Antitumor activity of Tigerinin-1: Necroptosis mediates toxicity in A549 cells.
Anti-angiogenesis
Anticancer peptides
Cytotoxicity
Human cancer cell lines
Necroptosis
Tigerinin-1
Journal
Biochimica et biophysica acta. General subjects
ISSN: 1872-8006
Titre abrégé: Biochim Biophys Acta Gen Subj
Pays: Netherlands
ID NLM: 101731726
Informations de publication
Date de publication:
09 2022
09 2022
Historique:
received:
08
04
2022
revised:
20
05
2022
accepted:
24
05
2022
pubmed:
1
6
2022
medline:
22
6
2022
entrez:
31
5
2022
Statut:
ppublish
Résumé
Tigerinins are antimicrobial peptides (AMPs) derived from the skin secretions of the Indian bullfrog Hoplobatrachus tigerinus. Tigerinin-1 (FCTMIPIPRCY-Am) peptide was synthesized by solid-phase Fmoc chemistry and investigated its antitumor activities. Tigerinin-1 was cytotoxic to human cancer cells. It causes necrosis by damaging the cell membrane and loss of lysosome integrity. Tigerinin-1triggers the expression of necroptosis pathway proteins. It generates reactive oxygen species (ROS) and induces oxidative stress-mediated genotoxicity. Tigerinin-1 inhibits cancer cell proliferation, reduces neovascularization, and down-regulates the vascular endothelial growth factor (VEGF), vascular endothelial growth factor receptor 2 (VEGFR2), and fibroblast growth factor (FGF) genes. Tigerinin-1 exhibited its potent antitumor properties in this study. Tigerinin-1 can be beneficial for developing novel therapeutics for cancer.
Sections du résumé
BACKGROUND
Tigerinins are antimicrobial peptides (AMPs) derived from the skin secretions of the Indian bullfrog Hoplobatrachus tigerinus.
METHODS
Tigerinin-1 (FCTMIPIPRCY-Am) peptide was synthesized by solid-phase Fmoc chemistry and investigated its antitumor activities.
RESULTS
Tigerinin-1 was cytotoxic to human cancer cells. It causes necrosis by damaging the cell membrane and loss of lysosome integrity. Tigerinin-1triggers the expression of necroptosis pathway proteins. It generates reactive oxygen species (ROS) and induces oxidative stress-mediated genotoxicity. Tigerinin-1 inhibits cancer cell proliferation, reduces neovascularization, and down-regulates the vascular endothelial growth factor (VEGF), vascular endothelial growth factor receptor 2 (VEGFR2), and fibroblast growth factor (FGF) genes.
CONCLUSIONS
Tigerinin-1 exhibited its potent antitumor properties in this study.
GENERAL SIGNIFICANCE
Tigerinin-1 can be beneficial for developing novel therapeutics for cancer.
Identifiants
pubmed: 35636711
pii: S0304-4165(22)00100-3
doi: 10.1016/j.bbagen.2022.130182
pii:
doi:
Substances chimiques
Antimicrobial Cationic Peptides
0
Vascular Endothelial Growth Factor A
0
tigerinin 1
0
Types de publication
Journal Article
Research Support, Non-U.S. Gov't
Langues
eng
Sous-ensembles de citation
IM
Pagination
130182Informations de copyright
Copyright © 2022 Elsevier B.V. All rights reserved.