Antitumor activity of Tigerinin-1: Necroptosis mediates toxicity in A549 cells
Anet Antony1, Shilpa Olakkaran1, Anupama Kizhakke Purayil1
1Department of Zoology, School of Biological Sciences, Central University of Kerala, Tejaswini Hills, Periya 671 320, Kasaragod, India.
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.
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