In vitro Antitumor Activity and Electrochemical Studies of Bio-Electroactive Anthraquinone Derivatives in Glioblastoma

This study investigated the antiglioblastoma potential of nine synthetic anthraquinone derivatives (SAQDs). SAQDs were tested for their in vitro cytotoxicity against PBMCs and GBM02 cells. For PBMC, SAQDs showed no cytotoxic effects up to 100 µM. Four most promising SAQDs (1, 4, 5, and 9) demonstrated significant activity against GBM02, with selectivity index >4.54 for 1, >1.30 for 4 and 5, and >1.19 for 9. These compounds induced morphological changes, incluing cell rounding, cytoplasmic vacuolation, and membrane rupture, and inhibited cell migration. Due to the pharmacological role of oxidative stress, electrochemical methods were used to compare the reductive and oxidative capacities of the SAQD with their antitumor activity. Considering the reported findings, it is feasible to confirm that some SAQDs have antitumor effects, supporting additional studies of AQ for developing novel anticancer medications. Due to the small number of compounds investigated, it was not possible to observe a relationship between electrochemical and biological data. However, the electrochemical data are new and could be used to prepare other compounds on this line. CV data revealed that the sulfone's electron-withdrawing effect facilitated the reduction. At the same time, the sulfides had shown less positive potential for oxidation waves due to the presence of electron-donating groups.

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Publication Details

Journal
Anais da Academia Brasileira de Ciências
Published
2025-01-01
DOI
https://doi.org/10.1590/0001-3765202520241466
Citations
1
Primary Topic
Bioactive Compounds and Antitumor Agents
Type
article
Field-Weighted Citation Impact
1.31

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article

In vitro Antitumor Activity and Electrochemical Studies of Bio-Electroactive Anthraquinone Derivatives in Glioblastoma

João Kaycke Sarmento da Silva, Vivaldo Moura‐Neto, Andresa K. A. de Almeida, Tamires A. do Nascimento et al.
1 citations
Anais da Academia Brasileira de Ciências
Bioactive Compounds and Antitumor Agents
1.31
article

In vitro Antitumor Activity and Electrochemical Studies of Bio-Electroactive Anthraquinone Derivatives in Glioblastoma

João Kaycke Sarmento da Silva, Vivaldo Moura‐Neto, Andresa K. A. de Almeida, Tamires A. do Nascimento, Marília Oliveira Fonseca Goulart, João Xavier de Araújo‐Júnior, Alysson Wagner Fernandes Duarte, Renata G. Almeida, Guilherme A. M. Jardim, Joice Fragoso Oliveira de Araujo, Magna Suzana Alexandre‐Moreira, Eufrânio N. da Silva Júnior, Aline Cavalcanti de Queiroz, Suellen Maria Albuquerque da Silva, Andressa Letícia Lopes da Silva, Pierre Barnabé Escodro, André F. A. Xavier
article en
1 citations

Abstract

This study investigated the antiglioblastoma potential of nine synthetic anthraquinone derivatives (SAQDs). SAQDs were tested for their in vitro cytotoxicity against PBMCs and GBM02 cells. For PBMC, SAQDs showed no cytotoxic effects up to 100 µM. Four most promising SAQDs (1, 4, 5, and 9) demonstrated significant activity against GBM02, with selectivity index >4.54 for 1, >1.30 for 4 and 5, and >1.19 for 9. These compounds induced morphological changes, incluing cell rounding, cytoplasmic vacuolation, and membrane rupture, and inhibited cell migration. Due to the pharmacological role of oxidative stress, electrochemical methods were used to compare the reductive and oxidative capacities of the SAQD with their antitumor activity. Considering the reported findings, it is feasible to confirm that some SAQDs have antitumor effects, supporting additional studies of AQ for developing novel anticancer medications. Due to the small number of compounds investigated, it was not possible to observe a relationship between electrochemical and biological data. However, the electrochemical data are new and could be used to prepare other compounds on this line. CV data revealed that the sulfone's electron-withdrawing effect facilitated the reduction. At the same time, the sulfides had shown less positive potential for oxidation waves due to the presence of electron-donating groups.

Anais da Academia Brasileira de CiênciasVol. 97(3)
Universidade Federal de Minas Gerais (BR), Instituto Estadual do Cérebro Paulo Niemeyer (BR), Universidade Federal de Alagoas (BR)
Coordenação de Aperfeiçoamento de Pessoal de Nível Superior, Fundação de Amparo à Pesquisa do Estado de Alagoas, Conselho Nacional de Desenvolvimento Científico e Tecnológico, Fundação de Amparo à Pesquisa do Estado de Minas Gerais, Instituto Nacional de Ciência e Tecnologia de Fármacos e Medicamentos
Openalex Percentile: Top 22%
Bioactive Compounds and Antitumor Agents
1.31
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