒性(IC50 = 1-2μM)。ZnPcGlc8的溶解度低,并且还会在水性介质中形成聚集体,因此导致两种不同的人类乳腺癌细胞系MDA-MB-231和MCF-7的摄取量最小。然而,糖基化的二氢卟酚被这两个细胞系有效地吸收,因此允许在细胞中和在小鼠的异种移植肿瘤模型中进行荧光成像。在这项研究中,我们发现二氢卟酚偶联物是最有前途的治疗剂。
更新日期:2019-12-30
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