In the paper, folic acid（FA）-mediated and β-cyclodextrin（β-CD） derivatives ftmctionalized magnetic Fe3O4 nanoparticles（MNPs） were successfully prepared as drug carriers for the targeted delivery and controlled...In the paper, folic acid（FA）-mediated and β-cyclodextrin（β-CD） derivatives ftmctionalized magnetic Fe3O4 nanoparticles（MNPs） were successfully prepared as drug carriers for the targeted delivery and controlled release of water-insoluble anticaneer drug. FA-sulfobutyl ether-β-CD-MNPs（FA-SBE-β-CD-MNPs）, FA-hydroxypropyl- β-CD-MNPs（FA-HP-β-CD-MNPs） and FA-carboxymethyl-β-CD-MNPs（FA-CM-β-CD-MNPs） were fabricated, and the loading efficiency and relative entrapment rate of curcumin are 12.04 mg/g, 95.56% for FA-SBE-β-CD-MNPs, 9.6 mg/g, 81.63% for FA-HP-β-CD-MNPs and 7.88 mg/g, 85,28% for FA-CM-β-CD-MNPs, respectively. Meanwhile, at pH：5.0, the optimal release rate of curcumin is about 46.07% for FA-SBE-β-CD-MNPs in 5 h. Cellular uptake in- dicates that curcumin can be selectively transported to targeting site and released from the internalized carriers. The in vitro cytotoxicity reveals that non-toxic FA-SBE-β-CD-MNPs have excellent biocompatibility on HepG2 cells in the tested concentrations. Therefore, FA-SBE-β-CD-MNPs could provide a promising platform for the targeting delivery of water insoluble anti-cancer drugs for different treatment needs of cancer therapy.展开更多
β-Amyloid（Afl） plaques and intracellular neurofibrillary lesions in the brain are markers of Alzheimer＇s disease（AD）. The ability to safely decrease Aft concentrations is potentially important as a preventive st...β-Amyloid（Afl） plaques and intracellular neurofibrillary lesions in the brain are markers of Alzheimer＇s disease（AD）. The ability to safely decrease Aft concentrations is potentially important as a preventive strategy for AD. The interactions between vanillin and Aft polypeptide were investigated via fluorescence spectroscopy and atomic force microscopy（AFM）. The results of fluorescence and synchronous spectroscopies illustrate that the intrinsic fluorescence of tyrosine（Tyr） residues in Aβ1-42 aggregates can be quenched strongly upon the formation of vanil- lin-Aβ-42 complex. Thioflavine T（ThT）-induced fluorescence changes indicated that Aβ1--42 aggregates could be disaggregated by vanillin, and the AFM images of Aβ1-42 enunciated the depolymerization of Aβ1-42 aggregates by vanillin in a dose-dependent manner. Vanillin may be a potential pharmacological agent for the treatment of AD.展开更多
基金Supported by the National Natural Science Foundation for the Youth, China（No.21205076） and the Applied Basic Research Project of Shanxi Province, China（No.201601D102017）.
文摘In the paper, folic acid（FA）-mediated and β-cyclodextrin（β-CD） derivatives ftmctionalized magnetic Fe3O4 nanoparticles（MNPs） were successfully prepared as drug carriers for the targeted delivery and controlled release of water-insoluble anticaneer drug. FA-sulfobutyl ether-β-CD-MNPs（FA-SBE-β-CD-MNPs）, FA-hydroxypropyl- β-CD-MNPs（FA-HP-β-CD-MNPs） and FA-carboxymethyl-β-CD-MNPs（FA-CM-β-CD-MNPs） were fabricated, and the loading efficiency and relative entrapment rate of curcumin are 12.04 mg/g, 95.56% for FA-SBE-β-CD-MNPs, 9.6 mg/g, 81.63% for FA-HP-β-CD-MNPs and 7.88 mg/g, 85,28% for FA-CM-β-CD-MNPs, respectively. Meanwhile, at pH：5.0, the optimal release rate of curcumin is about 46.07% for FA-SBE-β-CD-MNPs in 5 h. Cellular uptake in- dicates that curcumin can be selectively transported to targeting site and released from the internalized carriers. The in vitro cytotoxicity reveals that non-toxic FA-SBE-β-CD-MNPs have excellent biocompatibility on HepG2 cells in the tested concentrations. Therefore, FA-SBE-β-CD-MNPs could provide a promising platform for the targeting delivery of water insoluble anti-cancer drugs for different treatment needs of cancer therapy.
基金Supported by the National Natural Science Foundation of China（Nos.21205076, 21175086）, the Postdoctoral Science Foundation of China（No.2013M541203） and the Hundred-Talent Project of Shanxi Province, China.
文摘β-Amyloid（Afl） plaques and intracellular neurofibrillary lesions in the brain are markers of Alzheimer＇s disease（AD）. The ability to safely decrease Aft concentrations is potentially important as a preventive strategy for AD. The interactions between vanillin and Aft polypeptide were investigated via fluorescence spectroscopy and atomic force microscopy（AFM）. The results of fluorescence and synchronous spectroscopies illustrate that the intrinsic fluorescence of tyrosine（Tyr） residues in Aβ1-42 aggregates can be quenched strongly upon the formation of vanil- lin-Aβ-42 complex. Thioflavine T（ThT）-induced fluorescence changes indicated that Aβ1--42 aggregates could be disaggregated by vanillin, and the AFM images of Aβ1-42 enunciated the depolymerization of Aβ1-42 aggregates by vanillin in a dose-dependent manner. Vanillin may be a potential pharmacological agent for the treatment of AD.
