RESUMO

Protozoa of the genus Phytomonas are harmful parasites to several agricultural crops of economic importance. Due to their recognized biological activity, crude extracts of Piper aduncum, P. crassinervium, P. hispidum, and P. amalago leaves, were tested using the microdilution plate technique to assess the antiparasitic potential against Phytomonas serpens. Results showed that the ethanolic crude extract of P. crassinervium and P. amalago presented the best inhibitory concentration for 50% of the cells (IC50), 16.5 µg mL-1 in chloroform phase, and 18 µg mL-1 in aqueous phase, respectively, after 48 h treatment. Cytotoxicity analyses were performed using the colorimetric method of sulforhodamine-B in LLCMK2 mammalian cells. The chloroform phase of P. crassinervium was subjected to the fractionation process, in which the ethyl acetate and dichloromethane fractions obtained better IC50 values. Scanning electron microscopy (SEM) images showed alterations in the cell membrane of the treated parasites. The data obtained indicate a potential antiparasitic effect of the Piper species analyzed against P. serpens, being considered promising candidates for formulations of bioproducts to control the parasite.(AU)

Protozoários do gênero Phytomonas são parasitas prejudiciais a várias culturas agrícolas de importância econômica. Devido a sua atividade biológica reconhecida, extratos brutos de folhas de Piper aduncum, P. crassinervium, P. hispidum e P. amalago, foram testadas pela técnica de microdiluição em placa para avaliar o seu potencial antiparasitário contra Phytomonas serpens. Os resultados mostraram que o extrato bruto etanólico de P. crassinervium e P. amalago apresentaram as melhores concentrações inibitórias para 50% das células (IC50), 16,5 µg mL-1 na fase clorofórmio e 18 µg mL-1 na fase aquosa, respectivamente, após 48 h de tratamento. Análises de citotoxicidade foram realizadas através do método colorimétrico da sulforodamina-B, em células de mamíferos LLCMK2. A fase clorofórmio de P. crassinervium foi submetida ao processo de fracionamento, no qual as frações acetato de etila e diclorometano obtiveram melhores valores de IC50. Imagens de microscopia eletrônica de varredura (MEV) mostraram alterações na membrana celular dos parasitas tratados com fase aquosa de P. amalago. Os dados obtidos indicam potencial efeito antiparasitário das espécies de Piper analisadas contra P. serpens, sendo consideradas candidatas promissoras para formulações de bioprodutos para controle do parasito.(AU)

Assuntos

RESUMO

The crude hydroalcoholic extract from fruits of P. pubescens is widely used because of its anti-rheumatic, antinociceptive and anti-inflammatory activities. Furanoditerpenes have a vouacapan skeleton and are involved with the pharmacological activity of the oil extracted from P. pubescens fruits. Furanoditerpenes methyl 6α-acetoxy-7ß-hydroxyvouacapan-17ß-oate and methyl 6α-hydroxy-7ß-acetoxyvouacapan-17ß-oate from P. pubescens were isolated and identified. The present study developed and validated a GC-MS-SIM method for the separation and quantification of vouacapan constituents in a semipurified extract from P. pubescens fruits. The GC-MS analyses were carried out using a system equipped with a HP-5 capillary column (30 m × 0.25 mm). Temperature program: 100°C (4°C min(-1))-270°C (5 min), injector 260°C, detector 270°C. Helium was used as the carrier gas (0.7 bar, 1 mL min(-1)). The MS was taken at 70 eV. Scanning speed was 0.5 scans s(-1), from 50 to 650. Sample volume was 1 µL. Split 1:20. Analyses for validation of methodology were conducted by GC-MS-SIM (Single Ion Monitoring), where the ions monitored were 131, 145 and 146 (between 43 and 44.5 min), 105, 145 and 197 (from 44.5 to 45.3 min) and 131, 178 and 312 (from 45.3 to 48.5 min).Validation of the analytical method was based on the following parameters: linearity, robustness, limits of detection and quantification, precision (within-day and between-day variabilities), recovery and stability. The method was linear over a range of 12.81-2.56 µÎ³µΛ(-1) of vouacapan 1, 112.78-22.56 µg mL(-1) of vouacapan 2, and 333.34-66.67 µg mL(-1) of vouacapans 3 and 4, with detection limits of 0.39, 3.45 and 9,44 µg mL(-1) and quantification limits of 1.19, 10.47 and 28.62 µg mL(-1), respectively. Recovery values were 100.69%, 97.48% and 96.98% for vouacapans 1, 2 and 3-4, respectively. Thus, the method was efficient to separate and quantify furanoditerpenes in the extract or fraction.

Assuntos

RESUMO

An extract from seeds of Chenopodium quinoa Willd. (quinoa), termed hydrolyzed quinoa (HQ), was obtained by enzymatic hydrolysis from seeds of the quinoa variety BRS-Piabiru. Analysis of the physical and chemical properties of quinoa and HQ showed that the hydrolyzed extract is rich in essential amino acids, particularly those with branched chains (leucine, isoleucine, and valine). In addition, we evaluated the biological effects of HQ, particularly the toxicological potential. For this purpose, male Wistar rats were assigned randomly to four groups: (1) sedentary supplemented group, which received HQ (2,000 mg/kg); (2) sedentary control group, non-supplemented; (3) exercised supplemented group (i.e., rats subjected to aerobic physical exercise that received HQ [2,000 mg/kg]); and (4) exercised control group (i.e., rats subjected to aerobic physical exercise, non-supplemented). After 30 days, all groups were analyzed for levels of serum glucose, cholesterol, triacylglycerol, total protein, albumin, uric acid, and urea and activities of the enzymes alkaline phosphatase, aspartate aminotransferase, and alanine aminotransferase. Body weight gain, dietary intake, and lipid deposition were also analyzed. The results showed no hepatic and renal toxicity of HQ. Moreover, decreased food intake, body weight, fat deposition, and blood triacylglycerol level were observed in the supplemented groups (sedentary and exercised supplemented groups). These results suggest a potential use of HQ in human nutrition.

Assuntos

RESUMO

CONTEXT: The Asteraceae family has been of interest to researchers due to the presence of polyphenolic compounds, mainly flavonoids, which demonstrated antiviral activity. OBJECTIVE: The hydroethanol extract of the aerial parts of Acanthospermum australe (Loefl.) Kuntze (Asteraceae) and its fractions, were evaluated in vitro for their potential cytotoxic and antiviral activity against bovine herpesvirus and human poliovirus. MATERIALS AND METHODS: The sulforhodamine B colorimetric assay were used to evaluate the capacity of the hydroethanol extract and fractions to inhibit the lytic activity of herpes and poliovirus in infected cell cultures and their influence on the viability of uninfected cell cultures. RESULTS AND DISCUSSION: A progressive increase in the antiviral effect against herpesvirus was observed in the course of the purification process of the extract. The hydroethanol extract had a 50% antiviral effective concentration (EC(50)) at 70 µg/mL and 36 µg/mL for herpes and poliovirus, respectively, and it exhibited no cytotoxicity. The fractions F3 (dichloromethane) and F4 (dichloromethane: ethyl acetate (1:1 v/v)) both showed EC(50) at 6.25 µg/mL against herpesvirus, and these fractions showed cytotoxic concentrations (CC(50)) at 12.7 and 11.7 µg/mL, respectively. These fractions had no effect against poliovirus in the concentrations tested. From the bioactive F3, a diterpene lactone (acanthoaustralide-1-O-acetate) was isolated at a concentration of 0.5% and from F4 two flavonoids (quercetin and chrysosplenol D) were isolated at concentrations of 0.14 and 0.24%, respectively. CONCLUSION: The present study reports for the first time the antiviral activity of extracts and fractions from A. australe aerial parts.

Assuntos

RESUMO

Kielmeyera coriacea Mart. (Clusiaceae), known as "Pau Santo" or "Saco de Boi" in the central Brazilian plateau region, is used to treat several tropical diseases. The present study evaluated the toxic effects of dichloromethane (DcM) extract of Kielmeyera coriacea stems, administered to rodents. In the acute toxicity tests, mice receiving doses of this extract by the oral and intraperitoneal routes, showed reversible effects, with LD50 values of 1503.0 and 538.8 mg/kg, respectively. In the repeated-dose oral (90 days) toxicity tests, male and female Wistar rats were treated by gavage with different doses of DcM extract (5, 25 or 125 mg/kg). In biochemical and haematological evaluations, the results varied widely in respect to dose and sex, with no linear profile, and did not show clinical correlations. In the histopathological examinations, the groups exhibited some changes, but there were no significant differences between the groups compared to the controls. In conclusion, these investigations appeared to indicate the safety of acute and repeated oral administration of the DcM extract of Kielmeyera coriacea stems, which can therefore be continuously used with safety.

Assuntos

RESUMO

An antifungal protein of about 30,000 Da was isolated from seeds of Sorghum bicolor L. using chromatographic techniques, including gel filtration, ion exchange, and high-performance liquid chromatography in a reverse-phase column. This protein (termed 30 kD protein) showed a minimal inhibitory concentration of 36 microg/ml for Candida parapsilosis and C. tropicalis, and 18 microg/ml for C. albicans. The 30 kD protein inhibited adherence to the cover glass and formation of a germinative tube of C. albicans at concentrations over 300 and 150 microg/ml, respectively. Transmission electron microscopy of yeast forms of C. albicans after incubation with 18 mug/ml of the 30 kD protein for 24 h revealed marked ultrastructural changes in the fungus. No toxicity of the 30 kD protein to the culture of Hep2 cells at concentrations equal to or less than 1,000 microg/ml was observed.

Assuntos

RESUMO

O presente estudo foi conduzido para avaliar a atividade antibacteriana dos extratos etanol:água e aquoso das folhas, raízes e casca do caule de Psidium guajava L. As atividades antibacterianas dos extratos contra as bactérias foram testados usando o ensaio de microdiluição em caldo. O extrato aquoso das folhas, raízes e casca do caule de P. guajava foram ativos contra as bactérias Gram-positivas Staphylococcus aureus (CIMs=500, 125 e 250 µg/ml, respectivamente) e Bacillus subtilis (CIMs=500 µg/ml), e foram inativas contras as bactérias Gram-negativas Escherichia coli e Pseudomonas aeruginosa (CIMs >1000 µg/ml). Os extratos etanol:água apresentaram maior atividade quando comparados com os extratos aquosos. Com base nestes resultados, o extrato de folhas de P. guajava foi fracionado em cromatografia em coluna de sílica gel em um bioensaio de fracionamento direcionado, produzindo uma mistura de flavonoides, uma mistura de a e b-amirina e b-sitosterol. A mistura de flavonoides mostrou boa atividade sobre S. aureus com CIM de 25 µg/ml. O b-sitosterol foi inativo para todas as bactérias testadas.

RESUMO

The in vitro activity of parthenolide against Leishmania amazonensis was investigated. Parthenolide is a sesquiterpene lactone purified from the hydroalcoholic extract of aerial parts of Tanacetum parthenium. This isolated compound was identified through spectral analyses by UV, infrared, (1)H and (13)C nuclear magnetic resonance imaging, DEPT (distortionless enhancement by polarization transfer), COSY (correlated spectroscopy), HMQC (heteronuclear multiple-quantum coherence), and electron spray ionization-mass spectrometry. Parthenolide showed significant activity against the promastigote form of L. amazonensis, with 50% inhibition of cell growth at a concentration of 0.37 microg/ml. For the intracellular amastigote form, parthenolide reduced by 50% the survival index of parasites in macrophages when it was used at 0.81 microg/ml. The purified compound showed no cytotoxic effects against J774G8 macrophages in culture and did not cause lysis in sheep blood when it was used at higher concentrations that inhibited promastigote forms. Sodium dodecyl sulfate-polyacrylamide gel electrophoresis with gelatin as the substrate showed that the enzymatic activity of the enzyme cysteine protease increased following treatment of the promastigotes with the isolated compound. This finding was correlated with marked morphological changes induced by parthenolide, such as the appearance of structures similar to large lysosomes and intense exocytic activity in the region of the flagellar pocket, as seen by electron microscopy. These results provide new perspectives on the development of novel drugs with leishmanicidal activities obtained from natural products.

Assuntos

RESUMO

The plants belonging to Pfaffia genus are used in folk medicine to treat gastric disturbances. This study examined the effects of an aqueous extract of Pfaffia glomerata (Spreng) Pedersen (AEP) on the gastrointestinal tract. Wistar rats were pretreated orally (p.o.) with the AEP (125, 250, 500 and 1000 mg.kg(-1)) before induction of ulcers by hypothermic restraint stress (HRS, 3 h restraint stress at 4 degrees C), ethanol (ET, 70%; 0.5 ml/animal; p.o.) or indomethacin (IND, 20 mg.kg(-1); s.c.). Control animals received water (C) or ranitidine (60 mg.kg(-1)) p.o. The AEP protected rats against HRS and ET-induced ulcers, but was not able to protect the gastric mucosa against IND-induced ulcers. When injected into the duodenal lumen, the AEP reduced total acidity and both basal and histamine-stimulated acid secretion in pylorus-ligated rats. In addition, gastric secretion from AEP-treated animals exhibited increased concentrations of nitrite and nitrate. Treatment of animals with L-NAME (120 mg.kg(-1), p.o.) prevented both the reduction of total acidity and the increase in NOx levels promoted by AEP treatment. In conclusion, AEP effectively protected the gastric mucosa and inhibited gastric acid secretion in rats, probably by involving the histaminergic pathway and an enhanced production of nitric oxide in the stomach.

Assuntos