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1.
PPAR Res ; 2021: 8854921, 2021.
Artigo em Inglês | MEDLINE | ID: mdl-33790957

RESUMO

Controlling the inflammatory response to restore tissue homeostasis is a crucial step to maintain tooth vitality after pathogen removal from caries-affected dental tissues. The nuclear peroxisome proliferator-activated receptor beta/delta (PPARß/δ) is a ligand-activated transcription factor with emerging anti-inflammatory roles in many cells and tissues. However, its expression and functions are poorly understood in human dental pulp cells (hDPCs). Thus, this study evaluated PPARß/δ expression and assessed the anti-inflammatory effects evoked by activation of PPARß/δ in lipopolysaccharide- (LPS-) induced hDPCs. Our results showed that hDPCs constitutively expressed PPARß/δ mRNA/protein, and treatment with LPS increased PPARß/δ mRNA expression. The selective PPARß/δ agonist GW0742 significantly decreased inflammation-related mRNA expression in hDPCs (IL6, IL1ß, TNFα, MMP1, and MMP2) and RAW264.7 cells (Il6 and Tnfα). Further, PPARß/δ agonist attenuated MMP2/9 gelatinolytic activity in hDPCs. Previously LPS-conditioned hDPCs increased the migration of RAW264.7 cells through the membrane of a Transwell coculture system. Conversely, pretreatment with GW0742 markedly decreased macrophage recruitment. These findings provide among the first evidence that hDPCs express PPARß/δ. In addition, they suggest that activation of PPARß/δ by GW0742 can attenuate some cellular and molecular in vitro aspects related to the inflammatory process, pointing out to investigate its potential target role in dental pulp inflammation.

2.
Int J Pharm ; 328(2): 183-90, 2007 Jan 10.
Artigo em Inglês | MEDLINE | ID: mdl-16959452

RESUMO

Recently, it was demonstrated that two different formulations containing quercetin inhibit the UVB-induced cutaneous oxidative stress and inflammation. Therefore, in the present study it was evaluated the functional stability of those formulations by the antioxidant activity, the release of quercetin from the formulations, and its skin retention using modified Franz diffusion cells. Both formulations tested ((1) non-ionic emulsion with high lipid content and (2) anionic emulsion with low lipid content) remained functionally (hydrogen-donating ability) stable during 180 days. Furthermore, quercetin was released from both formulations as determined using nitrocellulose membrane. In vitro antioxidant activity of retained quercetin into the skin was observed for both formulations as detected by the inhibition of malondialdehyde formation. The effect of quercetin retention was time-dependent for formulation 1. Concluding, this study demonstrates that quercetin remains functionally stable in formulations, and measuring the antioxidant activity is an efficient approach to evaluate quercetin skin retention with minimal interference of the tissue products. Furthermore, the present results on skin retention explain the previous study on quercetin in vivo activities, and together, these data suggest that formulations containing quercetin may be used as topical active products to control UVB-mediated oxidative damage of the skin.


Assuntos
Antioxidantes/química , Antioxidantes/metabolismo , Quercetina/química , Quercetina/metabolismo , Pele/metabolismo , Administração Cutânea , Animais , Compostos de Bifenilo , Estabilidade de Medicamentos , Excipientes/química , Radicais Livres/química , Técnicas In Vitro , Picratos/química , Polissorbatos/química , Absorção Cutânea , Solubilidade , Suínos
3.
J Pharm Biomed Anal ; 32(1): 97-105, 2003 Apr 24.
Artigo em Inglês | MEDLINE | ID: mdl-12852452

RESUMO

Three different topical formulations were supplemented with superoxide dismutase (SOD) and evaluated concerning physical and chemical stabilities in order to determine the most stable formulation that would maintain SOD activity. Physical stability was evaluated by storing the formulation at room temperature, and at 37 and 45 degrees C for 28 days. Samples were collected at 7-day intervals for assessment of rheological behavior. Chemical stability was evaluated by the measurement of enzymatic activity in formulations stored at room temperature and at 45 degrees C for 75 days. The formulations showed a pseudoplastic behavior, with a flow index of less than 1. There was no significant difference in the initial values of flow index, hysteresis loop or minimum apparent viscosity. The simple emulsion and the one stabilized with hydroxyethylcellulose showed decreased viscosity by the 21st day and with higher temperature, but no significant changes concerning the presence of SOD. Although there were no significant changes concerning storage time or temperature, the formulation stabilized with hydroxyethylcellulose showed a marked loss of SOD activity. The addition of SOD to the formulations studied did not affect their physical stability. Simple emulsions or emulsions stabilized with carboxypolymethylene seem to be better bases for enzyme addition than emulsion stabilized with hydroxyethylcellulose.


Assuntos
Anti-Inflamatórios/química , Superóxido Dismutase/química , Administração Tópica , Anti-Inflamatórios/análise , Estabilidade de Medicamentos , Emulsões/química , Estabilidade Enzimática , Reprodutibilidade dos Testes , Reologia , Sensibilidade e Especificidade , Superóxido Dismutase/análise , Fatores de Tempo , Viscosidade
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