Abstract Background: The therapeutic arsenal for the treatment of Leishmaniasis is limited and includes toxic compounds (antimonials, amphotericin B, pentamidine and miltefosine). Given these aspects, the search for new compounds based on floristic biodiversity is crucial. In the present work, we report the isolation, characterization and antileishmanial activity of six related neolignans (1–6) of bioactive extract from Nectandra leucantha (Lauraceae) twigs. Methods: Dried and powdered twigs of N. leucantha were exhaustively extracted using n-hexane. The crude extract was dereplicated by HPLC/HRESIMS and subjected to column chromatography to yield pure compounds 1–6. Their chemical structures were identified via NMR and comparison of obtained data with those previously published in the literature. Biological assays of compounds 1–6 and their respective monomers (eugenol and methyleugenol) were performed using promastigote and amastigote forms of Leishmania (L.) infantum. Results: Dereplication procedures followed by chemical characterization of isolated compounds by NMR enabled the identification of related neolignans 1–6. Neolignans 2, 4 and 6 showed potential against amastigote forms of L. (L.) infantum (EC50 values of 57.9, 67.7 and 13.7 μM, respectively), while compounds 1 and 3 were inactive. As neolignans 2–4 are chemically related, it may be suggested that the presence of the methoxyl group at C4 constitutes an important structural aspect to increase antileishmanial potential against amastigote forms. Compound 6, which consists of a methylated derivative of compound 5 (inactive) showed antileishmanial activity similar to that of the standard drug miltefosine (EC50 =16.9 μM) but with reduced toxicity (SI = 14.6 and 7.2, respectively). Finally, two related monomers, eugenol and methyleugenol, were also tested and did not display activity, suggesting that the formation of dimeric compounds by oxidative coupling is crucial for antiparasitic activity of dimeric compounds 2, 4 and 6. Conclusion: This study highlights compound 6 against L. (L.) infantum amastigotes as a scaffold for future design of new compounds for drug treatment of visceral leishmaniasis.

Resumo A Mata Atlântica é reconhecida como um bioma rico em biodiversidade. Plantas de cambuci (Campomanesia phaea) produzem frutas que podem ser consumidas nas formas frescas e processadas, mas ainda são subutilizadas. O objetivo deste estudo foi descrever as características físico-químicas e os compostos bioativos em frutos de cambuci oriundos da Mata Atlântica brasileira, localizado na cidade de Natividade da Serra-SP, Brasil. Frutos de cambuci de cinquenta e nove acessos foram caracterizados de acordo com o peso fresco, o rendimento da polpa, a porcentagem de casca, os diâmetros longitudinal e transversal (DL e DT, respectivamente), o pH, o teor de sólidos solúveis (TSS), a acidez titulável (AT), a relação TSS/AT, o ácido ascórbico,os teores de compostos fenólicos totais e a atividade antioxidante, pelo método de DPPH. Os teores de sólidos solúveis variaram de 5,10 °Brix a 11,00 °Brix. A acidez titulável variou de 1,29 a 2,90 g de ácido citrico 100 g-1. O teor de ácido ascórbico foi de 31,12 a 139,38 mg 100 g-1. Os compostos fenólicos totais variaram de 330,5 mg GAE 100 g-1 a 3.526,04 mg GAE 100 g-1. A atividade antioxidante foi de 65,03 µmol Trolox g-1 de polpa de fruta (peso fresco) para 199,78 µmol Trolox g-1 de polpa de fruta (peso fresco), fator de 6.7 de diferença entre os extremos. Estes resultados demonstram que os frutos de cambuci se apresentam como uma fonte rica de ácido ascórbico, de compostos fenólicos totais e com alta capacidade antioxidante.

Abstract The Atlantic Forest is recognized as a biome rich in biodiversity. Cambuci trees (Campomanesia phaea) produce fruits that may be consumed as both fresh and processed forms but are still underutilized. The aim of this study was to describe the physicochemical characteristics and bioactive compounds in cambuci fruits from Brazilian Atlantic Forest, located at Natividade da Serra-SP, Brazil. Cambuci fruits of the fifty-nine accessions were characterized according to fresh weight, pulp yield, peel percentage, longitudinal and transversal diameters (LD and TD, respectively), pH, soluble solids content (SSC), titratable acidity (TA), SSC/TA ratio, ascorbic acid, total phenolic compounds content, and antioxidant activity using the DPPH assay. The soluble solids contents varied from 5.10 °Brix to 11.00 °Brix. The titratable acidity varied from 1.29 to 2.90 g citric acid 100 g-1. Ascorbic acid content was of 31.12 to 139.38 mg 100 g-1. Total phenolic compounds varied from 330.5 mg GAE 100 g-1 to 3,526.04 mg GAE 100 g-1. The antioxidant activity was of 65.03 µmol Trolox g-1 fruit pulp (fresh weight) to 199.78 µmol Trolox g-1 fruit pulp (fresh weight), a factor of 6.7 difference between the extremes. These results showed cambuci fruits presented as rich source of ascorbic acid, total phenolic compounds, and with high antioxidant capacity.

O sistema de ventilação natural facilita as trocas gasosas, em plantas cultivadas in vitro, ocasiona mudanças no tecido foliar, as quais podem ser avaliadas pela anatomia foliar, e possibilita um cultivo mais próximo ao da micropropagação fotoautotrófica. Este trabalho teve por objetivo avaliar os efeitos no crescimento in vitro e na anatomia foliar de Cattleya walkeriana, cultivadas em sistemas de ventilação natural e convencional, com diferentes concentrações de sacarose. As plantas receberam concentrações variadas de sacarose (0, 15, 30 e 45 g L-1), em combinação com diferentes sistemas de cultivo (micropropagação convencional e sistema de ventilação natural). O meio de cultura foi composto pelos sais do meio MS, solidificado com 7 g L-1 de ágar, sendo o pH ajustado para 5,8. Foram distribuídos 40 mL de meio de cultura, em frascos de 250 mL de conteúdo, os quais foram autoclavados, a 120 ºC, por 20 minutos. O maior crescimento das plantas, bem como a maior espessura do mesofilo, foram observados, com emprego de 20 g L-1 de sacarose, em sistema de ventilação natural. As plantas cultivadas em sistema de ventilação natural apresentaram maior espessura do mesofilo foliar, resposta diretamente relacionada com cultivos fotoautotróficos. O sistema de ventilação natural proporcionou estômatos com o formato mais elípticos e, possivelmente, mais funcionais.

Natural ventilation system facilitates gaseous exchanges in in vitro plants promoting changes in the leaf tissue, which can be evaluated through the leaf anatomy, and it allows a cultivation closer to the photoautrophic micropropagation. The objective of this work was to evaluate the effects on in vitro growth and on the leaf anatomy of Cattleya walkeriana grown in natural and conventional ventilation system with different concentrations of sucrose (0; 15; 30 and 45 L-1) combined with different cultivation systems (conventional micropropagation and natural ventilation system). The culture medium was composed of MS salts, solidified with 7 g L-1 of agar and pH adjusted to 5.8. Forty milliliters of culture medium were distributed in 250 mL flasks, autoclaved at 120 ºC for 20 minutes. The greater plant growth, as well as the greater thickness of the mesophyll was observed with the use of 20 g L-1 sucrose in natural ventilation system. Plants grown in natural ventilation system showed a thicker leaf mesophyll, which is directly related to photoautotrophic crops. The natural ventilation system induced more elliptical stomata and probably more functional formats.

The objective of this work was to evaluate the effects of protein and/or starch supplementation on the nutritional performance of cattle grazing on low-quality tropical forage. Five crossbred steers (Holstein × Gyr) with an average body weight (BW) of 397 kg that were fitted with ruminal and abomasal cannulae were used. The animals were kept in individual signal-grass (Bracharia decumbens) paddocks. Five treatments were evaluated: 1 - control (without supplementation); 2 - supplementation with 1 g of crude protein (CP) per kg of BW; 3 - supplementation with 2.5 g of starch per kg of BW; 4 - supplementation with CP and starch as described for treatments 2 and 3; and 5 - supplementation as described for treatment 4 but replacing the corn starch with a mixture of corn starch and nitrogenous compounds, thereby resulting in an energy supplement of 150 g CP/kg of dry matter. The experiment was performed according to a 5 × 5 Latin square design in a 2 × 2 + 1 factorial arrangement. The forage intake was not affected by any of the factors evaluated in this study. The production of microbial nitrogen in the rumen was not affected by nitrogen or starch supplementation. The apparent nitrogen balance was only increased when both starch and nitrogen were supplied. Supplementation with both starch and nitrogenous compounds for cattle grazing on low-quality tropical forage is characterized by an interactive metabolic effect that increases nitrogen accretion by the animals.

The effects of liquid vinasse (LV) in the diet for growing rabbits on performance, carcass yield and intestinal morphometry were assessed. Eighty New Zealand white rabbits were used in a randomized block design with five treatments (LV inclusion at 0, 25, 50, 75 and 100 g/kg diet) and four replications. There was no effect of the treatment on final weight, daily weight gain, mortality rate and carcass yield characteristics. The daily intakes of feed, dry matter, crude protein and energy and feed conversion decreased linearly with increase in LV in the diet. Including LV affected the duodenum crypt depth and the ilium villus perimeter and height linearly and affected the duodenum villus perimeter, height and the absorption surfaces and ilium crypt depth and absorption surface quadratically. There was no effect of including LV on jejunum morphometry. Vinasse can be used to feed growing rabbits at up to 87.8 g per kilogram of diet.

O objetivo deste estudo foi avaliar o efeito da inoculação dos fungos micorrízicos arbusculares (FMAs) e rizóbio no enraizamento, crescimento e nutrição de mudas de angico-vermelho (Anadenanthera macrocarpa (Benth) Brenan) propagadas via miniestaquia. Foram utilizadas seis progênies, das quais foram confeccionadas miniestacas com um par de folhas inteiras, bem como tubetes de 55 cm³ contendo substrato comercial Bioplant®. Foram testados quatro tratamentos: 8 kg m-3 de superfosfato simples (SS) misturados ao substrato; 4 kg m-3 de SS misturados ao substrato; 4 kg m-3 de SS misturados ao substrato e adição de suspensão contendo rizóbios; e 4 kg m-3 de SS e adição de suspensão contendo rizóbios e 5 g de solo contendo esporos de FMAs. Não houve interação entre os tratamentos para percentagem de sobrevivência das miniestacas e percentagem de miniestacas com raízes observadas na extremidade inferior do tubete, na saída da casa de vegetação (30 dias) e da casa de sombra (40 dias), provavelmente em função do sistema radicular ainda estar em formação. Houve diferenças entre as progênies para percentagem de sobrevivência das miniestacas, percentagem de miniestacas com raízes observadas na extremidade inferior do tubete, altura, diâmetro de colo e massa seca da parte aérea. As avaliações das características de crescimento das miniestacas enraizadas, principalmente com relação à sobrevivência a pleno sol (140 dias), evidenciam a eficiência dos rizóbios e FMAs na produção de mudas desta espécie. Conclui-se que a associação simbiótica com rizóbio e/ou FMA favorece a produção de mudas de A. macrocarpa via miniestaquia.

The objective of this study was to evaluate the effect of inoculation of arbuscular mycorrhizae fungi (AMF) and rhizobium on rooting, growth and nutrition of seedlings of angico-red (Anadenanthera macrocarpa (Benth) Brenan) propagated by minicutting. Six progenies were used, of which were prepared cuttings with a pair of complete leaves. It was used a 55 cm³container filled with commercial substrate Bioplant®. Four treatments were tested: 8 kg m-3 of superphosphate (SS) added to substrate; 4 kg m-3 SS added to substrate; 4 kg m-3 SS added to substrate and adition of a suspension solution containing rhizobium; 4 kg m-3 SS and suspension solution containing rhizobium plus 5 g of soil contaminated by AMF spores. There was no interaction among treatments for survival rate of cuttings and roots observed at bottom of the container, evaluated in the greenhouse exit (30 days) and the shade house exit (40 days), probably because the root system was still in formation. There were differences among the progeny for survival rate of the shoots, the percentage of cuttings with roots observed at bottom of the container, height, stem diameter and shoot dry weight. The evaluations of the growth characteristics of the cuttings in, particularly with respect to survival at full sun (140 days), demonstrate the efficiency of rhizobium and AMF on seedling production of this species. We conclude that the symbiotic association with rhizobium and / or FMA favors the production of seedlings of A. macrocarpa by minicutting.

OBJETIVO: Investigar a influência do uso da sinvastatina na fibrose peritoneal induzida em ratos pelo uso de solução de diálise peritoneal rica em glicose. MÉTODOS: Estudo prospectivo controlado, em ratos Wistar não urêmicos. Foram estudados 20 animais. Os animais foram submetidos diariamente à punção abdominal, sendo infundida solução de diálise peritoneal com glicose a 4,25% na dose de 10 ml/100 g de peso. Os animais foram divididos em dois grupos: experimental e controle. O grupo experimental recebeu sinvastatina na dose de 4 mg/kg/dia por gavagem. O grupo controle não recebeu nenhuma droga. Foram acompanhados por 21 e 49 dias. Ao final do período foram submetidos à procedimento cirúrgico para retirada de peritônio parietal e visceral. As amostras obtidas foram analisadas histologicamente, usando-se coloração Hematoxilina - Eosina e Sirius Red, para avaliação do grau de fibrose. RESULTADOS: A análise mostrou que a intensidade da fibrose, a espessura do peritônio e o número de células não atingiram diferença estatisticamente significante entre os grupos experimental e controle. CONCLUSÃO: A sinvastatina não foi capaz de alterar a intensidade da fibrose peritoneal induzida pelo uso de solução de diálise em ratos.

PURPOSE: To investigate the influence of using simvastatin on the peritoneal fibrosis induced in rats using peritoneal dialysis solution with glucoses 4.25%. METHODS: Prospective controlled study in 20 non-uremic Wistar rats. The animals received a peritoneal infusion of 10 ml/100 g of peritoneal dialysis solution glucose 4.25% on a daily basis. The animals were divided in two groups: experimental and control. The experimental group received simvastatin 4 mg/kg/d, by a gastric tube. The control group did not receive any drug. The follow-up was 21 and 49 days. At the end, one surgical procedure was performed to get histological samples of visceral and parietal peritoneum. The samples were analyzed using Hematoxylin Eosin and Sirius Red, to evaluate the severity of the fibrosis. RESULTS: The analysis showed that the intensity of the fibrosis, the peritoneal thickness and the cell number in experimental and control groups were not statistically significant different in experimental and control groups. CONCLUSION: The simvastatin do not decrease the intensity of fibrosis on the peritoneal membrane that happens on rats on peritoneal dialysis.

The emergence of strains of Schistosoma resistant to praziquantel has drawn attention to the search for new schistosomacide drugs. Imidazolidinic derivatives have performed outstandingly against adult S. mansoni worms when evaluated in vitro. The molecular modification of imidazolidine by way of bioisosteric replacement gives rise to variations in its biological response. This study verifies the potential of substituent groups in the derivatives (Z)3-benzyl-5-(2-fluoro-benzylidene)-imidazolidine-2,4-dione NE4, 3-benzyl-5-(4-chloro-arylazo)-4-thioxo-imidazolidin -2-ona PT5, 3-benzyl-5-(3-fluoro-benzylidene)-1-methyl-2-thioxo-imidazolidin-4-one JT53; 3-benzyl-1-methyl-5-(4-methyl-benzylidene)-2-thioxo-imidazolidin-4-one JT63; 3-benzyl-1-methyl-5-(4-methoxi-benzylidene)-2-thioxo -imidazolidin-4-one JT68; 3-(4-chloro-benzyl)-1-methyl-5-(4-methoxi-benzylidene)-2-thioxo-imidazolidin-4-one JT69; 3-(4-phenyl-benzyl)-1-methyl-5-(4-methoxi-benzylidene)-2-thioxo-imidazolidin-4-one JT72 by determining the viability in vitro of adult S. mansoni worms in the presence of these derivatives. The susceptibility of the worms obtained from mice and kept in culture in the presence of different concentrations was determined by way of schistosomacide kinetic, observed every 24 h over a period of eight days. The results show that the worms were more sensitive to the PT5 derivative at a concentration of 58 µM which killed 100% of the worms after 24 h of contact, also giving rise to alterations in the tegument surface of the worms with the formation of bubbles and peeling. These observations suggest a strong electronic contribution of the arylazo grouping in the biological response.