» Articles » PMID: 36170858

Guttiferone E Displays Antineoplastic Activity Against Melanoma Cells

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 IC 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 cells' 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.

Citing Articles

Antitumor Potential of Guttiferone E Combined With Carboplatin Against Osimertinib-resistant H1975 Lung Cancer Through Apoptosis.

Nathani A, Khan I, Tanimoto M, Mejia J, DE Miranda A, Rishi A Anticancer Res. 2024; 44(10):4175-4188.

PMID: 39348999 PMC: 11863775. DOI: 10.21873/anticanres.17248.


Efficacy and safety of guttiferone E in melanoma-bearing mice.

Ribeiro A, de Melo M, de Melo Junqueira M, Rodrigues M, de Souza T, Fernandes G Naunyn Schmiedebergs Arch Pharmacol. 2024; 397(7):5265-5274.

PMID: 38270618 DOI: 10.1007/s00210-024-02962-7.


Ruthenium(II) complex with 2-mercaptothiazoline ligand induces selective cytotoxicity involving DNA damage and apoptosis in melanoma cells.

de Melo M, Ribeiro A, Fernandes G, Squarisi I, de Melo Junqueira M, Batista A J Biol Inorg Chem. 2024; 29(1):159-168.

PMID: 38182820 DOI: 10.1007/s00775-023-02036-8.


ZFP57 promotes ovarian cancer progression by transcriptionally regulating BRCA1 and managing G1 checkpoint.

Fan W, Xiong R, Zhou Z, Zhang C, Han Y, Shi T J Cancer. 2023; 14(11):2039-2050.

PMID: 37497403 PMC: 10367923. DOI: 10.7150/jca.84601.