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1.
J Appl Microbiol ; 124(1): 75-84, 2018 Jan.
Artigo em Inglês | MEDLINE | ID: mdl-29072357

RESUMO

AIMS: This study aims to improve characteristics of Piper regnellii extract to make it applicable in formulations to treat dermatophytosis, also known as ringworm. METHODS AND RESULTS: Microparticles (MPs) were produced by spray drying with gelatin, alginate and chitosan as encapsulating agents; characterized by scanning electron microscopy, encapsulation efficiency, thermal analyses and X-ray diffraction; and tested against Trichophyton rubrum by broth microdilution. Produced MPs had a mean diameter less than 2 µm, an increase in stability and release of the extract and good results for encapsulation efficiency, being 85·6% to gelatin MP, 71·3% to chitosan MP and 60·6% to alginate. MPs preserved the antifungal activity of P. regnellii extract T. rubrum. CONCLUSION: Microencapsulation provided a significant improvement in the stability of the P. regnellii extract and better solubilization of chemical compounds, maintaining the antifungal effect against T. rubrum. SIGNIFICANCE AND IMPACT OF THE STUDY: These results are useful for developing a formulation to treat fungal infections caused by dermatophyte species.


Assuntos
Piper/química , Extratos Vegetais/farmacologia , Trichophyton/efeitos dos fármacos , Antifúngicos/farmacologia , Biopolímeros/farmacologia , Cromatografia Líquida de Alta Pressão , Microscopia Eletrônica de Varredura , Difração de Raios X
2.
J Helminthol ; 88(3): 321-6, 2014 Sep.
Artigo em Inglês | MEDLINE | ID: mdl-23561585

RESUMO

Dichloromethane and aqueous fractions from leaves and stems of Piper arboreum Aubl., P. aduncum L., P. amalago L., P. crassinervium H.B. & K., P. diospyrifolium Kunth, P. hispidum Sw. and P. xylosteoides (Kunth) Steud. were tested against adult worms of Schistosoma mansoni. The in vitro activity was evaluated in terms of mortality, number of separated worms and number of worms with reduced motor activity. Most dichloromethane fractions from all Piper species showed moderate schistosomicidal activity, but aqueous fractions were not active. The dichloromethane fraction of P. amalago leaves (at 100 µg/ml) showed the highest activity, resulting in worm mortality, the separation of worm pairs and reduced motor activity. Chromatographic fractionation of the dichloromethane fraction of P. amalago leaves led to the isolation of its major compound, which was also tested against adults of S. mansoni. The isolated piperamide N-[7-(3',4'-methylenedioxyphenyl)-2(Z),4(Z)-heptadienoyl] pyrrolidine, at 100 µ m, resulted in the mortality of all adult worms after 24 h of incubation. The findings suggest that species of Piper are potential sources of schistosomicidal compounds.


Assuntos
Amidas/farmacologia , Anti-Helmínticos/farmacologia , Piper/química , Extratos Vegetais/farmacologia , Schistosoma mansoni/efeitos dos fármacos , Amidas/química , Amidas/isolamento & purificação , Animais , Anti-Helmínticos/química , Anti-Helmínticos/isolamento & purificação , Locomoção/efeitos dos fármacos , Extratos Vegetais/química , Extratos Vegetais/isolamento & purificação , Folhas de Planta/química , Caules de Planta/química , Schistosoma mansoni/fisiologia , Análise de Sobrevida
3.
J Ethnopharmacol ; 116(3): 569-73, 2008 Mar 28.
Artigo em Inglês | MEDLINE | ID: mdl-18289815

RESUMO

Leaves of Piper ovatum are known in folk medicine as "joão burandi" or "anestésica" and in traditional Brazilian medicine are used to treat inflammatory disease. The hydroalcoholic extract, fractions, and a mixture of piperovatine (1) and piperlonguminine (2) in a proportion of 2:3 obtained from Piper ovatum were assayed for anti-inflammatory activity by means of carrageenan-induced pleurisy in rats and croton oil-induced ear edema in mice. The hydroalcoholic extract was analyzed by high-performance liquid chromatography. Fraction constituents were evaluated by phytochemical screening, and the mixture of amides (1 and 2) was identified by analyses of spectral data of (1)H and (13)C nuclear magnetic resonance. Acute toxicity of the extract also was evaluated. At 500mg/kg, the hydroalcoholic extract of Piper ovatum leaves did not reduce the volume of inflammatory pleural exudates compared with control animals. However, the hydroalcoholic extract and fractions F1-F3 at doses of 5.0mg/ear and a mixture of piperovatine (1) and piperlonguminine (2) at doses of 2.5, 1.25, and 0.625mg/ear significantly reduced the degree of ear edema. Taken together, the results indicate that the amide fractions piperovatine and piperlonguminine showed the greatest inhibitory activity of topical inflammation induced by croton oil.


Assuntos
Amidas/farmacologia , Anti-Inflamatórios/uso terapêutico , Edema/tratamento farmacológico , Fitoterapia , Piper/química , Extratos Vegetais/uso terapêutico , Amidas/uso terapêutico , Animais , Masculino , Camundongos , Extratos Vegetais/química , Extratos Vegetais/toxicidade , Folhas de Planta/química , Pleurisia/tratamento farmacológico , Ratos , Testes de Toxicidade Aguda
4.
Artigo em Inglês | MEDLINE | ID: mdl-28539966

RESUMO

Supercritical fluid extraction was used to extract the alkaloid N-[7-(3',4'-methylenedioxyphenyl)-2(Z),4(Z)-heptadienoyl]pyrrolidine from leaves of Piper amalago L. A three-level orthogonal array design matrix, OAD OA9(34), was used for optimization of the parameters of supercritical extraction of the alkaloid, employing supercritical carbon dioxide: extraction time (20, 40, and 60 min), temperature (40, 50, and 60°C), pressure (150, 200, and 250 bar), and the use of cosolvents (ethanol, methanol, and propyleneglycol). All parameters had significant effect on the alkaloid yield. The alkaloid yield after 60 min of extraction without cosolvents at 9 different conditions (32) in terms of temperature (40, 50, and 60°C) and pressure (150, 200, and 250 bar) was also evaluated. The optimal yield (≈3.8 mg g-1) was obtained with supercritical CO2 + methanol (5% v : v) at 40°C and 200 bar for 60 min of extraction.

5.
J Mycol Med ; 26(3): 217-26, 2016 Sep.
Artigo em Inglês | MEDLINE | ID: mdl-27499460

RESUMO

Three chalcones, 2'-hydroxy-4,4',6'-trimethoxychalcone, 2'-hydroxy-4,4',6'-tetramethoxychalcone, and 3,2'-dihydroxy-4,4',6'-trimethoxychalcone, were isolated from the leaves of Piper hispidum in a bioguided fractionation of crude extract. The antimicrobial activity of crude extract of P. hispidum leaves was determined against bacteria Escherichia coli, Pseudomonas aeruginosa, Bacillus subtilis, Staphylococcus aureus and yeasts Candida albicans, C. parapsilosis and C. tropicalis. Fractions and chalcones were tested against C. albicans and S. aureus. The checkerboard assay was performed to assess synergic interactions between extract and antifungal drugs, and the 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyl tetrazolium bromide (MTT) reduction assay was used to evaluate anti-biofilm effects of extract. The extract was active against yeasts, S. aureus and B. subtilis with MIC values between 15.6 and 62.5µg/mL. Synergistic effects of extract associated with fluconazole and nystatin were observed against C. albicans, with fractional inhibitory concentration indices of 0.37 and 0.24, respectively. The extract was also effective against C. albicans and S. aureus biofilm cells at concentrations of 62.5 and 200µg/mL, respectively. Thus, P. hispidum may be a possible source of bioactive substances with antimicrobial properties.


Assuntos
Anti-Infecciosos/farmacologia , Candida albicans/efeitos dos fármacos , Chalconas/farmacologia , Piper/química , Extratos Vegetais/farmacologia , Staphylococcus aureus/efeitos dos fármacos , Antibacterianos/isolamento & purificação , Antibacterianos/farmacologia , Anti-Infecciosos/isolamento & purificação , Antifúngicos/isolamento & purificação , Antifúngicos/farmacologia , Candida albicans/crescimento & desenvolvimento , Chalconas/isolamento & purificação , Fracionamento Químico , Testes de Sensibilidade Microbiana , Extratos Vegetais/isolamento & purificação , Staphylococcus aureus/crescimento & desenvolvimento
6.
Nat Prod Res ; 29(10): 953-7, 2015.
Artigo em Inglês | MEDLINE | ID: mdl-25310798

RESUMO

This study evaluated the wound healing effects of topical application of an emulsion containing the HPLC-standardised extract from Calophyllum brasiliense Cambess (Clusiaceae) leaves in rats. The macroscopic analysis demonstrated that the wounds treated with the C. brasiliense emulsion healed earlier than the wounds treated with emulsion base and Dersani®. The percentage of wound healing in the group treated with the C. brasiliense emulsion was significantly higher than in the other groups at 7 and 14 days. On day 14, the animals treated with the C. brasiliense emulsion exhibited a 90.67% reduction of the wound areas. The histological evaluation revealed that on day 21, the group treated with the C. brasiliense emulsion exhibited a significant increase in fibroblasts compared with the other groups. Thus, the C. brasiliense emulsion had healing properties in the topical treatment of wounds and accelerated the healing process.


Assuntos
Calophyllum/química , Extratos Vegetais/farmacologia , Pele/efeitos dos fármacos , Cicatrização/efeitos dos fármacos , Administração Cutânea , Animais , Cromatografia Líquida de Alta Pressão , Emulsões , Fibroblastos/efeitos dos fármacos , Masculino , Extratos Vegetais/administração & dosagem , Folhas de Planta/química , Ratos , Ratos Wistar
8.
Int J Tuberc Lung Dis ; 18(12): 1513-5, 2014 Dec.
Artigo em Inglês | MEDLINE | ID: mdl-25517821

RESUMO

SETTING: Department of Clinical Analysis and Biomedicine, State University of Maringa, Maringa, Parana, Brazil. OBJECTIVE: To evaluate the in vitro interaction between eupomatenoid-5 (EUP-5), extracted from Piper solmsianum C. DC. var. solmsianum, and first-line anti-tuberculosis drugs against Mycobacterium tuberculosis H37Rv and 20 clinical isolates. DESIGN: Resazurin drugs combination microtiter assay (REDCA) was performed to determine the interaction between EUP-5 and isoniazid, rifampicin (RMP) and ethambutol (EMB). RESULTS: Synergism was observed in M. tuberculosis H37Rv and eight clinical isolates with EUP-5+RMP, and in M. tuberculosis H37Rv and 17 clinical isolates with EUP-5+EMB combinations. CONCLUSION: EUP-5 is a promising compound for further studies on the development of anti-tuberculosis drugs.


Assuntos
Antituberculosos/farmacologia , Benzofuranos/farmacologia , Mycobacterium tuberculosis/efeitos dos fármacos , Fenóis/farmacologia , Piper , Extratos Vegetais/farmacologia , Antituberculosos/isolamento & purificação , Benzofuranos/isolamento & purificação , Farmacorresistência Bacteriana Múltipla , Sinergismo Farmacológico , Etambutol/farmacologia , Genótipo , Isoniazida/farmacologia , Testes de Sensibilidade Microbiana , Mycobacterium tuberculosis/genética , Fenóis/isolamento & purificação , Fitoterapia , Piper/química , Extratos Vegetais/isolamento & purificação , Folhas de Planta , Plantas Medicinais , Rifampina/farmacologia
9.
Phytomedicine ; 20(7): 600-4, 2013 May 15.
Artigo em Inglês | MEDLINE | ID: mdl-23474218

RESUMO

The present study determined the anti-Mycobacterium tuberculosis activities of supercritical CO2 extracts, neolignans eupomatenoid-5 (1), conocarpan (4) and eupomatenoid-3 (7) and their derivatives (2, 3, 5, 6, and 8) from Piper regnellii, as well as their cytotoxicities. The supercritical CO2 extract from leaves was purified by chromatographic methods, yielding compounds (1), (4) and (7), which were identified by (1)H NMR and comparison with literature data. Anti-M. tuberculosis activity (H37Rv and clinical isolates) was evaluated using a resazurin microtiter assay plate (REMA) to determine the MIC. The cytotoxicity assay was carried out in macrophages J774G.8 by sulforhodamine B colorimetric assay. The supercritical CO2 extracts from leaves and stems, and compound (4) showed activity against M. tuberculosis (MIC 15.6 µg/ml). Compound (1) showed the best activity (MIC 1.9 µg/ml), with good SI. Compounds (7) and (8) showed low activity against M. tuberculosis H37Rv. The derivative compounds did not show increased anti-M. tuberculosis activity. This is the first report, to our knowledge, to describe neolignans from P. regnellii with activity against M. tuberculosis, and compound (1) is a potential candidate for future antituberculosis drugs.


Assuntos
Antituberculosos/farmacologia , Mycobacterium tuberculosis/efeitos dos fármacos , Piper/química , Extratos Vegetais/química , Animais , Antituberculosos/química , Benzofuranos/química , Benzofuranos/farmacologia , Linhagem Celular/efeitos dos fármacos , Lignanas/química , Lignanas/farmacologia , Macrófagos/efeitos dos fármacos , Espectroscopia de Ressonância Magnética , Camundongos , Testes de Sensibilidade Microbiana , Estrutura Molecular , Fenóis/química , Fenóis/farmacologia , Extratos Vegetais/análise , Testes de Toxicidade/métodos
10.
Phytomedicine ; 19(3-4): 374-7, 2012 Feb 15.
Artigo em Inglês | MEDLINE | ID: mdl-21975171

RESUMO

Kielmeyera coriacea Mart. (Calophyllaceae) is known popularly as "Pau Santo". The hydroethanolic extract (HE) of Kielmeyera coriacea stems and its semi-pure dichloromethane (DCM) constituent produced an antidepressant-like effect in rats. The purpose of this study was to investigate the effects of repeated administration (21 days) by gavage of the DCM fraction (5, 10 or 15mg/kg) in rats submitted to the elevated T-maze (ETM), a model of generalized anxiety and panic disorders. The tricyclic antidepressant imipramine (15mg/kg) was used as a positive control. Rat locomotion was assessed using the open field test (OFT) following each drug treatment. The 2-hydroxy-1-methoxyxanthone (1), aucuparin (2), swertinin (3), 1,3,7-trihydroxy-2-(3-methylbut-2-enyl)-xanthone (4) and 1,3,5-trihydroxy-2-(3-methylbut-2-enyl)-xanthone (5) were identified in DCM fraction, and suggest that the xanthone (4) is related with the antidepressant-like profile of this plant. Pharmacological evaluation showed that DCM fraction (10 and 15 mg/kg) decreased the inhibitory avoidance latency from the closed arm and increased the one-way escape latency from the open arm in the ETM, which is indicative of anxiolytic and panicolytic effects, respectively, as occurs with the positive control, imipramine (15 mg/kg), when compared to their control group (vehicle). Locomotor activity was not significantly altered by the different treatments. This study suggests that the DCM fraction from stems of Kielmeyera coriacea can be an important therapeutic alternative in the treatment of anxiety disorders, such as generalized anxiety and panic disorders.


Assuntos
Ansiolíticos/farmacologia , Clusiaceae/química , Cloreto de Metileno/administração & dosagem , Cloreto de Metileno/farmacologia , Caules de Planta/química , Xantonas/farmacologia , Animais , Antidepressivos Tricíclicos/administração & dosagem , Antidepressivos Tricíclicos/farmacologia , Ansiedade/tratamento farmacológico , Comportamento Animal , Comportamento Exploratório , Imipramina/farmacologia , Masculino , Aprendizagem em Labirinto/efeitos dos fármacos , Cloreto de Metileno/química , Atividade Motora , Transtorno de Pânico/tratamento farmacológico , Extratos Vegetais/química , Extratos Vegetais/farmacologia , Ratos , Ratos Wistar , Xantonas/química
11.
Phytomedicine ; 19(3-4): 223-30, 2012 Feb 15.
Artigo em Inglês | MEDLINE | ID: mdl-22285848

RESUMO

We have previously demonstrated antileishmanial activity on Leishmania amazonensis of the natural (1-2), synthetic (7) and derivatives of coumarin (-) mammea A/BB (3-6) isolated from the dichloromethane extract of Calophyllum brasiliense leaves. The aim of the present study was to evaluate morphological and ultrastructural alterations in Leishmania amazonensis induced by these compounds. In promastigote forms, all seven compounds produced significant morphological and ultrastructural alterations, as revealed by scanning and transmission electron microscopy. The compound 5,7-dihydroxy-8-(2-methylbutanoyl)-6-(3-methylbutyl)-4-phenyl-chroman-2-one (3), the most active antileishmanial with LD50 of 0.9 µM), induced cell shrinkage and a rounded appearance of the cells. Parasites incubated in the presence of compound (3) showed ultrastructural changes, such as the appearance of mitochondrial swelling with a reduction in the density of the mitochondrial matrix and the presence of vesicles inside the mitochondrion, indicating damage and significant change in this organelle; abnormal chromatin condensation, alterations in the nuclear envelope, intense atypical cytoplasmic vacuolization, and the appearance of autophagic vacuoles were also observed. In addition, the compound (3) may be acting to depolarize the mitochondrial membrane potential of the cells, leading to death of the parasite.


Assuntos
Antiprotozoários/farmacologia , Calophyllum/química , Cumarínicos/química , Leishmania mexicana/efeitos dos fármacos , Membranas Mitocondriais/efeitos dos fármacos , Folhas de Planta/química , Antiprotozoários/química , Antiprotozoários/isolamento & purificação , Cromanos/isolamento & purificação , Cromanos/farmacologia , Cromatina/efeitos dos fármacos , Citometria de Fluxo , Concentração Inibidora 50 , Leishmania mexicana/ultraestrutura , Potencial da Membrana Mitocondrial , Microscopia Eletrônica , Mitocôndrias/efeitos dos fármacos , Mitocôndrias/ultraestrutura , Membrana Nuclear/efeitos dos fármacos , Testes de Sensibilidade Parasitária , Extratos Vegetais/química , Extratos Vegetais/farmacologia
12.
Rev. bras. plantas med ; Rev. bras. plantas med;17(2): 324-330, Apr-Jun/2015. graf
Artigo em Português | LILACS | ID: lil-746138

RESUMO

RESUMO: O presente estudo descreve as características morfo-anatômicas dos órgãos vegetativos e do pó da Piper ovatum Vahl de modo que os dados obtidos possam ser utilizados como referência em análises de controle de qualidade de amostras de fármacos, a fim de verificar sua autenticidade. As raízes, caules, pecíolos e folhas foram fixadas, seccionadas à mão livre e coradas, as secções transversais e paradérmicas foram analisadas por microscopia óptica e a superfície do limbo foi observada, também, por microscopia eletrônica de varredura (MEV). Os órgãos vegetativos da P. ovatum apresentam morfologia e anatomia similar às outras espécies de Piper. No entanto, não foram observadas inclusões celulares nas folhas de P. ovatum. Análises por MEV mostraram a presença de tricomas glandulares constituídos de pedúnculo unicelular e porção secretora globóide igualmente unicelular recoberto por cutícula, na epiderme abaxial das folhas. Também foi observada a presença de uma cutícula espessa e que origina crostas no limite entre uma célula e outra, em ambas as superfícies foliares. No mesófilo foi observada a presença de idioblastos oleíferos característica marcante de outras espécies de Piperaceae. Além disso, na microscopia do pó foram observados hipoderme e idioblastos oleíferos em fragmentos do limbo, fragmentos de fibras esclerenquimáticas do caule, além de células esclerosas isoladas ou em grupos no pecíolo. O perfil cromatográfico do extrato hidroetanólico das folhas de P. ovatum foi obtido por cromatografia líquida de alta eficiência (CLAE). Nas análises por CLAE foram identificados como substâncias majoritárias do extrato as amidas piperovatina e piperlonguminina nos tempos de retenção de 10,25 e 10,81 min., respectivamente.


ABSTRACT: The present study describes the morphological and anatomical characteristics of vegetative organs and powder of the Piper ovatum Vahl, in order to use the obtained data as reference in the quality control tests of pharmaceutical samples, investigating their authenticity. The roots, stems, petioles and leaves were fixed, freehand sectioned and stained according to usual microtechniques. The transverse and paradermal sections were analyzed by optical microscopy and the leaf surface was also observed by scanning electron microscopy (SEM). The vegetative organs of the P. ovatum show morphology and anatomy similar to other species of Piper. However, cellular inclusions were not observed in the P. ovatum leaves. The SEM analysis showed the presence of glandular trichomes consisting of a unicellular stalk and globular secretory portion covered by cuticle on the abaxial surface of the leaves. The SEM also had shown one thick cuticle forming crusts in the limit of the epidermal cells, on both leaf surfaces. In the mesophyll, we observed oil idioblasts, which are typical features of other species of Piperaceae. Moreover, in the powder of the P. ovatum we observed hypodermis and oil idioblasts in leaf fragments, fragments of sclerenchyma fibers from the stem and isolated sclereids or in petiole groups. The chromatographic profile of the hydroethanolic extract of the P. ovatum leaves was obtained by high performance liquid chromatography (HPLC). In this analysis, we identified the amides piperovatine and piperlonguminine in the retention times of 10.25 and 10.81 min., respectively, as majority compounds present in the extract.


Assuntos
Piperaceae/anatomia & histologia , Controle de Qualidade , Microscopia Eletrônica de Varredura/instrumentação , Cromatografia Líquida/métodos
13.
Phytomedicine ; 17(5): 333-8, 2010 Apr.
Artigo em Inglês | MEDLINE | ID: mdl-19800777

RESUMO

Leishmanicide potential of Calophyllum brasiliense leaves on promastigote and amastigote of Leishmania (Leishmania) amazonensis is evaluated. The LD(50) of dichloromethane extract and hexane fraction for promastigotes was respectively 40 microg/ml and 20 microg/ml. In mouse peritoneal macrophages infected with Leishmania amastigotes the Infection Index decreased respectively 100% and 84.2% in 80 microg/ml and 40 microg/ml concentrations of dichloromethane extract. Hexane fraction decreased infection index respectively by 98.7% and 91.3% within the same concentrations. It was found that pretreatment with dichloromethane extract or with hexane fraction of experimentally infected BALB/c mice decrease the volume of the lesions by L. (L.) amazonensis. Moreover, animals treated topically also revealed healing lesions. Besides, the parasite load in the animals' popliteal lymph nodes was significantly reduced in treated animals, showing that plant components actually control infection. Results show that crude extract and hexane fraction of C. brasiliense reveal a significant in vitro and in vivo leishmanicide activity.


Assuntos
Antiparasitários/uso terapêutico , Calophyllum/química , Leishmania/efeitos dos fármacos , Leishmaniose/tratamento farmacológico , Macrófagos Peritoneais/efeitos dos fármacos , Fitoterapia , Extratos Vegetais/uso terapêutico , Animais , Antiparasitários/farmacologia , Feminino , Leishmaniose/patologia , Linfonodos/parasitologia , Macrófagos Peritoneais/parasitologia , Masculino , Camundongos , Camundongos Endogâmicos BALB C , Camundongos Endogâmicos C57BL , Extratos Vegetais/química , Extratos Vegetais/farmacologia , Folhas de Planta
14.
Braz J Med Biol Res ; 42(6): 545-50, 2009 Jun.
Artigo em Inglês | MEDLINE | ID: mdl-19448904

RESUMO

Since the anti-inflammatory, antidiabetic and hypolipidemic effects of soy isoflavones may be mediated by activation of peroxisome proliferator-activated receptors (PPAR), the present study investigated whether the methanolic fractions obtained from soybean seeds (E1) and soybean seed coats with hypocotyls (E2) could influence PPARalpha, PPARgamma and PPARbeta/delta transcriptional activity. The isoflavones from E1 and E2 were quantified by HPLC analysis. E1 and E2 were rich in isoflavones (daidzin, glycitin, genistin, malonyldaidzin, malonylglycitin, malonylgenistin, daidzein, glycitein, and genistein). Moreover, E1 and E2 showed no evidence of genetically modified material containing the gene CP4 EPSPS. To investigate PPAR transcriptional activity, human promonocytic U-937 cells were treated with E1 and E2 (200, 400, 800, and 1600 microg/mL), positive controls or vehicle. Data are reported as fold-activation of the luciferase reporter driven by the PPAR-responsive element. Dose-response analysis revealed that E1 and E2 induced the transcriptional activity of PPARalpha (P < 0.001), with activation comparable to that obtained with 0.1 mM bezafibrate (positive control) at 1600 microg/mL (4-fold) and 800 microg/mL (9-fold), respectively. In addition, dose-response analysis revealed that E1 and E2 activated PPARbeta/delta (P < 0.05), and the activation at 800 microg/mL (4- and 9-fold, respectively) was comparable to that of 0.1 mM bezafibrate (positive control). However, no effect on PPARgamma was observed. Activation of PPARalpha is consistent with the lipid-lowering activity of soy isoflavones in vivo, but further studies are needed to determine the physiological significance of PPARbeta/delta activation.


Assuntos
Glycine max/química , Isoflavonas/farmacologia , Receptores Ativados por Proliferador de Peroxissomo/efeitos dos fármacos , Sementes/química , Ativação Transcricional/efeitos dos fármacos , Cromatografia Líquida de Alta Pressão , Humanos , Isoflavonas/isolamento & purificação , Sementes/genética , Glycine max/genética
15.
Phytomedicine ; 15(3): 202-8, 2008 Mar.
Artigo em Inglês | MEDLINE | ID: mdl-17890069

RESUMO

In this paper, we describe the purification of an antiviral peptide from seeds of Sorghum bicolor L. by a procedure that included gel filtration, ion exchange, and high-performance liquid chromatography (HPLC) in a reversed-phase column. Its molecular weight, determined by chromatographic mobility on the Shim-pack DIOL-150 gel permeation column in HPLC, was found to be 2000Da. The peptide designated 2kD peptide strongly inhibited the replication of herpes simplex virus type 1 (HSV-1), dose-dependently, at 40-90% of the control level, after incubation with 10-50 microM of the peptide, with EC(50) and EC(90) values of 6.25 and 15.25 microM, respectively. The IC(50) value of the 2kD peptide against Vero cells was 250 microM. Pre-incubation of HSV-1 with various concentrations of the 2kD peptide showed dose-dependent cytopathic effects (CPE) reduction patterns at concentrations from 6.25 to 50 microM. The presence of the 2kD peptide before HSV-1 infections showed moderate inhibition of virus-induced CPE as compared to during or after infections, with EC(50) values of 12.5, 6.25, and 6.25 microM, respectively. Similar results were observed when the 2kD peptide was assayed against bovine herpes virus (BHV), an enveloped virus like HSV-1. On the other hand, the 2kD peptide showed weak activity against poliovirus type 1, a non-enveloped virus. Taken together, these results indicate that the 2kD peptide was able not only to inhibit the initiation and the spread of infection, but also had an in vitro prophylactic effect against HSV-1 infection.


Assuntos
Peptídeos Catiônicos Antimicrobianos/farmacologia , Antivirais/farmacologia , Extratos Vegetais/farmacologia , Sorghum/química , Vírus/efeitos dos fármacos , Animais , Peptídeos Catiônicos Antimicrobianos/química , Peptídeos Catiônicos Antimicrobianos/isolamento & purificação , Antivirais/química , Bactérias/efeitos dos fármacos , Chlorocebus aethiops , Relação Dose-Resposta a Droga , Herpesvirus Bovino 1/efeitos dos fármacos , Herpesvirus Humano 1/efeitos dos fármacos , Concentração Inibidora 50 , Testes de Sensibilidade Microbiana , Peso Molecular , Extratos Vegetais/química , Poliovirus/efeitos dos fármacos , Sementes/química , Células Vero
17.
Rev. bras. pesqui. méd. biol ; Braz. j. med. biol. res;42(6): 545-550, June 2009. graf, tab
Artigo em Inglês | LILACS | ID: lil-512768

RESUMO

Since the anti-inflammatory, antidiabetic and hypolipidemic effects of soy isoflavones may be mediated by activation of peroxisome proliferator-activated receptors (PPAR), the present study investigated whether the methanolic fractions obtained from soybean seeds (E1) and soybean seed coats with hypocotyls (E2) could influence PPARα, PPARγ and PPARβ/δ transcriptional activity. The isoflavones from E1 and E2 were quantified by HPLC analysis. E1 and E2 were rich in isoflavones (daidzin, glycitin, genistin, malonyldaidzin, malonylglycitin, malonylgenistin, daidzein, glycitein, and genistein). Moreover, E1 and E2 showed no evidence of genetically modified material containing the gene CP4 EPSPS. To investigate PPAR transcriptional activity, human promonocytic U-937 cells were treated with E1 and E2 (200, 400, 800, and 1600 µg/mL), positive controls or vehicle. Data are reported as fold-activation of the luciferase reporter driven by the PPAR-responsive element. Dose-response analysis revealed that E1 and E2 induced the transcriptional activity of PPARα (P < 0.001), with activation comparable to that obtained with 0.1 mM bezafibrate (positive control) at 1600 µg/mL (4-fold) and 800 µg/mL (9-fold), respectively. In addition, dose-response analysis revealed that E1 and E2 activated PPARβ/δ (P < 0.05), and the activation at 800 µg/mL (4- and 9-fold, respectively) was comparable to that of 0.1 mM bezafibrate (positive control). However, no effect on PPARγ was observed. Activation of PPARα is consistent with the lipid-lowering activity of soy isoflavones in vivo, but further studies are needed to determine the physiological significance of PPARβ/δ activation.


Assuntos
Humanos , Isoflavonas/farmacologia , Receptores Ativados por Proliferador de Peroxissomo/efeitos dos fármacos , Sementes/química , Glycine max/química , Ativação Transcricional/efeitos dos fármacos , Cromatografia Líquida de Alta Pressão , Isoflavonas/isolamento & purificação , Sementes/genética , Glycine max/genética
18.
Rev. bras. farmacogn ; 15(3): 199-204, jul.-set. 2005. ilus, tab
Artigo em Português | LILACS | ID: lil-570912

RESUMO

O óleo essencial das folhas de Piper regnellii (Miq.) C. DC. var. pallescens (C. DC.) Yunck Piparaceae, coletadas no Horto de Plantas Medicinais da Universidade Estadual de Maringá, foi obtido por hidrodestilação. Uma análise preliminar por CG/EM e RMN 13C foi realizada. O b-mirceno (70 por cento) foi identificado como componente majoritário através da comparação dos espectros de massa e RMN 13C com dados da literatura. Quatro neolignanas foram isoladas do extrato hidroetanólico das folhas e identificadas: eupomatenóide-6, eupomatenóide-5, eupomatenóide-3 e conocarpano. As estruturas dessas substâncias foram estabelecidas por meio de estudos de RMN ¹H e 13C, ¹H x ¹H - COSY, HETCOR, HMBC, gNOE e EM.


The essential oil of Piper regnellii (Miq.) C. DC. var. pallescens (C. DC.) Yunck Piparaceae leaves, which were collected at a tree farm named Horto de Plantas Medicinais of the Universidade Estadual de Maringá, was obtained by hydrodistillation. A preliminary analysis by GC/MS was carried out. b-mirceno (70 percent) was identified as the main constituent by comparing MS and 13C NMR with the literature data. Four neolignans were isolated from the leaves and identified: eupomatenoid-6, eupomatenoid-5, eupomatenoid-3 and conocarpan. Their structures were established by extensive ¹H and 13C NMR, ¹H x ¹H - COSY, HETCOR, HMBC, gNOE and MS spectral studies.

19.
Rev. bras. farmacogn ; 13(supl.1): 21-24, 2003. ilus, tab
Artigo em Português | LILACS | ID: lil-526235

RESUMO

Foram selecionados extratos de 13 plantas utilizadas na medicina popular brasileira para avaliar a atividade antimicrobiana. Destes, 10 extratos apresentaram níveis variados de atividade antibacteriana. Cinco dos extratos testados, apresentaram compostos com valores de Rf similares a de compostos antibacterianos visíveis na bioautografia. Três destas plantas pertencem à família Compositae indicando que o mesmo composto pode ser responsável pela atividade antibacteriana destas plantas. Atividade anticandida foi observada em 9 extratos de plantas. Os resultados podem explicar o uso etnobotânico das espécies estudadas para o tratamento de várias doenças infecciosas.


Extracts of 13 Brazilian medicinal plants were screened for their antimicrobial activity against bacteria and yeast. Of these, 10 plant extracts showed varied levels of antibacterial activity. Five of the plant extracts presented compounds with Rf values similar to the antibacterial compounds visible on bioautogram. Of these, three plants belong to the Compositae family. This may mean that the same compounds are responsible for the antibacterial activity in these plants. Anticandidal activity was detected in 9 plant extracts. The results might explain the ethnobotanical use of the studied species for the treatment of various infectious diseases.

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