| Fajiang Mao,maofajiang,Xingli Wu,wuxingli,yuanchenyue,Chenyue Yuan,huanghaiyan,Haiyan Huang,Yanyan Qiu,qiuyanyan,renjianlin,Jianlin Ren,yinpeihao. Allosteric probe-modified liposome loading bufalin-fluorouracil complex for targeted colorectal cancer therapy. Oncol Transl Med, 2022, 8: 239-246. |
| 变构探针修饰的负载蟾毒灵和5-FU的脂质体靶向治疗结直肠癌研究 |
| Allosteric probe-modified liposome loading bufalin-fluorouracil complex for targeted colorectal cancer therapy |
| Received:June 30, 2022 Revised:October 24, 2022 |
| DOI：10.1007/s10330-022-0586-6 |
| 中文关键词: 蟾毒灵；5-氟尿嘧啶；结直肠癌；成像技术； |
| 英文关键词: bufalin; fluorouracil; colorectal cancer; imaging; therapy |
| 基金项目:上海市科委引导项目（19401935200）；上海中医药大学预算内科研项目（20LK065）） |
| Author Name | Affiliation | Postcode | | Fajiang Mao* | Department of Oncology, Shanghai Municipal Hospital of Traditional Chinese Medicine, Shanghai University of Traditional Chinese Medicine | 200071 | | maofajiang | Shanghai Municipal Hospital of Traditional Chinese Medicine,Shanghai University of Traditional Chinese | 200071 | | Xingli Wu | Department of Oncology, Shanghai Municipal Hospital of Traditional Chinese Medicine, Shanghai University of Traditional Chinese Medicine | 200071 | | wuxingli | Shanghai Municipal Hospital of Traditional Chinese Medicine,Shanghai University of Traditional Chinese Medicine | | | yuanchenyue | Shanghai Municipal Hospital of Traditional Chinese Medicine,Shanghai University of Traditional Chinese Medicine | | | Chenyue Yuan | Department of Oncology, Shanghai Municipal Hospital of Traditional Chinese Medicine, Shanghai University of Traditional Chinese Medicine | 200071 | | huanghaiyan | Shanghai Municipal Hospital of Traditional Chinese Medicine,Shanghai University of Traditional Chinese Medicine | | | Haiyan Huang | Department of Oncology, Shanghai Municipal Hospital of Traditional Chinese Medicine, Shanghai University of Traditional Chinese Medicine | 200071 | | Yanyan Qiu | Department of Oncology, Shanghai Municipal Hospital of Traditional Chinese Medicine, Shanghai University of Traditional Chinese Medicine | 200071 | | qiuyanyan | Shanghai Municipal Hospital of Traditional Chinese Medicine,Shanghai University of Traditional Chinese Medicine | | | renjianlin | Shanghai Municipal Hospital of Traditional Chinese Medicine,Shanghai University of Traditional Chinese Medicine | | | Jianlin Ren | Department of Oncology, Shanghai Municipal Hospital of Traditional Chinese Medicine, Shanghai University of Traditional Chinese Medicine | 200071 | | yinpeihao* | Interventional Cancer Institute of Chinese Integrative Medicine，Putuo Hospital, Shanghai University of Traditional Chinese Medicine | 200070 |
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| 中文摘要: |
| 蟾毒灵作为传统中药中华蟾酥的主要活性抗肿瘤单体，在肿瘤治疗中起着至关重要的作用。然而，溶解度差和系统毒性等固有问题大大降低了其抗癌功能，并造成了不必要的副作用。为了达到令人满意的治疗效果，必须开发创新的靶向系统，以精确有效地提供抗癌药物。在这项工作中，建立了一种新的、更有效的同时检测和杀死结直肠癌细胞的系统。在该方法中，设计了两个变构探针，包括一个报告探针和一个识别探针。该方法通过对靶细胞的基于探针的特异性识别和基于探针的信号报告，对细胞检测具有较高的灵敏度。布法林和氟尿嘧啶的联合应用赋予了该方法更好的肿瘤细胞抑制作用。这种方法将为细胞内生物分子检测和靶向癌细胞治疗提供新的机会。 |
| 英文摘要: |
| 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. |
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