radioprotectors
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The increasing risk of radiation exposure underlines the need for novel radioprotective agents. Hence, a series of novel 1-(2-hydroxyethyl)piperazine derivatives were designed and synthesized. Some of the compounds protected human cells against radiation-induced apoptosis and exhibited low cytotoxicity. Compared to the previous series of piperazine derivatives, compound 8 exhibited a radioprotective effect on cell survival in vitro and low toxicity in vivo. It also enhanced the survival of mice 30 days after whole-body irradiation (although this increase was not statistically significant). Taken together, our in vitro and in vivo data indicate that some of our compounds are valuable for further research as potential radioprotectors.
- MeSH
- analýza přežití MeSH
- ionizující záření MeSH
- lidé MeSH
- maximální tolerovaná dávka MeSH
- molekulární konformace MeSH
- molekulární modely MeSH
- molekulární struktura MeSH
- nádorové buněčné linie MeSH
- piperaziny aplikace a dávkování škodlivé účinky chemie farmakologie MeSH
- radioprotektivní látky aplikace a dávkování škodlivé účinky chemie farmakologie MeSH
- viabilita buněk účinky léků účinky záření MeSH
- vztah mezi dávkou a účinkem léčiva MeSH
- vztahy mezi strukturou a aktivitou MeSH
- Check Tag
- lidé MeSH
- Publikační typ
- časopisecké články MeSH
The goal of combined pharmacological approaches in the treatment of the acute radiation syndrome (ARS) is to obtain an effective therapy producing a minimum of undesirable side effects. This review summarizes important data from studies evaluating the efficacy of combining radioprotective agents developed for administration prior to irradiation and therapeutic agents administered in a post-irradiation treatment regimen. Many of the evaluated results show additivity, or even synergism, of the combined treatments in comparison with the effects of the individual component administrations. It can be deduced from these findings that the research in which combined treatments with radioprotectors/radiomitigators are explored, tested, and evaluated is well-founded. The requirement for studies highly emphasizing the need to minimize undesirable side effects of the radioprotective/radiomitigating therapies is stressed.
- MeSH
- akutní radiační syndrom farmakoterapie metabolismus patofyziologie prevence a kontrola MeSH
- amifostin terapeutické užití MeSH
- dinoproston terapeutické užití MeSH
- experimentální radiační poranění farmakoterapie metabolismus patofyziologie MeSH
- faktor stimulující kolonie granulocytů terapeutické užití MeSH
- fixní kombinace léků MeSH
- lidé MeSH
- metformin terapeutické užití MeSH
- misoprostol terapeutické užití MeSH
- radioprotektivní látky terapeutické užití MeSH
- rozvrh dávkování léků MeSH
- synergismus léků MeSH
- vitamin E terapeutické užití MeSH
- zvířata MeSH
- Check Tag
- lidé MeSH
- zvířata MeSH
- Publikační typ
- časopisecké články MeSH
- přehledy MeSH
Fullerenol C60(OH)24 nanoparticles (FNP) are promising radioprotectors in prevention of early and late ionizing radiation injury. The aim of this study was to compare the efficacy of FNP and amifostine (AMI) in protection of rats exposed to whole-body X-ray irradiation (7 or 8 Gy). Both compounds (FNP, 100 mg/kg ip; AMI, 300 mg/kg ip) were given 30 min before irradiation throughout the study. The general radioprotective efficacy of FNP and AMI were evaluated in rats irradiated with an absolutely lethal dose of X-rays (8 Gy) and their survival were monitored during the period of 30 days after irradiation. Both compounds were of comparable efficacy. Tissue-protective effects of tested compounds were assessed in rats irradiated with an sublethal dose of X-rays (7 Gy). For this purpose, the animals were sacrificed on the 7th and 28th day after irradiation. Their lung, heart, liver, kidney, small intestine and spleen were taken for histopathological and semiquantitative analysis. Careful examination of established tissue and vascular alteration revealed better radioprotective effects of FNP compared to those of AMI on the small intestine, lung and spleen, while AMI had better radioprotective effects than FNP in protection of the heart, liver and kidney. Results of this study confirmed high radioprotective efficacy of FNP in irradiated rats that was comparable to that of AMI, a well-known radioprotector.
- MeSH
- amifostin farmakologie terapeutické užití MeSH
- dávka záření MeSH
- experimentální radiační poranění terapie MeSH
- fullereny terapeutické užití MeSH
- LD50 MeSH
- modely u zvířat MeSH
- nanočástice terapeutické užití MeSH
- nanotrubičky MeSH
- potkani Wistar MeSH
- radiační ochrana MeSH
- radiační poranění patologie MeSH
- radioprotektivní látky MeSH
- zvířata MeSH
- Check Tag
- mužské pohlaví MeSH
- zvířata MeSH
- Publikační typ
- práce podpořená grantem MeSH
