Influence of extractive parameters on the preparation of a solution from <i>Psidium guajava</i> L.

The aim of this work is evaluate the influence of extractives parameters on tannin content of solutions obtained from leaves of P. guajava and the antimicrobial activity of the best extract solution. The type of extraction, drug proportion and alcohol concentration were studied following a factorial design and the responses evaluated were tannin content and dry residue. The tannins content was assayed by spectrophotometric method at 271nm using casein as precipitant agent and the dry residue was determined by gravimetric method. The statistical analysis demonstrated that only the alcohol concentrations have significant influence on tannins content, but on the dry residue both factors (drug and alcohol proportion) were important. In accordance of the results, the best extractive method was decoction on reflux during 15 min using alcohol concentration 50 % (v/v) as solvent and this extract solution shows a promising antimicrobial activity.Colegio de Farmacéuticos de la Provincia de Buenos Aire

Quantitative analysis of the hgh-affinity binding sites for [H-3]ouabain in the rat vas deferens and their immunological identification as the alpha(2) isoform of Na+/K+-ATPase

Binding assays were performed with [H-3]ouabain to investigate the presence of, and to characterize, a Na+/K+-ATPase isoform with high affinity for cardiac glycosides in the rat vas deferens. Nonlinear regression analysis of equilibrium experiments carried out with crude preparations in a Mg-P-i medium indicated the presence of high-affinity sites characterized with good precision (individual coefficients of variation = 11-35%) by their density (B-max = 0.42 to 0.72 pmol/mg protein) and dissociation constant (K-d = 0.069 to 0.136 mu M) values. the values of the dissociation rate constant (k(-1)) and the association rate constant (k(+1)) for these sites were 0.151 to 0.267 min(-1) and 2.87 to 3.60 mu M-1.min(-1), respectively. A higher number of low-affinity sites (K-d around 15 mu M), supposed to correspond to the alpha(1) isoform, was also identified, but their K-d and B-max values were not quantified precisely in this crude preparation. Western blot assays indicated hybridization with specific anti-alpha(1) and anti-alpha(2) isoform antibodies but not with anti-alpha(3) isoform antibody. Taken together, the present results indicate the existence of a low proportion of the alpha(2) isoform of Na+/K+-ATPase in the rat vas deferens that can be quantified precisely by [H-3]ouabain binding even in a crude membrane preparation that is suitable for studies under conditions of plasticity. (C) 1998 Elsevier Science Inc.Univ Fed Rio de Janeiro, Inst Ciencias Biomed, Dept Farmacol Basica & Clin, BR-21941590 Rio de Janeiro, BrazilUniv Fed Estado São Paulo, Escola Paulista Med, Dept Farmacol, BR-04034970 São Paulo, BrazilUniv Fed Estado São Paulo, Escola Paulista Med, Dept Farmacol, BR-04034970 São Paulo, BrazilWeb of Scienc

Synthesis of 1,2,3-Triazole Derivatives and &lt;em&gt;in Vitro&lt;/em&gt; Antifungal Evaluation on &lt;em&gt;Candida&lt;/em&gt; Strains

1,2,3-Triazoles have been extensively studied as compounds possessing important biological activities. In this work, we describe the synthesis of ten 2-(1-aryl-1&lt;em&gt;H&lt;/em&gt;-1,2,3-triazol-4-yl)propan-2-ols via copper catalyzed azide alkyne cycloaddition (CuAAc or &lt;em&gt;click chemistry&lt;/em&gt;). Next the&lt;em&gt; in vitro&lt;/em&gt; antifungal activity of these ten compounds was evaluated using the microdilution broth method against 42 isolates of four different &lt;em&gt;Candida&lt;/em&gt; species. Among all tested compounds, the halogen substituted triazole 2-[1-(4-chlorophenyl)-1&lt;em&gt;H&lt;/em&gt;-(1,2,3)triazol-4-yl]propan-2-ol, revealed the best antifungal profile, showing that further modifications could be done in the structure to obtain a better drug candidate in the future

Acute toxicity and laxative activity of Aloe ferox resin

Aloe ferox Mill., Xanthorrhoeaceae, resin is the solid residue obtained by evaporating the latex that drains from the leaves transversally cut. Aloe ferox has been used in folk medicine as anti-inflammatory, immunostimulant, anti-bacterial, anti-fungal, antitumor, laxative and to heal wounds and burns. The effects of the oral administration of A. ferox resin (10, 25, 50, 100 and 200 mg/kg) were evaluated on intestinal transit in mice and its acute toxicity (5.0 g/kg) in Wistar rats. The hydroxyanthracene derivatives present in the resin were expressed as aloin, identified by thin layer chromatography and quantified by spectrophotometry. The aloin (Rf 0.35) was identified and the percentage of hydroxyanthracene derivates expressed as aloin was 33.5%. A. ferox resin extract (50, 100 and 200 mg/kg) increased the gastrointestinal motility at a 30 min interval at 93.5, 91.8 and 93.8%, respectively, when compared to control group (46.5%). A single oral dose of the A. ferox resin extract did not induce signs of toxicity or death. Thus, the results demonstrate that A. ferox has laxative activity and that it is nontoxic, since LD50 could not be estimated and it is possibly higher than 5.0 g/kg

Toxicological reproductive study of Carapa guianensis Aublet (Andiroba) in female Wistar rats

Os efeitos do óleo extraído das sementes da Carapa guianensis (OS) foram investigados sobre variáveis reprodutivas e desenvolvimento da prole de ratas Wistar. Quatro grupos de fêmeas foram tratados per os com OS (0,375, 0,75 e 1,5 g/kg) ou água durante a gestação. Não houve diferenças significantes nas variáveis reprodutivas entre os grupos tratados e controle. Na prole, não foram registradas alterações, exceto aumento da atividade motora na menor dose do OS. Conclui-se que o óleo de Carapa guianensis não interfere na fertilidade de ratas Wistar e desenvolvimento da prole, entretanto o aumento da atividade motora pode indicar uma possível ação sobre o desenvolvimento do sistema nervoso central.The effects of the Carapa guianensis seed oil (SO) in the reproductive parameters and in the offspring development were investigated in Wistar rats. Four groups of female rats were treated orally with the SO (0,375, 0,75 and 1,5 g/kg) or water during the pregnancy. There were not significant differences in the reproductive parameters among the groups. In the offspring, there were no changes, except for an increase of the motor activity in the group SO 0,375 g/kg. It is concluded that the SO did not interfere on the fertility of Wistar rats and in the offspring development. However, the increase of the motor activity may indicate a possible action on the development of the central nervous system.Colegio de Farmacéuticos de la Provincia de Buenos Aire

Toxicological reproductive study of Carapa guianensis Aublet (Andiroba) in female Wistar rats

Os efeitos do óleo extraído das sementes da Carapa guianensis (OS) foram investigados sobre variáveis reprodutivas e desenvolvimento da prole de ratas Wistar. Quatro grupos de fêmeas foram tratados per os com OS (0,375, 0,75 e 1,5 g/kg) ou água durante a gestação. Não houve diferenças significantes nas variáveis reprodutivas entre os grupos tratados e controle. Na prole, não foram registradas alterações, exceto aumento da atividade motora na menor dose do OS. Conclui-se que o óleo de Carapa guianensis não interfere na fertilidade de ratas Wistar e desenvolvimento da prole, entretanto o aumento da atividade motora pode indicar uma possível ação sobre o desenvolvimento do sistema nervoso central.The effects of the Carapa guianensis seed oil (SO) in the reproductive parameters and in the offspring development were investigated in Wistar rats. Four groups of female rats were treated orally with the SO (0,375, 0,75 and 1,5 g/kg) or water during the pregnancy. There were not significant differences in the reproductive parameters among the groups. In the offspring, there were no changes, except for an increase of the motor activity in the group SO 0,375 g/kg. It is concluded that the SO did not interfere on the fertility of Wistar rats and in the offspring development. However, the increase of the motor activity may indicate a possible action on the development of the central nervous system.Colegio de Farmacéuticos de la Provincia de Buenos Aire

Chronic toxicological evaluation of the hydroalcoholic extract of Operculina alata (Ham.) Urban on biochemical and hematological parameters in female Wistar rats

O extrato hidroalcoólico (EHA) da Operculina alata (Ham.) Urban, é comercializado pelas propriedades laxantes e catárticas. Apesar da ampla utilização na Medicina tradicional, existem poucos estudos sobre a segurança de uso. Foram investigados efeitos da administração crônica do EHA sobre parâmetros bioquímicos e hematológicos. Não foram observados sinais de toxicidade aguda ou morte, nem alterações nos perfis bioquímicos e hematológicos, excetuando-se aumento significativo nos níveis séricos de glicose, alanina amino-transferase e fosfatase alcalina e redução na contagem de monócitos. Embora estatisticamente significativas, as alterações ocorreram dentro da faixa de referência para espécie. Aparentemente, essas alterações não estão relacionadas a efeitos tóxicos do extrato.The hydroalcoholic extract (HAE) of Operculina alata (Ham.) Urban is commercialized due to its laxatives and cathartic properties. Despite its large use in traditional medicine, there are few studies about its safety. The effects of the chronic administration of the HAE on hematological and biochemical parameters were investigated. Acute toxicity signs or deaths were not observed, nor alterations on hematological and biochemical parameters, except for a significant increase of the seric levels of glucose, alanine aminotransferase and alkaline phosphatase and also the decrease of monocytes counts. Although statistically significant, the alterations occurred on the reference values range and, apparently, they were not related to toxic effects of the extract.Colegio de Farmacéuticos de la Provincia de Buenos Aire

Effects of the oral treatment with Copaifera multijuga oil on reproductive performance of male Wistar rats

Copaiba oil, extracted from Copaifera multijuga Hayne, Fabaceae, is widely used for medicinal purposes, especially to treat inflammatory processes. However, there is no report regarding its effect on reproductive performance after used in repeated doses orally. The present study evaluated the effects of the oral administration of Copaiba oil (at doses of 200, 500 or 2500 mg/kg) or water (control) for eight weeks in male Wistar rats. Treated males mated untreated females, and parameters as fertility rates, absolute and relative mass of accessory sexual organs and histology and development of the offspring were evaluated. Chemical analysis revealed the presence of 22 components accounting for 99.11% of the Copaiba oil. The main compounds identified were sesquisterpenes. The reproductive toxicology results indicate that there was no difference between the treated groups compared with the control group in any of the parameters, suggesting that the oral treatment with C. multijuga oil for eight weeks does not affect reproductive performance of male Wistar rats