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    Streptomyces hygroscopicus UFPEDA 3370 was fermented in submerged cultivation and the biomass extract was partitioned, obtaining a fraction purified named EB1. After purification of EB1 fraction, nigericin free acid was obtained and identified. Nigericin presented cytotoxic activity against several cancer cell lines, being most active against HL-60 (human leukemia) and HCT-116 (human colon carcinoma) cell lines, presenting IC50 and (IS) values: 0.0014 μM, (30.0) and 0.0138 μM (3.0), respectively. On HCT-116, nigericin caused apoptosis and autophagy. In this study, nigericin was also screened both in vitro and in silico against a panel of cancer-related kinases. Nigericin was able to inhibit both JAK3 and GSK-3β kinases in vitro and its binding affinities were mapped through the intermolecular interactions with each target in silico. Copyright © 2020. Published by Elsevier B.V.


    Iza Mirela Rodini Garcia-Princival, Jefferson Luiz Princival, Emmanuel Dias da Silva, Sandrine Maria de Arruda Lima, Jhonattas Carvalho Carregosa, Alberto Wisniewski, Caio Cézar Oliveira de Lucena, Fernando Halwass, José Adonias Alves Franca, Luiz Felipe Gomes Rebello Ferreira, Marcelo Zaldini Hernandes, Karina Lidianne Alcântara Saraiva, Christina Alves Peixoto, Blandine Baratte, Thomas Robert, Stéphane Bach, Dayene Correia Gomes, Patricia Maria Guedes Paiva, Pascal Marchand, Maria do Desterro Rodrigues, Teresinha Gonçalves da Silva. Streptomyces hygroscopicus UFPEDA 3370: A valuable source of the potent cytotoxic agent nigericin and its evaluation against human colorectal cancer cells. Chemico-biological interactions. 2021 Jan 05;333:109316

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    PMID: 33285127

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