Department of Chemistry, Korea University, Seoul 02841, South Korea.
Department of Mechanical Engineering, Sogang University, Seoul 04107, South Korea.
Biomaterials. 2018 Feb;155:145-151. doi: 10.1016/j.biomaterials.2017.11.019. Epub 2017 Nov 20.
The high incidence of colorectal cancer worldwide is currently a major health concern. Although conventional chemotherapy and surgery are effective to some extent, there is always a risk of relapse due to associated side effects, including post-surgical complications and non-discrimination between cancer and normal cells. In this study, we developed a small molecule-based theranostic system, Gal-Dox, which is preferentially taken up by colon cancer cells through receptor-mediated endocytosis. After cancer-specific activation, the active drug Dox (doxorubicin) is released with a fluorescence turn-on response, allowing both drug localization and site of action to be monitored. The therapeutic potency of Gal-Dox was also evaluated, both in vivo and ex vivo, thus illustrating the potential of Gal-Dox as a colorectal cancer theranostic with great specificity.
全球结直肠癌发病率居高不下，目前是一个主要的健康关注点。虽然常规化疗和手术在一定程度上有效，但由于相关副作用，包括手术后并发症和对癌细胞与正常细胞的无差别杀伤，总是存在复发的风险。在这项研究中，我们开发了一种基于小分子的治疗诊断系统 Gal-Dox，它可以通过受体介导的内吞作用被结肠癌细胞优先摄取。在癌症特异性激活后，活性药物 Dox（阿霉素）被释放，并伴有荧光开启响应，从而可以监测药物的定位和作用部位。我们还评估了 Gal-Dox 的治疗效果，包括在体内和体外，因此说明了 Gal-Dox 作为一种具有高度特异性的结直肠癌治疗诊断试剂的潜力。
