RESUMO
The activities of the crude ethanol extract from Piper cubeba seeds, (-)-cubebin and its semi-synthetic derivatives were evaluated against oral pathogens. The crude ethanol extract was more active against Streptococcus salivarius (MIC value of 80 microg/mL). (-)-Cubebin displayed MIC values ranging from 0.20 mm for Streptococcus mitis to 0.35 mm for Enterococcus faecalis. The natural product (-)-cubebin and its semi-synthetic derivative (-)-hinokinin displayed bacteriostatic activity at all evaluated concentrations, as well as fungicidal activity against Candida albicans at 0.28 mm. The O-benzyl cubebin derivative showed fungistatic and fungicidal effects against C. albicans at 0.28 mm and 0.35 mm, respectively. Also, the other dibenzylbutyrolactone derivatives [(-)-6,6'-dinitrohinokinin and (-)-O-(N,N-dimethylaminoethyl)-cubebin] displayed bacteriostatic and fungistatic effects at the evaluated concentrations. Moreover, the semi-synthetic derivative (-)-6,6'-dinitrohinokinin was the most active compound against all the evaluated microorganisms. Therefore, it may be suggested that the presence of the carbonyl group at C-9 plus the introduction of polar groups in the aromatic rings improve the antimicrobial activity of dibenzylbutyrolactone compounds.
Assuntos
Anti-Infecciosos/farmacologia , Candida albicans/efeitos dos fármacos , Enterococcus faecalis/efeitos dos fármacos , Lignanas/farmacologia , Piper/química , Streptococcus/efeitos dos fármacos , 4-Butirolactona/análogos & derivados , 4-Butirolactona/química , 4-Butirolactona/farmacologia , Anti-Infecciosos/química , Anti-Infecciosos/isolamento & purificação , Benzodioxóis , Dioxóis/química , Dioxóis/farmacologia , Lignanas/química , Lignanas/isolamento & purificação , Testes de Sensibilidade Microbiana , Extratos Vegetais/química , Extratos Vegetais/farmacologiaRESUMO
Gelatin microparticles containing propolis ethanolic extractive solution were prepared by spray-drying technique. Particles with regular morphology, mean diameter ranging of 2.27 microm to 2.48 microm, and good entrapment efficiency for propolis were obtained. The in vitro antimicrobial activity of microparticles was evaluated against microorganisms of oral importance (Enterococcus faecalis, Streptococcus salivarius, Streptococcus sanguinis, Streptococcus mitis, Streptococcus mutans, Streptococcus sobrinus, Candida albicans, and Lactobacillus casei). The utilized techniques were diffusion in agar and determination of minimum inhibitory concentration. The choice of the method to evaluate the antimicrobial activity of microparticles showed be very important. The microparticles displayed activity against all tested strains of similar way to the propolis, showing greater activity against the strains of E. salivarius, S. sanguinis, S. mitis, and C. albicans.
Assuntos
Anti-Infecciosos/administração & dosagem , Anti-Infecciosos/uso terapêutico , Gelatina/química , Própole/administração & dosagem , Própole/uso terapêutico , Candida albicans/efeitos dos fármacos , Portadores de Fármacos , Etanol/química , Lacticaseibacillus casei/efeitos dos fármacos , Testes de Sensibilidade Microbiana , Tamanho da Partícula , Streptococcaceae/efeitos dos fármacosRESUMO
The anti-inflammatory and antinociceptive effects of the crude hydroalcoholic extract (PE) of Pfaffia glomerata roots was assessed in the carrageenan-induced rat paw edema at the doses of 100, 200 and 300 mg/kg, using different animal models. An anti-inflammatory dose effect response correlation of r=0.997 and Y=11.67x+0.02 was found. At the same doses, the extract-inhibited acetic acid-induced writhing in mice, but no dose response correlation was found. Oral administration of 100 mg/kg of PE and 0.5 mg/kg of dexamethazone inhibited by 29 and 61%, the granulomatous tissue formation (p>0.05), respectively. These results indicate the potential of this plant extract to treat chronic inflammation. At the assayed doses no significant activity was found in the hot plate test, as well as in the cell migration-induced by carrageenan.
Assuntos
Amaranthaceae , Analgésicos/uso terapêutico , Anti-Inflamatórios/uso terapêutico , Raízes de Plantas/química , Analgésicos/química , Animais , Anti-Inflamatórios/química , Carragenina , Relação Dose-Resposta a Droga , Edema/induzido quimicamente , Edema/tratamento farmacológico , Masculino , Camundongos , Medição da Dor , Fitoterapia , Extratos Vegetais/administração & dosagem , Extratos Vegetais/química , Extratos Vegetais/uso terapêutico , Ratos , Ratos WistarRESUMO
Three different concentrations (1, 10 and 50 microg/ml) of lyophilized hydroalcoholic crude extract of Pfaffia glomerata roots were assayed in vitro against strains of Trypanosoma cruzi (Y) and Leishmania braziliensis. It was observed that P. glomerata hydroalcoholic extract was relatively active within the tested concentrations for L. (V) braziliensis, but inactive against T. cruzi. Despite the fact that both protozoans belong to the Trypanosomatidae family, we suggest that the difference observed for activity should be related to the biological differences between the two parasite species.
Assuntos
Amaranthaceae/química , Antiprotozoários/farmacologia , Leishmania braziliensis/efeitos dos fármacos , Trypanosoma cruzi/efeitos dos fármacos , Animais , Antiprotozoários/química , Relação Dose-Resposta a Droga , Camundongos , Extratos Vegetais/química , Extratos Vegetais/farmacologia , Raízes de Plantas/química , Tripanossomicidas/farmacologiaRESUMO
This work reports the results of the in vitro assay against extracellular forms of Leishmania (viannia) braziliensis of eleven dibenzylbutyrolactone derivatives, either isolated from plants or obtained by synthesis. From these, only two showed relative biological activity against the parasite, the raceme mixtures of methylpluviatolide: IC50 = 496 mM and (-)-6,6'- dinitrocubebin: IC50 = 510,4 μM. Thus, it can be suggested that the metabolic pathway responsible for the biological activity of these compounds against this parasite genera differs from the one related to Trypanosoma cruzi, for which these compounds were quite active. This fact highly also suggests that this class of compounds is more selective against T. cruzi. Nevertheles, other lignans derivatives should be obtained to allow the fully evaluation of this class of lignans against Leishmaniosis.
Este trabalho apresenta os resultados de ensaios in vitro contra formas extracelulares de Leishmania (viannia) braziliensis de onze derivados de dibenzilbutirolactonas isolados de plantas ou obtidos através de síntese. Destes, só dois mostraram atividade biológica relativa contra o parasita, as misturas racêmicas de methilpluviatolide,: IC50 = 496 M e (-) -6,6' - dinitrocubebin: IC50 = 510,4 M. Assim, pode-se sugerir que o caminho metabólico responsável para a atividade biológica destas combinações contra estes gêneros de parasita difere do relacionado a Trypanosoma cruzi para o qual estas combinações foram bastante ativas. Este fato também sugere fortemente que essa classe de combinações é mais seletivo contra T. cruzi. Dessa forma, deveriam ser obtidos outros derivados de lignanas para permitir a completa avaliação desta classe de substâncias contra Leishmaniose.
RESUMO
This study evaluates the effect of subgingival irrigation with a 1% chlorhexidine collagen gel in periodontal pockets as an adjunct procedure to scaling and root planing (SRP). Thirty-seven sites with probing depth (PD) of 5-7 mm and BANA positive in 6 patients with chronic periodontal disease were selected. Sites were assigned to different treatment groups consisting of SRP only (group 1), SRP + irrigation with collagen gel (group 2), or SRP + irrigation with collagen gel containing 1% chlorhexidine (group 3). Subgingival irrigation was performed after initial SRP and at 7, 14 and 21 days. Clinical measurements including PD, plaque index (PI), gingival index (GI), gingival recession (GI), bleeding on probing (BOP) and clinical attachment level (CAL) were performed at the selected sites at baseline, 60 and 90 days and the BANA test was performed on plaque samples from the same sites at baseline and 90 days. There was an improvement in clinical parameters in all groups with a significantly greater decrease in GI and bleeding in the chlorhexidine group. There was a greater reduction of BANA positive sites in groups 2 and 3. The authors concluded that 1% chlorhexidine collagen gel is a promising adjunct to SRP in the treatment of adult periodontitis.