Abstract Exopolysaccharides (EPS) produced by Klebsiella oxytoca are of environmental, pharmaceutical, and medicinal interest. However, studies about the anti-inflammatory activity of EPS produced by this microorganism still remain limited. The aim of this study was to produce, characterize, and evaluate the anti-inflammatory activity of EPS from K. oxytoca in a pleurisy model. Colorimetric analysis revealed that precipitated crude exopolysaccharides (KEPSC) and deproteinated exopolysaccharides (KEPS) present high levels of total carbohydrates (65.57% and 62.82%, respectively). Analyses of uronic acid (7.90% in KEPSC and 6.21% in KEPS) and pyruvic acid (3.01% in KEPSC and 1.68% in KEPS) confirm that the EPS are acidic. Gas chromatography-mass spectrometry analyses demonstrated that the EPS consisted of rhamnose (29.83%), glucose (11.21%), galactose (52.45%), and mannose (6.50%). The treatment of an experimental pleurisy model in rats through subcutaneous administration of 50, 100, 200, and 400 mg/kg of KEPS decreased both the volume of inflammatory exudate and the number of leukocytes recruited to the pleural cavity. The present data showed that EPS production by K. oxytoca using the method described is easy to perform and results in a good yield. In addition, we show that KEPS exhibit anti-inflammatory activity when administered subcutaneously in rats.

Chemical investigation of Guettarda viburnoides (leaves) led to the isolation of ursolic acid, uncaric acid, secoxyloganin, and grandifloroside, along with a mixture of quercetin-3-O-β-D-galactopyranoside and quercetin-3-O-β-D-glucopyranoside, and of β-sitosterol and stigmasterol. The structures of the isolated compounds were elucidated on the basis of their NMR data. The crude extract, ethyl acetate fraction, aqueous-methanol fraction, and grandifloroside showed significant DPPH free-radical scavenging activities with IC50 ranging from 18.92 to 26.47 µg mL-1. The topical administration of the crude extract and fractions markedly reduced the croton oil-induced mice ear edema in 67.0%-99.0%. Inhibition of tissue MPO activity was also observed, which demonstrated an anti-inflammatory effect of the G. viburnoides species.

The phytochemical investigation of Sabicea brasiliensis roots led to the isolation of 5-O-caffeoylquinic acid, 3,5- and 4,5-O-dicaffeoylquinics acids, scopoletin, ursolic acid, a mixture of β-sitosterol, stigmasterol and campesterol, daucosterol and saccharose. The structures of the isolated compounds were assigned on the basis of one- and two-dimensional NMR spectroscopic methods and by comparison with literature data. The anti-inflammatory and antioxidant activities of the crude methanolic extract and its fractions were analyzed.

Phytochemical investigation of Aeschynomene fluminensis leaves and branches led to isolation of the flavonoid glycosides kaempferol 3,7-di-O-α-L-rhamnopyranoside, kaempferol 7-O-α-L-rhamnopyranoside, kaempferol 3-O-apiofuranosil-7-O- rhamnopyranoside, quercitin 3-O-α-L-rhamnopyranoside, quercitin 3-O-arabinofuranoside, 8-β-D-glucopyranosyl 4',5,7-trihydroxyflavanone, the isoflavonoid 4',7-di-hydroxy-isoflavone, the dimer epicatechin-(2β→7, 4β→8)- epicatechin, the polyol 3-O-methyl-chiro-inositol and two steroids in sitosterol and stigmasterol mixture. These compounds were identified by NMR ¹H and 13C and compared with literature data. Anti-inflammatory activity of the crude methanolic extract and its fractions was evaluated.

This phytochemical investigation of Guettarda pohliana leaves led to the isolation of the triterpenes pomolic acid, rotundic acid, 3β,6α,19α,23-tetrahydroxyurs-12-en-28-oic acid, clethric acid, ursolic acid and oleanolic acid, the monoterpenoids loliolide and secoxyloganin, besides daucosterol and steroids. The structures of the isolated compounds were assigned on the basis of NMR data, including two-dimensional NMR methods. The anti-inflammatory activity of the crude methanolic extracts from leaves and roots, as well as of their fractions, was evaluated.

CONTEXTO: A resposta inflamatória e o estresse oxidativo acentuados em decorrência da artrite reumatóide são capazes de promover neurodegeneração. Nessas condições, é possível que o sistema nervoso entérico seja afetado, diminuindo a qualidade de vida dos pacientes. No entanto, os sintomas da artrite no trato gastrointestinal são geralmente associados ao uso de medicamentos anti-inflamatórios do que a um possível dano neural. OBJETIVO: Verificar se a população geral de neurônios mioentéricos do íleo e do jejuno de ratos artríticos é afetada pela artrite. MÉTODOS: Foram utilizados 20 ratos Holtzmann, inicialmente com 58 dias de idade, divididos em 4 grupos: controle com 88 dias (C30); artrítico com 88 dias (Art30); controle com 118 dias (C60) e artrítico com 118 dias (Art60). Os animais dos grupos Art30 e Art60 receberam aos 58 dias de idade o adjuvante completo de Freund para indução da artrite. Os preparados totais de íleo e jejuno foram submetidos a imunoistoquímica para a proteína miosina-V. Realizou-se análises quantitativas e morfométricas dos neurônios. RESULTADOS: Os animais Art30 e Art60 apresentaram, respectivamente, redução de 2% e 6% na área intestinal em relação aos seus controles. Não foram observadas diferenças na densidade neuronal geral entre os quatro grupos (P>0,05). O grupo C60 apresentou redução de 14,4% e 10,9% na área média do corpo celular neuronal em relação ao grupo C30 (P<0,05). Os demais grupos apresentaram área média de corpo celular semelhante (P>0,05). CONCLUSÃO: A artrite não provocou alterações quantitativas ou morfológicas na população mioentérica geral, entretanto, estudos em andamento revelam alterações significativas em subpopulações de neurônios mioentéricos (nitrérgicos e VIP-érgicos).

CONTEXT: The inflammatory response itself and the consequent oxidative stress are able to promote neurodegeneration. So, it is possible that enteric nervous system is affected by inflammatory diseases threatening quality of life of patients. However, gastrointestinal symptoms of arthritis are usually attributed to anti-inflammatory drugs rather than neural damage. OBJECTIVE: To confirm if the general population of myenteric neurons from the ileum and jejunum of rats is affected by arthritis. METHODS: Twenty Holtzmann rats, 58-day-old male, were used and divided in four groups: control group (C30), arthritic group (Art30), older control group (C60) and older arthritic group (Art60). At 58 days old, the animals in groups Art30 and Art60 received an injection of the complete Freund's adjuvant in order to induce arthritis. The whole-mount preparations of ileum and jejunum were processed for myosin-V immunohistochemistry. Quantitative and morphometric analyses were performed. RESULTS: Groups Art30 and Art60 presented, respectively, a reduction of 2% and 6% in intestinal area when compared to their control groups. No significant differences were observed in general neuronal density among the four groups (P>0.05). Group C60 presented a reduction of 14.4% and 10.9% in mean neuronal cell body area when compared to group C30 (P<0.05), for the ileum and jejunum, respectively. The other groups had a similar mean neuronal cell body area (P>0.05). CONCLUSION: Arthritis does not promote quantitative or morphological damages in general myenteric population. However, studies in progress have revealed some significant alterations in myenteric neurons subpopulations (nitrergic and VIP-ergic neurons).

O presente estudo investigou o efeito do extrato bruto das folhas de yacon, obtido por extração a frio (Y C) ou a quente (Y H), ou por extração hidro-alcoólica (Y E), na glicemia de ratos diabéticos (induzidos por estreptozocina, 50 mg/kg, i.p.) e não diabéticos. Os animais foram tratados por via oral com os extratos (400 mg/kg) ou água por um período de 3, 7, 10 e 14 dias. Após o tratamento, os animais foram anestesiados e amostras de sangue foram coletadas para determinações dos níveis de glicose e creatinina plasmática e da atividade de enzimas (AST, ALT, ALP). Também foi avaliado o consumo de ração, água, volume de urina, peso corporal dos animais e a DL50 do Y E. O tratamento dos animais com Y E, por 14 dias, reduziu a glicemia de ratos diabéticos e não diabéticos. Adicionalmente, o Y E restaurou a atividade das enzimas que estavam alteradas, e melhorou o ganho de peso dos animais diabéticos. Estes resultados demonstraram que a efetividade do extrato de yacon está relacionada ao método de preparação do extrato e ao tempo de tratamento dos animais. O efeito do Y E na glicemia de ratos diabéticos não está relacionado à redução da ingesta ou a interferência do extrato na absorção intestinal de carboidratos.

The present study investigated the effect of crude extracts from yacon leaves, obtained by aqueous cold (Y C) or hot (Y H) extraction, or hydro-ethanolic extraction (Y E), on glycemia of the diabetic (induced by streptozotocine, 50 mg/kg, ip) and nondiabetic rats. The animals were treated orally with the extracts (400 mg/kg) or water for 3, 7, 10, and 14 days. After this period, the animals were anesthetized and blood samples were collected for measurement of plasmatic glucose and creatinine and activity of the enzymes (AST, ALT, ALP). Also were evaluated the consumption of food, water, urine volume, body weight of the animals and LD50 of Y E. Treatment with Y E for 14 days reduced glycemia in diabetic and nondiabetic animals. No similar reduction was observed in animals treated with Y C or Y H. Additionally, Y E restored the activity of the plasmatic enzymes that were altered, and improved weight gain in the diabetic animals. These results showed that the effectiveness of the yacon extracts is related to the method of preparation and to the time of treatment. The effect of Y E on glycemia in diabetic rats is not related to reduction of food intake or to interference of the extract with intestinal absorption of carbohydrates.

The phytochemical investigation of Chomelia obtusa leaves led to the isolation of four triterpenes (3-O-β-D-quinovopyranosyl-28-O-β-D-glycopyranosyl quinovic acid, 3-O-β-D-quinovopyranosyl-28-O-β-D-glycopyranosyl cincholic acid, and a mixture of ursolic and oleanolic acids), two flavonoids (3-O-β-D-glycopyranosyl quercetin, 3-O-[α-L-rhamnopyranosyl-(1→6)-β-D-galactopyranoside] quercetin), besides bornesitol and a mixture of 3,5- and 4,5-O-dicaffeoyl quinic acids. The structures of the isolated compounds were assigned on the basis of spectroscopic data, including two-dimensional NMR methods. The anti-inflammatory and antioxidant activities of the crude methanolic extract and of its fractions were evaluated. This is the first report on the chemical and biological investigation of the Chomelia genus.

A atividade antinociceptiva do extrato bruto e frações do Stryphnodendron adstringens (Mart.) Coville (barbatimão) foi avaliada. Foram usados três modelos experimentais para avaliação da dor: teste de contorção abdominal induzida pelo ácido acético, teste da formalina e teste da placa quente. Os resultados mostraram um efeito antinociceptivo evidente do barbatimão nos modelos experimentais de contorção induzida por ácido acético e dor induzida pela formalina. Por outro lado, o barbatimão não modificou significativamente o tempo de latência dos animais no teste da placa quente. Estes resultados sugerem que o extrato de barbatimão apresenta efeito antinociceptivo por mecanismos periféricos.

The antinociceptive activity of the crude extract and fractions of Stryphnodendron adstringens (Martius) Coville (barbatimão) was evaluated. Three experimental models of pain induction were used: abdominal writhing, formalin, and hot plate. The results demonstrated an antinociceptive effect of barbatimão in the experimental models of writhing induced by acetic acid and pain induced by formalin. However, the extracts did not significantly alter latency time on the hot plate in mice. These results suggest that barbatimão extract has a peripheral antinociceptive effect.

Elderly people are great consumers of medicines, and antimicrobial medicines are among those most frequently prescribed to patients. There are specific aspects related to the elderly that make the prescription, use and monitoring of antimicrobials highly complicated. Age-caused physiological changes result in alterations in their pharmacodynamic and pharmacokinetic traits, which may modify the development of the infection and the response to certain antimicrobial medicines. Due to the prevalence of chronic diseases, the elderly simultaneously consume many types of medicines, which may be the cause of adverse reactions or drug-drug interactions. Since the aspects mentioned above must be taken into account, special attention in infection treatment of the elderly is justified.

Los ancianos hacen parte de la población que más consume medicamentos, y los antimicrobianos están entre las clases de medicamentosas más frecuentemente prescritas para estos pacientes. Existen aspectos específicos del anciano que complican la prescripción y el control del uso del antimicrobiano. Las modificaciones fisiológicas decurrentes de la edad resultan en alteraciones en la farmacodinámica y en la farmacocinética, que pueden alterar el decurso de la infección y la respuesta a un determinado antimicrobiano. En función de la gran prevalencia de enfermedades crónicas, los ancianos hacen uso simultáneo de muchos medicamentos, lo que resulta en mayor riego de reacciones adversas o interacciones medicamentosas. Todos estos aspectos justifican atención especial en la conducción del tratamiento de la infección en el anciano.

Os idosos fazem parte da população que mais consome medicamentos e os antimicrobianos estão entre as classes medicamentosas mais freqüentemente prescritas para estes pacientes. Existem aspectos específicos do idoso que complicam a prescrição e o monitoramento do uso do antimicrobiano. As modificações fisiológicas decorrentes da idade resultam em alterações na farmacodinâmica e na farmacocinética, que podem alterar o decurso da infecção e a resposta a um determinado antimicrobiano. Em função da alta prevalência de doenças crônicas, os idosos fazem uso simultâneo de muitos medicamentos, o que resulta em maior risco de reações adversas ou interações medicamentosas. Todos estes aspectos justificam atenção especial na condução do tratamento da infecção no idoso.

A Paracoccidioidomicose é uma micose sistêmica endêmica em alguns países da América Latina. Essa doença afeta principalmente pulmões, gânglios e mucosas, além de causar diminuição da imunidade celular. O medicamento Canova tem sido utilizado com sucesso por pacientes imunodeprimidos, como por exemplo portadores de câncer e de AIDS. O objetivo desse trabalho foi avaliar aspectos bioquímicos em camundongos infectados com Paracoccidioides brasiliensis e os efeitos do medicamento Canova sobre esses parâmetros. Foram utilizados camundongos infectados com o isolado de Paracoccidioides brasiliensis Pb18 e tratados com o medicamento Canova durante dezessete semanas. Os parâmetros bioquímicos analisados foram níveis de atividade de aspartato amino transferase, alanina amino transferase, fosfatase alcalina e amilase, concentração de proteínas totais, albumina e globulinas. Os resultados obtidos sugerem que os animais que receberam tratamento com o medicamento Canova tiveram menores alterações funcionais nos seus órgãos internos.

The objective of this work was to evaluate biochemical parameters in Paracoccidioides brasiliensis infected mice and the effect of Canova medicine on these parameters. Mice infected with the isolate Paracoccidioides brasiliensis Pb18 and treated with Canova for 17 weeks were used. The biochemical parameters analysed were the levels of aspartate aminotransferase, alanine aminotransferase, alkaline phosphatase and amylase, and the concentration of total proteins, albumin and globulins. The results suggested that the animals that were treated with Canova had less functional alterations in their internal organs.