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1.
Molecules ; 18(1): 178-89, 2012 Dec 24.
Artigo em Inglês | MEDLINE | ID: mdl-23262447

RESUMO

4-nerolidylcatechol (4-NC) is an unstable natural product that exhibits important antioxidant, anti-inflammatory and other properties. It is readily obtainable on a multi-gram scale through straightforward solvent extraction of the roots of cultivated Piper peltatum or P. umbellatum, followed by column chromatography on the resulting extract. Semi-synthetic derivatives of 4-NC with one or two substituent groups (methyl, acetyl, benzyl, benzoyl) on the O atoms have been introduced that have increased stability compared to 4-NC and significant in vitro inhibitory activity against the human malaria parasite Plasmodium falciparum. Antioxidant and anti-inflammatory properties may be important for the antiplasmodial mode of action of 4-NC derivatives. Thus, we decided to investigate the antioxidant properties, cytotoxicity and stability of 4-NC derivatives as a means to explore the potential utility of these compounds. 4-NC showed high antioxidant activity in the DPPH and ABTS assays and in 3T3-L1 cells (mouse embryonic fibroblast), however 4-NC was more cytotoxic (IC50 = 31.4 µM) and more unstable than its derivatives and lost more than 80% of its antioxidant activity upon storage in solution at -20 °C for 30 days. DMSO solutions of mono-O-substituted derivatives of 4-NC exhibited antioxidant activity and radical scavenging activity in the DPPH and ABTS assays that was comparable to that of BHA and BHT. In the cell-based antioxidant model, most DMSO solutions of derivatives of 4-NC were less active on day 1 than 4-NC, quercetin and BHA and more active antioxidants than BHT. After storage for 30 days at -20 °C, DMSO solutions of most of the derivatives of 4-NC were more stable and exhibited more antioxidant activity than 4-NC, quercetin and BHA and exhibited comparable antioxidant activity to BHT. These findings point to the potential of derivatives of 4-NC as antioxidant compounds.


Assuntos
Antimaláricos/farmacologia , Antioxidantes/farmacologia , Catecóis/química , Catecóis/farmacologia , Piper/química , Células 3T3-L1 , Animais , Antimaláricos/química , Antioxidantes/química , Hidroxianisol Butilado/química , Hidroxianisol Butilado/farmacologia , Hidroxitolueno Butilado/química , Hidroxitolueno Butilado/farmacologia , Sobrevivência Celular/efeitos dos fármacos , Concentração Inibidora 50 , Malária/tratamento farmacológico , Camundongos , Dinâmica não Linear , Raízes de Plantas/química , Plasmodium falciparum/efeitos dos fármacos , Plasmodium falciparum/crescimento & desenvolvimento
2.
Acta Cir Bras ; 29(4): 280-6, 2014 Apr.
Artigo em Inglês | MEDLINE | ID: mdl-24760030

RESUMO

PURPOSE: To investigate the effects of occupational exposure to waste anesthetic gases on genetic material and antioxidant status in professionals during their medical residency. METHODS: The study group consisted of 15 medical residents from Anesthesiology and Surgery areas, of both genders, mainly exposed to isoflurane and to a lesser degree to sevoflurane and nitrous oxide; the control group consisted of 15 young adults not exposed to anesthetics. Blood samples were drawn from professionals during medical residency (eight, 16 and 22 months of exposure to waste anesthetic gases). DNA damage was evaluated by comet assay, and antioxidant defense was assessed by total thiols and the enzymes glutathione peroxidase (GPX), superoxide dismutase (SOD) and catalase (CAT). RESULTS: When comparing the two groups, DNA damage was significantly increased at all time points evaluated in the exposed group; plasma thiols increased at 22 months of exposure and GPX was higher at 16 and 22 months of exposure. CONCLUSION: Young professionals exposed to waste anesthetic gases in operating rooms without adequate scavenging system have increased DNA damage and changes in redox status during medical residency. There is a need to minimize exposure to inhalation anesthetics and to provide better work conditions.


Assuntos
Anestésicos Inalatórios/toxicidade , Antioxidantes/análise , Dano ao DNA , Internato e Residência/estatística & dados numéricos , Exposição Ocupacional/efeitos adversos , Adulto , Análise de Variância , Catalase/sangue , Feminino , Glutationa Peroxidase/sangue , Humanos , Isoflurano/toxicidade , Masculino , Óxido Nitroso/toxicidade , Salas Cirúrgicas , Estresse Oxidativo , Compostos de Sulfidrila/sangue , Superóxido Dismutase/sangue , Fatores de Tempo
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