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Furan inhibitory activity against tyrosinase and impact on B16F10 cell toxicity

Marcela Rodrigues Barros1, Thaís Meira Menezes1, Lucas Pereira da Silva1

  • 1Laboratório de Química Biológica, Departamento de Química Fundamental, Universidade Federal de Pernambuco, Recife 50670-901, PE, Brazil.

International Journal of Biological Macromolecules
|June 25, 2019
PubMed

Insights

Carboxyl-furan derivatives show potent competitive inhibition of mushroom tyrosinase (mTYR). These compounds also exhibit differential toxicity against melanoma cells, suggesting a link between tyrosinase inhibition and anticancer effects.

Area of Science:

  • Biochemistry
  • Enzymology
  • Dermatology

Background:

  • Tyrosinase activity is crucial in melanogenesis and linked to skin disorders.
  • Understanding tyrosinase inhibition is vital for melanoma treatment.
  • Numerous inhibitors exist, but their impact on melanoma cell viability requires further study.

Purpose of the Study:

  • To evaluate the inhibitory effects of furan derivatives on mushroom tyrosinase (mTYR).
  • To investigate the mechanism of inhibition (competitive/non-competitive, reversible/irreversible).
  • To assess the impact of these derivatives on melanoma cell viability.

Main Methods:

  • Spectroscopic techniques
  • Kinetic assays
  • Theoretical calculations
  • Cell viability assays (B16F10 melanoma cells)

Main Results:

  • All tested furan derivatives inhibited mTYR activity.
  • Carboxyl-furan derivatives (F3, F4) were more effective inhibitors than keto-derivatives (F1, F2).
  • Inhibition by carboxyl-furans was competitive and reversible.
  • Furan derivatives displayed differential toxicity against B16F10 melanoma cells.

Conclusions:

  • Furan derivatives, particularly carboxyl-furans, are effective competitive inhibitors of mushroom tyrosinase.
  • The observed toxicity of furan derivatives towards melanoma cells may be linked to their tyrosinase inhibitory properties.
  • These findings suggest potential therapeutic applications for furan derivatives in skin conditions and melanoma.
Keywords:
FuranInhibitionMelanomaSpectroscopyTyrosinase

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