The aqueous dispersion of ZnO quantum dots (QDs) with strong blue emission (quantum yield of 76%) was synthesized through a simple solution route. The water stability of such QDs is provided by the hydroxyl groups on their surface, and the strong blue emission is suggested to arise from the formation of surface ZnO/oleic acid complexes. Under irradiation, these complexes are thought to absorb the excitation light with 3.54 eV and then generate the blue emission with 2.82 eV.
ZnS/ZnO heteronanostructures were prepared to serve as the photoanode of the dye-sensitized solar cells. Two nanostructures, namely, ZnS/ZnO coaxial nanowires and ZnS/ZnO hierarchical nanowires (ZnS nanoparticles on ZnO nanowires), were successfully synthesized by chemical bath deposition and chemical etching processes, respectively. For both of the nanostructures, the ZnS coating can enhance photocurrent and conversion efficiency compared with the bare ZnO nanowires. We propose that ZnS layers in the two nanostructures take effect in different ways in that the ZnS compact layer in the coaxial structure retards the back transfer of electrons to the dye and electrolyte, while the coarse surface of ZnS nanoparticles in the hierarchical nanowires significantly enhances the adsorption of dye molecules. Hence, the ideal photoanode structure for high power-conversion efficiency should have both the compact shell layer and the high surface roughness.
A series of amino acid monoester prodrugs of floxuridine was synthesized and evaluated for the improvement of oral bioavailability and the feasibility of target drug delivery via oligopeptide transporters. All floxuridine 5′-amino acid monoester prodrugs exhibited PEPT1 affinity, with inhibition coefficients of Gly-Sar uptake (IC50) ranging from 0.7 – 2.3 mM in Caco-2 and 2.0 – 4.8 mM in AsPC-1 cells, while that of floxuridine was 7.3 mM and 6.3 mM, respectively. Caco-2 membrane permeabilities of floxuridine prodrugs (1.01 – 5.31 x 10-6 cm/sec) and floxuridine (0.48 x 10-6 cm/sec) were much higher than that of 5-FU (0.038 x 10-6 cm/sec). MDCK cells stably transfected with the human oligopeptide transporter PEPT1 (MDCK/hPEPT1) exhibited enhanced cell growth inhibition in the presence of the prodrugs. This prodrug strategy offers great potential, not only for increased drug absorption but also for improved tumor selectivity and drug efficacy.
Nanodiamonds with sizes of 3–6nm were prepared by irradiating graphite suspension using a long-pulse-width (1.2ms) laser at room temperature and normal pressure. The low power density and long pulse laser generated a lower temperature and a lower pressure, which determine the stable size of nanodiamonds. On the other hand, the low degree of supercooling allows a rather low growth velocity, and a disordered structure formed at the diamond surface retards the epitaxy growth. The above two factors dynamically limit the final size of nanodiamonds. Our results suggest that the growth of nanodiamonds follows the Wilson-Frenkel law, and the long pulse laser is propitious to producing fine nanodiamonds.
A prodrug strategy was applied to guanidino-containing analogs to increase oral absorption via hPEPT1 and hVACVase. L-Valine, L-isoleucine and L-phenylalanine esters of [3-(hydroxymethyl)phenyl]guanidine (3-HPG) were synthesized and evaluated for transport and activation. In HeLa/hPEPT1 cells, Val-3-HPG and Ile-3-HPG exhibited high affinity to hPEPT1 (IC 50 : 0.65 and 0.63 mM, respectively), and all three L-amino acid esters showed higher uptake (2.6-to 9-fold) than the parent compound 3-HPG. Val-3-HPG and Ile-3-HPG demonstrated remarkable Caco-2 permeability enhancement, and Val-3-HPG exhibited comparable permeability to valacyclovir. In rat perfusion studies, Val-3-HPG and Ile-3-HPG permeabilities were significantly higher than 3-HPG, and exceeded/matched the high-permeability standard metoprolol, respectively. All the L-amino acid 3-HPG esters were effectively activated in HeLa and Caco-2 cell homogenates, and were found to be good substrates of hVACVase (k cat /K m in mM −1 ·s −1 : Val-3-HPG, 3370; Ile-3-HPG, 1580; Phe-3-HPG, 1660). In conclusion, a prodrug strategy is effective at increasing the intestinal permeability of polar guanidino analogs via targeting hPEPT1 for transport and hVACVase for activation.
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