Novel Low-Toxic Derivative of Celastrol Maintains Protective Effect against Acute Renal Injury.

Published on Mar 6, 2018
· DOI :10.1021/ACSOMEGA.7B01890
Xun Hu2
Estimated H-index: 2
(Sichuan University),
Mengdi Jia5
Estimated H-index: 5
(Sichuan University)
+ 3 AuthorsQing Lin12
Estimated H-index: 12
(Sichuan University)
Sources
Abstract
: This study aimed to novelly design and synthesize an amide derivative as a potential substitute of celastrol (CLT). We constituted the compound celastrol-glucosamine (CLG) by conjugating 1-(2-aminoethoxy)-2-glucosamine to celastrol (CLT) and confirmed its chemical structure by 1H NMR, 13C NMR, and LC-MS/MS. Then, the potential efficacy of the CLG was investigated on renal ischemia-reperfusion injury animal models. The results demonstrated that the decorated compound CLG could completely reverse the disease progression as same as CLT. Furthermore, the toxicity of CLG was also fully evaluated in rat blood, liver, kidney, heart, spleen, lung, and reproductive system. Compared to the performance of CLT on normal organs, CLG could remarkably maintain high safety and significantly reduce the side effects. Taken together, the CLG could keep the same efficacy as CLT while processing lower toxicity in vivo.
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