RESUMEN
ß-Cyclodextrin modified camptothecin (CPT-CD) was synthesized through esterification reaction and "click chemistry" to greatly improve the solubility of CPT in aqueous solution, and then, a supramolecular nanoparticle was constructed by strong noncovalent interaction between ß-cyclodextrin and adamantane and amphiphilic interaction by simply mixing CPT-CD and adamantane modified hyaluronic acid (HA-ADA) together. The obtained nanoparticle had a hydrophilic HA shell, which could target and recognize HA receptors overexpressed on the surface of cancer cells, and a hydrophobic CPT core, which could protect CPT from hydrolyzation. The results of cytotoxicity experiments showed that the nanoparticle we have designed in this work exhibited similar anticancer activities to, but with much lower side effects than, the commercial chemotherapeutic drug CPT in vitro. We believe that this work might provide a strategy for improving the treatment performance of CPT in laboratory and clinical settings.
Asunto(s)
Antineoplásicos Fitogénicos/administración & dosificación , Camptotecina/administración & dosificación , Preparaciones de Acción Retardada/química , beta-Ciclodextrinas/química , Adamantano/química , Animales , Antineoplásicos Fitogénicos/química , Camptotecina/química , Preparaciones de Acción Retardada/farmacocinética , Portadores de Fármacos/administración & dosificación , Portadores de Fármacos/química , Ensayos de Selección de Medicamentos Antitumorales , Dispersión Dinámica de Luz , Células HCT116/efectos de los fármacos , Humanos , Ácido Hialurónico/química , Ratones , Microscopía de Fuerza Atómica , Microscopía Electrónica de Transmisión , Células 3T3 NIH/efectos de los fármacos , Nanopartículas/administración & dosificación , Nanopartículas/química , SolubilidadRESUMEN
Conversion of cellulose to 1-(furan-2-yl)-2-hydroxyethanone has been demonstrated in concentrated zinc chloride solution under microwave irradiation. Compared with the conventional oil-bath heating mode, microwave irradiation significantly reduced the reaction time and increased the yield of 1-(furan-2-yl)-2-hydroxyethanone. A typical degradation reaction with cellulose produced 1-(furan-2-yl)-2-hydroxyethanone in 12.0% molar yield in ZnCl(2) solution (ZnCl(2)-H(2)O ratio=2.25:1, w/w) with microwave irradiation at 600 W for 5 minutes at 135°C.