Journal
BIOMEDICINE & PHARMACOTHERAPY
Volume 70, Issue -, Pages 268-273Publisher
ELSEVIER FRANCE-EDITIONS SCIENTIFIQUES MEDICALES ELSEVIER
DOI: 10.1016/j.biopha.2015.01.027
Keywords
Targeted drug delivery; Peptide drug conjugate; Epidermal growth factor receptor
Funding
- Supporting Program of the Twelfth Five-year Plan for Science and Technology Research of China [2012ZX10002014-006]
- National Natural Science Foundation of China [81302708]
- Medical-Engineering Joint Funds of Shanghai Jiao Tong University [YG2013MS41]
- Shanghai Cancer Institute [SB14-05]
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The nonspecific toxicity of anticancer drug doxorubicin (DOX) toward both tumor and normal cells can result in serious side effects, thereby limiting its clinical applications. In this wok, epidermal growth factor receptor (EGFR) antagonist peptide GE11 was introduced into DOX structure via a disulfide bond which can be cleaved by reduced glutathione (GSH). We have investigated the intracellular delivery and in vitro cytotoxicity of GE11-DOX conjugate and free DOX in high (SMMC-7721) and low (MCF-7) EGFR expressing cancer cell models. GE11-DOX accumulated at higher levels in SMMC-7721 cells than in MCF-7 cells, while the cellular uptake of free DOX was almost the same in both cells. Furthermore, pretreating with anti-EGFR monoclonal antibody reduced intracellular accumulation of GE11-DOX in SMMC-7721, indicating the involvement of EGFR pathway in the transport of conjugate. Our results suggest that GE11-DOX conjugate has the potential to be a therapeutic agent for treating EGFR overexpressing tumor. (C) 2015 Elsevier Masson SAS. All rights reserved.
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