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| Content Provider | World Health Organization (WHO)-Global Index Medicus |
|---|---|
| Author | Campos, Patrícia Mazureki Prudente, Arthur Silveira Horinouchi, Cíntia Delai da Silva Cechinel-Filho, Valdir Fávero, Giovani Marino Cabrini, Daniela Almeida Otuki, Michel Fleith |
| Description | Country affiliation: Brazil Author Affiliation: Campos PM ( Department of Pharmaceutical Sciences, Federal University of Parana, CEP 80210-170, Curitiba, PR, Brazil.); Prudente AS ( Department of Pharmacology, Federal University of Parana, CEP 81530-900, Curitiba, PR, Brazil.); Horinouchi CD ( Department of Pharmacology, Federal University of Parana, CEP 81530-900, Curitiba, PR, Brazil.); Cechinel-Filho V ( Investigation Centre of Pharmaceutical Chemistry, University of Itajai Valley, CEP 88302-202, Itajai, SC, Brazil.); Fávero GM ( Department of Biological Sciences, State University of Ponta Grossa, CEP 84030-900, Ponta Grossa, PR, Brazil.); Cabrini DA ( Department of Pharmacology, Federal University of Parana, CEP 81530-900, Curitiba, PR, Brazil.); Otuki MF ( Department of Pharmacology, Federal University of Parana, CEP 81530-900, Curitiba, PR, Brazil. Electronic address: michelotuki@yahoo.com.br.) |
| Abstract | ETHNOPHARMACOLOGY RELEVANCE: GB-2a is a I3-naringenin-II8-eriodictyol compound isolated from Garcinia gardneriana (Planchon & Triana) Zappi, a plant used in folk medicine for the treatment of skin disorders. AIM OF STUDY: In the search for new depigmenting agents, this study was carried out to investigate the in vitro effects of GB-2a isolated from G. gardneriana (Planchon & Triana) Zappi in B16F10 melanoma cells. MATERIALS AND METHODS: The effects of GB-2a were evaluated through determination of melanin biosynthesis in B16F10 melanoma cells in comparison with the reference drug kojic acid (500µM). In parallel, the GB-2a effect was assessed in a cell viability assay. Mushroom tyrosinase activity assays were conducted to verify the effect of this enzyme. In order to ascertain the nature of enzyme inhibition on tyrosinase, kinetics analysis of the GB-2a was performed with L-tyrosine and L-3,4-dihydroxyphenylalanine (L-DOPA) substrates. RESULTS: The results showed that GB-2a biflavonoid significantly inhibited the melanin content, without reducing cell viability. GB-2a also showed a strong antityrosinase activity in the mushroom tyrosinase assay. GB-2a inhibited the tyrosinase activity, exerting a mixed inhibition. For the L-tyrosine substrate the inhibition was in non-competitive mode and for L-DOPA it was in uncompetitive mode. CONCLUSION: GB-2a biflavonoid promoted inhibition on tyrosinase activity and reduced melanin biosynthesis in B16F10 cells, which suggests great potential for medical and cosmetic uses as a depigmenting agent. |
| File Format | HTM / HTML |
| ISSN | 03788741 |
| Volume Number | 174 |
| e-ISSN | 18727573 |
| Journal | Journal of Ethnopharmacology |
| Language | English |
| Publisher | Elsevier |
| Publisher Date | 2015-11-04 |
| Publisher Place | Ireland |
| Access Restriction | One Nation One Subscription (ONOS) |
| Subject Keyword | Discipline Ethnopharmacology Flavanones Therapeutic Use Garcinia Melanins Antagonists & Inhibitors Melanoma, Experimental Drug Therapy Plant Extracts Plant Leaves Animals Cell Survival Drug Effects Physiology Dose-response Relationship, Drug Isolation & Purification Pharmacology Metabolism Mice Journal Article Research Support, Non-u.s. Gov't |
| Content Type | Text |
| Resource Type | Article |
| Subject | Drug Discovery Pharmacology |
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