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Kojic Acid Showed Consistent Inhibitory Activity on Tyrosinase from Mushroom and in Cultured B16F10 Cells Compared with Arbutins

Summary

This study compared four skin-whitening compounds to find the best one for use as a testing standard in laboratories. Kojic acid was found to be the most reliable choice because it effectively blocks the enzyme tyrosinase, which produces skin pigment, without damaging cells. The researchers tested these compounds both in test tubes and in actual melanoma cells to understand how they work differently.

Background

Tyrosinase inhibitors are important for preventing excessive melanin synthesis and enzymatic browning. Kojic acid and arbutins (α-arbutin, β-arbutin, deoxyarbutin) are commonly used as positive controls in tyrosinase inhibition studies, but contradictory results exist regarding their efficacy and inhibition mechanisms.

Objective

To compare the inhibitory activities and mechanisms of kojic acid, α-arbutin, β-arbutin, and deoxyarbutin on mushroom tyrosinase monophenolase and diphenolase activities, and to evaluate their effects on B16F10 melanoma cells to identify the most suitable positive control compound.

Results

Kojic acid competitively inhibited monophenolase and showed mixed-type inhibition on diphenolase. α-arbutin and β-arbutin inhibited monophenolase but activated diphenolase. Deoxyarbutin only extended lag time for monophenolase but competitively inhibited diphenolase. In cells, kojic acid inhibited tyrosinase activity and reduced melanin without affecting cell viability at tested concentrations.

Conclusion

Kojic acid is the most suitable positive control among the four compounds as it consistently inhibits both monophenolase and diphenolase activities of mushroom tyrosinase and reduces cellular melanin content without cytotoxicity. The study provides explanations for contradictory results in literature and highlights the importance of using consistent experimental conditions when comparing tyrosinase inhibitors.
  • Published in:Antioxidants (Basel),
  • Study Type:Experimental Study,
  • Source: PMC8944748, PMID: 35326152, DOI: 10.3390/antiox11030502
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