Romano Mariana, Uchiyama Mayara K, Cardoso Roberta M, Toma Sergio H, Baptista Mauricio S, Araki Koiti
Department of Fundamental Chemistry, Institute of Chemistry, University of São Paulo, São Paulo, Brazil, Avenida Professor Lineu Prestes, 748, São Paulo, São Paulo, 05508-000, Brazil.
Department of Biochemistry, Institute of Chemistry, University of São Paulo, São Paulo, Brazil, Avenida Professor Lineu Prestes, 748, São Paulo, São Paulo, 05508-000, Brazil.
Nanomedicine (Lond). 2020 Oct;15(25):2475-2492. doi: 10.2217/nnm-2020-0214. Epub 2020 Sep 18.
To develop a series of superparamagnetic iron oxide nanoparticles (SPIONs) by coconjugating them with ibuprofen (ibu) and glycerol phosphate (glycerol) or ibu and glucose-1-phosphate and to assess capacity of these conjugates to inhibit the release of nitric oxide (NO) in macrophages, even at low concentrations. The SPION conjugates were characterized and their properties evaluated showing the influence of those ligands on colloidal stability and inhibition of NO-release demonstrated. The cytotoxicity and possible anti-inflammatory activity were evaluated using murine macrophages (RAW 247.6). SPION-glycerol phosphate/ibu conjugates inhibited the NO production induced by lipopolysaccharides, indicating a potential anti-inflammatory activity. SPION conjugated with ibu was shown to inhibit NO-release even at very low concentrations, suggesting possible action against inflammatory diseases.
通过将超顺磁性氧化铁纳米颗粒（SPIONs）与布洛芬（ibu）和甘油磷酸酯（甘油）或ibu和葡萄糖-1-磷酸共轭，制备一系列共轭物，并评估这些共轭物即使在低浓度下抑制巨噬细胞中一氧化氮（NO）释放的能力。对SPION共轭物进行了表征并评估了其性质，显示了这些配体对胶体稳定性的影响，并证明了对NO释放的抑制作用。使用小鼠巨噬细胞（RAW 247.6）评估了细胞毒性和可能的抗炎活性。SPION-甘油磷酸酯/ibu共轭物抑制了脂多糖诱导的NO产生，表明具有潜在的抗炎活性。与ibu共轭的SPION即使在非常低的浓度下也能抑制NO释放，表明可能对炎症性疾病有作用。
