Antitumor activity of Tigerinin-1: Necroptosis mediates toxicity in A549 cells.

Autor: Antony A; Department of Zoology, School of Biological Sciences, Central University of Kerala, Tejaswini Hills, Periya 671 320, Kasaragod, India., Olakkaran S; Department of Zoology, School of Biological Sciences, Central University of Kerala, Tejaswini Hills, Periya 671 320, Kasaragod, India., Purayil AK; Department of Zoology, School of Biological Sciences, Central University of Kerala, Tejaswini Hills, Periya 671 320, Kasaragod, India., Shekh S; Department of Chemistry, School of Chemical Sciences, Central University of Karnataka, Kalaburagi 585 367, Karnataka, India., Gowd KH; Department of Chemistry, School of Chemical Sciences, Central University of Karnataka, Kalaburagi 585 367, Karnataka, India., Gurushankara HP; Department of Zoology, School of Biological Sciences, Central University of Kerala, Tejaswini Hills, Periya 671 320, Kasaragod, India. Electronic address: gurushankara@cukerala.ac.in.
Jazyk: angličtina
Zdroj: Biochimica et biophysica acta. General subjects [Biochim Biophys Acta Gen Subj] 2022 Sep; Vol. 1866 (9), pp. 130182. Date of Electronic Publication: 2022 May 28.
DOI: 10.1016/j.bbagen.2022.130182
Abstrakt: 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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Databáze: MEDLINE