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Chem Biol Interact. 2016 Dec 25;260:141-153. doi: 10.1016/j.cbi.2016.11.010. Epub 2016 Nov 10.

Modulatory effects of new curcumin analogues on gamma-irradiation - Induced nephrotoxicity in rats.

Author information

1
Drug Radiation Research Department, National Center for Radiation Research and Technology (NCRRT), Egyptian Atomic Energy Authority (EAEA), P.O. Box: 29, Nasr City, Cairo, Egypt. Electronic address: afmismail@gmail.com.
2
Drug Radiation Research Department, National Center for Radiation Research and Technology (NCRRT), Egyptian Atomic Energy Authority (EAEA), P.O. Box: 29, Nasr City, Cairo, Egypt.

Abstract

In the present study, a new series of 2-amino-pyran-3-carbonitrile derivatives of curcumin 2-7 have been synthesized via one-pot simple and efficient protocol, involving the reaction of curcumin 1 with substituted-benzylidene-malononitrile to modify the 1,3-diketone moiety. The structures of the synthesized compounds 2-7 were elucidated by microanalytical and spectral data, which were found consistent with the assigned structures. The nephroprotective mechanism of these new curcumin analogues was evaluated on the post-gamma-irradiation (7 Gy) - induced nephrotoxicity in rats. Activation of Nrf2 by these curcumin analogues is responsible for the amendment of the antioxidant status, impairment of NF-κB signal, thus attenuate the nephrotoxicity induced post-γ-irradiation exposure. 4-Chloro-phenyl curcumin analogue 7 showed the most potent activity. In conclusion, the results of the present study demonstrate a promising role of these new curcumin analogues to attenuate the early symptoms of nephrotoxicity induced by γ-irradiation in rats via activation of Nrf2 gene expression. These new curcumin analogues need further toxicological investigations to assess their therapeutic index.

KEYWORDS:

Antioxidant; Curcumin analogues; Gamma-radiation; Nephrotoxicity; Nuclear Factor Erythroid-related Factor-2

PMID:
27838230
DOI:
10.1016/j.cbi.2016.11.010
[Indexed for MEDLINE]

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