RESUMO
Rapanea ferruginea antioxidant and antitumoral properties were not explored before in literature. This study aimed to investigate these biological activities for the R. ferruginea leaf extract and correlate them with its phenolic content and influence in biological membrane dynamics. Thus, in this study, anti/pro-oxidative properties of R. ferruginea leaf extract by in vitro DPPH and TBARS assays, with respect to the free radical reducing potential and to its activity regarding membrane free radical-induced peroxidation, respectively. Furthermore, preliminary tests related to the extract effect on in vitro glioma cell viability were also performed. In parallel, the phenolic content was detected by HPLC-DAD and included syringic and trans-cinnamic acids, quercetrin, catechin, quercetin, and gallic acid. In an attempt to correlate the biological activity of R. ferruginea extract and its effect on membrane dynamics, the molecular interaction between the extract and a liposomal model with natural-sourced phospholipids was investigated. Location and changes in vibrational, rotational, and translational lipid motions, as well as in the phase state of liposomes, induced by R. ferruginea extract, were monitored by Fourier-transform infrared spectroscopy, nuclear magnetic resonance, differential scanning calorimetry, and UV-visible spectroscopy. In its free form, the extract showed promising in vitro antioxidant properties. Free-form extract (at 1000µ g/mL) exposure reduced glioma cell in vitro viability in 40%, as evidenced by MTT tests. Pro-oxidant behavior was observed when the extract was loaded into liposomes. A 70.8% cell viability reduction was achieved with 500 µg/mL of liposome-loaded extract. The compounds of R. ferruginea extract ordered liposome interface and disorder edits a polar region. Phenolic content, as well as membrane interaction and modulation may have an important role in the oxidative and antitumoral activities of the R. ferruginea leaf extract.
Assuntos
Sobrevivência Celular/efeitos dos fármacos , Myrsine/química , Extratos Vegetais/química , Extratos Vegetais/farmacologia , Antioxidantes/metabolismo , Catequina/farmacologia , Linhagem Celular Tumoral , Ácido Gálico/farmacologia , Glioma/metabolismo , Humanos , Lipossomos/química , Oxirredução/efeitos dos fármacos , Fenol/química , Quercetina/análogos & derivados , Quercetina/farmacologia , Espécies Reativas de Oxigênio/metabolismo , Espectroscopia de Infravermelho com Transformada de FourierRESUMO
Objetivando comparar a eficácia do etodolac, um novo antiinflamatório näo hormonal, com diclofenaco no alívio dos sinais e sintomas de pacientes com traumatismos esportivos agudos ocorridos há menos de 48 horas, realizou-se estudo duplo-cego, randomizado, de grupos paralelos. Um grupo (41 pacientes) recebeu etodolac 200 mg via oral a cada oito horas por sete dias e outro (41 pacientes) recebeu diclofenaco 50 mg via oral nas mesmas condiçöes. As avaliaçöes clínicas foram realizadas no pré-tratamento e nos 1§, 3§ e 7§ dias de tratamento, sendo avaliado os seguintes sinais e sintomas: dor em repouso; dor à movimentaçäo ativa e passiva; dor à palpaçäo; edema, rubor e calor local; prejuízo funcional. Os grupos eram homogêneos no prê-tratamento. A análise estatística mostrou melhora de todos os sinais e sintomas nos dois grupos de tratamento. O teste de igualdade de probabilidades evidenciou diferença significante entre os grupos etodolac e diclofenaco, com maior alívio para o primeiro, com relaçäo a dor à palpaçäo e rubor local no 3§ dia de tratamento e nos intervalos pré-3§ dia e 1§ - 3§ dia (p < 0,05). Para os demais sintomas, näo foi evidenciado nenhuma diferença significante. A tolerabilidade foi considerada boa para ambas as drogas