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首页> 外文期刊>Chemico-biological interactions >Modulatory effects of new curcumin analogues on gamma-irradiation - Induced nephrotoxicity in rats
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Modulatory effects of new curcumin analogues on gamma-irradiation - Induced nephrotoxicity in rats

机译：新姜黄素类似物对γ射线辐射诱导的大鼠肾毒性的调节作用

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摘要

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-kappa B signal, thus attenuate the nephrotoxicity induced post-gamma-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 gamma-irradiation in rats via activation of Nrf2 gene expression. These new curcumin analogues need further toxicological investigations to assess their therapeutic index. (C) 2016 Elsevier Ireland Ltd. All rights reserved.
机译：在本研究中，通过一锅简单而有效的方法合成了一系列新的姜黄素2-7的2-氨基-吡喃-3-甲腈衍生物，涉及姜黄素1与取代的亚苄基-丙二腈的反应1,3-二酮部分。通过微观分析和光谱数据阐明了合成的化合物2-7的结构，发现其与指定的结构一致。这些新姜黄素类似物的肾保护机制是在γ射线辐照后（7 Gy）诱导的大鼠肾毒性中评估的。这些姜黄素类似物对Nrf2的激活负责抗氧化剂状态的修正，NF-κB信号的损伤，从而减弱了γ-射线照射后引起的肾毒性。 4-氯苯基姜黄素类似物7显示出最有效的活性。总之，本研究的结果表明，这些新的姜黄素类似物通过激活Nrf2基因表达，可减轻由γ射线照射引起的大鼠肾毒性的早期症状。这些新的姜黄素类似物需要进一步的毒理学研究，以评估其治疗指数。 （C）2016 Elsevier Ireland Ltd.保留所有权利。

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