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Santi MD, Peralta MA, Puiatti M, et al. Melanogenic inhibitory effects of Triangularin in B16F0 melanoma cells, in vitro and molecular docking studies. Bioorg Med Chem. 2019;27(16):3722-3728doi: 10.1016/j.bmc.2019.06.041.
Santi, M. D., Peralta, M. A., Puiatti, M., Cabrera, J. L., & Ortega, M. G. (2019). Melanogenic inhibitory effects of Triangularin in B16F0 melanoma cells, in vitro and molecular docking studies. Bioorganic & medicinal chemistry, 27(16), 3722-3728. https://doi.org/10.1016/j.bmc.2019.06.041
Santi, María D, et al. "Melanogenic inhibitory effects of Triangularin in B16F0 melanoma cells, in vitro and molecular docking studies." Bioorganic & medicinal chemistry vol. 27,16 (2019): 3722-3728. doi: https://doi.org/10.1016/j.bmc.2019.06.041
Santi MD, Peralta MA, Puiatti M, Cabrera JL, Ortega MG. Melanogenic inhibitory effects of Triangularin in B16F0 melanoma cells, in vitro and molecular docking studies. Bioorg Med Chem. 2019 Aug 15;27(16):3722-3728. doi: 10.1016/j.bmc.2019.06.041. Epub 2019 Jun 27. PMID: 31272835.
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Bioorg Med Chem. 2019 Aug 15;27(16):3722-3728. doi: 10.1016/j.bmc.2019.06.041. Epub 2019 Jun 27.

Melanogenic inhibitory effects of Triangularin in B16F0 melanoma cells, in vitro and molecular docking studies.

Bioorganic & medicinal chemistry

María D Santi, Mariana A Peralta, Marcelo Puiatti, José Luis Cabrera, María G Ortega

Affiliations

  1. Farmacognosia, Departamento de Ciencias Farmacéuticas, Facultad de Ciencias Químicas, Universidad Nacional de Córdoba, Ciudad Universitaria, Haya de la torre y Medina Allende, Edificio Ciencias II, X5000HUA Córdoba, Argentina; Instituto Multidisciplinario de Biología Vegetal (IMBIV-CONICET), Ciudad Universitaria, X5000HUA Córdoba, Argentina.
  2. Instituto de Investigaciones en Físico-Química de Córdoba (INFIQC), Departamento de Química Orgánica, Facultad de Ciencias Químicas, Universidad Nacional de Córdoba, Ciudad Universitaria, Haya de la torre y Medina Allende, Edificio Ciencias II, X5000HUA Córdoba, Argentina.
  3. Farmacognosia, Departamento de Ciencias Farmacéuticas, Facultad de Ciencias Químicas, Universidad Nacional de Córdoba, Ciudad Universitaria, Haya de la torre y Medina Allende, Edificio Ciencias II, X5000HUA Córdoba, Argentina; Instituto Multidisciplinario de Biología Vegetal (IMBIV-CONICET), Ciudad Universitaria, X5000HUA Córdoba, Argentina. Electronic address: [email protected].

PMID: 31272835 DOI: 10.1016/j.bmc.2019.06.041

Abstract

The lack of secure therapies for hyperpigmentation disorders, without serious adverse effects, and the latest reports relating melanogenic disorders with development of neurodegenerative diseases, encourage the continuing search for new drugs for the treatment of such disorders. In this sense, the plant kingdom is an important source of bioactive natural products with great potential for the research and development of new therapeutics. The present study evaluated the anti-melanogenic activity of the natural methoxylated chalcone, 2',6'-dihydroxy-4'-methoxy-3'-methylchalcone (Triangularin, T), on diphenolase activity from mushroom tyrosinase and on murine B16F0 melanoma cell model. In addition, molecular modelling studies were carried out in order to understand the inhibitory activity observed. T showed a potent anti-melanogenic activity being more active than kojic acid (KA) on tyrosinase isolated of both sources and on intracellular tyrosinase. Molecular docking studies displayed important interactions between T and the active site of tyrosinase. Our results suggest that T may be useful for the treatment of hyperpigmentary disorders.

Copyright © 2019 Elsevier Ltd. All rights reserved.

Keywords: Anti-melanogenic activity; Dalea elegans; Molecular modelling studies; Triangularin

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