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Article

Anticancer and Immunomodulatory Activities of a Novel Water-Soluble Derivative of Ellipticine

1
Programa de Pós-Graduação em Hematologia, Universidade do Estado do Amazonas, Av. Djalma Batista, 3578-Flores, Manaus-AM, Brazil
2
Instituto Nacional de Pesquisas da Amazônia, Av. André Araújo, 2.936-Petrópolis-Manaus-AM, Brazil
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Institute of Organic Chemistry, National Academy of Sciences of Ukraine, Murmanska Str. 5, 02660 Kyiv, Ukraine
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JSC “Farmak”, Kyrylivska str. 63, 04080 Kyiv, Ukraine
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Department of Chemistry, University of Helsinki, 00014 Helsinki, Finland
*
Author to whom correspondence should be addressed.
Molecules 2020, 25(9), 2130; https://doi.org/10.3390/molecules25092130
Received: 23 March 2020 / Revised: 21 April 2020 / Accepted: 22 April 2020 / Published: 1 May 2020
(This article belongs to the Section Medicinal Chemistry)
Cancer still remains a major public health concern around the world and the search for new potential antitumor molecules is essential for fighting the disease. This study evaluated the anticancer and immunomodulatory potential of the newly synthetized ellipticine derivate: sodium bromo-5,11-dimethyl-6H-pyrido[4,3-b]carbazole-7-sulfonate (Br-Ell-SO3Na). It was prepared by the chlorosulfonation of 9-bromoellipticine. The ellipticine-7-sulfonic acid itself is not soluble, but its saponification with sodium hydroxide afforded a water-soluble sodium salt. The cytotoxicity of Br-Ell-SO3Na was tested against cancerous (K562 cell line) and non-cancerous cells (Vero cell line and human peripheral blood mononuclear cells (PBMC)) using a Methylthiazoletetrazolium (MTT) assay. Cell cycle arrest was assessed by flow cytometry and the immunomodulatory activity was analyzed through an enzyme-linked immunosorbent assay (ELISA). The results showed that the Br-Ell-SO3Na molecule has specific anticancer activity (IC50 = 35 µM) against the K562 cell line, once no cytotoxicity effect was verified against non-cancerous cells. Cell cycle analysis demonstrated that K562 cells treated with Br-Ell-SO3Na were arrested in the phase S. Moreover, the production of IL-6 increased and the expression of IL-8 was inhibited in the human PBMC treated with Br-Ell-SO3Na. The results demonstrated that Br-Ell-SO3Na is a promising anticancer molecule attested by its noteworthy activity against the K562 tumor cell line and immunomodulatory activity in human PBMC cells. View Full-Text
Keywords: ellipticine; 9-bromoellipticine; sodium 9-bromo-5,11-dimethyl-6H-pyrido[4,3-b]carbazole-7-sulfonate; immunomodulation; antitumor molecule ellipticine; 9-bromoellipticine; sodium 9-bromo-5,11-dimethyl-6H-pyrido[4,3-b]carbazole-7-sulfonate; immunomodulation; antitumor molecule
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MDPI and ACS Style

Costa de Oliveira, R.; Soares Pontes, G.; Kostyuk, A.; Coutinho Camargo, G.B.; Dhyani, A.; Shvydenko, T.; Shvydenko, K.; Grafov, A. Anticancer and Immunomodulatory Activities of a Novel Water-Soluble Derivative of Ellipticine. Molecules 2020, 25, 2130. https://doi.org/10.3390/molecules25092130

AMA Style

Costa de Oliveira R, Soares Pontes G, Kostyuk A, Coutinho Camargo GB, Dhyani A, Shvydenko T, Shvydenko K, Grafov A. Anticancer and Immunomodulatory Activities of a Novel Water-Soluble Derivative of Ellipticine. Molecules. 2020; 25(9):2130. https://doi.org/10.3390/molecules25092130

Chicago/Turabian Style

Costa de Oliveira, Regiane, Gemilson Soares Pontes, Aleksandr Kostyuk, Gabriel B. Coutinho Camargo, Anamika Dhyani, Tetiana Shvydenko, Kostiantyn Shvydenko, and Andriy Grafov. 2020. "Anticancer and Immunomodulatory Activities of a Novel Water-Soluble Derivative of Ellipticine" Molecules 25, no. 9: 2130. https://doi.org/10.3390/molecules25092130

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