9 research outputs found

    Impact of seasonal and Organ-Related Fluctuations on the anthelmintic properties and chemical profile of Cladium mariscus (L.) Pohl Extracts

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    The use of plants and their metabolites stands as a promising option to tackle parasitic infections by gastrointestinal nematodes (GIN) in integrated control strategies. Still, the influence of environmental and phenological factors, and their interactions, in the wild on the metabolomics and biological properties of target plant species, is often disregarded. In this work, we hypothesized that variations in the anthelmintic (AH) properties and chemical composition of extracts from the salt tolerant species Cladium mariscus L. Pohl (sawgrass) may be influenced by seasonal factors and organ-parts. To test this hypothesis, acetone/water extracts were prepared from dried biomass obtained from aerial organs collected from sawgrass in consecutive seasons and tested against Haemonchus contortus and Trichostrongylus colubriformis by the larval exsheathment inhibition assay (LEIA) and egg hatching inhibition assay (EHIA). To ascertain the role of plant organ, the activity of leaves and inflorescences extracts from summer samples was compared. The role of polyphenols in the anthelmintic activity depending on GINs and fluctuations across seasons and plant organs was assessed using polyvinylpolypyrrolidone (PVPP), coupled with an in-depth chemical profiling analysis using high-performance liquid chromatography completed with electrospray ionization mass spectrometric detection (HPLC-ESI-MSn). Main differences in anthelmintic activities were observed for summer and autumn samples, for both assays. Moreover, inflorescences' extracts were significantly more active than those from leaves against both parasite species on EHIA and against H. contortus on LEIA. Application of PVPP totally inhibit the AH effects based on EHIA and only partly for LEIA. Non-treated PVPP extracts were predominantly composed of flavan-3-ols, proanthocyanidins, luteolin and glycosylated flavonoids, while two flavonoid glycosides were quantified in all PVPP-treated samples. Thus, the activity of such compounds should be further explored, although some unknown metabolites remain to be identified. This study reinforces the hypothesis of the AH potential of sawgrass and of its polyphenolic metabolites uses as nutraceutical and/or phytotherapeutic drugs.info:eu-repo/semantics/publishedVersio

    Quercetin pentaacetate inhibits in vitro human respiratory syncytial virus adhesion.

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    Made available in DSpace on 2020-12-12T01:06:20Z (GMT). No. of bitstreams: 0 Previous issue date: 2020-01-15 Fundação de Amparo à Pesquisa do Estado de São Paulo (FAPESP) Human respiratory syncytial virus (hRSV) is one of the main etiological agents of diseases of the lower respiratory tract and is often responsible for the hospitalization of children and the elderly. To date, treatments are only palliative and there is no vaccine available. Natural products show exceptional structural diversity and they have played a vital role in drug research. Several investigations focused on applied structural modification of natural products to improved metabolic stability, solubility and biological actions them. Quercetin is a flavonoid that presents several biological activities, including anti-hRSV role. Some works criticize the pharmacological use of Quercetin because it has low solubility and low specificity. In this sense, we acetylated Quercetin structure and we used in vitro and in silico assays to compare anti-hRSV function between Quercetin (Q0) and its derivative molecule (Q1). Q1 shows lower cytotoxic effect than Q0 on HEp-2 cells. In addition, Q1 was more efficient than Q0 to protect HEp-2 cells infected with different multiplicity of infection (0.1–1 MOI). The virucidal effects of Q0 and Q1 suggest interaction between these molecules and viral particle. Dynamic molecular results suggest that Q0 and Q1 may interact with F-protein on hRSV surface in an important region to adhesion and viral infection. Q1 interaction with F-protein showed ΔG= -14.22 kcal/mol and it was more stable than Q0. Additional, MTT and plate assays confirmed that virucidal Q1 effects occurs during adhesion step of cycle hRSV replication. In conclusion, acetylation improves anti-hRSV Quercetin effects because Quercetin pentaacetate could interact with F-protein with lower binding energy and better stability to block viral adhesion. These results show alternative anti-hRSV strategy and contribute to drug discovery and development. Universidade Estadual Paulista UNESP (FCLAssis) Universidade Estadual Paulista UNESP IBILCE Centro Multiusuário de Inovação Biomolecular (CMIB) Universidade Estadual Paulista UNESP IBILCE Department of Biology University of Rome Tor Vergata, Via della Ricerca Scientifica 1 Universidade Estadual Paulista UNESP (FCLAssis) Universidade Estadual Paulista UNESP IBILCE Centro Multiusuário de Inovação Biomolecular (CMIB) Universidade Estadual Paulista UNESP IBILCE FAPESP: 2014/12298-

    Sapindaceae do noroeste paulista: lista de espécies e chave de identificação baseada em caracteres vegetativos

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    The species identification is usually an obstacle for conservation studies and management. Sapindaceae species are particularly difficult to identify partially due to inconsistent fruit production which is an important feature in defining genera and species. Because of this difficulty of finding fertile material at particular times of the year, the main focus of this study was to identify species of Sapindaceae in northwestern São Paulo and to produce an identification key based on vegetative morphology such as the form and number of leaflets, the number of vascular cylinders in branches to the species of liana, the presence or absence of domatia, and type of indumentum, among others. In this study, researchers identified species of Sapindaceae present in 18 fragments of native vegetation in the region that includes the Turvo Grande, São José dos Dourados, parts of the Low Pardo, Low Tietê and Tietê-Batalha Hydric Resources Management Unit (UGHRIs). An identification key was developed based on herbarium materials and contained 23 species distributed in 11 genera

    Divulgação dos metabólitos bioativos envolvidos nos efeitos anténticos in vitro de plantas tolerantes ao sal através de uma abordagem combinada usando PVPP e HPLC-ESI-MSn

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    Strategies to reduce dependence on synthetic drugs for the treatment of gastrointestinal nematodes (GIN) infections in ruminants include the search for novel anthelmintic scafolds on plants, yet salt-tolerant plants remain overlooked. This study aims to evaluate the in vitro anthelmintic properties of selected salt-tolerant plants against GIN, and identify the potential bioactive secondary metabolites involved. For that purpose, 80% acetone/water extracts were prepared from dried biomass of aerial organs of nine salt-tolerant plant species and tested against Haemonchus contortus and Trichostrongylus colubriformis by the Larval Exsheathment Inhibition Assay (LEIA) and Egg Hatching Inhibition Assay (EHIA). Pistacia lentiscus, Limoniatrum monopetalum, Cladium mariscus and Helychrisum italicum picardi were the most active in both GIN and life stages. To investigate the role of polyphenols in the anthelmintic activity, four selected extracts were treated with polyvinylpolypyrrolidone (PVPP), and non-treated and treated samples were further characterized by high-performance liquid chromatography with electrospray ionization mass spectrometric detection (HPLC-ESI-MSn). While polyphenols seem responsible for the EHIA properties, they are partially accountable to LEIA results. Several phenolics involved in the anthelmintic efects were identifed and discussed. In sum, these species are rich sources of anthelmintic compounds and, therefore, are of major interest for nutraceutical and/or phytotherapeutic applications against GIN in ruminants.info:eu-repo/semantics/publishedVersio

    Germinação de sementes e desenvolvimento inicial de Erythrina mulungu (Mart. ex. Benth)

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    The aim of this study was to determine the best pre-germination treatments for seeds and the best size container for seedlings growing of coral tree Erythrina mulungu (Mart. ex. Benth). Among the treatments applied to seeds, scarification with sulfuric acid during 10 minutes and cutting stylus in the region opposite to hilum resulted, respectively, in highest values of germination percentage (82.8% and 82.1%) and rates of germination speed (1.15 and 1.71). The biometric variables indicated no effect of container size on leaf area and dry mass plants. At 63 days after sowing, although with Dickson quality score statistically similar (mean 0.26), only plants grown in small and large bags reached the diameter collect close to 5 mm, minimum recommended for field planting. According to the results, for initial development of coral tree, it is recommended pre-seed treatment with sulfuric acid commercial, sowing in plastic bags of 17 x 20 cm, and wait 63 days before planting in the field.Objetivou-se escolher os melhores tratamentos pré-germinativos para as sementes e tamanhos de recipiente para o desenvolvimento inicial de plantas de Erythrina mulungu (Mart. ex. Benth). Dentre os tratamentos aplicados, a escarificação com ácido sulfúrico por 10 minutos e o corte com estilete na região oposta ao hilo resultaram, respectivamente, nos maiores resultados de porcentagem de germinação (82,8% e 82,1%) e índices de velocidade de germinação (1,15 e 1,71). Não foram observados efeitos do tamanho do recipiente sobre a área foliar e a produção de massa seca das plantas. Aos 63 dias após a semeadura, embora com índice de qualidade de Dickson estatisticamente similares (média de 0,26), somente as plantas cultivadas nos recipientes pequenos e grandes atingiram o diâmetro de coleto próximo de 5 mm, valor mínimo recomendado para o plantio em campo. Assim, para o desenvolvimento inicial desta espécie, recomenda-se o pré-tratamento das sementes com ácido sulfúrico comercial, semeadura em sacos plásticos para mudas de 17 x 20 cm, e aguardo de 63 dias até o plantio em campo

    Anti-Candida and anti-Cryptococcus evaluation of 15 non-alkaloidal compounds from Pterogyne nitens

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    Objective: To evaluate anti-Candida and anti-Cryptococcus activities of 15 non-alkaloidal compounds from Pterogyne nitens Tulasne (Leguminosae), a South American medicinal plant. Methods: Compounds were submitted to antifungal assays, using microdilution method described by Clinical and Laboratory Standards Institute document, with minor modifications. Five species of Candida and two species of Cryptococcus, including clinical isolates were screened. Antifungal activity was expressed by minimum inhibitory concentration (MIC). Amphotericin B and fluconazole were used as standard antifungal drugs. Results: Among tested compounds, six substances presented fungal growth inhibition (MIC < 31.2 μg/mL) [three flavone derivatives (1–3), a glycosylated flavonol derivative (5) and two phenolic acids (10 and 12)]. Sorbifolin (1), exhibited potent antifungal activity, demonstrating MIC value of 3.90 μg/mL against Candida glabrata ATCC 90030, Cryptococcus gattii 118 and fluconazole-resistant clinical isolate of Cryptococcus neoformans var. grubii. Pedalin (2) and nitensoside B (3), two glycosylated flavone derivatives, were active against Cryptococcus neoformans ATCC 90012 (MIC = 7.80 μg/mL). Conclusions: Flavone derivatives from Pterogyne nitens can serve as prototypes for the design and development of innovative anti-Candida and anti-Cryptococcus hits
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