RESUMO
AIMS: To evaluate the ability of Candida parapsilosis and Candida glabrata to develop phenotypic resistance to a benzophenone enriched fraction obtained from Brazilian red propolis (BZP-BRP) as compared to fluconazole (FLC). To investigate possible synergy between BZP-BRP and FLC and anidulafungin (AND). METHODS AND RESULTS: To analyse the development of resistance, isolates susceptible to these antifungals were cultured in increasing concentrations of FLC and BZP-BRP. The increase in FLC minimum inhibitory concentration for all isolates was evident and the majority developed resistance, whereas none isolated became less susceptible to BZP-BRP. Synergism was investigated by checkerboard method. BZP-BRP demonstrated synergy with FLC and indifference with AND for most isolates. CONCLUSIONS: In conclusion, the synergism observed with FLC suggests that BZP-BRP could be a possible therapeutic strategy for the treatment of infections related to FLC-resistant Candida sp. SIGNIFICANCE AND IMPACT OF THE STUDY: The indiscriminate use of antifungals results in the emergence of drug-resistant strains among previously susceptible populations. BZP-BRP can become an alternative for the treatment of persistent infections caused by Candida sp.
Assuntos
Antifúngicos/farmacologia , Candida/efeitos dos fármacos , Extratos Vegetais/farmacologia , Própole/química , Brasil , Candida/classificação , Candida/genética , Candida/metabolismo , Farmacorresistência Fúngica , Sinergismo Farmacológico , Fluconazol/farmacologia , Testes de Sensibilidade MicrobianaRESUMO
The coumarins 5-methoxy-6,7-methylenedioxycoumarin 1 5-(3-methyl-2-butenyloxy)-6,7-methylenedioxycoumarin 2 and 5-(2,3-dihydroxy-3-methylbutyloxy)-6,7-methylenedioxycoumarin 3 isolated from Pterocaulon species showed significant cytotoxicity against two glioma cells lines. Compound 1 presented IC(50) values of 34.6 µM and 31.6 µM against human (U138-MG) and rat (C6) glioma cells, respectively, and this compound was at least two times more potent than compounds 2 and 3. This result could be explained by the planar conformation adopted by 1 through a non-classical hydrogen bond between a hydrogen of the methoxy and the oxygen of the methylenedioxy groups. Another important finding was that the cytotoxic effect induced by 1 in glioma cells was not observed in organotypic cultures, indicating a selective cytotoxicity for tumor cells.
Assuntos
Antineoplásicos/isolamento & purificação , Apoptose/efeitos dos fármacos , Asteraceae/química , Benzodioxóis/isolamento & purificação , Cumarínicos/isolamento & purificação , Citotoxinas/isolamento & purificação , Animais , Antineoplásicos/farmacologia , Benzodioxóis/farmacologia , Linhagem Celular Tumoral , Sobrevivência Celular/efeitos dos fármacos , Neoplasias do Sistema Nervoso Central/tratamento farmacológico , Neoplasias do Sistema Nervoso Central/patologia , Cumarínicos/farmacologia , Citotoxinas/farmacologia , Glioma/tratamento farmacológico , Glioma/patologia , Hipocampo/citologia , Hipocampo/efeitos dos fármacos , Humanos , Ligação de Hidrogênio , Concentração Inibidora 50 , Masculino , Especificidade de Órgãos , Ratos , Ratos Wistar , Relação Estrutura-Atividade , Técnicas de Cultura de TecidosRESUMO
Plants of the genus Pterocaulon (Asteraceae) are popularly used in the treatment of skin diseases caused by fungi and bacteria. The aim of this work was to investigate the in vitro activity of the crude methanolic extracts obtained from the aerial parts of Pterocaulon polystachyum, P. balansae, P. lorentzii, P. lanatum, and P. cordobense against 24 Sporothrix schenckii clinical isolates and determine the minimum inhibitory concentration (MIC) and the minimum fungicidal concentration (MFC). MIC were performed by the broth microdilution method according guidelines recommended by Clinical and Laboratory Standards Institute for filamentous fungi and MFC were determined for transference of aliquots of the well that showed 100% of growth inhibition into tubes with culture medium. The extract from P. polystachyum was the most active sample, presenting MIC range of 156 and 312µg/mL. The popular use of these plants corroborates the importance of ethnopharmacological surveys and opens the possibility for finding new clinically effective antifungal agents.
RESUMO
Crude methanolic extracts and fractions from the aerial parts of seven species of Hypericum (H. caprifoliatum Cham. and Schltdl., H. carinatum Griseb., H. connatum Lam., H. ternum A. St.-Hil., H. myrianthum Cham. and Schltdl., H. piriai Arechav. and H. polyanthemum Klotzsch ex Reichardt) growing in southern Brazil were analyzed for their in vitro antifungal activity against a panel of standardized and clinical opportunistic pathogenic yeasts and filamentous fungi, including dermatophytes, by the agar dilution method. Chloroform and hexane extracts of H. ternum showed the greatest activity among extracts tested.
Assuntos
Antifúngicos/farmacologia , Candida/efeitos dos fármacos , Hypericum , Fitoterapia , Extratos Vegetais/farmacologia , Antifúngicos/administração & dosagem , Antifúngicos/uso terapêutico , Humanos , Testes de Sensibilidade Microbiana , Componentes Aéreos da Planta , Extratos Vegetais/administração & dosagem , Extratos Vegetais/uso terapêuticoRESUMO
The crude methanolic extracts of six species of Hypericum growing in southern Brazil (Hypericum caprifoliatum Cham. & Schlecht., H. carinatum Griseb., H. connatum Lam., H. myrianthum Cham. & Schlecht., H. polyanthemum Klotzsch ex Reichardt and H. ternum A. St. Hil.) were screened for their antiproliferative activity against two cell lines (HT-29 human colon carcinoma cells and H-460 non-small cell lung carcinoma). The most active crude extracts were those from H. caprifoliatum, H. myrianthum and, to a lesser extent, from H. connatum. All plants were submitted to fractionation with solvents in increasing polarity and re-assayed for the two cell lines used previously, as well as U-373 human malignant glioma cells. The most active fractions were the hexane fractions obtained from H. caprifoliatum, H. myrianthum and H. ternum.
Assuntos
Antineoplásicos Fitogênicos/farmacologia , Hypericum , Fitoterapia , Extratos Vegetais/farmacologia , Antineoplásicos Fitogênicos/administração & dosagem , Antineoplásicos Fitogênicos/uso terapêutico , Brasil , Linhagem Celular Tumoral/efeitos dos fármacos , Proliferação de Células/efeitos dos fármacos , Células HT29/efeitos dos fármacos , Humanos , Medicina Tradicional , Extratos Vegetais/administração & dosagem , Extratos Vegetais/uso terapêuticoRESUMO
This study reports the antimicrobial evaluation of the species most commonly used in Rio Grande do Sul (RS), the southernmost state of Brazil, for treating conditions likely to be associated with microorganisms. A four-stage process of documentation and evaluation was conducted: (a). review of RS ethnobotanical studies; (b). analysis of traditional uses; (c). literature survey on phytochemical and pharmacological data; (d). microbiological screening of selected plants. From the 149 species initially identified, 49 were cited as being used for microbial associated conditions in at least two other regions in RS, and 18 were further selected for screening. The crude methanol extract of these 18 plants were evaluated against seven microorganisms using the diffusion agar test. Extracts from Chaptalia nutans, Cordia monosperma, Echinodorus grandiflorus, Eugenia uniflora, Leonurus sibiricus, Luehea divaricata, Malva sylvestris, Ocotea odorifera, Parapiptadenia rigida, Pluchea sagittalis, Psidium cattleyanum and Senna neglecta were active against at least one microorganism. Although preliminary, these results are useful for rationalizing the use of medicinal plants in established systems of traditional medicine in primary health care.
Assuntos
Anti-Infecciosos/farmacologia , Extratos Vegetais/farmacologia , Plantas Medicinais , Brasil , Etnofarmacologia , Medicina Tradicional , População RuralRESUMO
The crude methanolic extracts of six species of Hypericum [H. caprifoliatum Cham. & Schlecht., H. carinatum Griseb., H. connatum Lam., H. ternum A. St. Hil., H. myrianthum Cham. & Schlecht. and H. polyanthemum Klotzsch ex Reichardt] growing in southern Brazil were analyzed for antimicrobial activity against several microorganisms (bacteria and fungi). The most active plant was H. caprifoliatum, which showed activity against Staphylococcus aureus. Only H. polyanthemum and H. ternum extracts were active against Bacillus subtilis. None of the crude methanolic extracts showed activity against S. epidermidis, Escherichia coli or Saccharomyces cerevisiae. Extracts from these species were evaluated chemically and tannin, flavonoid and phenolic acids were the prominent compounds. The plants contained quercitrin, hyperoside (except H. connatum) and, less frequently, isoquercitrin and chlorogenic acid. In contrast to H. perforatum, which has high concentrations of rutin, these species do not produce this flavonoid or it appears as traces. The tannin concentration varied between 5.1 and 16.7% in H. myrianthum and H. ternum, respectively.
Assuntos
Anti-Infecciosos/farmacologia , Bactérias/efeitos dos fármacos , Hypericum , Fungos Mitospóricos/efeitos dos fármacos , Fitoterapia , Extratos Vegetais/farmacologia , Anti-Infecciosos/administração & dosagem , Anti-Infecciosos/uso terapêutico , Antifúngicos/administração & dosagem , Antifúngicos/farmacologia , Antifúngicos/uso terapêutico , Relação Dose-Resposta a Droga , Humanos , Testes de Sensibilidade Microbiana , Componentes Aéreos da Planta , Extratos Vegetais/administração & dosagem , Extratos Vegetais/uso terapêutico , Taninos/administração & dosagem , Taninos/química , Taninos/farmacologia , Taninos/uso terapêuticoRESUMO
The total methanol crude extracts and petroleum ether, chloroform, and methanol fractions obtained from Hypericum species, H. caprifoliatum, H. carinatum, H. connatum, H. cordatum, H. myrianthum, H. piriai, H. polyanthemum and H. brasiliense, all native to South Brazil, were assayed for monoamine oxidase A (MAO A) and MAO B inhibitory activity in rat brain mitochondrial preparations at concentrations ranging from 1 to 20microg mL(-1). Three benzopyrans, HP1 (6-isobutyryl-5,7-dimethoxy-2,2-dimethylbenzopyran), HP2 (7-hydroxy-6-isobutyryl-5-methoxy-2,2-dimethylbenzopyran) and HP3 (5-hydroxy-6-isobutyryl-7-methoxy-2,2dimethylbenzopyran) isolated from H. polyanthemum were also tested at maximal concentrations of 150, 150 and 75/microM, respectively. The lipophilic extracts of H. polyanthemum, H. caprifoliatum and H. piriai displayed MAO A inhibitory activity greater than 50%. Among the benzopyrans, only HP3 showed significant activity, with an IC50 value of 22 microM. The total methanol crude extracts of aerial parts from H. carinatum, H. connatum, H. cordatum, H. polyanthemum and H. piriai were evaluated for antidepressant activity in the Porsolt's forced swimming test in Wistar rats (270 mg kg(-1) day(-1); i.p); however, none of them showed activity.
Assuntos
Inibidores Enzimáticos/farmacologia , Hypericum/química , Inibidores da Monoaminoxidase/farmacologia , Monoaminoxidase/metabolismo , Extratos Vegetais/farmacologia , Animais , Antidepressivos/farmacologia , Encéfalo , Brasil , Depressão/tratamento farmacológico , Modelos Animais de Doenças , Inibidores Enzimáticos/isolamento & purificação , Mitocôndrias/enzimologia , Inibidores da Monoaminoxidase/isolamento & purificação , Ratos , Ratos Wistar , NataçãoRESUMO
Three plant species, Hypericum connatum, Hypericum caprifoliatum, Hypericum polyanthemum (Guttiferae), growing in Southern of Brazil were chemically investigated and tested for their antiviral activity against feline immunodeficiency virus (FIV). The chemical analysis revealed the presence of polyphenolic compounds such as tannins and flavonoids. Hypericin was not detected in these species. The aqueous extract (AE), the aqueous extract with low tannin concentration (LTCAE) and the methanolic extract (ME) were tested for their cytotoxic properties in concentrations of 50-150 microg/ml. AE was toxic to CRFK for the three species in all concentrations. LTCAE and ME varied between different concentrations being not toxic or allowing 80% of cell growth. LTCAE and ME (10-50 microg/ml) were analyzed for antiviral activity by inhibition of CPE and measuring FIV genome from cell culture supernatant. LTCAE of all species in this work did not cause any inhibition of FIV. Although no difference was seen in CPE, a lower number of viral particles in the supernatant was observed when FIV infected cells were treated with ME of H. connatum. These results suggest that some plants of the genus Hypericum from Southern Brazil contain compounds with potential antiviral activity against lentiviruses.
Assuntos
Antivirais/farmacologia , Hypericum , Vírus da Imunodeficiência Felina/efeitos dos fármacos , Extratos Vegetais/farmacologia , Preparações de Plantas/farmacologia , Animais , Antivirais/isolamento & purificação , Brasil , Gatos , Células Cultivadas , Extratos Vegetais/isolamento & purificaçãoRESUMO
From the aerial parts of Hypericum polyanthemum Klotzsch ex Reichardt (Guttiferae), three chromenes, 6-isobutyryl-5,7-dimethoxy-2,2-dimethyl-benzopyran; 7-hydroxy-6-isobutyryl-5-methoxy-2,2-dimethyl-benzopyran and 5-hydroxy-6-isobutyryl-7-methoxy-2,2-dimethyl-benzopyran were isolated. Their structures were determined by NMR spectroscopic analyses.