Cargando…
Novel Low-Toxic Derivative of Celastrol Maintains Protective Effect against Acute Renal Injury
[Image: see text] 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 (1)H...
Autores principales: | , , , , , |
---|---|
Formato: | Online Artículo Texto |
Lenguaje: | English |
Publicado: |
American Chemical Society
2018
|
Acceso en línea: | https://www.ncbi.nlm.nih.gov/pmc/articles/PMC6045326/ https://www.ncbi.nlm.nih.gov/pubmed/30023844 http://dx.doi.org/10.1021/acsomega.7b01890 |
_version_ | 1783339644065153024 |
---|---|
author | Hu, Xun Jia, Mengdi Fu, Yu Zhang, Pei Zhang, Zhirong Lin, Qing |
author_facet | Hu, Xun Jia, Mengdi Fu, Yu Zhang, Pei Zhang, Zhirong Lin, Qing |
author_sort | Hu, Xun |
collection | PubMed |
description | [Image: see text] 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 (1)H NMR, (13)C 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. |
format | Online Article Text |
id | pubmed-6045326 |
institution | National Center for Biotechnology Information |
language | English |
publishDate | 2018 |
publisher | American Chemical Society |
record_format | MEDLINE/PubMed |
spelling | pubmed-60453262018-07-16 Novel Low-Toxic Derivative of Celastrol Maintains Protective Effect against Acute Renal Injury Hu, Xun Jia, Mengdi Fu, Yu Zhang, Pei Zhang, Zhirong Lin, Qing ACS Omega [Image: see text] 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 (1)H NMR, (13)C 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. American Chemical Society 2018-03-06 /pmc/articles/PMC6045326/ /pubmed/30023844 http://dx.doi.org/10.1021/acsomega.7b01890 Text en Copyright © 2018 American Chemical Society This is an open access article published under a Creative Commons Non-Commercial No Derivative Works (CC-BY-NC-ND) Attribution License (http://pubs.acs.org/page/policy/authorchoice_ccbyncnd_termsofuse.html) , which permits copying and redistribution of the article, and creation of adaptations, all for non-commercial purposes. |
spellingShingle | Hu, Xun Jia, Mengdi Fu, Yu Zhang, Pei Zhang, Zhirong Lin, Qing Novel Low-Toxic Derivative of Celastrol Maintains Protective Effect against Acute Renal Injury |
title | Novel Low-Toxic Derivative of Celastrol Maintains
Protective Effect against Acute Renal Injury |
title_full | Novel Low-Toxic Derivative of Celastrol Maintains
Protective Effect against Acute Renal Injury |
title_fullStr | Novel Low-Toxic Derivative of Celastrol Maintains
Protective Effect against Acute Renal Injury |
title_full_unstemmed | Novel Low-Toxic Derivative of Celastrol Maintains
Protective Effect against Acute Renal Injury |
title_short | Novel Low-Toxic Derivative of Celastrol Maintains
Protective Effect against Acute Renal Injury |
title_sort | novel low-toxic derivative of celastrol maintains
protective effect against acute renal injury |
url | https://www.ncbi.nlm.nih.gov/pmc/articles/PMC6045326/ https://www.ncbi.nlm.nih.gov/pubmed/30023844 http://dx.doi.org/10.1021/acsomega.7b01890 |
work_keys_str_mv | AT huxun novellowtoxicderivativeofcelastrolmaintainsprotectiveeffectagainstacuterenalinjury AT jiamengdi novellowtoxicderivativeofcelastrolmaintainsprotectiveeffectagainstacuterenalinjury AT fuyu novellowtoxicderivativeofcelastrolmaintainsprotectiveeffectagainstacuterenalinjury AT zhangpei novellowtoxicderivativeofcelastrolmaintainsprotectiveeffectagainstacuterenalinjury AT zhangzhirong novellowtoxicderivativeofcelastrolmaintainsprotectiveeffectagainstacuterenalinjury AT linqing novellowtoxicderivativeofcelastrolmaintainsprotectiveeffectagainstacuterenalinjury |