Planta Med 2023; 89(02): 158-167
DOI: 10.1055/a-1890-5446
Biological and Pharmacological Activity
Original Papers

Guttiferone E Displays Antineoplastic Activity Against Melanoma Cells

Arthur Barcelos Ribeiro
1   University of Franca, Avenida Dr. Armando Salles Oliveira, Franca, São Paulo, Brazil
,
Heloiza Diniz Nicolella
1   University of Franca, Avenida Dr. Armando Salles Oliveira, Franca, São Paulo, Brazil
,
1   University of Franca, Avenida Dr. Armando Salles Oliveira, Franca, São Paulo, Brazil
,
Jennyfer Andrea Aldana Mejía
2   School of Pharmaceutical Sciences of Ribeirão Preto, University of São Paulo, Ribeirão Preto, São Paulo, Brazil
,
Matheus Hikaru Tanimoto
2   School of Pharmaceutical Sciences of Ribeirão Preto, University of São Paulo, Ribeirão Preto, São Paulo, Brazil
,
Sérgio Ricardo Ambrósio
1   University of Franca, Avenida Dr. Armando Salles Oliveira, Franca, São Paulo, Brazil
,
Jairo Kenupp Bastos
2   School of Pharmaceutical Sciences of Ribeirão Preto, University of São Paulo, Ribeirão Preto, São Paulo, Brazil
,
Renato Pereira Orenha
1   University of Franca, Avenida Dr. Armando Salles Oliveira, Franca, São Paulo, Brazil
,
Renato Luis Tame Parreira
1   University of Franca, Avenida Dr. Armando Salles Oliveira, Franca, São Paulo, Brazil
,
1   University of Franca, Avenida Dr. Armando Salles Oliveira, Franca, São Paulo, Brazil
› Institutsangaben

Gefördert durch: Fundação de Amparo à Pesquisa do Estado de São Paulo #2017/04138-8 Gefördert durch: Fundação de Amparo à Pesquisa do Estado de São Paulo #2018/25770-7
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Abstract

Guttiferone E (GE) is a benzophenone found in Brazilian red propolis. In the present study, the effect of GE on human (A-375) 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 µM 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 cellsʼ density. GE (10 µM) 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.

Supporting Information



Publikationsverlauf

Eingereicht: 28. Januar 2022

Angenommen nach Revision: 10. Juni 2022

Artikel online veröffentlicht:
28. September 2022

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