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Open Access 01-12-2021 | Melanoma | Research

Anti-proliferative and pro-apoptotic activity of glycosidic derivatives of lawsone in melanoma cancer cell

Authors: Mariana Nobre Farias de Franca, Raquel Geralda Isidório, João Henrique Oliveira Bonifacio, Edmilson Willian Propheta dos Santos, Jileno Ferreira Santos, Flaviano Melo Ottoni, Waldecy de Lucca Junior, Ricardo Scher, Ricardo José Alves, Cristiane Bani Corrêa

Published in: BMC Cancer | Issue 1/2021

Abstract

Background

Melanoma is a malignant cancer that affects melanocytes and is considered the most aggressive skin-type cancer. The prevalence for melanoma cancer for the last five year is about one million cases. The impact caused of this and other types of cancer, revel the importance of research into potential active compounds. The natural products are an important source of compounds with biological activity and research with natural products may enable the discovery of compounds with potential activity in tumor cells.

Methods

The Sulforhodamine B was used to determine cell density after treatment with lawsone derivatives. Apoptosis and necrosis were analyzed by flow cytometer. Morphological changes were observed by fluorescence using the Phalloidin/FITC and DAPI stains. The clonogenic and wound healing assays were used to analyze reduction of colonies formation and migratory capacity of melanoma cells, respectability.

Results

In pharmacological screening, seven compounds derived from lawsone were considered to have high cytotoxic activity (GI > 75%). Three compounds were selected to assess the inhibitory concentration for 50% of cells (IC₅₀), and the compound 9, that has IC₅₀ 5.3 μM in melanoma cells, was selected for further analyses in this cell line. The clonogenic assay showed that the compound is capable of reducing the formation of melanoma colonies at 10.6 μM concentration. The compound induced apoptotic morphological changes in melanoma cells and increased by 50% the cells dying from apoptosis. Also, this compound reduced the migratory capacity of melanoma cells.

Conclusions

The results of this study showed that the evaluated lawsone derivatives have potential activity on tumor cells. The compound 9 is capable of inducing cell death by apoptosis in melanoma cells (B16F10).

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Title: Anti-proliferative and pro-apoptotic activity of glycosidic derivatives of lawsone in melanoma cancer cell
Authors: Mariana Nobre Farias de Franca
Raquel Geralda Isidório
João Henrique Oliveira Bonifacio
Edmilson Willian Propheta dos Santos
Jileno Ferreira Santos
Flaviano Melo Ottoni
Waldecy de Lucca Junior
Ricardo Scher
Ricardo José Alves
Cristiane Bani Corrêa
Publication date: 01-12-2021
Publisher: BioMed Central
Keywords: Melanoma
Melanoma
Published in: BMC Cancer / Issue 1/2021
Electronic ISSN: 1471-2407
DOI: https://doi.org/10.1186/s12885-021-08404-4

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