Anticancer Activity of Euplotin C, Isolated from the Marine Ciliate Euplotes crassus , Against Human Melanoma Cells

Marine Drugs
Sara CarpiGraziano Di Giuseppe

Abstract

Cutaneous melanoma is the most serious type of skin cancer, so new cytotoxic weapons against novel targets in melanoma are of great interest. Euplotin C (EC), a cytotoxic secondary metabolite of the marine ciliate Euplotes crassus, was evaluated in the present study on human cutaneous melanoma cells to explore its anti-melanoma activity and to gain more insight into its mechanism of action. EC exerted a marked cytotoxic effect against three different human melanoma cell lines (A375, 501Mel and MeWo) with a potency about 30-fold higher than that observed in non-cancer cells (HDFa cells). A pro-apoptotic activity and a decrease in melanoma cell migration by EC were also observed. At the molecular level, the inhibition of the Erk and Akt pathways, which control many aspects of melanoma aggressiveness, was shown. EC cytotoxicity was antagonized by dantrolene, a ryanodine receptor (RyR) antagonist, in a concentration-dependent manner. A role of RyR as a direct target of EC was also suggested by molecular modelling studies. In conclusion, our data provide the first evidence of the anti-melanoma activity of EC, suggesting it may be a promising new scaffold for the development of selective activators of RyR to be used for the treatment...Continue Reading

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Citations

Nov 21, 2019·Expert Review of Molecular Diagnostics·Sara CarpiPaola Nieri
Oct 20, 2018·International Journal of Oncology·George Mihai NitulescuDenisa Margina
Oct 20, 2019·Nutrients·Egeria ScodittiRaffaele De Caterina
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Feb 16, 2021·Bioorganic & Medicinal Chemistry·Wen-Yu LuYan-Chao Wu
Aug 10, 2020·Biomedicine & Pharmacotherapy = Biomédecine & Pharmacothérapie·Jiaen WeiZunnan Huang

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Methods Mentioned

BETA
light microscopy
NMR
ELISA
electrophoresis
PCR

Software Mentioned

GraphPad
AUTODOCK
ImageJ
ImageJ64
AUTODOCK4
SANDER
Macromodel
GraphPad Prism
MOLSURF
Maestro

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