Understanding how management can prevent degradation of the structurally fragile soils of the Amazonian periphery.

The dynamics and responses to mulching management processes, which affect sustainability in tropical agroecosystems, remain poorly understood. Therefore, this study aims to evaluate and distinguish the short-and long-term effects of mulch of leguminous biomass on fertility of a tropical soil enriched with calcium. This experiment was conducted using the treatments: Long-term mulching (LTM) consisted of planting without mulch in 2019 in soil that had been mulched for six years previously, while short-term mulching (STM) consisted of planting without mulch for six years and with mulch only in 2019. LTM + STM consisted of planting in mulched soil for seven years (from 2013 to 2019), while LTM + synthetic nitrogen (LTM + sN) consisted of the LTM treatment with the addition of 150 kg N ha-1. The remaining treatments were STM + sN; LTM + STM + sN; bare soil with sN, and bare soil without sN as control. In areas with LTM the interactions between products derived from biomass, sN, and Ca resulted in higher total SOC and BS, while STM maintained soil moisture, decreased penetration resistance, and enhanced N uptake providing biological nitrogen able to replace sN for maize nutrition. The positive effects of short- and long-term mulching were cumulative as they increased accumulated N by maize in 163%, and maize grain yield by 125% (4.77-10.78 Mg ha-1) compared to cultivation with sN without mulch. Our results showed that interactions between continuos mulch of leguminous biomass, Ca and sN prevent degradation of agricultural land in Amazonian conditions. Therefore, this combination must be recommended to prevent Amazonian soil management, which in turn reduces the risk of new deforestation in Amazonian periphery.

Naphthoquinone Derivatives Targeting Melanoma.

Cancer is responsible for high mortality rates worldwide, representing a serious health problem. In this sense, melanoma corresponds to the most aggressive type of skin cancer, being the cause of the highest death rates. Therapeutic strategies for the treatment of melanoma remain limited, with problems associated with toxicity, serious side effects, and mechanisms of resistance. The potential of natural products for the prevention and treatment of melanoma has been reported in different studies. Among these compounds, naphthoquinones (1,2-naphthoquinones and 1,4-naphthoquinones) stand out for their diverse pharmacological properties, including their antitumor activity. Thus, this review covers different studies found in the literature on the application of natural naphthoquinones targeting melanoma, providing information regarding the mechanisms of action investigated for these compounds. Finally, we believe that this review provides a comprehensive basis for the use of natural naphthoquinones against melanoma and that it may contribute to the discovery of promising compounds, specifically naphthoquinones, aimed at the treatment of this cancer.

Natural Coumarin Derivatives Targeting Melanoma.

In general, a cancerous process starts from uncontrolled cell growth, apoptosis, and rapid proliferation of cellular clones, as well as, reactive oxygen species (ROS) and imbalance of ROS-antioxidant production also could be involved in the genesis of the disease. Cancer has accounted for millions of deaths worldwide every year, representing a relevant threat to human lives. In this context, malignant melanoma represents the most aggressive and deadliest type of cancer, leading to increased rates of patient deaths. Natural active compounds have demonstrated their pharmacological benefits in several different studies. Among these compounds, coumarin analogs have demonstrated promising biological profiles, considering their efficacy and low toxicity. In this context, this phytochemical oxygenated core has been broadly investigated since it presents several biological properties of interest in the medicinal field. Herein, we reported a complete compilation of studies focused on natural coumarins against melanoma, as well as, tyrosinase since it is a cooper-catalyzed oxidase that performs an essential role during melanogenesis (Eu-melanins and Pheo-melanins), which is associated with melanoma. Thus, three different subclasses of natural coumarin were described in detail, such as simple coumarin core, furanocoumarins, pyranocoumarins, and pyrone-substituents. Additionally, insights on tyrosinase have been provided, allowing an overview of some structural/functional aspects of its enzyme, such as the presence of a binuclear type 3 cooper coordination at the binding site of this target, acting as cofactors. Posteriorly, several coumarin-based analogs with anti-tyrosinase activity also were reported and discussed. Finally, we believe that unprecedented review can be a valuable source of information, which can be used to design and develop novel coumarin-based analogs targeting melanoma and also tyrosinase enzyme, contributing to the advances in the field of natural products.

Coumarin-Based Compounds as Inhibitors of Tyrosinase/Tyrosine Hydroxylase: Synthesis, Kinetic Studies, and In Silico Approaches.

Cancer represents the main cause of morbidity and mortality worldwide, constituting a serious health problem. In this context, melanoma represents the most aggressive and fatal type of skin cancer, with death rates increasing every year. Scientific efforts have been addressed to the development of inhibitors targeting the tyrosinase enzyme as potential anti-melanoma agents due to the importance of this enzyme in melanogenesis biosynthesis. Coumarin-based compounds have shown potential activity as anti-melanoma agents and tyrosinase inhibitors. In this study, coumarin-based derivatives were designed, synthesized, and experimentally evaluated upon tyrosinase. Compound FN-19, a coumarin-thiosemicarbazone analog, exhibited potent anti-tyrosinase activity, with an IC50 value of 42.16 ± 5.16 µM, being more active than ascorbic acid and kojic acid, both reference inhibitors. The kinetic study showed that FN-19 acts as a mixed inhibitor. Still, for this compound, molecular dynamics (MD) simulations were performed to determine the stability of the complex with tyrosinase, generating RMSD, RMSF, and interaction plots. Additionally, docking studies were performed to elucidate the binding pose at the tyrosinase, suggesting that the hydroxyl group of coumarin derivative performs coordinate bonds (bidentate) with the copper(II) ions at distances ranging from 2.09 to 2.61 Å. Then, MM/PBSA calculations revealed that van der Waals interactions are the most relevant intermolecular forces for complex stabilization. Furthermore, it was observed that FN-19 has a binding energy (ΔEMM) value similar to tropolone, a tyrosinase inhibitor. Therefore, the data obtained in this study will be useful for designing and developing novel coumarin-based analogs targeting the tyrosinase enzyme.

Hybrid-Compounds Against Trypanosomiases.

Neglected tropical diseases (NTDs) are a global public health problem associated with approximately 20 conditions. Among these, Chagas disease (CD), caused by Trypanosoma cruzi, and human African trypanosomiasis (HAT), caused by T. brucei gambiense or T. brucei rhodesiense, affect mainly the populations of the countries from the American continent and sub- Saharan Africa. Pharmacological therapies used for such illnesses are not yet fully effective. In this context, the search for new therapeutic alternatives against these diseases becomes necessary. A drug design tool, recently recognized for its effectiveness in obtaining ligands capable of modulating multiple targets for complex diseases, concerns molecular hybridization. Therefore, this review aims to demonstrate the importance of applying molecular hybridization in facing the challenges of developing prototypes as candidates for the treatment of parasitic diseases. Therefore, studies involving different chemical classes that investigated and used hybrid compounds in recent years were compiled in this work, such as thiazolidinones, naphthoquinones, quinolines, and others. Finally, this review covers several applications of the exploration of molecular hybridization as a potent strategy in the development of molecules potentially active against trypanosomiases, in order to provide information that can help in designing new drugs with trypanocidal activity.

Um mapeamento de teses e dissertações sobre ginástica rítmica no Brasil / A mapping of theses and dissertations about rhythmic gymnastics in Brazil / Un mapeo de tesis y disertaciones sobre la gimnasia rítmica en Brasil

A Ginástica Rítmica tem crescido dentro dos países e tem instigado novas produções científicas. Diante disso, o presente estudo tem como objetivo identificar o perfil das teses e dissertações sobre a modalidade indexadas em bases de dados nacionais. O caminho metodológico percorrido possui caráter exploratório e descritivo. Procurou-se evidenciar e caracterizar as instituições envolvidas nas produções sobre a modalidade e identificar quais são os enfoques temáticos. O escopo do estudo foi composto por 42 produções referentes exclusivamente à Ginástica Rítmica, no período de 1988-2019. Encontrou-se assuntos vinculados à saúde, treinamento, história, estética e formação profissional. Esses cinco assuntos encontrados foram analisados através do Modelo Analítico dos 5E's de Marchi Júnior (2015). Ao final, o presente estudo pôde contribuir com o meio acadêmico ao mapear as teses e dissertações que abordam unicamente a Ginástica Rítmica no Brasil, evidenciando as vertentes menos investigadas e, assim, passíveis de serem temas de novas pesquisas.

Rhythmic Gymnastics has grown within the countries and has instigated new scientific productions. Therefore, this study aims to identify the profile of theses and dissertations on the sport indexed in national databases. The methodological path followed has an exploratory and descriptive character. It was tried to evidence and characterize the institutions involved in the productions about the modality and to identify which are the thematic focuses. The scope of the study was composed of 42 productions related exclusively to Rhythmic Gymnastics, in the period 1988-2019. Subjects related to health, training, history, aesthetics and professional training were found. These five subjects found were analyzed through the 5E's Analytical Model of Marchi Júnior (2015). In the end, this study could contribute to the academic environment by mapping the theses and dissertations that address only the Rhythmic Gymnastics in Brazil evidencing the less investigated aspects and, thus, likely to be subjects of new researches.

La Gimnasia Rítmica ha crecido dentro de los países y ha impulsado nuevas producciones científicas. Por lo tanto, este estudio tiene como objetivo identificar el perfil de las tesis y disertaciones sobre el deporte indexado en las bases de datos nacionales. El camino metodológico seguido tiene un carácter exploratorio y descriptivo. Se trató de evidenciar y caracterizar las instituciones involucradas en las producciones sobre la modalidad e identificar cuáles son los focos temáticos. El ámbito del estudio estuvo compuesto por 42 producciones relacionadas exclusivamente con la Gimnasia Rítmica, en el período 1988-2019. Se encontraron temas relacionados con la salud, el entrenamiento, la historia, la estética y la formación profesional. Estos cinco temas encontrados fueron analizados a través del Modelo Analítico de las 5E's de Marchi Júnior (2015). Al final, este estudio podría contribuir al ámbito académico mediante el mapeo de las tesis y disertaciones que abordan sólo la Gimnasia Rítmica en Brasil evidenciando los aspectos menos investigados y, por lo tanto, susceptibles de ser temas de nuevas investigaciones.

Novel Sustainable-by-Design HDAC Inhibitors for the Treatment of Alzheimer's Disease.

Alzheimer's disease (AD) represents a global problem, with an estimation of the majority of dementia patients in low- and middle-income countries by 2050. Thus, the development of sustainable drugs has attracted much attention in recent years. In light of this, taking inspiration from the HDAC inhibitor vorinostat (1), we develop the first HDAC inhibitors derived from cashew nut shell liquid (CNSL), an inexpensive agro-food waste material. CNSL derivatives 8 and 9 display a HDAC inhibitory profile similar to 1, together with a more promising safety for 9 compared to 1. Moreover, both compounds and particularly 9 were able to effectively modulate glial cell-induced inflammation and to revert the pro-inflammatory phenotype. All these results demonstrate that the use of inexpensive food waste materials could be successfully applied for the development of accessible and sustainable drug candidates for the treatment of AD.

Vivências no processo de parturição: antagonismo entre o desejo e o medo / Experiencias en el proceso de parturición: antagonismo entre el deseo y el miedo / Experiences on the childbirth process: antagonism between desire and fear

Objetivo: Discutir a vivência de mulheres no processo de parturição. Método: Estudo descritivo, qualitativo, realizado em um Centro Municipal de Saúde no Rio de Janeiro, em 2015, com 17 mulheres com até 42 dias de pós-parto. Empregou-se a técnica de entrevista semiestruturada e a técnica de análise de conteúdo na modalidade temático-categorial. Resultados: As participantes são multíparas, o parto realizado em maternidades públicas, e não receberam orientação no pré-natal sobre a parturição. Sentiram-se acolhidas, relacionaram a dor das contrações uterinas ao sofrimento físico, durante o trabalho de parto tiveram a opção de ingerir alimentos e água, adotaram a posição de litotomia, e o parceiro participou como acompanhante. Os profissionais de saúde, todavia, assumiram uma postura de controle sobre seus corpos no processo de parturição. Conclusão: Os resultados ratificam a importância de os casais serem orientados sobre a gestação e o parto, para que possam vivenciá-los de forma ativa e segura

Objective: To discuss the experience of women in the parturition process. Method: A descriptive, qualitative study conducted at a Municipal Health Center in Rio de Janeiro in 2015, with 17 women with up to 42 days postpartum. The technique of semi-structured interview was used, as well as the technique of content analysis in the thematic categorical modality. Results: Participants were multipara, childbirth occurred in public maternity hospitals, and they did not receive prenatal orientation on parturition. They felt welcomed, related the pain of uterine contractions to physical suffering, during labor they had the option of ingesting food and water, adopted the lithotomy position, and the partner participated as companion. Health professionals, however, took a controlling stance on their bodies in the parturition process. Conclusion: The results confirm the importance of couples being oriented on gestation and childbirth in order to experience childbirth in an active and safe way

Objetivo: Analizar la experiencia de mujeres en el proceso de parturición. Método: Estudio descriptivo, cualitativo, realizado en un Centro Municipal de Salud de Rio de Janeiro, en 2015, con 17 mujeres con hasta 42 días de posparto. Se utilizó la técnica de entrevista semiestructurada y la técnica de análisis de contenido en la modalidad temático-categorial. Resultados: Las participantes son multíparas, el parto realizado en maternidades públicas, y no recibieron orientación en el prenatal sobre la parturición. Se sintieron acogidas, vincularon el dolor de las contracciones uterinas AL sufrimiento físico, durante el trabajo de parto tuvieron la opción de ingerir alimentos y agua, adoptaron la posición de litotomía, y el compañero participó como acompañante. Los profesionales de salud, sin embargo, asumieron una postura de control sobre sus cuerpos en el proceso de parturición. Conclusión: Los resultados confirman la importancia de que las parejas reciban orientación sobre la gestación y el parto, para que puedan experimentar el parto de forma activa y segura

Inappropriate Prescribing in Older Hospitalized Adults: A Comparison of Medical Specialties.

OBJECTIVES: To evaluate the prevalence and number of potentially inappropriate medications (PIMs) in hospitalized older adults, comparing prescription patterns of medical specialties. DESIGN: Retrospective cohort study. SETTING: Tertiary general hospital. PARTICIPANTS: All older adults hospitalized from January through May 2015 (N = 1,900). MEASUREMENTS: Information on medications prescribed during the first and last days of hospitalization was collected and evaluated regarding PIMs using Beers and Screening Tool of Older People's Prescriptions (STOPP) criteria. Medical specialties (internal medicine, cardiology, gastroenterology, infectious disease, nephrology, neurology, pneumology) were compared regarding the prevalence of PIMs and the increase in the number of PIMs during hospitalization. RESULTS: The number of individuals with PIMs increased significantly according to both criteria (62.3% to 66.6% according to Beers criteria, 43.4% to 50.0% according to STOPP criteria). The most common PIMs were sliding-scale insulin (26.9%), clonazepam (9.5%), and periciazine (6.4%) using Beers criteria and spironolactone (10.3%), acetylsalicylic acid (9.8%), and periciazine (8.7%) using STOPP criteria. Neurology, infectious disease, and pneumology had the highest numbers of PIMs, and neurology, pneumology, and cardiology had a greater increase in PIMs during hospitalization than the other specialties. CONCLUSION: This study demonstrates the high and growing prevalence of PIMs in the hospital environment, according to Beers and STOPP criteria. Educational measures and specific pharmaceutical interventions for each specialty are needed to change this situation.

Associação entre artrite reumatoide e citrulinização proteica por porphyromonas gingivalis: revisão de literatura / Association between Rheumatoid Arthritis and protein citrulinization by Porphyromonas gingivalis: Literature Review

A presença de peptidil-arginina deaminase (PADs), enzimas de Porphyromonas gingivalis (P. gingivalis), encontradas em pacientes com periodontite, são capazes de quebrar a tolerância imune, mediante citrulinização proteica, culminando, em um paciente suscetível, ao desenvolvimento da artrite reumatoide (AR). O objetivo desta revisão de literatura é avaliar uma possível correlação entre a periodontite e AR por meio da citrulinização proteica realizada por P. gingivalis. Para o desenvolvimento desta revisão de literatura, foi realizada uma busca na base de dados eletrônicas PUBMED, no período de maio a agosto de 2017. Foi utilizada uma estratégia de busca otimizada com as seguintes palavraschave: rheumatoid arthritis, periodontal disease e P. gingivalis. Assim, foram encontrados um total de 83 artigos, sendo selecionados inicialmente por título e resumo por um revisor e, posteriormente, por outro revisor, selecionando pelos critérios de inclusão: artigos completos escritos em língua portuguesa, espanhola ou inglesa; ter 10 anos ou menos de publicação. Ao final da seleção foram obtidos 22 artigos; destes, 15 incluídos por serem estudos clínicos em animais ou humanos. De acordo com este estudo, foi possível correlacionar positivamente a periodontite e a AR por meio da citrulinização proteica realizada pela bactéria P. gingivalis. Contudo, a mediação por PADs não é a única e exclusiva forma de correlação entre essas doenças, sendo necessários mais estudos para estabelecer outras possíveis correlações. (AU)

The presence of peptidyl arginine deaminase (PADs), an enzyme associated to Porphyromonas gingivalis (P. gingivalis), found in patients with periodontitis, can lead to the breakdown of immune tolerance by means of protein citrulinization, leading to a development of rheumatoid arthritis (RA) in susceptible patients. The objective of this literature review is to evaluate a possible correlation between periodontitis and RA through protein citrulinization performed by P. gingivalis. For the development of this literature review, a search was performed on the electronic database PUBMED from May to August 2017. An optimized search strategy was used with the following keywords: rheumatoid arthritis, periodontal disease and P. gingivalis. A total of 83 articles were found, being initially selected by title and abstract by one reviewer and later by another reviewer selecting by inclusion criteria: Complete articles written in Portuguese, Spanish or English; have 10 years or less of publication. At the end of the selection, 22 articles were obtained; of these, 15 included by being clinical studies in animals or humans. According to this study, it is possible to positively correlate periodontitis and RA with protein citrulinization performed by P. gingivalis. However, mediation by PADs is not the only and exclusive form of correlation between these diseases, and further studies are needed to establish other possible correlations. (AU)

O Programa Mais Médicos e a atenção básica no Brasil: uma revisão integrativa / The Mais Médicos Program and basic care in Brazil: an integrative review

Objetivou-se analisar a produção científica acerca do Programa Mais Médicos na Atenção Básica brasileira. Foi realizada busca nas bases de dados indexadas LILACS, MEDLINE e SCIELO utilizando-se para pesquisa o termo “Mais Médicos” e como descritores, Programas Nacionais de Saúde e Atenção Primária à Saúde. Foram incluídos produções científicas que abordassem o Programa Mais Médicos como tema central, escritos em inglês ou português, publicados no período de 2013 à 2015. Como questão norteadora do estudo elegeu-se a seguinte indagação: Como está caracterizada a produção científica acerca do Programa Mais Médicos no Brasil? Encontrou-se 18 artigos, no entanto 04 destes se alinharam aos critérios de inclusão e serviram como fruto de análise. As outras produções encontradas tratavam-se de editoriais e outras publicações, deste modo, foram excluídas da pesquisa. Observou-se que as produções foram de origem brasileira, (2) 2014 e (2) 2015 e foram realizadas por equipe multiprofissional provenientes de Universidades Públicas.

Aimed analyze the scientific production about the Program Mais Médicos in the Brazilian Basic Attention. A search was performed in indexed databases LILACS, MEDLINE and SCIELO using to search the term "Mais Médicos" and as descriptors: National Health Programs and Primary Health Care. The study included publications that addressed the Program Mais Médicos as central theme, written in English or Portuguese, published between 2013 to 2015. Como guiding question of the study was elected the following question: how is characterized the scientific production about the Program Mais Médicos in Brazil? It was found 18 articles however 04 of these lined the inclusion criteria and served as an analysis result. The other found productions treated to editorials and other publications and were excluded from the study. It was observed that all the scientific productions were from Brazil (2) 2014 and (2) 2015 and were performed by multidisciplinary team from Public Universities.

Motor deficits and beta oscillations are dissociable in an alpha-synuclein model of Parkinson's disease.

Parkinson's disease (PD) is a neurodegenerative disorder characterised by progressive motor symptoms resulting from chronic loss of dopaminergic neurons in the nigrostriatal pathway. The over expression of the protein alpha-synuclein in the substantia nigra has been used to induce progressive dopaminergic neuronal loss and to reproduce key histopathological and temporal features of PD in animal models. However, the neurophysiological aspects of the alpha-synuclein PD model have been poorly characterised. Hereby, we performed chronic in vivo electrophysiological recordings in the corticostriatal circuit of rats injected with viral vector to over express alpha-synuclein in the right substantia nigra. Our model, previously shown to exhibit mild motor deficits, presented moderate dopaminergic cell loss but did not present prominent local field potential oscillations in the beta frequency range (11-30 Hz), considered a hallmark of PD, during the 9 weeks after onset of alpha-synuclein over expression. Spinal cord stimulation, a potential PD symptomatic therapy, was applied regularly from sixth to ninth week after alpha-synuclein over expression onset and had an inhibitory effect on the firing rate of corticostriatal neurons in both control and alpha-synuclein hemispheres. Dopamine synthesis inhibition at the end of the experiment resulted in severe parkinsonian symptoms such as akinesia and increased beta and high-frequency (>90 Hz) oscillations. These results suggest that the alpha-synuclein PD model with moderate level of dopaminergic depletion does not reproduce the prominent corticostriatal beta oscillatory activity associated to parkinsonian conditions.

Produtividade de pastagens de Coastcross-1 em consórcio com diferentes leguminosas de ciclo hibernal / Productivity of Coastcross-1 pastures mixed with cool-season legumes

Objetivou-se com esta pesquisa avaliar três sistemas forrageiros constituídos por Coastcross-1 (CC) + 100kg de N ha-1 ano-1 + ervilhaca comum; CC + 100kg de N ha-1 ano-1 + trevo vesiculoso; e CC + 200kg de N ha-1 ano-1. Durante o período experimental (345 dias), foram realizados treze pastejos. Para avaliação, foram utilizadas vacas em lactação da raça Holandesa. Foram avaliadas a massa de forragem, composição botânica, relação folha/colmo; taxa de acúmulo diário, produção e consumo de forragem; eficiência de pastejo e taxa de lotação. Os valores médios de produção de forragem e lotação foram de 21,0; 20,3 e 24,3t ha-1; 7,0; 6,5 e 7,7 unidades animais ha-1 dia-1, para os respectivos sistemas forrageiros. Melhores resultados foram obtidos no consórcio de CC com ervilhaca e no cultivo singular de CC.(AU)

The objective of this research was to evaluate three grazing systems with Coastcross-1 (CC) + 100kg N ha-1 year-1 + common vetch; CC + 100kg N ha-1 year-1 + arrowleaf clover; and CC + 200kg N ha-1 year-1. Thirteen grazing cycles were performed during the experimental period (345 days). Lactating Holstein cows were used in the evaluation. The forage mass, botanical composition, leaf/stem ratio; daily accumulation rate, production and forage intake; grazing efficiency and stocking rate were evaluated. The average of forage production and stocking rate were 21.0, 20.3, 24.3t ha-1 and 7.0, 6.5, 7.7 animal units ha-1 day-1 for the respective forage systems. Better results were found on Coastcross-1 mixed with common vetch and Coastcross-1 alone.(AU)

Produtividade de pastagens de Coastcross-1 em consórcio com diferentes leguminosas de ciclo hibernal / Productivity of Coastcross-1 pastures mixed with cool-season legumes

Objetivou-se com esta pesquisa avaliar três sistemas forrageiros constituídos por Coastcross-1 (CC) + 100kg de N ha-1 ano-1 + ervilhaca comum; CC + 100kg de N ha-1 ano-1 + trevo vesiculoso; e CC + 200kg de N ha-1 ano-1. Durante o período experimental (345 dias), foram realizados treze pastejos. Para avaliação, foram utilizadas vacas em lactação da raça Holandesa. Foram avaliadas a massa de forragem, composição botânica, relação folha/colmo; taxa de acúmulo diário, produção e consumo de forragem; eficiência de pastejo e taxa de lotação. Os valores médios de produção de forragem e lotação foram de 21,0; 20,3 e 24,3t ha-1; 7,0; 6,5 e 7,7 unidades animais ha-1 dia-1, para os respectivos sistemas forrageiros. Melhores resultados foram obtidos no consórcio de CC com ervilhaca e no cultivo singular de CC.

The objective of this research was to evaluate three grazing systems with Coastcross-1 (CC) + 100kg N ha-1 year-1 + common vetch; CC + 100kg N ha-1 year-1 + arrowleaf clover; and CC + 200kg N ha-1 year-1. Thirteen grazing cycles were performed during the experimental period (345 days). Lactating Holstein cows were used in the evaluation. The forage mass, botanical composition, leaf/stem ratio; daily accumulation rate, production and forage intake; grazing efficiency and stocking rate were evaluated. The average of forage production and stocking rate were 21.0, 20.3, 24.3t ha-1 and 7.0, 6.5, 7.7 animal units ha-1 day-1 for the respective forage systems. Better results were found on Coastcross-1 mixed with common vetch and Coastcross-1 alone.

Chemical constituents and pharmacological profile of Gunnera manicata L. extracts

Gunnera perpensa L. (Gunneraceae) is a native South African plant widely used in traditional medicine as an antibacterial and antifungal. In southern Brazil there is the native species called Gunnera manicata L. that also belongs to the Gunneraceae. Nevertheless, there is no information about chemical and pharmacological properties of South American Gunnera species. Therefore this study aimed at assessing the phytochemical and pharmacological profiles of aqueous and methanol Brazilian G. manicata extracts. The results showed that antimicrobial activity in an agar diffusion assay was effective against Staphylococcus aureus and Candida albicans . Phenolic compounds were investigated by liquid chromatography coupled with a tandem mass spectrometer (LC-MS/MS) and all extracts presented gallic acid and only the methanol extract obtained from the leaves exhibited hyperoside. Rutin, quercetin and chlorogenic acid were not found in the samples analysed. Total phenolic content was higher in methanol extract and total flavonoid content was low in all extracts. Antioxidant activity was evaluated by the 2,2-diphenyl-1-picryl-hydrazyl (DPPH) radical test, and all samples presented good to moderate antioxidant activity. These results encourage complementary studies on the chemical composition of the plant extracts focusing on isolation and structure elucidation of their active compounds.

Gunnera perpensa L. (Gunneraceae) é uma planta nativa do sul da África utilizada na medicina tradicional como antibiótico e antifúngico. Gunnera manicata L. é uma planta nativa do sul do Brasil também da família Gunneraceae e, apesar disso, não há informações sobre suas propriedades químicas e farmacológicas. Assim, o objetivo deste estudo foi avaliar o perfil fitoquímico e farmacológico dos extratos aquoso e metanólico de G. manicata. Os resultados do ensaio microbiológico de difusão em ágar demonstraram que os extratos testados foram ativos contra Staphylococcus aureus e Candida albicans. A presença de compostos fenólicos foi investigada pela técnica de Cromatografia Líquida acoplada a espectrômetro de massas em Tandem (CL-EM/EM). Em todas as amostras analisadas verificou-se a presença de ácido gálico e somente o extrato metanólico das folhas apresentou hiperosídeo. Rutina, quercetina e ácido clorogênico não foram encontrados. O conteúdo total de compostos fenólicos foi maior nos extratos metanólicos e o conteúdo de flavonóides totais foi baixo em todos os extratos. A atividade antioxidante foi avaliada pelo teste da atividade do radical 2,2-diphenyl-1-picril-hidrazil (DPPH) e todas as amostras apresentaram boa a moderada atividade antioxidante. Esses resultados encorajam estudos complementares da composição química dos extratos com foco no isolamento e na elucidação estrutural dos compostos ativos.

Uliginosin B, a phloroglucinol derivative from Hypericum polyanthemum: a promising new molecular pattern for the development of antidepressant drugs.

In this study we have demonstrated that cyclohexane extract of Hypericum polyanthemum (POL) and its main phloroglucinol derivative uliginosin B (ULI) present antidepressant-like activity in rodent forced swimming test (FST). The involvement of monoaminergic neurotransmission on the antidepressant-like activity of ULI was evaluated in vivo and in vitro. POL 90 mg/kg (p.o.) and ULI 10 mg/kg (p.o.) reduced the immobility time in the mice FST without altering locomotion activity in the open-field test. The combination of sub-effective doses of POL (45 mg/kg, p.o.) and ULI (5 mg/kg, p.o.) with sub-effective doses of imipramine (10 mg/kg, p.o.), bupropion (3 mg/kg, p.o.) and fluoxetine (15 mg/kg, p.o.) induced a significant reduction on immobility time in FST. The pretreatment with SCH 23390 (15 µg/kg, s.c., dopamine D1 receptor antagonist), sulpiride (50 mg/kg, i.p., dopamine D2 receptor antagonist), prazosin (1mg/kg, i.p., α1-adrenoceptor antagonist), yohimbine (1mg/kg, i.p., α2-adrenoceptor antagonist) and pCPA (100 mg/kg/day, i.p., p-chlorophenilalanine methyl ester, inhibitor of serotonin synthesis, for four consecutive days) before ULI administration (10 mg/kg, p.o.) significantly prevented the anti-immobility effect in FST. ULI was able to inhibit synaptosomal uptake of dopamine (IC50 = 90 ± 38 nM), serotonin (IC50 = 252 ± 13 nM) and noradrenaline (280 ± 48 nM), but it did not bind to any of the monoamine transporters. These data firstly demonstrated the antidepressant-like effect of POL and ULI, which depends on the activation of the monoaminergic neurotransmission in a different manner from the most antidepressants.

Supercritical extraction of phloroglucinol and benzophenone derivatives from Hypericum carinatum: quantification and mathematical modeling.

The aerial parts of Hypericum carinatum (Guttiferae) were extracted with supercritical carbon dioxide under constant temperature (40, 50 or 60°C) and gradual pressure increase (90, 120, 150 and 200 bar) aiming at the recovery of enriched fractions containing uliginosin B, cariphenone A and cariphenone B, compounds of pharmaceutical interest. The yields of these substances were determined by high-performance liquid chromatography and compared with those obtained with n-hexane maceration. The supercritical-fluid extraction showed higher selectivity than the conventional solvent extraction method. After defining 40°C and 90 bar as the best conditions to obtain the target compounds, a mathematical model was used for the extraction process and a good correlation was achieved with the experimental data.

Supercritical fluid extraction and high performance liquid chromatographic determination of benzopyrans and phloroglucinol derivative in Hypericum polyanthemum.

The aerial parts of Hypericum polyanthemum Klotzsch ex Reichardt (Guttiferae) were successively extracted with supercritical carbon dioxide (SC CO(2)) under pressures of 90, 120, 150 and 200 bar at different temperatures (40, 50 and 60 degrees C), and compared with the n-hexane extract obtained by ultrasound-assisted extraction. The samples obtained were examined regarding extraction yield and HPLC quantification of the main secondary metabolites, the benzopyrans HP1 (6-isobutyryl-5,7-dimethoxy-2,2-dimethylbenzopyran), HP2 (7-hydroxy-6-isobutyryl-5-methoxy-2,2-dimethyl-benzopyran) and HP3 (5-hydroxy-6-isobutyryl-7-methoxy-2,2-dimethyl) and the phloroglucinol derivative, uliginosin B. SFE presented higher selectivity than the n-hexane maceration, and the best condition to extract the target metabolites has been determined to be at 50 degrees C and for the high molecular-weight compound, uliginosin B, higher pressures were required.

Phenolic compounds profiles during ex vitro acclimatization of micropropagated Hypericum polyanthemum.

Accumulation of benzopyrans and total phenolic compounds were assessed in acclimatized field grown plants of Hypericum polyanthemum, an endemic species of southern Brazil, harvested at different developmental stages. The HPLC analysis of bioactive compounds 6-isobutyryl-5,7-dimethoxy-2,2-dimethylbenzopyran (HP1), 7-hydroxy-6-isobutyryl-5-methoxy-2,2-dimethyl-benzopyran (HP2) and 5-hydroxy-6-isobutyryl-7-methoxy-2,2-dimethyl-benzopyran (HP3) revealed that the three benzopyrans are accumulated both in the vegetative and reproductive parts with maximum contents observed after 18 weeks (in the former) and 20 weeks (in the later) of plant growth (1.92+/-0.085 g % DW and 2.62+/-0.13 g % DW in the vegetative and reproductive parts, respectively). Highest contents of HP1 (1.56+/-0.12 g % DW) and HP2 (0.19+/-0.01 g % DW) were quantified in the green floral buds of the plants, whereas HP3 reached the highest level (1.02+/-0.08 g % DW) in the overblown flowers. The evaluation of total phenolic compounds showed that the vegetative parts accumulated the highest levels of the metabolites (51.93+/-0.67 mg QE (g DW)(-1)) after 16 weeks of plant growth. Considering the reproductive parts, the open flowers accumulated the greatest levels of the bioactive compounds (75.99+/-0.95 mg QE (g DW)(-1)). The results show that H. polyanthemum can be efficiently propagated and acclimatized to produce benzopyrans and other phenolic compounds.