Inhibitory Effects of Resveratrol Analogs on Mushroom Tyrosinase Activity
Autor: | Adilson David da Silva, Paula Rafaela Rocha, Nádia Rezende Barbosa Raposo, Raquel Teixeira, Danielle Cristina Zimmermann Franco, Gustavo S.G. de Carvalho |
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Jazyk: | angličtina |
Rok vydání: | 2012 |
Předmět: |
structure-activity
Tyrosinase Pharmaceutical Science tyrosinase Resveratrol Article Analytical Chemistry lcsh:QD241-441 Melanin Hydroxylation chemistry.chemical_compound Skin Pigmentation Disorder lcsh:Organic chemistry Stilbenes Drug Discovery Molecular modification medicine Enzyme Inhibitors Physical and Theoretical Chemistry integumentary system Monophenol Monooxygenase Chemistry Organic Chemistry Skin whitening Hyperpigmentation chemical synthesis mushroom tyrosinase activity activity in vitro Enzyme Activation Biochemistry Chemistry (miscellaneous) Molecular Medicine medicine.symptom Agaricales |
Zdroj: | Molecules; Volume 17; Issue 10; Pages: 11816-11825 Molecules, Vol 17, Iss 10, Pp 11816-11825 (2012) Molecules |
ISSN: | 1420-3049 |
DOI: | 10.3390/molecules171011816 |
Popis: | Skin pigmentation disorders typically involve an overproduction or uneven distribution of melanin, which results in skin spots. Resveratrol can inhibit tyrosinase, the active enzyme in the synthesis of melanin, but it does not inhibit the synthesis of melanin to an extent that enables its use alone as a skin whitening agent in pharmaceutical formulations, so its use as a coadjuvant in treatment of hyperpigmentation is suggested. Six resveratrol analogs were tested for tyrosinase inhibitory activity in vitro. Among the analogs tested, compound D was the most powerful tyrosinase inhibitor (IC50 = 28.66 µg/mL), two times more active than resveratrol (IC50 = 57.05 µg/mL), followed by the analogs A, E, B, F and C, respectively. This demonstrated that the hydroxylation at C4' on the phenolic ring was the molecular modification with most importance for the observed activity. |
Databáze: | OpenAIRE |
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