Objective Bufalin, the main active anti-tumor monomer of toad venom, is crucial in cancer treatment. However, intrinsic issues, such as poor solubility and systematic toxicity, have considerably mitigated its anticancer functions and caused unwanted side effects. It is essential to develop innovative targeting systems to precisely and efficiently deliver anticancer drugs to achieve satisfying therapeutic efficiency.Methods This work established a novel and more efficient system for simultaneously detecting and killing colorectal cancer cells. The proposed method designed two allosteric probes, a report probe and a recognize probe. The method exhibited high sensitivity towards cell detection via the recognizing probe identifying target cancer cells and the report probe's signal report. Combining bufalin and fluorouracil endowed better tumor cell inhibition. Results We observed significantly enhanced fluorescence dots surrounding the HCT-116 cell membranes. No fluorescence increments in the other three cells were identified, indicating that the established liposome complex could specifically bind with target cells. In addition, the best ratio of bufalin to fluorouracil was 0.15 and 0.5, respectively. This improved the anti-tumor effects and achieved more than 60％ tumor cell inhibition. Conclusion This method will provide new opportunities for intracellular biomolecule detection and targeted cancer cell therapy.

Fajiang Mao;Xingli Wu;Chenyue Yuan;Haiyan Huang;Yanyan Qiu;Jianlin Ren;PeihaoYin

Department of Oncology,Shanghai Municipal Hospital of Traditional Chinese Medicine,Shanghai University of Traditional Chinese Medicine,Shanghai 200071,China;Interventional Cancer Institute of Chinese Integrative Medicine,Putuo Hospital,Shanghai University of Traditional Chinese Medicine,Shanghai 200062,China

肿瘤学与转化医学（英文）

[1]Fajiang Mao;Xingli Wu;Chenyue Yuan;Haiyan Huang;Yanyan Qiu;Jianlin Ren;PeihaoYin-.Allosteric probe-modified liposome loading bufalin-fluorouracil complex for targeted colorectal cancer therapy)[J].肿瘤学与转化医学（英文）,2022(05):239-246

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