Structure-activity relationship of compounds which are anti-schistosomiasis active

O método do orbital molecular AM1 foi empregado para calcular um conjunto de descritores moleculares para vinte neolignanas sintéticas com atividade anti-esquistossomose. O método de reconhecimento de padrão (análise de componentes principais ACP, análise de conglomerados AC e análise de discriminante) foi utilizado para obter a relação entre a estrutura molecular e a atividade biológica. O conjunto de moléculas foi classificado em dois grupos de acordo com seus graus de atividade biológica. Estes resultados permitem que, projete-se racionalmente novos compostos, potenciais candidatos à síntese e à avaliação biológica.

A structure-activity relationship (SAR) study of neolignan compounds with anti-schistosomiasis activity

Um conjunto de dezoito compostos de neolignanas com atividade antiesquistossomose foi estudado com o método semi-empírico PM3 e outros métodos teóricos com o intuito de avaliar algumas propriedades (variáveis ou descritores) moleculares selecionadas e correlacioná-las com a atividade biológica. Análise exploratória dos dados (análise de componentes principais, PCA, e análise hierárquica de agrupamentos, HCA), análise discriminante (DA) e o método KNN foram utilizados na obtenção de possíveis correlações entre os descritores calculados e a atividade biológica em questão e na predição da atividade antiesquistossimose de algumas moléculas teste. Os descritores moleculares responsáveis pela separação entre os compostos ativos e inativos foram: energia de hidratação (HE), refratividade molecular (MR) e carga sobre o átomo C19 (Q19). Estes descritores fornecem informações a respeito do tipo de interação que pode ocorrer entre os compostos e seu respectivo receptor biológico. Após a construção do modelo para compostos ativos e inativos, os métodos PCA, HCA, DA e KNN foram empregados em um estudo de predição. Foram estudados 10 novos compostos e somente 5 deles foram classificados como ativos contra esquistossomose.

Fatores físicos e idade da matriz na incubação de ovos de codornas japonesas (Coturnix coturnix japonica)

Pós-graduação em Zootecnia - FCAV

In vitro evaluation of permeation, toxicity and effect of praziquantel-loaded solid lipid nanoparticles against Schistosoma mansoni as a strategy to improve efficacy of the schistosomiasis treatment

Coordenação de Aperfeiçoamento de Pessoal de Nível Superior (CAPES)

Assessing Paternity in Japanese Quails (Coturnix Japonica) Using Microsatellite Markers - Inferences for Its Mating System and Reproductive Success

Conselho Nacional de Desenvolvimento Científico e Tecnológico (CNPq)

Nanostructured Lipid Carriers as a Strategy to Improve the In Vitro Schistosomiasis Activity of Praziquantel

Praziquantel (PZQ) is a pyrazinoisoquinoline anthelmintic that was discovered in 1972 by Bayer Germany. Currently, due to its efficacy, PZQ is the drug of choice against all species of Schistosoma. Although widely used, PZQ exhibits low and erratic bioavailability because of its poor water solubility. Nanostructured lipid carriers (NLC), second-generation solid lipid nanoparticles, were developed in the 1990s to improve the bioavailability of poorly water soluble drugs. The aim of this study was to investigate nanostructured lipid carriers as a strategy to improve the efficacy. of PZQ in S. mansoni treatment. We prepared NLC2 and NLC4 by adding seventy percent glycerol monostearate (GMS) as the solid lipid, 30% oleic acid (OA) as the liquid lipid and two surfactant systems containing either soybean phosphatidylcholine/poloxamer (PC/P-407) or phosphatidylcholine/Tween 60 (PC/T60), respectively. The carriers were characterized by nuclear magnetic resonance, differential scanning calorimetry, thermogravimetric analysis and Fourier transform-infrared spectroscopy. The safety profile was evaluated using red cell hemolysis and in vitro cytotoxicity assays. The results showed that the encapsulation of PZQ in NLC2 or NLC4 improved the safety profile of the drug. Treatment efficacy was evaluated on the S. mansoni BH strain. PZQ-NLC2 and PZQ-NLC4 demonstrated an improved efficacy in comparison with free PZQ. The results showed that the intestinal transport of free PZQ and PZQ-NLC2 was similar. However, we observed that the concentration of PZQ absorbed was smaller when PZQ was loaded in NLC4. The difference between the amounts of absorbed PZQ could indicate that the presence of T60 in the nanoparticles (NLC4) increased the rigid lipid matrix, prolonging release of the drug. Both systems showed considerable in vitro activity against S. mansoni, suggesting that these systems may be a promising platform for the administration of PZQ for treating schistosomiasis.

Há associação entre desempenho sexual e vocalização em codornas japonesas (Coturnix japonica)?

O presente trabalho teve como objetivos relacionar o desempenho sexual das codornas japonesas com o canto, nos machos. Foi determinado o perfil de comportamento sexual das codornas e foi constatado que os machos apresentam diferenças individuais conspícuas entre os grupos de maus e bons copuladores. Foi descrito também a taxa de vocalização e determinados os parâmetros acústicos, entretanto mostraram-se semelhantes entre os grupos testados, apesar de apresentarem diferenças na estrutura sonográfica. Houve diferenças no índice gonadossomático entre os dois perfis, porém não se mostraram significativos. Não houve correlação entre o desempenho sexual de machos de codorna japonesa e a taxa de vocalização, apesar de uma tendência dos bons copuladores cantarem mais freqüentemente

Efeito do fornecimento de diferentes níveis de alumínio dietético na qualidade óssea de codornas poedeiras (Coturnix japonica)

O alumínio está presente de forma marcante em nosso cotidiano, com várias possibilidades de contaminação para o ser humano e animais, através da ingestão de alimentos ou aditivos presentes nos alimentos ou, também, através do uso de medicamentos. Por apresentar uma forte carga elétrica, um forte poder de polarização e características similares com elementos da hidroxiapatita, o alumínio age como um competidor de nutrientes na matriz óssea, Por isso, ele pode ser causa danos à saúde dos seres vivos, como a osteoporose. Diante disso, a presente pesquisa teve como objetivos estudar a influência de diferentes níveis de alumínio na dieta de codornas poedeiras, sobre as características físicas e químicas de seus ossos. A densidade e a porosidade óssea foram determinadas pelo método de imersão em água, utilizando o princípio de Arquimedes. Os resultados obtidos mostraram que concetrações até 20 mg de alumínio por kg de ração fornecida causa uma diminuição na densidade óssea e volta a aumentar para concetrações maiores que este limiar. A porosidade óssea, segue o inverso da densidade. Ela aumenta com concetrações até 20 mg de alumínio por kg de ração fornecida e volta a diminuir para concetrações menores

Turnover do carbono em sangue e plasma, nas fases crescimento e postura, de codornas japonesas (Coturnix coturnix japonica)

Fundação de Amparo à Pesquisa do Estado de São Paulo (FAPESP)

Comparison of growth curve parameters of organs and body components in meat- (Coturnix coturnix coturnix) and laying-type (Coturnix coturnix japonica) quail show interactions between gender and genotype

The objective of this study was to estimate growth parameters of carcass components (wing, thighs and drumsticks, back and breast) and organs (heart, liver, gizzard and gut) in males and females of one meat-type quail strain (Coturnix coturnix coturnix) and two laying strains (Coturnix coturnix japonica) designated either yellow or red.A total of 1350 quail from 1 to 42d old were distributed in a completely randomised design, with 5 replicates of each strain. The carcass component weights and body organs were analysed weekly and evaluated using the Gompertz function; growth rates were evaluated through derivative equations.The meat-type strain presented the highest growth rates in carcass components and organs. Across strains, females showed the highest weight of internal organs at maturity compared to males.Females had greater growth potential in breast, wings and back than males for both yellow and red laying quail.

Pseudotumoral form of cerebral Schistosomiasis Mansoni

The authors report a case of 36-year-old woman presented with epileptic seizures and headaches. Magnetic resonance imaging (MRI) revealed an enhancing lesion with surrounding edema and mild mass effect in the left frontal lobe. Stereotactic brain biopsy demonstrated intraparenchymal granulomas surrounding S. mansoni eggs. Praziquantel was started (60mg/kg of body weight, in a single dose), followed by Prednisone (80mg/day) for seven days to treat the cerebral edema. The patient's symptoms resolved following medical treatment and the follow-up MRI yielded normal findings.

Effectiveness of hyperbaric oxygen for experimental treatment of schistosomiasis mansoni using praziquantel-free and encapsulated into liposomes: Assay in adult worms and oviposition

The treatment of schistosomiasis depends on a single drug: praziquantel (PZQ). However, this treatment presents limitations such as low and/or erratic bioavailability that can contribute to cases of tolerance. Improvements to the available drug are urgently needed and studies with a controlled system of drug release, like liposomes, have been gaining prominence. The present study evaluated the activity and synergy between liposomal-praziquantel (lip.PZQ) and hyperbaric oxygen therapy (HBO). Mice received doses of 60 or 100mg/kg PZQ or lip.PZQ, 50 days post-infection, and after the treatment, were exposed to HBO (3 atmosphere absolute - ATA) for 1h. The viability of adult worms and oviposition were analyzed, by necropsy and Kato-Katz examination performed after 15 days of treatment. A concentration of 100mg/kg of lip.PZQ+HBO was more effective (48.0% reduction of worms, 83.3% reduction of eggs/gram of feces) and 100% of the mice had altered of oograms (indicating interruption of oviposition) compared to other treatments and to the Control group (infected and untreated). It is known that PZQ requires participation of the host immune system to complete its antischistosomal activity and that HBO is able to stimulate the immune system. The drug became more available in the body when incorporated into liposomes and, used with HBO, the HBO worked as an adjuvant. This explains the decreases of oviposition and worms recovered form hepatic portal system.

Turnover do δ¹³C na substituição de dietas com ingredientes de diferentes ciclos fotossintéticos em ovos de codornas japonesas (Coturnix coturnix japonica)

Fundação de Amparo à Pesquisa do Estado de São Paulo (FAPESP)

Distribution of North Pacific right whales (Eubalaena japonica) as shown by 19th and 20th century whaling catch and sighting records

North Pacific right whales (Eubalaena japonica) were extensively exploited in the 19th century, and their recovery was further retarded (severely so in the eastern population) by illegal Soviet catches in the 20th century, primarily in the 1960s. Monthly plots of right whale sightings and catches from both the 19th and 20th centuries are provided, using data summarized by Scarff (1991, from the whale charts of Matthew Fontaine Maury) and Brownell et al. (2001), respectively. Right whales had an extensive offshore distribution in the 19th century, and were common in areas (such as the Gulf of Alaska and Sea of Japan) where few or no right whales occur today. Seasonal movements of right whales are apparent in the data, although to some extent these reflect survey and whaling effort. That said, these seasonal movements indicate a general northward migration in spring from lower latitudes, and major concentrations above 40°N in summer. Sightings diminished and occurred further south in autumn, and few animals were recorded anywhere in winter. These north-south migratory movements support the hypothesis of two largely discrete populations of right whales in the eastern and western North Pacific. Overall, these analyses confirm that the size and range of the right whale population is now considerably diminished in the North Pacific relative to the situation during the peak period of whaling for this species in the 19th century. For management purposes, new surveys are urgently required to establish the present distribution of this species; existing data suggest that the Bering Sea, the Gulf of Alaska, the Okhotsk Sea, the Kuril Islands and the coast of Kamchatka are the areas with the greatest likelihood of finding right whales today.

The Role of Target Therapies in Schistosomiasis-Associated Pulmonary Arterial Hypertension

Background: Schistosomiasis-associated pulmonary arterial hypertension (Sch-PAH) may be one of the most prevalent forms of pulmonary arterial hypertension (PAH) worldwide. However, the clinical and hemodynamical response to specific PAH therapy in Sch-PAH is not known. Methods: We retrospectively analyzed the charts of all patients with Sch-PAH who initiated specific PAH treatment between June 2003 and June 2010 in a single PAH reference center in Sao Paulo, Brazil. Clinical and hemodynamical data were retrospectively collected and evaluated in two periods: baseline and posttreatment. Results: The study population consisted of 12 patients with Sch-PAH. They were treated with phosphodiseterase-5 inhibitors (seven patients), endothelin receptor antagonists (four patients), or combination therapy (one patient). Mean treatment period was 34.9 +/- 15.5 months. Patients with Sch-PAH presented significant improvements in terms of functional class, 6-min walk test distance (439 +/- 85 to 492 +/- 79 m, P = .032), cardiac index (2.66 +/- 0.59 to 3.08 +/- 0.68 L/min/m(2), P = .028), and indexed pulmonary vascular resistance (20.7 +/- 11.6 to 15.9 +/- 9 W/m(2), P = .038) with the introduction of specific PAH treatment. Conclusions: We conclude that specific PAH therapy may be of benefit to patients with Sch-PAH, considering clinical, functional, and hemodynamic parameters. CHEST 2012; 141(4):923-928