In vivo analgesic activity, toxicity and phytochemical screening of the hydroalcoholic extract from the leaves of Psidium cattleianum Sabine

Ethnopharmacological relevance: Psidium cattleianum Sabine is extensively used in Brazilian traditional medicine to treat several diseases including painful disorders. Aim of the study to investigate the toxicity and the possible analgesic activities of the hydroalcoholic extract from the leaves of Psidium cattleianum Sabine (ELPCS), to support its use in folk medicine. To screen the major phytochemical constituents of this extract and evaluate their antioxidant activity. Materials and methods: ELPCS was assessed for its antioxidant activity using the DPPH model. Its analgesic activity was examined using mouse models of acetic acid-induced writhing and hot plate paw licking models. The major phytochemical constituents of the extract were screened; their toxicity on LLC-MK2 mammalian cells was evaluated. Results: ELPCS exhibited significant peripheral analgesic activity at doses of 60, 80, 100, 200 and 400 mg/kg in mice, but it did not display central analgesic activity and not was toxic to LLC-MK2 cell (LD 50>400 μg/mL). The extract exhibited free radical scavenging activity as evidenced by IC 50 values (15.9 μg/mL) obtained by the DPPH method. Phytochemical screening detected flavonoids, saponins, cardiac glycosides, anthraquinones, and tannins. Conclusions: The results of the experimental studies proved the analgesic activity of ELPCS and supported the traditional use of this plant. © 2013 Elsevier B.V. All rights reserved.

Dihydroflavonols from the leaves of Derris urucu (Leguminosae): structural elucidation and DPPH radical-scavenging activity

Derris urucu é uma planta da Amazônia com propriedades inseticida e ictiotóxica. Estudos com esta espécie reportam a presença de flavonóides, principalmente rotenóides, bem como de estilbenos. A partir do extrato etanólico das folhas de Derris urucu (Leguminosae), três novos diidroflavonóides, denominados urucuol A (1), B (2) e C (3) e o diidroflavonol isotirumalina (4), foram isolados e identificados. As estruturas destes compostos foram elucidadas por uma extensiva análise espectroscópica de RMN uni e bidimensional, UV, IV e dados de EM, além de comparação com dados da literatura. Os compostos isolados (1-4) foram avaliados quanto ao seu potencial sequestrador do radical DPPH• e apresentaram baixo poder antioxidante quando comparados ao antioxidante comercial trans-resveratrol.

A new flavonoid derivative from leaves of Oxandra Sessiliflora R. E. Fries

A fração em acetato de etila (EtOAc) obtida a partir da partição do extrato de etanol (EtOH) das folhas de O. sessiliflora R. E. Fries (Annonaceae) foi submetida a diversos procedimentos cromatográficos, incluindo cromatografia líquida de alta eficiência (HPLC), o que resultou no isolamento dos flavonóides: quercetina-3-O-α-L-ramnopiranosil-(1→4)-β-D-glucopiranosídeo (1), inédito na literatura, canferol-3-O-α-L-ramnopiranosil-(1→4)-β-D-glucopiranosídeo (2), rutina (3) e canferol-3-O-rutinosídeo (4). As estruturas foram definidas através da análise dos espectros de ressonância magnética nuclear (NMR) de ¹H e de 13C (1D e 2D) e espectrometria de massas.

Antifungal activity of flavonoids from Heteropterys byrsonimifolia and a commercial source against Aspergillus ochraceus: In silico interactions of these compounds with a protein kinase

Coordenação de Aperfeiçoamento de Pessoal de Nível Superior (CAPES)

Ethanolic extract of Mimosa caesalpiniifolia leaves: Chemical characterization and cytotoxic effect on human breast cancer MCF-7 cell line

Fundação de Amparo à Pesquisa do Estado de São Paulo (FAPESP)

Phytotoxicity of ethanolic extract of turnip leaves (raphanus sativus l.)

The study of allelopathic activity has been aim of research that evaluates mainly species used in green fertilization. Raphanus sativus L. stands out among these species, because it shows high capacity for nutrient recycling, specially nitrogen and phosphorus, what makes it an advantageous cover plant in crop rotation systems. Considering the exposed, the present study had as objective the evaluation of the allelopathic and phytotoxic potentials of different concentrations of the R. sativus leaves ethanolic extract by mean of seeds germination analyses and development of lettuce seedlings, evaluating the phytotoxicity by determination of the mitotic index of lettuce root cells, realizing the phytochemical profile and investigating the antioxidant activity. It was possible to verify that the R. sativus extract interferes in the germination index, decreasing the germinability (5 mg. mL(-1) = 9.84%; 10 mg. mL(-1) = 11.91% and 20 mg. mL(-1)= 57.51%). In the lettuce seedlings growth, the extract of this species affected the roots and hypocotyls growth. It was possible to observe phenols and total flavonoids in the extract for the concentration of 1000 mu g. mL(-1)(161mg and 83.57 mg, respectively). It was also observed, higher antioxidant activity for the concentration of 1000 mu g. mL(-1) (89.76%). In the phytotoxicity assay was observed a dose dependent effect in the mitotic index and in the cellular events during cellular division. In this study it was possible to conclude that this species has allelochemical compounds which are able to interfere directly on the stabilization and development of other species.

Flavonoid Detection in Hydroethanolic Extract of Pouteria torta (Sapotaceae) Leaves by HPLC-DAD and the Determination of Its Mutagenic Activity

Fundação de Amparo à Pesquisa do Estado de São Paulo (FAPESP)

Antinociceptive, anti-inflammatory and gastroprotective effects of a hydroalcoholic extract from the leaves of Eugenia punicifolia (Kunth) DC. in rodents

Conselho Nacional de Desenvolvimento Científico e Tecnológico (CNPq)

Phytotoxicity of Solanum aculeatissimum Jacq: leaves extract

The objective of this study was to evaluate the phytotoxicity of Solanum aculeatissimum Jacq. leaves ethanolic extract in seeds germination, development and fixation of Lactuca sativa seedlings. The same study also aimed to assess the mitotic index of lettuce roots meristematic cells, quantification of phenols and total flavonoids and triage by mean of phytochemical testing of the main secondary metabolites classes. Bioassays of germination, development of root and hypocotyl were carried out in Petri dishes using achenes of Lactuca sativa L. cv. 'Grand Rapids' (lettuce). Concomitantly, were evaluated the physico-chemical characteristics (pH, osmotic potential and electrical conductivity), mitotic index, quantification of total phenols and flavonoids and determination of phytochemical profile of the treatments extract. The results obtained in the bioassays demonstrate that the ethanol extract of S. aculeatissimuma presents phytotoxic potential in the development of lettuce seedlings, given that the concentration of 20 mg/ml showed greater inhibition (41% of germination). The extract contains significant amounts of antioxidants, total flavonoid and phenols, where the concentration 1000µg/mL showed higher values (86.50%). Furthermore, it was possible to observe the presence of compounds with allelopathic activity in the phytochemical screening test as coumarins, tannins, terpenes, flavonoids and alkaloids. Given the above it is clear that the ethanolic extract of S. aculeatissimum presents allelopathic substances with phytotoxic activity that can affect the germination and development of other plant species in their natural environment.

Antinociceptive, anti-inflammatory and gastroprotective effects of a hydroalcoholic extract from the leaves of Eugenia punicifolia (Kunth) DC. in rodents

Conselho Nacional de Desenvolvimento Científico e Tecnológico (CNPq)

Schistosomicidal evaluation of flavonoids from two species of Styrax against Schistosoma mansoni adult worms

Context: Schistosomiasis is a major health problem worldwide. Thus, the search for new schistosomicidal agents from natural sources can provide prototypes for drug discovery. Objective: The present study investigated the chemical composition of the EtOAc fractions of Styrax pohlii Pohl (Styracaceae) (EF-SP) aerial parts and S. camporum A. DC. leaves (EF-SC), as well as schistosomicidal activities against Schistosoma mansoni adult worms, which have not yet been studied. Materials and methods: The crude ethanol extracts of S. camporum leaves and S. pohlii aerial parts (EE-SC and EE-SP) were partitioned with n-hexane, EtOAc, and n-BuOH. The EtOAc fractions were purified by preparative HPLC. The crude extracts, EtOAc fractions and pure compounds were tested against S. mansoni adult worms in vitro. Results: The purification procedure resulted in the isolation of kaempferol-3-O-(2 '',4 ''-di-O-(E)-p-coumaroyl)-beta-D-glucopyranoside (1), kaempferol-3-O-(2 '',6 ''-di-O-(E)-p-coumaroyl)-beta-D-glucopyranoside (2), quercetin (3), and kaempferol (4). The bioassay results indicated that EE-SC, EF-SC, EF-SP, and compounds 2 and 4 are able to separate coupled S. mansoni adult worms. Additionally, EE-SC, EF-SP, and compound 4 killed the adult schistosomes in vitro at 100 mu g/mL and 100 mu M. Discussion and conclusion: This is the first time that the presence of compounds 1-2 in S. pohlii and 3-4 in S. camporum has been reported. Additionally, biological results indicated that S. pohlii and S. camporum have great potential as a source of active compounds.

SEASONAL VARIATION OF THE MAJOR SECONDARY METABOLITES PRESENT IN THE EXTRACT OF Eremanthus mattogrossensis Less (Asteraceae: Vernonieae) LEAVES

The species Eremanthus mattogrossensis, known as "veludo do cerrado" (cerrado velvet), is native to the Brazilian Cerrado. Because the amount of metabolites present in plants may be influenced by biological and environmental factors, here we conducted an HPLC-DAD-MS/MS investigation of the metabolite concentrations found in the MeOH/H2O extract of the leaves of this species. The main compounds were identified and quantified, and the metabolites were grouped by chemical class (caffeoylquinic acids, flavonoids, and sesquiterpene lactone). Statistical analysis indicated a straight correlation between the quantity of metabolites and seasonality, suggesting that environmental properties elicit important metabolic responses.

Cytotoxicity of cashew flavonoids towards malignant cell lines

The leaves of the Cashew plant (Anacardium occidentale L.) are used by the folk medicine in South America and West Africa. This plant is rich in flavonoids, which are polyphenolic compounds widespread in plants, and that have diverse physiological effects. In a sub-acute toxicity assay it was found that an ethanolic extract of Cashew leaves elicited lymphopenia in rats. The extract was also found to be cytotoxic and to induce apoptosis in Jurkat (acute lymphoblastic leukemia) cells. The crude ethanolic extract was fractionated and resolved by HPLC. One of the four fractions obtained led to the isolation of the biflavonoid agasthisflavone. [H-3]-thymidine incorporation assays and flow cytometry analysis showed that the isolated compound displayed a high anti-proliferative effect in Jurkat cells with an IC50 of 2.4 mu g/ml (4.45 mu M). The effect of agathisflavone on the acute promyelocytic leukemia cell line HL60, Burkitt lymphoma Raji cells and Hep-2 laryngeal carcinoma cells was also tested. The two latter ones were only mildly affected by agathisflavone. It is also shown that agathisflavone induces apoptosis in Jurkat cells and it this proposed that this is the likely mechanism of agathisflavone specific cytotoxicity. (C) 2010 Elsevier GmbH. All rights reserved.

A Validated Chromatographic Method for the Determination of Flavonoids in Copaifera langsdorffii by HPLC

Hydroethanolic extracts of C. langsdorffii leaves have therapeutic potential. This work reports a validated chromatographic method for the quantification of polar compounds in the hydroethanolic extract of C. langsdorffii leaves. A reliable HPLC method was developed using two monolithic columns linked in series (100 x 4.6 mm - C-18), with nonlinear gradient elution, and UV detection set at 257 nm. A procedure for the extraction of flavonols was also developed, which involved the use of 70% aqueous ethanol and the addition of benzophenone as the internal standard. The developed method led to a good detection response as the values for linearity were between 10.3 and 1000 mu g/mL, and those for recovery between 84.2 and 111.1%. The detection limit ranged from 0.02 to 1.70 mu g/mL and the quantitation limit from 0.07 to 5.1 mu g/mL, with a maximum RSD of 5.24%. Five compounds, rutin, quercetin-3-O-alpha-L-rhamnopyranoside, kaempferol-3-O-alpha-L-rhamnopyranoside, quercetin and kaempferol, were quantified. This method could, therefore, be used for the quality control of hydroethanolic extracts of Copaifera leaves and their cosmetic and pharmaceutical products.

Effect of hydroalcoholic extract from Copaifera langsdorffii leaves on urolithiasis induced in rats

Copaifera langsdorffii Desf. commonly known as "copaiba", produce a commercially valuable oil-resin that is extensively used in folk medicine for anti-inflammatory, antimicrobial and antiseptic purposes. We have found the hydroalcoholic extract of this plant leaf has the potential to treat urolithiasis, a problem affecting similar to 7% of the population. To isolate the functional compounds C. langsdorffii leaves were dried, ground, and macerated in a hydroalcoholic solution 7:3 to produce a 16.8% crude extract after solvent elimination. Urolithiasis was induced by introduction of a calcium oxalate pellet (CaOx) into the bladders of adult male Wistar rats. The treated groups received the crude extract by oral gavage at 20 mg/kg body weight daily for 18 days. Extract treatment started 30 days after CaOx seed implantation. To monitor renal function sodium, potassium and creatinine concentrations were analyzed in urine and plasma, and were found to be in the normal range. Analyses of pH, magnesium, phosphate, calcium, uric acid, oxalate and citrate levels were evaluated to determine whether the C. langsdorffii extract may function as a stone formation prevention agent. The HPLC analysis of the extract identified flavonoids quercitrin and afzelin as the major components. Animals treated with C. langsdorffii have increased levels of magnesium and decreased levels of uric acid in urinary excretions. Treated animals have a significant decrease in the mean number of calculi and a reduction in calculi mass. Calculi taken from extract treated animals were more brittle and fragile than calculi from untreated animals. Moreover, breaking calculi from untreated animals required twice the amount of pressure as calculi from treated animals (6.90 +/- A 3.45 vs. 3.00 +/- A 1.51). The extract is rich in flavonoid heterosides and other phenolic compounds. Therefore, we hypothesize this class of compounds might contribute significantly to the observed activity.