Hanada Sanshiro, Fujioka Kouki, Futamura Yasuhiro, Manabe Noriyoshi, Hoshino Akiyoshi, Yamamoto Kenji
Vice Director-General's Lab, Research Institute, National Center for Global Health and Medicine, Tokyo 162-8655, Japan.
Int J Mol Sci. 2013 Jan 10;14(1):1323-34. doi: 10.3390/ijms14011323.
Silicon quantum dots (Si-QDs) have great potential for biomedical applications, including their use as biological fluorescent markers and carriers for drug delivery systems. Biologically inert Si-QDs are less toxic than conventional cadmium-based QDs, and can modify the surface of the Si-QD with covalent bond. We synthesized water-soluble alminoprofen-conjugated Si-QDs (Ap-Si). Alminoprofen is a non-steroid anti-inflammatory drug (NSAID) used as an analgesic for rheumatism. Our results showed that the "silicon drug" is less toxic than the control Si-QD and the original drug. These phenomena indicate that the condensed surface integration of ligand/receptor-type drugs might reduce the adverse interaction between the cells and drug molecules. In addition, the medicinal effect of the Si-QDs (i.e., the inhibition of COX-2 enzyme) was maintained compared to that of the original drug. The same drug effect is related to the integration ratio of original drugs, which might control the binding interaction between COX-2 and the silicon drug. We conclude that drug conjugation with biocompatible Si-QDs is a potential method for functional pharmaceutical drug development.
硅量子点（Si-QDs）在生物医学应用方面具有巨大潜力，包括用作生物荧光标记物和药物递送系统的载体。生物惰性的Si-QDs比传统的镉基量子点毒性更小，并且可以通过共价键修饰Si-QD的表面。我们合成了水溶性的阿明洛芬共轭硅量子点（Ap-Si）。阿明洛芬是一种非甾体抗炎药（NSAID），用作治疗风湿病的镇痛药。我们的结果表明，这种“硅药物”比对照Si-QD和原药的毒性更小。这些现象表明，配体/受体型药物的凝聚表面整合可能会减少细胞与药物分子之间的不良相互作用。此外，与原药相比，Si-QDs的药用效果（即对COX-2酶的抑制作用）得以维持。相同的药物效果与原药的整合比例有关，这可能控制COX-2与硅药物之间的结合相互作用。我们得出结论，药物与生物相容性Si-QDs共轭是功能性药物开发的一种潜在方法。
