Laboratory of Macromolecular Engineering, Department of Pharmaceutical Chemistry, Faculty of Pharmacy, Universitas Gadjah Mada, Sekip Utara II, 55281 Yogyakarta, Indonesia.
Cancer Chemoprevention Research Center, Faculty of Pharmacy, Universitas Gadjah Mada, Sekip Utara II, 55281 Yogyakarta, Indonesia.
Asian Pac J Cancer Prev. 2021 Jan 1;22(1):151-155. doi: 10.31557/APJCP.2021.22.1.151.
The progress from Boron Neutron Capture Therapy (BNCT) development urged us to explore new targeted and selective boron carriers. Firstly, we reported the successful synthesis of CCB-2 which exerts a cytotoxic effect against triple negative breast cancer (TNBC) cells. We introduced the new modification of CCB-2 with sugar and alcohol sugars to enhance its solubility in hoping to increase cellular uptake.
CCB-2 fructose complex (CCB-2-F), CCB-2 sorbitol complex (CCB-2-Sor), and CCB-2 xylitol complex (CCB-2-Xy) were obtained with small size within nano-specific particle. All the compounds were then determined for their cytotoxic activities through MTT assay.
All compounds were performed cytotoxic activities against TNBC 4T1 and HER-2 positive MCF-7/HER2 cells with good selectivity when tested in immortalized fibroblast cells.
Overall, we provided a new modification of CCB-2 through complexation with sugars. Still, further evaluations are needed to develop more efficient CCB-2 as the new candidate of anticancer agent, notably in breast cancer.
硼中子俘获治疗（BNCT）的进展促使我们探索新的靶向和选择性硼载体。首先，我们成功合成了对三阴性乳腺癌（TNBC）细胞具有细胞毒性作用的 CCB-2。我们引入了糖和糖醇对 CCB-2 的新修饰，以提高其在希望增加细胞摄取的水中的溶解度。
CCB-2 果糖复合物（CCB-2-F）、CCB-2 山梨醇复合物（CCB-2-Sor）和 CCB-2 木糖醇复合物（CCB-2-Xy）的粒径均在纳米级范围内。然后通过 MTT 测定法测定所有化合物的细胞毒性活性。
所有化合物均对 TNBC 4T1 和 HER-2 阳性 MCF-7/HER2 细胞具有细胞毒性活性，在永生化成纤维细胞中测试时对其具有良好的选择性。
总的来说，我们通过与糖的复合物化对 CCB-2 进行了新的修饰。然而，仍需要进一步评估以开发更有效的 CCB-2 作为新的抗癌药物候选物，特别是在乳腺癌中。
