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Anticancer properties of 4-thiazolidinone derivatives depend on peroxisome proliferator-activated receptor gamma

Konrad A Szychowski1, Marcin L Leja2, Danylo V Kaminskyy3

  • 1Department of Public Health, Dietetics and Lifestyle Disorders, Faculty of Medicine, University of Information Technology and Management in Rzeszow, Sucharskiego 2, 35-225 Rzeszow, Poland.

European Journal of Medicinal Chemistry
|October 15, 2017
PubMed

Insights

Novel 4-thiazolidinone derivatives show potent anticancer activity against squamous carcinoma cells, primarily through the peroxisome proliferator-activated receptor gamma (PPARγ) pathway. These new compounds demonstrate greater efficacy than approved drugs like Rosiglitazone.

Area of Science:

  • Pharmacology
  • Oncology
  • Molecular Biology

Background:

  • Peroxisome proliferator-activated receptors (PPARs) are crucial in chronic diseases like cancer.
  • PPAR modulators are established treatments, driving research into new therapeutic agents.

Purpose of the Study:

  • To investigate the role of PPARs in the cytotoxic and pro-apoptotic effects of novel 4-thiazolidinone derivatives.
  • To compare the efficacy of new derivatives against approved PPAR modulators in human squamous carcinoma cells.

Main Methods:

  • Treatment of SCC-15 cells with novel and approved 4-thiazolidinones.
  • PPAR-specific siRNA gene silencing for PPARα, PPARβ, and PPARγ.
  • Measurement of mRNA expression, cell viability, metabolism, and caspase-3 activity.

Main Results:

  • Novel 4-thiazolidinones decreased mRNA expression of PPARα, PPARβ, and PPARγ in SCC-15 cells.
  • PPARγ knockdown mitigated the cytotoxic effects of the compounds, indicating a key role for PPARγ.
  • New derivatives exhibited superior anticancer potential compared to Rosiglitazone and Pioglitazone.

Conclusions:

  • Novel 4-thiazolidinone derivatives exert anticancer effects predominantly via the PPARγ pathway in SCC-15 cells.
  • The studied compounds function as PPAR agonists, with potential for greater efficacy than existing treatments.
Keywords:
CytotoxicityPPARsSCC-15ThiazolidinoneThiazolothiopyranes

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