RESUMO
Quinolones and fluoroquinolones are widely used to treat uropathogenic Escherichia coli infections. Bacterial resistance to these antimicrobials primarily involves mutations in gyrA and parC genes. To date, no studies have examined the potential relationship between biochemical characteristics and quinolone resistance in uropathogenic E. coli strains. The present work analyzed the quinolone sensitivity and biochemical activities of fifty-eight lactose-negative uropathogenic E. coli strains. A high percentage of the isolates (48.3%) was found to be resistant to at least one of the tested quinolones, and DNA sequencing revealed quinolone resistant determining region gyrA and parC mutations in the multi-resistant isolates. Statistical analyses suggested that the lack of ornithine decarboxylase (ODC) activity is correlated with quinolone resistance. Despite the low number of isolates examined, this is the first study correlating these characteristics in lactose-negative E. coli isolates.
Assuntos
Farmacorresistência Bacteriana Múltipla/genética , Infecções por Escherichia coli/tratamento farmacológico , Fluoroquinolonas/uso terapêutico , Lactose/metabolismo , Ácido Nalidíxico/uso terapêutico , Ornitina Descarboxilase/genética , Infecções Urinárias/tratamento farmacológico , Escherichia coli Uropatogênica/genética , Antibacterianos/uso terapêutico , Brasil , DNA Girase/genética , DNA Topoisomerase IV/genética , Descarboxilação/genética , Descarboxilação/fisiologia , Infecções por Escherichia coli/microbiologia , Humanos , Testes de Sensibilidade Microbiana , Ornitina/metabolismo , Infecções Urinárias/microbiologia , Escherichia coli Uropatogênica/efeitos dos fármacos , Escherichia coli Uropatogênica/enzimologia , Escherichia coli Uropatogênica/isolamento & purificaçãoRESUMO
Quinolones and fluoroquinolones are widely used to treat uropathogenic
Assuntos
Humanos , Farmacorresistência Bacteriana Múltipla/genética , Infecções por Escherichia coli/tratamento farmacológico , Fluoroquinolonas/uso terapêutico , Lactose/metabolismo , Ácido Nalidíxico/uso terapêutico , Ornitina Descarboxilase/genética , Infecções Urinárias/tratamento farmacológico , Escherichia coli Uropatogênica/genética , Antibacterianos/uso terapêutico , Brasil , DNA Girase/genética , DNA Topoisomerase IV/genética , Descarboxilação/genética , Descarboxilação/fisiologia , Infecções por Escherichia coli/microbiologia , Testes de Sensibilidade Microbiana , Ornitina/metabolismo , Infecções Urinárias/microbiologia , Escherichia coli Uropatogênica/efeitos dos fármacos , Escherichia coli Uropatogênica/enzimologia , Escherichia coli Uropatogênica/isolamento & purificaçãoRESUMO
Garcinia gardneriana is popularly used in skin disorders; therefore, this article investigated the effect of G. gardneriana extracts from leaves, bark and seeds and two isolated compounds in ear oedema and leucocytes migration caused by croton oil. The topical application of the extract of G. gardneriana leaves was able to reduce (70 ± 3%, and ID(50) 0.33 mg/ear) ear oedema, while the seeds (51 ± 5%) and the wood (60 ± 12%) extracts were less effective. In a time-course evaluation, the leaf extract (1 mg/ear) was effective when applied 2 hr before and until 3 hr after the stimulation, presenting a higher effectiveness when applied right after croton oil (83 ± 7% inhibition). In addition, the leaf extract was able to diminish the myeloperoxidase (MPO) activity in 64 ± 13%, which suggests the inhibition of leucocyte infiltration that was confirmed by histological analysis. Also, both biflavonoids isolated from the leaves of G. gardneriana, fukugetin (or morelloflavone) and 13-naringenin-II 8-eriodictyol (GB-2a), were able to reduce ear oedema, with ID(50) values of 0.18 (0.10-0.28) and 0.22 (0.15-0.31) mg/ear, respectively, besides the inhibition of MPO activity of 52 ± 6% and 64 ± 5%, respectively. Using the fluorescent probe 2',7'-dichlorodihydrofluorescein diacetate, the leaf extract, fukugetin and GB-2a topically applied to the ear treated with croton oil reduced 52 ± 15%, 63 ± 17% and 83 ± 4%, respectively, the production of reactive oxygen species of the skin. Thus, these results reveal the anti-inflammatory effect of G. gardneriana leaves for topical usage, and both biflavonoids are responsible for this effect.
Assuntos
Anti-Inflamatórios/farmacologia , Garcinia/química , Inflamação/tratamento farmacológico , Extratos Vegetais/farmacologia , Administração Cutânea , Animais , Anti-Inflamatórios/administração & dosagem , Anti-Inflamatórios/isolamento & purificação , Movimento Celular/efeitos dos fármacos , Modelos Animais de Doenças , Inflamação/patologia , Concentração Inibidora 50 , Leucócitos/efeitos dos fármacos , Leucócitos/metabolismo , Masculino , Camundongos , Peroxidase/efeitos dos fármacos , Peroxidase/metabolismo , Extratos Vegetais/administração & dosagem , Espécies Reativas de Oxigênio/metabolismo , Dermatopatias/tratamento farmacológico , Dermatopatias/patologia , Fatores de TempoRESUMO
In order to verify the topical antiinflammatory effect of epicuticular wax from leaves of Eugenia beaurepaireana, it was tested in mice croton oil-induced inflammation. Our findings show that topical application of Eugenia beaurepaireana epicuticular wax was significantly active in inhibiting both oedema (Inhibitory dose 50 percent (ID50) = 0.31 (0.26 - 0.39) mg.ear -1, inhibition = 79 ± 6 percent) and tissue myeloperoxidase activity (indicative of polymorphonuclear leukocytes influx) (ID50 =0.34 (0.20 - 0.41) mg.ear -1, inhibition = 77 ± 4 percent) in mice ear treated with croton oil. Two main compounds were detected on epicuticular wax of E. beaurepaireana. These compounds were identified as α- and β-amyrin by flame ionization detection (GC-FID) and spectroscopic methods (IR, NMR ÕH and 13C). In conclusion, the results indicate a topical antiinflammatory activity for the Eugenia specie studied and, that, at least in part, α- and β-amyrin are responsible for this activity.
A atividade antiinflamatória tópica da cera epicuticular das folhas de Eugenia beaurepaireana foi avaliada pelo modelo do edema de orelha induzido pelo óleo de cróton em camundongos. Os resultados do estudo mostram que a aplicação tópica da cera epicuticular de Eugenia beaurepaireana inibiu significativamente a formação do edema (Dose inibitória 50 por cento (DI50) = 0,31 (0,26 - 0,39) mg.orelha-1, inibição = 79 ± 6 por cento) e a atividade da mieloperoxidase tissular (indicativo do influxo de leucócitos polimorfonucleares) (DI50 =0,34 (0,20 - 0,41) mg.orelha-1, inibição = 77 ± 4 por cento) em camundongos tratados com o óleo de cróton. Dois compostos majoritários foram detectados e isolados da cera epicuticular de E. beaurepaireana. Estes compostos foram identificados como os triterpenos α-amirina e β-amirina, através de técnicas cromatográficas (CG-FID) e espectroscópicas (IV, RMN ÕH e 13C). Em conclusão, os resultados indicam que a espécie E. beaurepaireana apresenta um efeito antiinflamatório tópico relevante, sendo os compostos α-amirina e β-amirina responsáveis, pelo menos em parte, por esta atividade.
Assuntos
Animais , Masculino , Camundongos , Anti-Inflamatórios , Ceras/química , Folhas de Planta/fisiologia , Myrtaceae/química , Plantas Medicinais , Análise de Variância , Interpretação Estatística de DadosRESUMO
Serjania erecta Radlk (Sapindaceae), commonly called cinco-folhas or cipó-cinco-folhas in Brazil, is thought to be effective for treating several inflammatory diseases. In order to verify the topical anti-inflammatory effect of Serjania erecta, hydroalcoholic extract and fractions were obtained by extraction in solvents of increasing polarity and were tested in mouse models using croton-oil-induced inflammation. Our findings showed that topical application of Serjania erecta hydroalcoholic extract (0.01-3.0 mg/ear), and the dichloromethane (0.03-1.0 mg/ear), ethyl acetate (0.03-1.0 mg/ear), and hexane (0.003-1.0 mg/ear) fractions revealed significant activity, causing a dose-dependent reduction of croton-oil ear edema (ID(50)=0.14 mg/ear, 0.23 mg/ear, 0.14 mg/ear, 0.04 mg/ear, respectively). The extract and all tested fractions also decreased tissue myeloperoxidase activity (indicative of polymorphonuclear leukocytes influx) in mouse-ears treated with croton oil with a maximum inhibition of 72% at 3.0 mg/ear for the hydroalcoholic extract and 81%, 78%, and 83% at 1.0mg/ear for dichloromethane, ethyl acetate and hexane fractions, respectively. As expected, dexamethasone (0.05 mg/ear) was effective in inhibiting both edema and myeloperoxidase activity (99% and 82%, respectively). In conclusion, our results indicate a topical anti-inflammatory effect for the species of Serjania studied.
Assuntos
Anti-Inflamatórios/farmacologia , Inflamação/tratamento farmacológico , Extratos Vegetais/farmacologia , Sapindaceae/química , Administração Cutânea , Animais , Anti-Inflamatórios/isolamento & purificação , Brasil , Óleo de Cróton , Modelos Animais de Doenças , Relação Dose-Resposta a Droga , Edema/tratamento farmacológico , Masculino , Medicina Tradicional , Camundongos , Peroxidase/efeitos dos fármacos , Peroxidase/metabolismo , Extratos Vegetais/administração & dosagem , Dermatopatias/tratamento farmacológico , Solventes/químicaRESUMO
Eugenia brasiliensis Lam., a plant from the south of Brazil, is used in the popular medicine for rheumatism treatment. This study reports that topical application of hydroalcoholic extract, fractions and isolated compounds from E. brasiliensis caused an inhibition of ear oedema in response to topical application of croton oil on the mouse ear. For oedema inhibition, the estimated ID50 values (dose reducing the inflammatory response by 50% relative to the control value) for hydroalcoholic extract and fractions (hexane, ethyl acetate and dichloromethane) were 0.17, 0.29, 0.13 and 0.14 mg/ear, respectively, with inhibition of 79+/-7%, 87+/-6%, 88+/-5% and 96+/-2%, respectively. Isolated phenolic compounds (quercetin, catechin and gallocatechin) were also effective in inhibiting the oedema (inhibition of 61+/-5%, 66+/-2% and 37+/-9%, respectively). Moreover, both extract and isolated compounds caused inhibition of polymorphonuclear cells influx (inhibition of 85+/-6%, 81+/-5%, 73+/-6% and 76+/-6%, respectively). The histological analysis of the ear tissue clearly confirmed that the extract and compounds of E. brasiliensis inhibited the influx of polymorphonuclear cells to mouse ear skin after application of croton oil. Furthermore, hydroalcoholic extract was also effective in inhibiting the arachidonic acid-mediated mouse ear oedema (ID50 value was 1.94 mg/ear and inhibition of 60+/-7%). Therefore, these results consistently support the notion that E. brasiliensis possesses topical anti-inflammatory activity.