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The Curcumin Analog C-150, Influencing NF-?B, UPR and Akt/Notch Pathways Has Potent Anticancer Activity In Vitro and In Vivo.

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.

SUBMITTER: Hackler L

PROVIDER: S-EPMC4778904 | biostudies-literature | 2016

REPOSITORIES: biostudies-literature

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The Curcumin Analog C-150, Influencing NF-κB, UPR and Akt/Notch Pathways Has Potent Anticancer Activity In Vitro and In Vivo.

Hackler László L Ózsvári Béla B Gyuris Márió M Sipos Péter P Fábián Gabriella G Molnár Eszter E Marton Annamária A Faragó Nóra N Mihály József J Nagy Lajos István LI Szénási Tibor T Diron Andrea A Párducz Árpád Á Kanizsai Iván I Puskás László G LG

PloS one 20160304 3

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 Droso ...[more]

PMID: 26943907

Dataset Information

The Curcumin Analog C-150, Influencing NF-?B, UPR and Akt/Notch Pathways Has Potent Anticancer Activity In Vitro and In Vivo.

Publications

The Curcumin Analog C-150, Influencing NF-κB, UPR and Akt/Notch Pathways Has Potent Anticancer Activity In Vitro and In Vivo.

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