Guttiferone E Displays Antineoplastic Activity Against Melanoma Cells

Autor(es)

Ribeiro, Arthur Barcelos ; Nicolella, Heloiza Diniz ; Domingos da Silva, Lucas Henrique ; Aldana Mejia, Jennyfer Andrea ; Tanimoto, Matheus Hikaru ; Ambrosio, Sergio Ricardo ; Bastos, Jairo Kenupp ; Orenha, Renato Pereira ; Tame Parreira, Renato Luis ; Tavares, Denise Crispim

• Tipo de documento: Artigo Científico
• Fonte: Planta Medica; v. N/A, p. 10-pg., 2022-09-28.

Resumo

Guttiferone E (GE) is a benzophenone found in Brazilian red propolis. In the present study, the effect of GE on human (A375) and murine (B16-F10) melanoma cells was investigated. GE significantly reduced the cellular viability of melanoma cells in a time-dependent manner. In addition, GE demonstrated antiproliferative effect, with IC50 values equivalent to 9.0 and 6.6 mu M for A-375 and B16-F10 cells, respectively. The treatment of A-375 cells with GE significantly increased cell populations in G0/G1 phase and decreased those in G2/M phase. Conversely, on B16-F10 cells, GE led to a significant decrease in the populations of cells in G0/G1 phase and concomitantly an increase in the population of cells in phase S. A significantly higher percentage of apoptotic cells was observed in A-375 (43.5%) and B16-F10 (49.9%) cultures after treatment with GE. Treatments with GE caused morphological changes and significant decrease to the melanoma cells' density. GE (10 mu M) inhibited the migration of melanoma cells, with a higher rate of inhibition in B16-F10 cells (73.4%) observed. In addition, GE significantly reduced the adhesion of A375 cells, but showed no effect on B16-F10. Treatment with GE did not induce changes in P53 levels in A375 cultures. Molecular docking calculations showed that GE is stable in the active sites of the tubulin dimer with a similar energy to taxol chemotherapy. Taken together, the data suggest that GE has promising antineoplastic potential against melanoma. (AU)

• Processo FAPESP: 18/25770-7 - Estudos in vitro, in vivo e in silico da atividade antineoplásica da gutiferona e em melanoma
• Beneficiário: Arthur Barcelos Ribeiro
• Modalidade de apoio: Bolsas no Brasil - Mestrado
• Processo FAPESP: 17/04138-8 - Realização de estudos químicos, analíticos, biológicos, farmacológicos e tecnológicos para preenchimento das lacunas no desenvolvimento do setor de própolis brasileiro
• Beneficiário: Jairo Kenupp Bastos
• Modalidade de apoio: Auxílio à Pesquisa - Temático