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

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 signif

SUBMITTER: Hu X 

PROVIDER: S-EPMC6045326 | biostudies-literature | 2018 Mar

REPOSITORIES: biostudies-literature