FLAVONOIDS ISOLATED FROM DALEA ELEGANS INHIBIT MELANOGENESIS IN MOUSE B16 MELANOMA CELLS

SANTI, MARIA D.; PERALTA, MARIANA A.; CABRERA, JOSE L.; ORTEGA, M. GABRIELA

Mar del Plata

Congreso; XLVIII ANNUAL MEETING ARGENTINE SOCIETY OF EXPERIMENTAL PHARMACOLOGY (SAFE); 2016

Sociedad Argentina de Farmacología Experimental (SAFE)

FLAVONOIDS ISOLATED FROM DALEA ELEGANS INHIBIT MELANOGENESIS IN MOUSEB16MELANOMA CELLSMARÍA DANIELA SANTI,MARIANA PERALTA, JOSÉ LUIS CABRERA, MARÍA GABRIELA ORTEGAFacultadde Ciencias Químicas,Universidad Nacional de Córdoba,IMBIV-CONICET,ArgentinaTyrosinaseinhibitor compounds have importance in thetreatmentof hyperpigmentation diseases and are usedaswhiteners agents in cosmetics. Several currently marketedwhitenershave adverse effects; for example Kojicacid(KA) is genotoxic, hepatocarcinogenic and producesdermatitis.For this reason is important the researching fornewinhibitors of tyrosinase. Previously we have reportedanimportant inhibitory activity on mushroom tyrosinaseby a prenylated flavanone (8PP) and achalcone (Triangularin)isolatedfrom roots and aerial parts of DaleaelegansGillies ex Hook. & Arn. In order to investigatethiscondition in cell line, we evaluate the melanogenesisinhibitionof these compounds on mouse B16 melanomacellsthrough the tyrosinase intracelular inhibition and theextracelularmelanin inhibition by spectrophotometricallymeasuringof the adduct formation between 3-methyl-2-benzothiazolinoneand dopaquinona. The cytotoxicityassay was performedby MTT methodology. The maximumnon-cytotoxicconcentration (MNCC) for 8PP, TriangularinandKA were of 10 μM, 100 μM and 5000 μM, respectivelyandaccording with these results we evaluated themelanogenesisinhibition. The results demonstrated thatthesecompounds have the ability to penetrate the membraneofB16 cells and inhibit the tyrosinase intracelularatnon-cytotoxic concentrations. Comparing the inhibition%of each compound with reference inhibitor KA,8PPand Triangularin would be two hundred-fold andFive-fold more active than KA, respectively.In addition,ithas been observed that these compounds decreasedextracellularmelanin. The 50 % of inhibition for 8PP andTriangularinwere 1 and 25 μM, respectively. For KA, the50% of inhibition was 2000 μM. So, 8PP and Triangularinwouldbe two thousand and eighty-fold more active thanKA,respectively. It would be needed PCR and Westernblotstudies to establish the mechanisms by which thesecompounds act onmelanin biosynthesis.