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An Unrevealed Molecular Function of Corannulene Buckybowl Glycoconjugates in Selective Tumor Annihilation by Targeting the Cancer-Specific Warburg Effect
Advanced Science ( IF 14.3 ) Pub Date : 2022-03-07 , DOI: 10.1002/advs.202105315 Shengnan Liu 1 , Ziru Sun 1 , Min Liang 1, 2 , Weijie Song 1, 3 , Ru Zhang 1, 4 , Yunli Shi 1 , Yujun Cui 1, 5 , Qingzhi Gao 1
Advanced Science ( IF 14.3 ) Pub Date : 2022-03-07 , DOI: 10.1002/advs.202105315 Shengnan Liu 1 , Ziru Sun 1 , Min Liang 1, 2 , Weijie Song 1, 3 , Ru Zhang 1, 4 , Yunli Shi 1 , Yujun Cui 1, 5 , Qingzhi Gao 1
Affiliation
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The biomedical application of corannulene π-bowls is historically limited by low solubility and bioavailability despite the potential in their unique electronic properties for new functional materials. Herein, the unexpected role and molecular mechanism of Corranulene π-bowls are uncovered in biomedical applications as an effective anticancer agent for Warburg effect mediated selective tumor targeting. The corannulene triazolyl monosaccharides Cor-sugars exhibit highly potent cytotoxicity against human cancer cells and effectively inhibit xenograft growth of hyperglycolytic tumors. Particularly, the galactose-conjugated Cor-gal exhibits superior in vivo anticancer efficacy in A549 tumor models with outstanding safety profile compared to doxorubicin. Moreover, the combined treatment of Cor-gal with immune checkpoint inhibitor results in an effective synergy in treating H460 human lung carcinoma. An uptake mechanism study reveals that Cor-sugars exploit tumor-specific glucose transporter glucose transporter 1 (GLUT1) for targeted cell delivery and intra-tumoral accumulation through the cancer-specific Warburg effect. Their significant anticancer activity is attributed to multiphasic DNA-binding and cell cycle alteration effects. This study uncovers new molecular properties of corannulene buckybowl and enabling their potential new applications in biomedical engineering.
中文翻译：
Corannulene Buckybowl 糖缀合物通过靶向癌症特异性 Warburg 效应在选择性肿瘤湮灭中的未揭示分子功能
corannulene π -bowls的生物医学应用在历史上受到低溶解度和生物利用度的限制，尽管它们具有用于新功能材料的独特电子特性的潜力。在此，Corranulene π的意想不到的作用和分子机制- 碗在生物医学应用中被发现是一种有效的抗癌剂，用于 Warburg 效应介导的选择性肿瘤靶向。Corannulene 三唑基单糖 Cor-sugars 对人类癌细胞表现出高效的细胞毒性，并有效抑制高糖酵解肿瘤的异种移植物生长。特别是，与多柔比星相比，半乳糖缀合的 Cor-gal 在 A549 肿瘤模型中表现出优异的体内抗癌功效，具有出色的安全性。此外，Cor-gal 与免疫检查点抑制剂的联合治疗在治疗 H460 人肺癌方面产生了有效的协同作用。一项摄取机制研究表明，Cor-sugars 利用肿瘤特异性葡萄糖转运蛋白葡萄糖转运蛋白 1 (GLUT1) 通过癌症特异性 Warburg 效应进行靶向细胞递送和肿瘤内积累。它们显着的抗癌活性归因于多相 DNA 结合和细胞周期改变效应。这项研究揭示了corannulene buckybowl的新分子特性，并使其在生物医学工程中具有潜在的新应用。
更新日期：2022-03-07
中文翻译：
Corannulene Buckybowl 糖缀合物通过靶向癌症特异性 Warburg 效应在选择性肿瘤湮灭中的未揭示分子功能
corannulene π -bowls的生物医学应用在历史上受到低溶解度和生物利用度的限制，尽管它们具有用于新功能材料的独特电子特性的潜力。在此，Corranulene π的意想不到的作用和分子机制- 碗在生物医学应用中被发现是一种有效的抗癌剂，用于 Warburg 效应介导的选择性肿瘤靶向。Corannulene 三唑基单糖 Cor-sugars 对人类癌细胞表现出高效的细胞毒性，并有效抑制高糖酵解肿瘤的异种移植物生长。特别是，与多柔比星相比，半乳糖缀合的 Cor-gal 在 A549 肿瘤模型中表现出优异的体内抗癌功效，具有出色的安全性。此外，Cor-gal 与免疫检查点抑制剂的联合治疗在治疗 H460 人肺癌方面产生了有效的协同作用。一项摄取机制研究表明，Cor-sugars 利用肿瘤特异性葡萄糖转运蛋白葡萄糖转运蛋白 1 (GLUT1) 通过癌症特异性 Warburg 效应进行靶向细胞递送和肿瘤内积累。它们显着的抗癌活性归因于多相 DNA 结合和细胞周期改变效应。这项研究揭示了corannulene buckybowl的新分子特性，并使其在生物医学工程中具有潜在的新应用。
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