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Chem Biol Interact ; 333: 109316, 2021 Jan 05.
Artículo en Inglés | MEDLINE | ID: mdl-33285127

RESUMEN

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-3ß kinases in vitro and its binding affinities were mapped through the intermolecular interactions with each target in silico.


Asunto(s)
Antineoplásicos/farmacología , Neoplasias Colorrectales/patología , Nigericina/farmacología , Inhibidores de Proteínas Quinasas/farmacología , Streptomyces/química , Antineoplásicos/química , Antineoplásicos/metabolismo , Apoptosis/efectos de los fármacos , Dominio Catalítico , Línea Celular Tumoral , Humanos , Janus Quinasa 3/antagonistas & inhibidores , Janus Quinasa 3/química , Janus Quinasa 3/metabolismo , Simulación del Acoplamiento Molecular , Nigericina/química , Nigericina/metabolismo , Inhibidores de Proteínas Quinasas/química , Inhibidores de Proteínas Quinasas/metabolismo
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