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In vitro anti-proliferative and anti-angiogenic activities of thalidomide dithiocarbamate analogs

Bishoy Y A El-Aarag1, Tomonari Kasai2, Magdy A H Zahran3

  • 1Chemistry Department, Faculty of Science, Menofia University, Egypt; Division of Chemistry and Biotechnology, Graduate School of Natural Science and Technology, Okayama University, Okayama 7008530, Japan.

International Immunopharmacology
|May 27, 2014
PubMed

Insights

New thalidomide dithiocarbamate analogs show significant anti-cancer and anti-angiogenic effects. These novel compounds effectively inhibit tumor cell proliferation and angiogenesis, unlike thalidomide itself.

Area of Science:

  • Oncology
  • Pharmacology
  • Cell Biology

Background:

  • Inhibition of angiogenesis is a key cancer treatment strategy.
  • Thalidomide's anti-angiogenic properties have spurred research into its analogs.
  • Understanding the mechanisms of anti-angiogenesis is crucial for developing new cancer therapies.

Purpose of the Study:

  • To investigate the anti-proliferative and anti-angiogenic activities of two thalidomide dithiocarbamate analogs.
  • To assess the effects of these analogs on cytokine and matrix metalloproteinase expression.
  • To compare the efficacy of the analogs with thalidomide in cancer models.

Main Methods:

  • Assessed anti-proliferative effects on HUVECs and MDA-MB-231 cells.
  • Evaluated angiogenesis via wound healing, migration, tube formation, and nitric oxide assays.
  • Measured expression levels of IL-6, IL-8, TNF-α, VEGF165, and MMP-2.

Main Results:

  • Thalidomide showed no significant anti-proliferative or anti-angiogenic effects at tested concentrations.
  • Thalidomide dithiocarbamate analogs exhibited potent anti-proliferative and anti-angiogenic activities without cytotoxicity.
  • Analogs suppressed key inflammatory cytokines and MMP-2 expression more effectively than thalidomide, with Analog 1 showing highest potency.

Conclusions:

  • Thalidomide dithiocarbamate analogs possess significant anti-tumor and anti-angiogenic potential.
  • These novel analogs represent promising candidates for further development as cancer therapeutics.
  • Analog 1 demonstrated superior efficacy, warranting further investigation for clinical applications.
Keywords:
AngiogenesisMigrationNOThalidomide dithiocarbamate analogsVEGF

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