title: Self-aggregation of amphiphilic [60]fullerenyl focal point functionalized PAMAM dendrons into pseudodendrimers: DNA binding involving dendriplex formation.
abstract: In this research, we successfully performed a "click" synthesis of amphiphilic poly(amido amine) dendron-bearing fullerenyl conjugate (C60 G1 ) using a copper(I)-catalyzed azide-alkyne cycloaddition reaction. The strong hydrophobicity of the C60 moiety induces self-assembly of C60 G1 into core-shell-like "pseudodendrimers" with a uniform size distribution and positively charged peripherals. The pseudodendrimers were well-characterized by atomic force microscopy (AFM), transmission electron microscopy, and dynamic light scattering. On the basis of electrostatic interactions, the polycationic C60 G1 assembly can serve as a nonviral gene vector. An ethidium bromide displacement assay and agarose gel electrophoresis both indicated that C60 G1 assembly forms stable complexes with the cyclic reporter gene (pEGFP-C1) at low nitrogen-to-phosphorous (N/P) ratios. AFM analysis revealed a dynamic complex-formation process, and confirmed the synthesis of C60 G1 /pEGFP-C1 hybrids with a particle dimensions less than 200 nm. Fluorescence microscopy and flow cytometry revealed that 51% of HeLa and 43% of MCF-7 cells are positive to the YOYO-1-labeled hybrids at an N/P ratio of 2, being comparable to TurboFect-mediated delivery.
authors.affiliation: School of Medical Applied Chemistry, Chung Shan Medical University, Taichung, 40201, Taiwan.
authors.forename: Cheng-Hsiang
authors.initials: CH
authors.lastname: Hung
authors.forename: Wen-Wei
authors.initials: WW
authors.lastname: Chang
authors.forename: Ssu-Ching
authors.initials: SC
authors.lastname: Liu
authors.forename: Shang-Jung
authors.initials: SJ
authors.lastname: Wu
authors.forename: Chih-Chien
authors.initials: CC
authors.lastname: Chu
authors.forename: Ya-Ju
authors.initials: YJ
authors.lastname: Tsai
authors.forename: Toyoko
authors.initials: T
authors.lastname: Imae
mesh_terms: D004247:DNA / Q000378:metabolism*; D050091:Dendrimers / Q000138:chemical synthesis / Q000737:chemistry*; D005434:Flow Cytometry; D005453:Fluorescence; D037741:Fullerenes / Q000737:chemistry*; D018014:Gene Transfer Techniques; D006367:HeLa Cells; D006801:Humans; D061986:MCF-7 Cells; D018625:Microscopy, Atomic Force; D013050:Spectrometry, Fluorescence; D017550:Spectroscopy, Fourier Transform Infrared; D013501:Surface-Active Agents / Q000737:chemistry*
chemical_list: D050091:Dendrimers; D037741:Fullerenes; C104700:PAMAM Starburst; D013501:Surface-Active Agents; D004247:DNA
keywords: PAMAM dendrimer; amphiphilic dendrons; click chemistry; fullerene; gene delivery