title: Photodynamic therapy of a 2-methoxyestradiol tumor-targeting drug delivery system mediated by Asn-Gly-Arg in breast cancer.
abstract: Fullerene (C60) has shown great potential in drug delivery. In this study we exploited modified fullerene (diadduct malonic acid-fullerene-Asn-Gly-Arg peptide [DMA-C60-NGR]) as an antitumor drug carrier in order to build a new tumor-targeting drug delivery system. We also investigated the synergistic enhancement of cancer therapy using photodynamic therapy (PDT) induced by DMA-C60-NGR and 2-methoxyestradiol (2ME). Cytotoxicity tests indicated that DMA-C60-NGR had no obvious toxicity, while our drug delivery system (DMA-C60-2ME-NGR) had a high inhibition effect on MCF-7 cells compared to free 2ME. The tumor-targeting drug delivery system could efficiently cross cell membranes, and illumination induced the generation of intracellular reactive oxygen species and DNA damage. Furthermore, DMA-C60-2ME-NGR with irradiation had the highest inhibition effect on MCF-7 cells compared to the other groups. DMA-C60-NGR combined with 2ME showed a good synergistic photosensitization effect for inhibiting the growth of MCF-7 cells, demonstrating that DMA-C60-2ME-NGR may be promising for high treatment efficacy with minimal side effects in future therapy.
authors: School of Pharmaceutical Sciences, Zhengzhou University, Zhengzhou, People's Republic of China.
authors: Jinjin
authors: J
authors: Shi
authors: Zhenzhen
authors: Z
authors: Wang
authors: Lei
authors: L
authors: Wang
authors: Honghong
authors: H
authors: Wang
authors: Lulu
authors: L
authors: Li
authors: Xiaoyuan
authors: X
authors: Yu
authors: Jing
authors: J
authors: Zhang
authors: Rou
authors: R
authors: Ma
authors: Zhenzhong
authors: Z
authors: Zhang
mesh_terms: D000077584:2-Methoxyestradiol; D000818:Animals; D017209:Apoptosis / Q000187:drug effects; D001943:Breast Neoplasms / Q000188:drug therapy* / Q000378:metabolism* / Q000473:pathology; D049109:Cell Proliferation / Q000187:drug effects; D002470:Cell Survival / Q000187:drug effects; D053938:DNA Fragmentation / Q000187:drug effects; D004337:Drug Carriers / Q000008:administration & dosage* / Q000737:chemistry / Q000493:pharmacokinetics; D004958:Estradiol / Q000008:administration & dosage / Q000031:analogs & derivatives* / Q000737:chemistry; D005260:Female; D037741:Fullerenes / Q000008:administration & dosage / Q000737:chemistry / Q000493:pharmacokinetics; D006801:Humans; D061986:MCF-7 Cells; D008314:Malonates / Q000008:administration & dosage / Q000737:chemistry / Q000493:pharmacokinetics; D051379:Mice; D009842:Oligopeptides / Q000008:administration & dosage* / Q000737:chemistry / Q000493:pharmacokinetics; D010778:Photochemotherapy / Q000379:methods*; D017319:Photosensitizing Agents / Q000008:administration & dosage / Q000493:pharmacokinetics; D017382:Reactive Oxygen Species / Q000378:metabolism
chemical_list: D004337:Drug Carriers; D037741:Fullerenes; D008314:Malonates; C526428:NGR peptide; D009842:Oligopeptides; D017319:Photosensitizing Agents; D017382:Reactive Oxygen Species; D004958:Estradiol; D000077584:2-Methoxyestradiol
keywords: drug delivery system; fullerene; photodynamic therapy; tumor targeting
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