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.

当前全世界范围内大肠癌的高发病率是主要的健康问题。尽管常规的化学疗法和手术在一定程度上有效，但是由于相关的副作用（包括手术后并发症以及癌症与正常细胞之间的非歧视性），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方法系统，Gal-Dox，该系统优先通过受体介导的内吞作用被结肠癌细胞吸收。在癌症特异性激活后，活性药物Dox（阿霉素）以荧光开启反应释放，从而可以监测药物定位和作用部位。还在体内评估了Gal-Dox的治疗效力和离体，因此说明了Gal-Dox作为结肠直肠癌治疗方法的潜力，具有很高的特异性。