Literature DB >> 31844979

Combined treatment of AT101 and demethoxycurcumin yields an enhanced anti-proliferative effect in human primary glioblastoma cells.

Moiken Mehner1, Carolin Kubelt1, Vivian Adamski1, Christina Schmitt2, Michael Synowitz1, Janka Held-Feindt3.   

Abstract

PURPOSE: Glioblastoma multiforme (GBM) is a poorly curable disease due to its profound chemoresistance. Despite recent advances in surgery, radiotherapy and chemotherapy, the efficient treatment of GBMs is still a clinical challenge. Beside others, AT101, the R-(-) enantiomer of gossypol, and demethoxycurcumin (DMC), a curcumin-related demethoxy compound derived from Curcuma longa, were considered as possible alternative drugs for GBM therapy.
METHODS: Using different human primary GBM cell cultures in a long-term stimulation in vitro model, the cytotoxic and anti-proliferative effects of single and combined treatment with 5 µM AT101 and 5 µM or 10 µM DMC were investigated. Furthermore, western blots on pAkt and pp44/42 as well as JC-1 staining and real-time RT-PCR were performed to understand the influence of the treatment at the molecular and gene level.
RESULTS: Due to enhanced anti-proliferative effects, we showed that combined therapy with both drugs was superior to a single treatment with AT101 or DMC. Here, by determination of the combination index, a synergism of the combined drugs was detectable. Phosphorylation and thereby activation of the kinases p44/42 and Akt, which are involved in proliferation and survival processes, were inhibited, the mitochondrial membrane potential of the GBM cells was altered, and genes involved in dormancy-associated processes were regulated by the combined treatment strategy.
CONCLUSION: Combined treatment with different drugs might be an option to efficiently overcome chemoresistance of GBM cells in a long-term treatment strategy.

Entities:  

Keywords:  AT101; Cytotoxicity; Demethoxycurcumin; Glioblastoma; Proliferation

Mesh:

Substances:

Year:  2019        PMID: 31844979     DOI: 10.1007/s00432-019-03107-7

Source DB:  PubMed          Journal:  J Cancer Res Clin Oncol        ISSN: 0171-5216            Impact factor:   4.553


  34 in total

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Review 5.  Recent advances in gossypol derivatives and analogs: a chemistry and biology view.

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Journal:  Future Med Chem       Date:  2017-07-19       Impact factor: 3.808

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7.  Comparative antioxidant activities of curcumin and its demethoxy and hydrogenated derivatives.

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8.  Characterization and modeling of the oligomeric state and ligand binding behavior of purified translocator protein 18 kDa from Rhodobacter sphaeroides.

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9.  Interrogation of gossypol therapy in glioblastoma implementing cell line and patient-derived tumour models.

Authors:  M A Jarzabek; V Amberger-Murphy; J J Callanan; C Gao; A M Zagozdzon; L Shiels; J Wang; K L Ligon; B E Rich; P Dicker; W M Gallagher; J H M Prehn; A T Byrne
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10.  ABCG2 downregulation in glioma stem cells enhances the therapeutic efficacy of demethoxycurcumin.

Authors:  Long Chen; Lei Shi; Wenhua Wang; Youxin Zhou
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3.  AT101-Loaded Cubosomes as an Alternative for Improved Glioblastoma Therapy.

Authors:  Dorota K Flak; Vivian Adamski; Grzegorz Nowaczyk; Kosma Szutkowski; Michael Synowitz; Stefan Jurga; Janka Held-Feindt
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4.  Glioblastoma multiforme (GBM): An overview of current therapies and mechanisms of resistance.

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5.  Effects of the Anti-Tumorigenic Agent AT101 on Human Glioblastoma Cells in the Microenvironmental Glioma Stem Cell Niche.

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  5 in total

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