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1.
Molecules ; 17(10): 11816-25, 2012 Oct 09.
Artículo en Inglés | MEDLINE | ID: mdl-23047482

RESUMEN

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 (IC(50) = 28.66 µg/mL), two times more active than resveratrol (IC(50) = 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.


Asunto(s)
Agaricales/enzimología , Inhibidores Enzimáticos/farmacología , Monofenol Monooxigenasa/antagonistas & inhibidores , Estilbenos/farmacología , Activación Enzimática/efectos de los fármacos , Inhibidores Enzimáticos/química , Monofenol Monooxigenasa/metabolismo , Resveratrol , Estilbenos/química
2.
Braz. j. pharm. sci ; 48(3): 399-404, July-Sept. 2012. graf, tab
Artículo en Inglés | LILACS | ID: lil-653453

RESUMEN

In order to treat hyperpigmentation-related problems, there has been a global trend in developing cosmetics claiming to have skin-whitening properties, which act by inhibiting melanin biosynthesis. The objective of this work was to evaluate the in vitro mushroom tyrosinase inhibitory activity of five Amazonian native flora oils, and so to verify the possibility of their incorporation into cosmetic products. In addition, the fatty acid composition of the essential oils was determined by gas chromatography-flame ionisation detection in order to determine the main components of these oils. The tyrosinase inhibitory activity of the tested oils was found to be in the following order: açaí (IA50 = 66.08 µg mL-1) > tucumã > patauá > pracaxi > castanha do Brasil. This study suggests that açaí oil has great potential in the treatment of hyperpigmentation and other related disorders, due to its considerable tyrosinase inhibitory activity.


Com o intuito de se tratar problemas dermatológicos de hiperpigmentação, há uma tendência mundial no desenvolvimento de cosméticos que possuam propriedades despigmentantes, os quais agem inibindo a biossíntese de melanina. O objetivo deste trabalho foi avaliar in vitro a atividade de inibição da tirosinase de cogumelo de cinco óleos de plantas nativas da Amazônia e, desta forma, verificar a possibilidade de sua incorporação em produtos cosméticos. Ainda, a composição de ácidos graxos dos óleos foi determinada por cromatografia gasosa com detecção por ionização de chama, no intuito de determinar os principais componentes destes óleos. A atividade de inibição da tirosinase dos óleos testados foi encontrada na seguinte ordem: açaí (IA50 = 66,08 µg mL-1) > tucumã > patauá > pracaxi > castanha do Brasil. Este estudo sugere que o óleo de açaí possui grande potencial para o tratamento da hiperpigmentação cutânea e doenças correlatas, devido à sua considerável atividade de inibição da tirosinase.


Asunto(s)
Aceites de Plantas/análisis , Ecosistema Amazónico/clasificación , Agaricales/clasificación , Técnicas In Vitro/instrumentación , Monofenol Monooxigenasa/farmacología , Hiperpigmentación/prevención & control , Blanqueadores/farmacocinética , Melaninas/farmacocinética
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