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https://www.arca.fiocruz.br/handle/icict/57724
STREPTOMYCES HYGROSCOPICUS UFPEDA 3370: A VALUABLE SOURCE OF THE POTENT CYTOTOXIC AGENT NIGERICIN AND ITS EVALUATION AGAINST HUMAN COLORECTAL CANCER CELLS
Autor(es)
Afiliação
Fundação Oswaldo Cruz, Instituto Aggeu Magalhães, Laboratório de Ultraestrutura, Recife, PE, Brazil.
Universidade Federal de Pernambuco, Departamento de Antibióticos, Recife, Pernambuco, Brasil.
Universidade Federal de Pernambuco, Departamento de Química Fundamental, Recife, Pernambuco, Brasil.
Universidade Federal de Sergipe, Departamento de Química, Aracaju, Sergipe, Brasil.
Universidade Federal de Pernambuco, Departamento de Ciências Farmacêuticas, Laboratório de Química Teórica Medicinal (LQTM), Recife, PE, Brazil.
Instituto de Ciências e Tecnologia em Neuroimunomodulação (INCT-NIM)
Universidade Federal de Pernambuco, Departamento de Bioquímica, Recife, Pernambuco, Brasil.
Universite de Nantes, Cibles et médicaments des infections et du cancer, IICiMed, EA 1155, Nantes, F-44000, France.
Universidade Federal de Pernambuco, Departamento de Antibióticos, Recife, Pernambuco, Brasil.
Sorbonne Université, CNRS, UMR8227, Integrative Biology of Marine Models Laboratory (LBI2M), Station Biologique de Roscoff, F-29680, Roscoff, France; Sorbonne Université, CNRS, FR2424, Kinase Inhibitor Specialized Screening Facility - KISSf, Station Biologique, F-29688, Roscoff, France. Electronic address: baratte@sb-roscoff.fr.
Sorbonne Université, CNRS, UMR8227, Integrative Biology of Marine Models Laboratory (LBI2M), Station Biologique de Roscoff, F-29680, Roscoff, France; Sorbonne Université, CNRS, FR2424, Kinase Inhibitor Specialized Screening Facility - KISSf, Station Biologique, F-29688, Roscoff, France.
Sorbonne Université, CNRS, UMR8227, Integrative Biology of Marine Models Laboratory (LBI2M), Station Biologique de Roscoff, F-29680, Roscoff, France; Sorbonne Université, CNRS, FR2424, Kinase Inhibitor Specialized Screening Facility - KISSf, Station Biologique, F-29688, Roscoff, France.
Resumo em Inglês
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.
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