期刊
JOURNAL OF INORGANIC BIOCHEMISTRY
卷 166, 期 -, 页码 87-93出版社
ELSEVIER SCIENCE INC
DOI: 10.1016/j.jinorgbio.2016.11.004
关键词
Ruthenium metallodrug; Fluorescence; MCM-41; SBA-15; Cathepsin inhibition; Drug encapsulation
资金
- Spanish Ministry of Economy and Competitiveness and UE Feder Program [CTQ2014-53486R]
- Spanish Ministry of Economy and Competitiveness and UE Feder Program (CRM Juan de la Cierva Contract)
- Junta de Andalucia [P09-FQM-4981]
- CEI BioTic Granada [CEI2015-MP-BS39]
- COST action [CM1105]
Two novel anthracene-based half-sandwich organometallic Ru(II) compounds, namely, [Ru(p-cymene)(L-1)Cl-2] (1) and [Ru(p-cymene)(L-2)Cl-2] (2) (L-1 = 1-(anthracen-9-yI)-N-(pyridin-3-ylmethyl)methanamine; L-2 = 1-(anthracen-9-y1)-N-(pyridin-4-ylmethyl)methanamine) have been synthesized and characterized. We demonstrate that the fluorescence properties of these complexes are highly affected by the linking position of the anthracene unit, as only 2 shows fluorescence emission in the blue region. Regarding their biological activity, both ruthenium metallodrugs show interaction with different biological targets such as S-donor amino acids (cysteine) and proteases (cysteine cathepsin B). Moreover, 1 and 2 show in vitro cytotoxicity against HL-60 cancer cell line (IC50 = 84.5 and 87.0 mu M for 1 and 2, respectively), with cell death occurring via apoptosis. Further studies have shown that diffusion into cells is the main mechanism of metallodrug uptake. Finally, as a proof of concept, these ruthenium complexes have been successfully encapsulated into MCM-41 and SBA-15 mesoporous silicas using two different incorporation strategies (impregnation and grinding). (C) 2016 Elsevier Inc. All rights reserved.
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