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Novel bexarotene derivatives: Synthesis and cytotoxicity evaluation for glioma cells in 2D and 3D in vitro models.

Author: AkasovRoman, AkimovMikhail G, BezuglovVladimir V, BurovSergey, DudinaPolina V, GamisoniaAlina M, GretskayaNatalia M, MarkvichevaElena, SerkovIgor V, SherstyanykhGalina, ZakharovStanislav S

Comparative StudyResearch that compares multiple groups/interventions to determine differences/similarities in outcomes/characteristics.
Journal ArticleAn article published in an academic or professional journal that reports original research or scholarly analysis.

Overview

Bexarotene (BXR) is a retinoid that inhibits glioblastoma cell growth and migration but has side effects. This study investigated two novel BXR derivatives, BXR-NEA and BXR-DA, with improved selectivity and cytotoxicity against glioblastoma cells. Both derivatives showed higher toxicity for rat C6 and human U-87MG glioma cells compared to BXR, with IC50 values in the range of 28-42 µM for BXR derivatives and 122-152 µM for BXR. The derivatives induced apoptosis in glioblastoma cells, as evidenced by annexin staining and caspase activation. Moreover, BXR-DA and BXR-NEA demonstrated better selectivity for tumor cells compared to BXR and effectively inhibited cell migration in a scratch assay. These results suggest that BXR derivatives hold promise for glioblastoma treatment.
Paper Details　
Original Abstract of the Article :
Glioblastoma (GBM) is an aggressive and lethal form of brain cancer with a high invasion capacity and a lack of effective chemotherapeutics. Retinoid bexarotene (BXR) inhibits the neurospheroidal colony formation and migration of primary glioblastoma cells but has side effects. To enhance the BXR gl...See full text at original site
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引用元：
https://doi.org/10.1016/j.ejphar.2020.173346

データ提供：米国国立医学図書館（NLM）

Novel Bexarotene Derivatives: A Glimpse into the Future of Glioma Treatment

The field of cancer research is always striving for new and improved treatments. This study delves into the realm of glioblastoma, a particularly aggressive brain cancer, and explores the potential of novel bexarotene derivatives. This study employed a combination of chemical modification, in vitro models, and cytotoxicity evaluation to assess the efficacy of these new compounds. The authors successfully synthesized two novel derivatives, BXR-NEA and BXR-DA, which exhibited enhanced cytotoxicity against glioma cells compared to the original bexarotene. These promising findings suggest that these derivatives may hold significant potential as future therapeutic options for glioblastoma.

BXR Derivatives: A Potent Weapon Against Glioma Cells

The research reveals that both BXR-DA and BXR-NEA demonstrated significantly higher toxicity towards rat C6 and human U-87MG glioma cells than the original bexarotene. The study also highlighted the importance of 3D in vitro models, as these derivatives exhibited a more pronounced selectivity against tumor cells in comparison to the parental drug. The results suggest that these novel compounds could offer a promising alternative for treating glioblastoma, potentially leading to better treatment outcomes for patients.

Looking Ahead: A Brighter Future for Glioma Patients

The research findings suggest that BXR derivatives may offer a significant advantage in the treatment of glioblastoma. The enhanced cytotoxicity, improved selectivity, and inhibition of cell migration all point towards a potential future therapeutic strategy for this aggressive form of brain cancer. However, it is important to note that these are preliminary findings, and further research is necessary to confirm their safety and efficacy in human clinical trials.

Dr.Camel's Conclusion

This study unveils the potential of novel bexarotene derivatives in combating glioblastoma, a challenging foe. Like a camel traversing a vast desert in search of an oasis, these derivatives offer a glimmer of hope for those seeking a cure. The enhanced cytotoxicity and selectivity observed in this research are like stepping stones, paving the way for a future where we can effectively combat this devastating disease.

Date :
  1. Date Completed 2021-05-18
  2. Date Revised 2021-05-18
Further Info :

Pubmed ID

32659303

DOI: Digital Object Identifier

10.1016/j.ejphar.2020.173346

SNS
PICO Info
in preparation
Languages

English

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