Streptomyces hygroscopicus UFPEDA 3370: A valuable source of the potent cytotoxic agent nigericin and its evaluation against human colorectal cancer cells.
Chem Biol Interact
; 333: 109316, 2021 Jan 05.
Article
in En
| MEDLINE
| ID: mdl-33285127
ABSTRACT
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.
Key words
Full text:
1
Database:
MEDLINE
Main subject:
Streptomyces
/
Colorectal Neoplasms
/
Protein Kinase Inhibitors
/
Nigericin
/
Antineoplastic Agents
Limits:
Humans
Language:
En
Year:
2021
Type:
Article