Streptomyces hygroscopicus UFPEDA 3370: A valuable source of the potent cytotoxic agent nigericin and its evaluation against human colorectal cancer cells

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 mu M, (30.0) and 0.0138 mu M (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-3 beta kinases in vitro and its binding affinities were mapped through the intermolecular interactions with each target in silico.

Automated summary

The study demonstrated cytotoxic activity of Nigericin against several cancer cell lines, especially HL-60 and HCT-116. Nigericin induced apoptosis and autophagy in HCT-116 cells. Additionally, Nigericin was able to inhibit JAK3 and GSK-3 beta kinases in vitro and its binding affinities were mapped through intermolecular interactions with each target in silico.