The curcumin analog C-150, influencing NF-κB, UPR and Akt/Notch pathways has potent anticancer activity in vitro and in vivo

László Hackler, Béla Ózsvári, Márió Gyuris, P. Sípos, Gabriella Fábián, Eszter Molnár, Annamária Marton, Nóra Faragó, József Mihály, Lajos István Nagy, Tibor Szénási, Andrea Diron, A. Párducz, Iván Kanizsai, L. Puskás

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Abstract

C-150 a Mannich-type curcumin derivative, exhibited pronounced cytotoxic effects against eight glioma cell lines at micromolar concentrations. Inhibition of cell proliferation by C-150 was mediated by affecting multiple targets as confirmed at transcription and protein level. C-150 effectively reduced the transcription activation of NFkB, inhibited PKC-alpha which are constitutively over-expressed in glioblastoma. The effects of C-150 on the Akt/Notch signaling were also demonstrated in a Drosophila tumorigenesis model. C-150 reduced the number of tumors in Drosophila with similar efficacy to mitoxantrone. In an in vivo orthotopic glioma model, C-150 significantly increased the median survival of treated nude rats compared to control animals. The multi-target action of C-150, and its preliminary in vivo efficacy would render this curcumin analogue as a potent clinical candidate against glioblastoma.

Original languageEnglish
Article numbere0149832
JournalPLoS One
Volume11
Issue number3
DOIs
Publication statusPublished - Mar 1 2016

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ASJC Scopus subject areas

  • Agricultural and Biological Sciences(all)
  • Biochemistry, Genetics and Molecular Biology(all)
  • Medicine(all)

Cite this

Hackler, L., Ózsvári, B., Gyuris, M., Sípos, P., Fábián, G., Molnár, E., Marton, A., Faragó, N., Mihály, J., Nagy, L. I., Szénási, T., Diron, A., Párducz, A., Kanizsai, I., & Puskás, L. (2016). The curcumin analog C-150, influencing NF-κB, UPR and Akt/Notch pathways has potent anticancer activity in vitro and in vivo. PLoS One, 11(3), [e0149832]. https://doi.org/10.1371/journal.pone.0149832