PEGylated conjugated linoleic acid stimulation of apoptosis via a p53-mediated signaling pathway in MCF-7 breast cancer cells

Ji Hye Seo, Hyun-Seuk Moon, In Yong Kim, Ding Ding Guo, Hong Gu Lee, Yun Jaie Choi, Chong Su Cho

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20 Citations (Scopus)

Abstract

The objective of this study was to investigate whether PEGylated conjugated linoleic acid (PCLA), as compared with conjugated linoleic acid (CLA) alone, displays anti-cancer properties in MCF-7 breast cancer cells. To generate PCLA, CLA was simply coupled to poly(ethylene glycol) (PEG) at the melting state of PEG without a solvent or a catalyst. The coupling reaction generated an ester linkage between the carboxyl group of CLA and hydroxyl one of PEG. The half-life of the generated PCLA was 52 h at pH 7.4 at 37 °C, indicating that PCLA potentially acts as a pro-drug. Apoptosis of MCF-7 breast cancer cells treated with PCLA showed a dose response to PCLA concentration during treatment. In addition, pro-apoptotic proteins such as Bax were up-regulated, whereas anti-apoptotic proteins, such as Bcl-2, were down-regulated by treatment with both CLA and PCLA. The tumor suppressor gene p53 was significantly up-regulated by treatment with increasing concentrations of PCLA, suggesting that PCLA-induced apoptosis is regulated by a p53-mediated signaling pathway. Overall, the anti-cancer effects of PCLA on MCF-7 breast cancer cells may have therapeutic significance.

Original languageEnglish
Pages (from-to)621-626
Number of pages6
JournalEuropean Journal of Pharmaceutics and Biopharmaceutics
Volume70
Issue number2
DOIs
Publication statusPublished - 2008 Oct 1
Externally publishedYes

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Keywords

  • Anti-cancer
  • Conjugated linoleic acid (CLA)
  • Nanoparticle
  • PEGylation
  • Poly (ethylene glycol) (PEG)
  • Pro-drug

ASJC Scopus subject areas

  • Biotechnology
  • Pharmaceutical Science

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