Restoring chemo-sensitivity to temozolomide via targeted inhibition of poly (ADP-ribose) polymerase-1 by naringin in glioblastoma

نویسندگان

چکیده

Abstract Inclining mortality with a constant plummet in the survival rates associated glioblastoma still stands as an inveterate predicament. The only promising therapy temozolomide (TMZ) is now side-lined due to escalated resistance mediated by Poly (ADP-ribose) Polymerase-1 (PARP-1). In light of this, very study was designed evaluate potential active phyto component named naringin, inhibiting PARP-1, using silico and vitro methods. Under settings, inhibitor bound crystal structure i.e., 4UND retrieved molecular docking studies were performed against naringin Schrodinger software. cytotoxicity apoptotic detection assay C6 glioma cells. Docking revealed high affinity low binding energy at inhibition site good stability. An increase cells observed TMZ combination when compared alone. Isobologram plot confirmed synergistic effect drug combination. A significant number drugs, evaluated acridine orange ethidium bromide staining reassured reversal resistance. conclusion, chemosensitivity restored successful PARP-1 hence proven effective reversing

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ژورنال

عنوان ژورنال: Chemical Papers

سال: 2021

ISSN: ['1336-9075', '2585-7290', '0366-6352']

DOI: https://doi.org/10.1007/s11696-021-01700-0