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Evaluation of Anti-Inflammatory Drug-Conjugated Silicon Quantum Dots: Their Cytotoxicity and Biological Effect
Vice Director-General's Lab, Research Institute, National Center for Global Health and Medicine, Tokyo 162-8655, Japan
Department of Molecular Cell Biology, Institute of DNA Medicine, Jikei University School of Medicine, Tokyo 105-8461, Japan
* Author to whom correspondence should be addressed.
Received: 20 December 2012; in revised form: 1 January 2013 / Accepted: 5 January 2013 / Published: 10 January 2013
Abstract: 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.
Keywords: silicon quantum dot; alminoprofen; cyclooxygenase-2; cytotoxicity and biological effect
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Hanada, S.; Fujioka, K.; Futamura, Y.; Manabe, N.; Hoshino, A.; Yamamoto, K. Evaluation of Anti-Inflammatory Drug-Conjugated Silicon Quantum Dots: Their Cytotoxicity and Biological Effect. Int. J. Mol. Sci. 2013, 14, 1323-1334.
Hanada S, Fujioka K, Futamura Y, Manabe N, Hoshino A, Yamamoto K. Evaluation of Anti-Inflammatory Drug-Conjugated Silicon Quantum Dots: Their Cytotoxicity and Biological Effect. International Journal of Molecular Sciences. 2013; 14(1):1323-1334.
Hanada, Sanshiro; Fujioka, Kouki; Futamura, Yasuhiro; Manabe, Noriyoshi; Hoshino, Akiyoshi; Yamamoto, Kenji. 2013. "Evaluation of Anti-Inflammatory Drug-Conjugated Silicon Quantum Dots: Their Cytotoxicity and Biological Effect." Int. J. Mol. Sci. 14, no. 1: 1323-1334.