Autor: |
Lemos, Larissa Maria Scalon, Ọlọ́ba-Whẹ̀nù, Oluwakemi Adekunbi, Olasupo, Idris Abiodun, Balogun, Sikiru Olaitan, Macho, Antonio, Pavan, Eduarda, de Oliveira Martins, Domingos Tabajara |
Zdroj: |
Journal of Biomolecular Structure and Dynamics; January 2025, Vol. 43 Issue: 1 p197-210, 14p |
Abstrakt: |
AbstractBrasiliensic acid (Bras) is a chromanone isolated from Calophyllum brasilienseCambèss. bark extracts with confirmed potential activity on gastric ulcer and Helicobacter pyloriinfection. This study aimed to investigate the in vitroand in vivotoxicity of Bras and molecular docking studies on its interactions with the H. pylori virulence factors and selected gastric cancer-related proteins. Cytotoxicity was evaluated by alamarBlue© assay, genotoxicity by micronucleus and comet assays, and on cell cycle by flow cytometry, using Chinese hamster epithelial ovary cells. Bras was not cytotoxic to CHO-K1 cells, and caused no chromosomal aberrations, nor altered DNA integrity. Furthermore, Bras inhibited damages to DNA by H2O2at 1.16 µM. No cell cycle arrest was observed, but apoptosis accounted for 31.2% of the cell death observed in the CHO-K1 at 24 h incubation of the IC50. Oral acute toxicity by Hippocratic screening test in mice showed no relevant behavioral change/mortality seen up to 1,000 mg/kg. The molecular docking approach indicated potential interactions between Bras and the various targets for peptic ulcer and gastric cancer, notably CagA virulence factor of H. pyloriand VEGFR-2. In conclusion, Bras is apparently safe and an optimization for Bras can be considered for gastric ulcer and cancer.Communicated by Ramaswamy H. Sarma |
Databáze: |
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