Phytochemical study of Lantana camara flowers, ecotoxicity, antioxidant, in vitro and in silico acetylcholinesterase: molecular docking, MD, and MM/GBSA calculations.

Lantana camara L. (Verbenaceae), commonly called lead cambará, has often been used in folk medicine as antiseptic, antispasmodic, against hemorrhages, flu, colds, and diarrheic. This plant is considered a weed and an ornamental and medicinal plant and is an essential source of natural organic compounds, mainly flavonoids. This work aims to investigate the chemical composition and evaluate the biological properties such as antioxidant and acetylcholinesterase of the constituents from L. camara flowers. In addition, the computational simulation was carried out with the constituents identified. The results showed that methanolic extract of the flowers of L. camara presents toxicity, antioxidant activity with 97.8% inhibition percentage in the concentration of 0.25 mg mL-1 against the DPPH radical, and acetylcholinesterase activity. The phytochemical study of extract from L. camara flowers resulted in LC-MS identification of 18 polyphenolic compounds, such as phenolic acid derivatives, phenylethanoid glycosides, and flavonoids. In the in silico study, flavonoid isoverbascoside showed affinity energy of -9.9 kcal.mol-1 with the AChE enzyme. Their phytochemical content, mainly the presence of flavonoids and phenolic compounds in L. camara extracts, may be related to the antioxidant and anticholinesterase potential observed.

Physical quality of seeds of Moquiniastrum polymorphum / Qualidade física de sementes de Moquiniastrum polymorphum

Abstract This study aimed to analyze the physical properties of the seeds of Moquiniastrum polymorphum when processed by mini-SAS, X-ray and seed blower systems. The seeds were purchased from Seeds Caiçara, located in Penápolis-SP. After purchase, the seed lot was characterized by standard tests. In the X-ray test the seeds were classified according to their internal morphology as filled, unfilled or malformed. The seed blower was set at six opening settings, resulting in light and heavy fractions. The evaluations were performed by weighing the seeds that remained in the blower (heavy fraction) and by the amount of filled seeds indicated by the X-ray test. The germination tests were composed of four replicates of 50 seeds. The mini-SAS was used for external evaluation. It was concluded that the combined use of the seed blower and the X-ray test was efficient for the evaluation and determination of the physical quality of the seeds of M. polymorphum. The seed blower at opening settings 5 resulted in the best lot quality. The external parameters were not able to qualitatively evaluate the seeds of M. polymorphum.

Resumo O presente estudo objetivou analisar as propriedades físicas das sementes de Moquiniastrum polymorphum por meio dos equipamentos raios-X, mini-SAS e soprador de sementes. As sementes foram adquiridas da empresa Sementes Caiçara em matrizes localizadas no município de Penápolis-SP. Após adquirido e beneficiado, o lote de sementes foi caracterizado por meio de testes padrões. No teste de raios-X as sementes foram classificadas de acordo com sua morfologia interna como cheias, vazias ou mal formadas. O soprador de sementes foi ajustado em seis aberturas, resultando em frações leves e pesadas. As avaliações foram realizadas pesando-se as sementes que permaneceram no soprador (fração pesada) e pela quantidade de sementes cheias pela análise de raios-X. Posteriormente foram realizados testes de germinação compostos por quatro repetições de 50 sementes. Na avaliação externa das sementes utilizou-se o equipamento mini-SAS. Após análise dos dados, concluiu-se que a utilização em conjunto dos equipamentos soprador de sementes e raios-X foi eficiente para avaliação e determinação da qualidade física das sementes de M. polymorphum. O soprador de sementes na regulagem da abertura 5 resultou na melhor qualidade do lote. Os parâmetros externos não foram capazes de avaliar qualitativamente as sementes de M. polymorphum.

Suppressive effects of Vochysia divergens aqueous leaf extract and its 5-methoxyflavone on murine macrophages and lymphocytes.

ETHNOPHARMACOLOGICAL RELEVANCE: Vochysia divergens Pohl (Vochysiaceae), popularly known as "Cambará", is a tree that is resistant to the seasonal floods in the Pantanal, and usually found in monodominant stands called "Cambarazal". The inhabitants of the Pantanal exploit this tree for medicinal uses. Infusions and decoctions of its leaves are taken as teas, particularly for the treatment of asthma, flu and diarrhea, according to the local tradition transmitted empirically through the generations. AIM OF THE STUDY: To evaluate the beneficial health effects related to the ethnomedicinal uses of V. divergens (Vd) by using biomonitored fractionation of an aqueous leaf extract. MATERIALS AND METHODS: The aqueous leaf extract was obtained by decoction, and then the extract was fractionated by a combination of separation techniques including precipitation, organic partition and chromatography. Chromatographic analyses of the active samples were carried out using HPLC-DAD-MS. Flavonoid 1 was isolated from the n-BuOH fraction through classic chromatographic techniques. The inhibitory effects and cytotoxicity of the Vd extract, fractions and flavonoid 1 on NO and TNF-α production were assessed in LPS-stimulated RAW 264.7 macrophage cultures. Additionally, suppression on the proliferation of BALB/c lymphocytes was estimated by [3H] thymidine incorporation. The antioxidant activity of the samples was verified by SNP and DPPH assays and the suppression of the iNOS protein expression was evaluated through Western blotting. RESULTS: The HPLC-DAD-MS analysis of the Vd extract led to the identification of 5-methoxyluteolin-7-O-ß-glucopyranoside (2), rutin (4) and the tannin galloyl-HHDP-glucopyranoside (3), besides the main flavonoid 3',5-dimethoxyluteolin-7-O-ß-glucopyranoside (1), which was biologically evaluated in comparison with luteolin aglycone. The Vd extract, n-BuOH fraction and flavonoid 1 inhibited NO and TNF-α production by LPS-stimulated macrophages. The reduction of NO levels was mediated mainly by suppression of the iNOS expression. In addition, both the Vd extract (IC50 13.6 µg/mL) and flavonoid 1 (IC50 19.8 µg/mL; 41.6 µM) strongly inhibited stimulated lymphocyte proliferation when compared to the immunosuppressive agent cyclosporin A (IC50 43.8 µg/mL; 36.4 µM). The Vd extract also showed a scavenging activity toward DPPH and NO free radicals. This is the first report describing the immunomodulatory potential of V. divergens and its major flavonoid (1). CONCLUSION: Our findings showed that the aqueous leaf extract of V. divergens and its flavonoid reduced the production of excessive pro-inflammatory markers, collaborating with the Pantanal folk medicinal tradition that recommends the tea of cambará leaves for both asthma and flu. In addition, this study contributes to the knowledge of the pharmacological properties of 5-methoxy flavones, a poorly investigated subclass of flavonoids.

Buddleja thyrsoides Lam. crude extract presents antinociceptive effect on an arthritic pain model in mice.

Arthritis is a chronic inflammatory disease which reduces the life quality of affected individuals. Therapeutic tools used for treating inflammatory pain are associated with several undesirable effects. Buddleja thyrsoides Lam., known as 'Barbasco' or 'Cambara', is mostly used in several disorders and possesses antirheumatic, anti-inflammatory, and analgesic properties. Here, we investigated the antinociceptive and anti-inflammatory effects of the B. thyrsoides crude extract applied orally and topically in acute pain models and an arthritic pain model induced by complete Freund's adjuvant (CFA) paw injection in male mice (25-30 g). The high-performance liquid chromatography (HPLC) of the B. thyrsoides extract crude revealed the presence of the lupeol, stigmasterol, and ß-sitosterol. The stability study of the B. thyrsoides gel did not show relevant changes at low temperatures. The oral treatment with the B. thrysoides extract prevented the capsaicin-induced spontaneous nociception and the acetic acid-induced abdominal writhing, but did not alter the thermal threshold in the tail immersion test. The B. thyrsoides antinociceptive effect was not reversed by naloxone in the capsaicin test. The B. thyrsoides oral or topical treatment reversed the CFA-induced mechanical allodynia and thermal hyperalgesia with maximum inhibition (Imax) of 69 ± 6 and 68 ± 5% as well as 78 ± 15 and 87 ± 12%, respectively. Moreover, the topical but not oral treatment inhibited the CFA-induced cell infiltration, but did not reduce the paw edema significantly. The oral treatment with B. thyrsoides did not cause adverse effects. These findings suggest that the oral or topical treatment with B. thyrsoides presents antinociceptive actions in an arthritic pain model without causing adverse effects.

Physical quality of seeds of Moquiniastrum polymorphum

Abstract This study aimed to analyze the physical properties of the seeds of Moquiniastrum polymorphum when processed by mini-SAS, X-ray and seed blower systems. The seeds were purchased from Seeds Caiçara, located in Penápolis-SP. After purchase, the seed lot was characterized by standard tests. In the X-ray test the seeds were classified according to their internal morphology as filled, unfilled or malformed. The seed blower was set at six opening settings, resulting in light and heavy fractions. The evaluations were performed by weighing the seeds that remained in the blower (heavy fraction) and by the amount of filled seeds indicated by the X-ray test. The germination tests were composed of four replicates of 50 seeds. The mini-SAS was used for external evaluation. It was concluded that the combined use of the seed blower and the X-ray test was efficient for the evaluation and determination of the physical quality of the seeds of M. polymorphum. The seed blower at opening settings 5 resulted in the best lot quality. The external parameters were not able to qualitatively evaluate the seeds of M. polymorphum.

Resumo O presente estudo objetivou analisar as propriedades físicas das sementes de Moquiniastrum polymorphum por meio dos equipamentos raios-X, mini-SAS e soprador de sementes. As sementes foram adquiridas da empresa Sementes Caiçara em matrizes localizadas no município de Penápolis-SP. Após adquirido e beneficiado, o lote de sementes foi caracterizado por meio de testes padrões. No teste de raios-X as sementes foram classificadas de acordo com sua morfologia interna como cheias, vazias ou mal formadas. O soprador de sementes foi ajustado em seis aberturas, resultando em frações leves e pesadas. As avaliações foram realizadas pesando-se as sementes que permaneceram no soprador (fração pesada) e pela quantidade de sementes cheias pela análise de raios-X. Posteriormente foram realizados testes de germinação compostos por quatro repetições de 50 sementes. Na avaliação externa das sementes utilizou-se o equipamento mini-SAS. Após análise dos dados, concluiu-se que a utilização em conjunto dos equipamentos soprador de sementes e raios-X foi eficiente para avaliação e determinação da qualidade física das sementes de M. polymorphum. O soprador de sementes na regulagem da abertura 5 resultou na melhor qualidade do lote. Os parâmetros externos não foram capazes de avaliar qualitativamente as sementes de M. polymorphum.

Sesquiterpene lactones of Moquiniastrum polymorphum subsp. floccosum have antineoplastic effects in Walker-256 tumor-bearing rats.

BACKGROUND AND AIM: This study aimed to evaluate the in vivo antitumor actions and toxicity of the dichloromethane fraction (F1B) of Moquiniastrum polymorphum subsp. floccosum (formerly Gochnatia polymorpha ssp. floccosa), composed of sesquiterpene lactones, against Walker-256 carcinosarcoma in rats. METHODS: Male Wistar rats received 100 mg kg(-1) F1B per day orally for 16 days after subcutaneous inoculation of Walker-256 cells in the pelvic limb. The tumor progression was monitored, and after treatment, tumor weight, oxidative stress, plasma biochemistry, inflammatory parameters, gene expression and histology of tumor and/or liver were evaluated. The toxicity of F1B was analyzed through the relative weight of organs. Additionally, an LD50 test was performed in mice. RESULTS: F1B treatment significantly reduced tumor volume and weight. There was no difference in oxidative stress in tumor tissue after treatment. F1B treatment modified hepatic glutathione and superoxide dismutase, and normalized plasma glucose, alkaline phosphatase, and amylase. F1B did not affect the activity of myeloperoxidase and N-acetylglucosaminidase or the nitric oxide levels in tumor tissue. However, F1B decreased the tumor necrosis factor (TNF)-α levels. Additionally, F1B increased apoptosis in the tumor, mediated by up-regulation of the p53 and Bax gene expression. No clinical signs of toxicity or death were observed in the rats treated with F1B. The LD50 calculated for mice was 1209 mg kg(-1). CONCLUSIONS: F1B, which is rich in sesquiterpene lactones, showed antitumor activity against Walker-256 carcinosarcoma. This effect may be, at least in part, related to the induction of apoptosis and inhibition of TNF-α signaling.

Growth rhythm of Vochysia divergens Pohl (Vochysiaceae) in the Northern Pantanal / Ritmo de crescimento de Vochysia divergens Pohl (Vochysiaceae) no Pantanal Norte

The Pantanal is the largest wetland in the world, characterized by high biodiversity, but large areas have been invaded by Vochysia divergens, a flood- adapted pioneer and native tree of the riparian forest and Brazilian Savanna. Seasonality in rainfall causes annual rhythms in the tree's physiology, in which climatic stress factors induce a cambial dormancy in trees and, in consequence, growth zones in the trunk. Current analysis evaluates the seasonal variation of the diameter increase of V. divergens specimens in a seasonal floodable forest of the Northern Brazilian Pantanal. Field sampling was conducted between January and December 2012. Air temperature, relative humidity and precipitation were measured at a micrometeorological station, water level was measured by graded tape, and soil water content was measured by a portable TDR sensor. Diameter growth was monitored by dendrometric bands and aboveground litter production was sampled by litter traps. The annual diameter increase was 4.0 mm. There was correlation between diameter increment and climate and phenology, with the highest increase during the flooding period and the lowest during the dry season and reproductive period. Climate and phenology affected the growth rhythm of V. divergens.

O Pantanal é a maior area úmida do mundo, com alta diversidade de plantas e animais, mas vastas áreas são invadidas por Vochysia divergens Pohl (Vochysiaceae), que é uma árvore pioneira bem adaptada à inundação e nativa de matas ripárias e cerrado. A sazonalidade da chuva leva a ritmos anuais na fisiologia das árvores em que fatores de estresse climático induzem à dormência cambial e, consequentemente às zonas de crescimento no caule. Assim, o objetivo deste estudo foi avaliar a variação sazonal do incremento diamétrico de indivíduos de V. divergens em uma floresta sazonalmente inundável no pantanal norte. As coletas ocorreram de janeiro a dezembro/2012. A temperatura do ar, umidade relativa e precipitação foram obtidas por estação micrometeorológica, o nível de água no solo por trena graduada e o conteúdo de água no solo por sensor TDR. O incremento diamétrico foi monitorado por bandas dendrométricas e a produção de liteira por coletores. O incremento diamétrico anual foi 4,0 mm. Houve correlação do incremento diamétrico com clima e fenologia, com maior incremento na inundação e menor na estação seca e no período reprodutivo da espécie. Portanto, o ritmo de crescimento de V. divergens foi afetado pelo clima e fenologia.

Antimicrobial activity of crude extracts and fractions of Vernonia polyanthes Less (assa-peixe) flowers / Atividade antimicrobiana de extrato bruto e de frações de flores de Vernonia polyanthes Less (assa-peixe)

ABSTRACT Vernonia polyanthes, known as “assa-peixe”, is a plant native to Brazil, and the decoction or infusion of its flowers, roots and leaves are used in folk medicine, being considered sources of diuretic, balsamic, anti-rheumatic substances, and are used in cases of bronchitis and persistent cough. The aim of the study was to evaluate the antimicrobial activity of the extract/fractions obtained by methanol maceration and infusion of V. polyanthes flower, also including qualitative identification of flower compounds, through phytochemical evaluation, using colorimetric tests. Identification tests for the presence of anthraquinones, tannins, flavonoids, saponins and alkaloids were performed. Microbiological evaluation was made through agar diffusion assay, using Escherichia coli, Staphylococcus aureus and Pseudomonasaeruginosa as test organisms. From the performed colorimetric tests it was possible to verify the presence of tannins and flavonoids in both extracts. Alkaloids were also observed in the macerated extract. The ethyl acetate fraction from the agar diffusion assay, from both extracts, presented microbial activity over Staphylococcus aureus. It was possible to qualitatively identify the floral compounds, and to show the differences between extraction methods, being methanol considered the best solvent to the extraction.

RESUMO Vernonia polyanthes, conhecida como assa-peixe, é planta nativa do Brasil e suas flores, raízes e folhas, em decocção ou infusão, são empregadas na medicina caseira como diuréticas, balsâmicas, e anti-reumáticas, usadas nos casos de bronquite e tosse persistente. O objetivo do trabalho foi avaliar a atividade antimicrobiana do extrato/frações obtidos por maceração em metanol e infusão de flores de V. polyanthes, incluindo também a identificação qualitativa dos compostos presentes nas flores, através da avaliação fitoquímica, empregando testes colorimétricos. Foram realizados testes para identificação de antraquinonas, taninos, flavonóides, saponinas e alcalóides. A avaliação microbiológica foi realizada por meio de ensaio de difusão em ágar, empregando Escherichia coli, Staphylococcusaureus e Pseudomonas aeruginosa. A partir dos testes colorimétricos foi possível verificar a presença de taninos e flavonóides em ambos os extratos. Ainda, no extrato macerado, foi observada a presença de alcalóides. No ensaio de difusão em ágar, a fração acetato de etila de ambos os extratos, apresentou atividade antimicrobiana sobre Staphylococcus aureus. Foi possível identificar qualitativamente os compostos da flor, demonstrando diferença entre as técnicas de extração, sendo que o metanol resultou em melhor poder extrativo.

Investigação de surto de doença exantemática por enterovirus não pólio em município turístico da serra gaúcha / Investigation of an outbreak of non polio enterovirus in a tourist municipality of Rio Grande do Sul

Confirmar a ocorrência de surto, descrever o surto em relação a tempo, lugar e pessoa, identificar o agente etiológico e realizar medidas de prevenção e controle. (AU)