O perfil semiológico do paciente portador de hemorragia digestiva alta

OBJETIVO: O seguinte estudo objetivou descrever a semiologia do paciente portador de hemorragia digestiva alta, considerando como determinante na avaliação de potencias focos hemorrágicos. METODOLOGIA: Foram realizadas buscas nas plataformas do SciELO, LILACS, PubMed, Scopus e Google Scholar,utilizando os descritores gastrointestinal bleeding, peptic ulcerous disease e varicose hemorrhage, sendo identificados 35 estudos, dos quais foram incluídos 13 artigos completos. Desses estudos, 5 avaliaram as principais etiologias, 2 o surgimento de novos testes diagnósticos, 2 analisaram os aspectos epidemiológicos e 1 a sintomatologia apresentada pelo acometimento da hemorragia digestiva alta. Observou-se inicialmente a abundâncias de informações conceituais sobre o sangramento, como um transtorno clínico comum, acompanhada de inúmeras manifestações, considerando que o foco hemorrágico pode ocorrer em qualquer porção do trato gastrointestinal. Neste estudo, todas as publicações eleitas apresentaram o quadro semiológico composto por algia abdominal, indícios de choque hipovolêmico e taquicardia, alguns exibiram quedas abruptas da pressão arterial, odinofagia, êmese, náuseas e estado ictérico. Os pacientes implicados, cronicamente, já manifestaram ocorrências prévias, devido ao caráter recidivante torna-se essencial investigar a existência de varizes, fístula aorto-entérica, angiodisplasia e doença ulcerosa. CONCLUSÃO: Elucida-se que a hemorragia digestiva alta representa a principal causa de sangramento do trato gastrointestinal, majoritamente manifesta-se como hematêmese ou melena e cursam com o quadro sintomatológico que auxilia na avaliação da gravidade deste e o embasamento de potenciais focos de sangramento e que contribuam para disseminação de informações e intervenções futuras

New steroidal saponins and antiulcer activity from Solanum paniculatum L.

Solanum paniculatum L. (Solanaceae) is a plant species widespread throughout tropical America, especially in the Brazilian Savanna region. It is used in Brazil for culinary purposes and in folk medicine to treat liver and gastric dysfunctions, as well as hangovers. Fractionation of the ethanolic extracts (70%) from aerial parts (leaves and twigs) of S. paniculatum led to the isolation of the two new saponins (22R, 23S, 25R)-3β, 6α, 23-trihydroxy-5α-spirostane 6-O-β-d-xylopyranosyl-(1″″ → 3″′)-O-[β-d-quinovopyranosyl(1″′ → 2′)]-O-[α-l-rhamnopyranosyl(1″ → 3′)]-O-β-d-quinovopyranoside (1) and diosgenin 3-O-β-d-glucopyranosyl(1″ → 6′)-O-β-d-glucopyranoside (2) together with four know compounds: caffeic acid (3), diosgenin β-d-glucopyranoside (4), rutin (5), and quercetin 3-O-α-l-rhamnopyranosyl (1″′ → 6″)-O-β-d-galactopyranoside (6). The structures of these compounds were elucidated by extensive use of 1D and 2D NMR experiments along with HRESIMS analyses. Different doses (31.25–500 mg/kg) of ethanolic extract of leaves from S. paniculatum were evaluated against gastric ulcer induced by ethanol in rats. The lower dose of extract able to promote antiulcer effect was 125 mg/kg. The treatment with S. paniculatum by oral route was able to decrease gastric lesion area and also reduced levels of myeloperoxidase (MPO) in the gastric mucosa. Our results reveal for the first time, steroidal saponins from S. paniculatum and the antiulcer effect of this species at this lower dose.Fundação de Amparo à Pesquisa do Estado de São Paulo (FAPESP

Antileishmanial Activity of Dimeric Flavonoids Isolated from <i>Arrabidaea brachypoda</i>

Leishmaniasis are diseases caused by parasites belonging to Leishmania genus. The treatment with pentavalent antimonials present high toxicity. Secondary line drugs, such as amphotericin B and miltefosine also have a narrow therapeutic index. Therefore, there is an urgent need to develop new drugs to treat leishmaniasis. Here, we present the in vitro anti-leishmanial activity of unusual dimeric flavonoids purified from Arrabidaea brachypoda. Three compounds were tested against Leishmana sp. Compound 2 was the most active against promastigotes. Quantifying the in vitro infected macrophages revealed that compound 2 was also the most active against intracellular amastigotes of L. amazonensis, without displaying host cell toxicity. Drug combinations presented an additive effect, suggesting the absence of interaction between amphotericin B and compound 2. Amastigotes treated with compound 2 demonstrated alterations in the Golgi and accumulation of vesicles inside the flagellar pocket. Compound 2-treated amastigotes presented a high accumulation of cytoplasmic vesicles and a myelin-like structure. When administered in L. amazonensis-infected mice, neither the oral nor the topical treatments were effective against the parasite. Based on the high in vitro activity, dimeric flavonoids can be used as a lead structure for the development of new molecules that could be useful for structure-active studies against Leishmania

Dimeric flavonoids from Arrabidaea brachypoda and assessment of their anti-Trypanosoma cruzi activity.

Submitted by Ana Maria Fiscina Sampaio ([email protected]) on 2014-09-26T17:32:45Z No. of bitstreams: 1 Rocha C Dimeric Flavonoids....pdf: 1066770 bytes, checksum: a5b3e18ce047987fdf06cfd92e572bbb (MD5)Approved for entry into archive by Ana Maria Fiscina Sampaio ([email protected]) on 2014-09-26T17:33:00Z (GMT) No. of bitstreams: 1 Rocha C Dimeric Flavonoids....pdf: 1066770 bytes, checksum: a5b3e18ce047987fdf06cfd92e572bbb (MD5)Made available in DSpace on 2014-09-26T17:59:03Z (GMT). No. of bitstreams: 1 Rocha C Dimeric Flavonoids....pdf: 1066770 bytes, checksum: a5b3e18ce047987fdf06cfd92e572bbb (MD5) Previous issue date: 2014Universidade Estadual Paulista. Laboratório de Biodiversidade e Sustentabilidade. UNESP Coastal Campus, Parque BitaruThe nonpolar fraction of an aqueous ethanol extract of the roots of Arrabidaea brachypoda, a Brazilian medicinal plant, demonstrated significant in vitro activity against Trypanosoma cruzi, the parasite responsible for Chagas disease. Targeted isolation of the active constituents led to the isolation of three new dimeric flavonoids (1-3), and their structures were elucidated using UV, NMR, and HRMS analysis, as well as by chemical derivatization. The anti-T. cruzi activity and cytotoxicity toward mammalian cells were determined for these substances. Compound 1 exhibited no activity toward T. cruzi, while flavonoids 2 and 3 exhibited selective activity against these trypomastigotes. Compounds 2 and 3 inhibited the parasite invasion process and its intracellular development in host cells with similar potencies to benznidazole. In addition, compound 2 reduced the blood parasitemia of T. cruzi-infected mice. This study has revealed that these two dimeric flavonoids represent potential anti-T. cruzi lead compounds for further drug development

Ilex paraguariensis supplementation may be an effective nutritional approach to modulate oxidative stress during perimenopause

Perimenopause is a period in a woman´s life that precedes menopause and is characterized by hormonal changes that result in increased oxidative stress. Since oxidative stress is associated with age-related diseases and perimenopausal symptoms including somato-vegetative manifestations, nutritional antioxidant supplementation may be an effective approach to minimizing this stress. Mate tea (MT) (Ilex paraguariensis), a typical and inexpensive beverage consumed in the Brazilian south-east, Argentina and Uruguay, increases antioxidant defense. We hypothesized that MT could minimize oxidative stress during perimenopause by modulating enzymatic antioxidant defense. To test this, we analyzed the lipid oxidative damage and antioxidant defense in erythrocytes and liver of rats, after MT treatment. Female Wistar rats (aged 16 months) in proven perimenopause period received 20 mg/kg BW/day of mate tea, by gavage (PM + MT group) or water (PM group). Female rats aged 4 months (AD group) received water. Erythrocytes and liver were used to determine lipid oxidative damage, determined by malondialdehyde (MDA); superoxide dismutase (SOD), glutathione peroxidase (GPx) and catalase (CAT) activities. Total plasma antioxidant capacity was examined by ferric reducing antioxidant power assay (FRAP) and estrogen by radioimmunoassay. MT increased FRAP and did not change estrogen levels. Increased SOD and GPx, and reduced MDA were observed in both tissues studied. Increased CAT activity was observed only in the liver. We confirmed the hypothesis that MT was capable of minimizing oxidative stress in this period of life by modulating antioxidant defense.Fil: Pereira, Ariana Aparecida Ferreira. Universidade Estadual Paulista Julio de Mesquita Filho; BrasilFil: Tirapeli, Keny Gonçalves. Universidade Estadual Paulista Julio de Mesquita Filho; BrasilFil: Chaves Neto, Antonio Hernandes. Universidade Estadual Paulista Julio de Mesquita Filho; BrasilFil: da Silva Brasilino, Matheus. Universidade Estadual Paulista Julio de Mesquita Filho; BrasilFil: da Rocha, Cláudia Quintino. Universidade Estadual Paulista Julio de Mesquita Filho; BrasilFil: Belló Klein, Adriane. Universidade Federal do Rio Grande do Sul; BrasilFil: Llesuy, Susana Francisca. Consejo Nacional de Investigaciones Científicas y Técnicas. Oficina de Coordinación Administrativa Houssay. Instituto de Bioquímica y Medicina Molecular. Universidad de Buenos Aires. Facultad Medicina. Instituto de Bioquímica y Medicina Molecular; ArgentinaFil: Dornelles, Rita Cássia Menegati. Universidade Federal do Rio Grande do Sul; BrasilFil: Nakamune, Ana Cláudia de Melo Stevanato. Universidade Federal do Rio Grande do Sul; Brasi

Anatomical differentiation and metabolomic profiling: a tool in the diagnostic characterization of some medicinal Plantago species

There is a large list of plants used by the population as medicine, but in some case the choice of the right plant becomes a real drawback in phytotherapy, since it is often difficult to differentiate morphologically between the active and inactive species. Plantago species are widely used throughout the world as analgesic, anti-inflammatory, expectorant, digestive and wound healing. Nonetheless, Plantago spp. share very strong morphological similarities, which hinders their correct botanical identification and, in addition, they are equivocally marketed by the same common name “Plantain”. Therefore, the establishment of a reliable approach to distinguish unambiguously closely related species arises as an important task in the development of herbal medicines. In this work, we report a method that combines anatomical leaf features and chemical composition of four Plantago species to generate a multivariate model, which allows the differentiation of these species. Descriptive leaf anatomy was converted into a binary matrix to create a qualitative/quantitative non-metric multidimensional scaling (nmMDS) based on Jaccard index. The main results show that P. lanceolata L. is the most distinct species, the only one that owns mesophyll isolateral, colateral vascular bundle and a glandular trichome with spindle cells. Plantago major L. also has a unique glandular trichome, with enlarged basal cell and collar cell. This statistical-based anatomical approach is suitable to solve similar drawbacks in plant medicines of any other plant-cases. In addition, it was generated a nmMDS to chemical markers by mass spectrometry (FIA–ESI–IT–MS), to define how similar the species are regarding their chemical composition. Plantago major showed all compounds evaluated and is the only species to have the compounds hellicoside (m/z 655) and lavandulifolioside (m/z 755). The conversion of anatomical features into statistical data with the chemical composition emerges as a useful approach toward the quantitative differentiation of morphologically close related specimens.Fil: Mesquita, Leonardo Mendes de Souza. Universidade de Sao Paulo; BrasilFil: Delevati Colpo, Karine. Consejo Nacional de Investigaciones Científicas y Técnicas. Centro Científico Tecnológico Conicet - La Plata. Instituto de Limnología "Dr. Raúl A. Ringuelet". Universidad Nacional de La Plata. Facultad de Ciencias Naturales y Museo. Instituto de Limnología; ArgentinaFil: da Rocha, Cláudia Quintino. University of Maranhão ; BrasilFil: Gatte Picchi, Douglas. Universidade de Sao Paulo; BrasilFil: Pereira Tangerina, Marcelo Marucci. Universidade de Sao Paulo; BrasilFil: Zachello Nunes, Beatriz. Universidade de Sao Paulo; BrasilFil: Gonçalves Martins, Maria Bernadete. Universidade de Sao Paulo; BrasilFil: Vilegas, Wagner. Universidade de Sao Paulo; Brasi

<i>In vitro</i> anthelmintic effects of <i>Spigelia anthelmia</i> protein fractions against <i>Haemonchus contortus</i>

<div><p>Gastrointestinal nematodes are a significant concern for animal health and well-being, and anthelmintic treatment is mainly performed through the use of chemical products. However, bioactive compounds produced by plants have shown promise for development as novel anthelmintics. The aim of this study is to assess the anthelmintic activity of protein fractions from <i>Spigelia anthelmia</i> on the gastrointestinal nematode <i>Haemonchus contortus</i>. Plant parts were separated into leaves, stems and roots, washed with distilled water, freeze-dried and ground into a fine powder. Protein extraction was performed with sodium phosphate buffer (75 mM, pH 7.0). The extract was fractionated using ammonium sulfate (0–90%) and extensively dialyzed. The resulting fractions were named LPF (leaf protein fraction), SPF (stem protein fraction) and RPF (root protein fraction), and the protein contents and activities of the fractions were analyzed. <i>H</i>. <i>contortus</i> egg hatching (EHA), larval exsheathment inhibition (LEIA) and larval migration inhibition (LMIA) assays were performed. Proteomic analysis was conducted, and high-performance liquid chromatography (HPLC) chromatographic profiles of the fractions were established to identify proteins and possible secondary metabolites. <i>S</i>. <i>anthelmia</i> fractions inhibited <i>H</i>. <i>contortus</i> egg hatching, with LPF having the most potent effects (EC₅₀ 0.17 mg mL^-1). During LEIA, SPF presented greater efficiency than the other fractions (EC₅₀ 0.25 mg mL^-1). According to LMIA, the fractions from roots, stems and leaves also reduced the number of larvae, with EC₅₀ values of 0.11, 0.14 and 0.21 mg mL^-1, respectively. Protein analysis indicated the presence of plant defense proteins in the <i>S</i>. <i>anthelmia</i> fractions, including protease, protease inhibitor, chitinase and others. Conversely, secondary metabolites were absent in the <i>S</i>. <i>anthemia</i> fractions. These results suggest that <i>S</i>. <i>anthelmia</i> proteins are promising for the control of the gastrointestinal nematode <i>H</i>. <i>contortus</i>.</p></div

In Vitro Anti-Inflammatory Activity in Arthritic Synoviocytes of A. brachypoda Root Extracts and Its Unusual Dimeric Flavonoids

Arrabidaea brachypoda is a plant commonly used for the treatment of kidney stones, arthritis and pain in traditional Brazilian medicine. Different in vitro and in vivo activities, ranging from antinociceptive to anti-Trypanosoma cruzi, have been reported for the dichloromethane root extract of Arrabidaea brachypoda (DCMAB) and isolated compounds. This work aimed to assess the in vitro anti-inflammatory activity in arthritic synoviocytes of the DCMAB, the hydroethanolic extract (HEAB) and three dimeric flavonoids isolated from the DCMAB. These compounds, brachydin A (1), B (2) and C (3), were isolated both by medium pressure liquid and high-speed counter current chromatography. Their quantification was performed by mass spectrometry on both DCMAB and HEAB. IL-1β activated human fibroblast-like synoviocytes were incubated with both extracts and isolated compounds to determine the levels of pro-inflammatory cytokine IL-6 by enzyme-linked immunosorbent assay (ELISA). DCMAB inhibited 30% of IL-6 release at 25 µg/mL, when compared with controls while HEAB was inactive. IC50 values determined for 2 and 3 were 3-fold higher than 1. The DCMAB activity seems to be linked to higher proportions of compounds 2 and 3 in this extract. These observations could thus explain the traditional use of A. brachypoda roots in the treatment of osteoarthritis

Involvement of Opioid System, TRPM8, and ASIC Receptors in Antinociceptive Effect of Arrabidaea brachypoda (DC) Bureau

Arrabidaea brachypoda (DC) Bureau is a medicinal plant found in Brazil. Known as "cipó-una", it is popularly used as a natural therapeutic agent against pain and inflammation. This study evaluated the chemical composition and antinociceptive activity of the dichloromethane fraction from the roots of A. brachypoda (DEAB) and its mechanism of action. The chemical composition was characterized by high-performance liquid chromatography, and this fraction is composed only of dimeric flavonoids. The antinociceptive effect was evaluated in formalin and hot plate tests after oral administration (10-100 mg/kg) in male Swiss mice. We also investigated the involvement of TRPV1 (transient receptor potential vanilloid 1), TRPA1 (transient receptor potential ankyrin 1), TRPM8 (transient receptor potential melastatin 8), and ASIC (acid-sensing ion channel), as well as the opioidergic, glutamatergic, and supraspinal pathways. Moreover, the nociceptive response was reduced (30 mg/kg) in the early and late phase of the formalin test. DEAB activity appears to involve the opioid system, TRPM8, and ASIC receptors, clearly showing that the DEAB alleviates acute pain in mice and suggesting the involvement of the TRPM8 and ASIC receptors and the opioid system in acute pain relief

Plant Metabolites as SARS-CoV-2 Inhibitors Candidates: In Silico and In Vitro Studies

Since it acquired pandemic status, SARS-CoV-2 has been causing all kinds of damage all over the world. More than 6.3 million people have died, and many cases of sequelae are in survivors. Currently, the only products available to most of the world&rsquo;s population to fight the pandemic are vaccines, which still need improvement since the number of new cases, admissions into intensive care units, and deaths are again reaching worrying rates, which makes it essential to compounds that can be used during infection, reducing the impacts of the disease. Plant metabolites are recognized sources of diverse biological activities and are the safest way to research anti-SARS-CoV-2 compounds. The present study computationally evaluated 55 plant compounds in five SARS-CoV-2 targets such Main Protease (Mpro or 3CL or MainPro), RNA-dependent RNA polymerase (RdRp), Papain-Like Protease (PLpro), NSP15 Endoribonuclease, Spike Protein (Protein S or Spro) and human Angiotensin-converting enzyme 2 (ACE-2) followed by in vitro evaluation of their potential for the inhibition of the interaction of the SARS-CoV-2 Spro with human ACE-2. The in silico results indicated that, in general, amentoflavone, 7-O-galloylquercetin, kaempferitrin, and gallagic acid were the compounds with the strongest electronic interaction parameters with the selected targets. Through the data obtained, we can demonstrate that although the indication of individual interaction of plant metabolites with both Spro and ACE-2, the metabolites evaluated were not able to inhibit the interaction between these two structures in the in vitro test. Despite this, these molecules still must be considered in the research of therapeutic agents for treatment of patients affected by COVID-19 since the activity on other targets and influence on the dynamics of viral infection during the interaction Spro x ACE-2 should be investigated