RESUMEN
The objective of this study was to determine the chemical profile and to evaluate the antibacterial activity of the essential oils of Piper species and modulation of the antibiotic activity, using the microdilution method to determine the minimum inhibitory concentration. The chemical components were characterized by gas chromatography coupled to mass spectrometry, which revealed ß-copaen-4-α-ol (31.38%), spathulenol (25.92%), and germacrene B (21.53%) as major constituents of the essential oils of Piper arboreum, Piper aduncum, and Piper gaudichaudianum, respectively. The essential oils analyzed in this study did not present a clinically relevant activity against standard and multiresistant Escherichia coli. However, in the case of multiresistant Staphylococcus aureus, there was a significant activity, corroborating with reports in the literature, where Gram-positive bacteria are more susceptible to antimicrobial activity. The essential oils modulated the effect of the antibiotics norfloxacin and gentamicin, having on the latter greater modulating effect; however, for erythromycin, no statistically significant effect was observed. In conclusion, the results obtained in this study demonstrated that the essential oils of the analyzed Piper species present an inhibitory effect against S. aureus and modulate antibiotic activity, most of which presents synergistic activity.
Asunto(s)
Antibacterianos/química , Aceites Volátiles/química , Piper/química , Aceites de Plantas/química , Antibacterianos/farmacología , Escherichia coli/efectos de los fármacos , Aceites Volátiles/farmacología , Aceites de Plantas/farmacología , Sesquiterpenos/análisis , Sesquiterpenos de Germacrano/análisis , Staphylococcus aureus/efectos de los fármacosRESUMEN
The present study aimed to evaluate the antibacterial and modulatory activity of the Turnera subulate methyl extract in isolation or in combination with aminoglycoside antibiotics, using the microdilution method. The Turnera subulata methyl extract was used in isolation in the antibacterial assays and in combination with antibiotics in the modulation assays. All tests were performed in triplicates. The Turnera subulata methyl extract presented both antibacterial and antibiotic-modulatory effects in vitro, in isolation and in association with aminoglycosides. The extract activity depends on the bacterial strain and may be associated with the presence of tannins and flavonols. However, further studies are required to characterize the Turnera subulata potential for the development of new drugs against multiresistant bacteria.
Asunto(s)
Extractos Vegetales/farmacología , Turnera/química , Aminoglicósidos/farmacología , Antibacterianos/farmacología , Bacterias/efectos de los fármacos , Pruebas de Sensibilidad Microbiana , Extractos Vegetales/químicaRESUMEN
The indiscriminate use of antibiotics has made bacterial resistance an important public health problem, since many antibiotics have become ineffective. Phototherapy can be considered an alternative to reduce the abusive use of antimicrobials, thus impacting microbial resistance. The objective of this study was to determine the chemical profile and to evaluate the effect of blue LED lights on the antibacterial activity of essential oils from Piper species, as well as their aminoglycoside antibiotic activity modulation using the microdilution method to determine the Minimum Inhibitory Concentration (MIC). The antibiotic activity modulating effect of these oils was also determined using the broth microdilution method with 96-well plates which were exposed to LED light for 20â¯min. Chemical components were characterized by gas chromatography coupled to mass spectrometry, revealing ß-copaen-4-α-ol, germacrene A and germacrene B as major essential oil constituents for Piper arboreum (OEPar), Piper aduncum (OEPad) and Piper gaudichaudianum (OEPg), respectively. OEPar obtained a MIC of 512⯵g/mL against Staphylococcus aureus and a MICâ¯≥â¯1024⯵g/mL against Escherichia coli. OEPad and OEPg showed MIC valuesâ¯≥â¯1024⯵g/mL against the utilized strains. The essential oils modulated the effect of the antibiotics amikacin and gentamicin, with this effect being potentiated when exposed to blue LED. The blue LED light in the absence of the essential oil also showed an ability to modulate aminoglycoside antibiotic activity in this study, presenting mostly synergistic effects. In conclusion, the results obtained in this study demonstrate that photodynamic therapy using blue LED light interferes with the antibacterial action of P. arboreum, P. aduncum and P. gaudichaudianum essential oils and aminoglycoside antibiotic activity.
Asunto(s)
Antibacterianos/química , Aceites Volátiles/química , Fotoquimioterapia/métodos , Piper/química , Extractos Vegetales/química , Aceites de Plantas/química , Amicacina/farmacología , Antibacterianos/farmacología , Bacterias/efectos de los fármacos , Evaluación Preclínica de Medicamentos , Sinergismo Farmacológico , Gentamicinas/farmacología , Luz , Pruebas de Sensibilidad Microbiana , Aceites Volátiles/farmacología , Extractos Vegetales/farmacología , Aceites de Plantas/farmacologíaRESUMEN
Cissampelos sympodialis Eichler is well studied and investigated for its antiasthmatic properties, but there are no data in the literature describing antibacterial properties of alkaloids isolated from this botanical species. This work reports the isolation and characterization of phanostenine obtained from roots of C. sympodialis and describes for the first time its antimicrobial and antibiotic modulatory properties. Phanostenine was first isolated from Cissampelos sympodialis and its antibacterial activities were determined. Chemical structures of the alkaloid isolate were determined using spectroscopic and chemical analyses. Phanostenine was also tested for its antibacterial activity against standard strains and clinical isolates of Escherichia coli and Staphylococcus aureus. Minimal inhibitory concentration (MIC) was determined in a microdilution assay and for the evaluation of antibiotic resistance-modifying activity. MIC of the antibiotics was determined in the presence or absence of phanostenine at sub-inhibitory concentrations. The evaluation of antibacterial activity by microdilution assay showed activity for all strains with better values against S. aureus ATCC 12692 and E. coli 27 (787.69â mm). The evaluation of aminoglycoside antibiotic resistance-modifying activity showed reduction in the MIC of the aminoglycosides (amikacin, gentamicin and neomycin) when associated with phanostenine, MIC reduction of antibiotics ranging from 21 % to 80 %. The data demonstrated that phanostenine possesses a relevant ability to modify the antibiotic activity inâ vitro. We can suggest that phanostenine presents itself as a promising tool as an adjuvant for novel antibiotics formulations against bacterial resistance.
Asunto(s)
Alcaloides/química , Antibacterianos/química , Derivados del Benceno/química , Cissampelos/química , Compuestos Heterocíclicos de 4 o más Anillos/química , Alcaloides/aislamiento & purificación , Alcaloides/farmacología , Antibacterianos/aislamiento & purificación , Antibacterianos/farmacología , Derivados del Benceno/aislamiento & purificación , Derivados del Benceno/farmacología , Cissampelos/metabolismo , Farmacorresistencia Bacteriana/efectos de los fármacos , Compuestos de Anillos Fusionados , Compuestos Heterocíclicos de 4 o más Anillos/aislamiento & purificación , Compuestos Heterocíclicos de 4 o más Anillos/farmacología , Pruebas de Sensibilidad Microbiana , Extractos Vegetales/química , Raíces de Plantas/química , Raíces de Plantas/metabolismo , Staphylococcus aureus/efectos de los fármacosRESUMEN
Bacterial resistance has risen as an important health problem with impact on the pharmaceutical industry because many antibiotics have become ineffective, which has affected their commercialization. The Brazilian biodiversity is marked by a vast variety of natural products with significant therapeutic potential, which could bring new perspectives in the treatment of infections caused by resistant microorganisms. The present study aimed to evaluate the antibacterial effect of the essential oil obtained from Eugenia jambolana (EjEO) using the method of microdilution method to determine the Minimum Inhibitory Concentration (MIC). The modulatory effect of this oil on antibiotic activity was determined using both the broth microdilution and gaseous contact methods. The antibacterial effect of the association of the gaseous contact and the use of a LED unit with red and blue lights was also determined. The chemical components of the EjEO were characterized by HPLC, which revealed the presence of α-pinene as a major constituent. The EjEO presented a MIC≥128µg/mL against S. aureus and ≥1024µg/mL against E. coli. The combination of the EjEO with antibiotics presented synergism against E. coli and antagonism against S. aureus. An antagonistic effect was obtained from the association of EjEO with amikacin and erythromycin by the method of gaseous contact. On the other hand, the association of EjEO with ciprofloxacin presented a synergistic effect against S. aureus and E. coli exposed to LED lights. A similar effect was observed in the association of the EjEO with norfloxacin presented synergism against S. aureus in the same conditions. In conclusion, our results demonstrated that the essential oil obtained from Eugenia jambolana interfere with the action of antibiotics against bacteria exposed to LED lights. Thus, further researches are required to elucidate the mechanisms underlying these effects, which could open new perspectives in the development of new antibacterial therapies.
Asunto(s)
Antibacterianos/farmacología , Luz , Aceites Volátiles/farmacología , Aceites de Plantas/farmacología , Syzygium/química , Escherichia coli/efectos de los fármacos , Escherichia coli/efectos de la radiación , Pruebas de Sensibilidad Microbiana , Staphylococcus aureus/efectos de los fármacos , Staphylococcus aureus/efectos de la radiaciónRESUMEN
La evaluación de la actividad antioxidante ha sido una cuestión relevante teniendo en cuenta su importancia para la salud humana. Estudios recientes muestran que el uso de plantas en forma de jugos o tés como fuentes de antioxidantes naturales, que se pueden utilizar como complemento para el tratamiento de diversas enfermedades. En este contexto, evaluado el potencial antioxidante in vitro, de extractos de Eugenia jambolana Lam y Psidium myrsinites DC. A. y cuantificar fenoles y flavonoides presentes en los extractos. La peroxidación lipídica ha sido evaluada por la técnica de TBARS (sustancias reactivas al ácido tiobarbitúrico). De acuerdo con los resultados, mostraron una mejor actividad antioxidante del extracto de psidium myrsinites DC. A. Para poner a prueba TBARS con fosfolípido de huevo extrae redujo los niveles basales en el proceso de peroxidación de lípidos, la CI50 del extracto etanolico de Euguenia jambolana (EEFEJ) mostró los mejores resultados, con un más bajo valor de la CI50 en comparación con el extracto hidroetanolico de Psidium mirsinites, demostrado ser más efectivo. Por lo tanto, a través de estas pruebas se puede ver que los extractos de las hojas de la especie, Eugenia jambolana Lam y Psidium myrsinites DC. A., la actividad antioxidante de exposiciones, sustancias fenólicas directamente relacionados producidos a partir de su metabolismo secundario.
The evaluation of the antioxidant activity has been a relevant and important issue to human health. Recent studies show that the use of plants juices or teas as sources of natural antioxidants, which can be used as an adjuvant in the treatment of several diseases. In this context, was evaluated the in vitro antioxidant potential of the extracts of Psidium myrsinites DC. and Eugenia jambolana Lam. The total of phenols and flavonoids were quantified in the extracts. Lipid peroxidation was evaluated by the technique of TBARS (thiobarbituric acid reactive substances). According to the results, was showed a better antioxidant activity in the extract of Psidium myrsinites DC. A. In the TBARS assay with egg phospholipid the extracts reduced the basal levels in the process of lipid peroxidation and the IC50 of ethanol extract of Eugenia jambolana (EEFEJ) showed the best results with a lower value of IC50 compared with hydroethanol extract of Psidium mirsinites, demonstrating be more effective. Therefore, through these tests can be seen that extracts from the leaves of the species, Eugenia and Psidium jambolana Lam myrsinites DC. A., exhibit antioxidant activity, directly related phenolic substances produced from the secondary metabolism.
Asunto(s)
Humanos , Antioxidantes/síntesis química , Eugenia jambosa/uso terapéutico , Peroxidación de Lípido/efectos de los fármacos , Psidium/efectos de los fármacos , Fitoquímicos/uso terapéutico , Extractos Vegetales/uso terapéuticoRESUMEN
Medicinal plants are often the only therapeutic resource for many communities and ethnic groups. Cordia verbenacea DC., "Erva-baleeira," is one of the species of plants currently used to produce a phytotherapeutic product extracted from its leaves. The present study aimed to establish its chemical profile, antibacterial activity and resistance-modulating potential. The C. verbenacea extracts were prepared from fresh leaves using solvents as methanol and hexane. Ethyl Acetate was used for the preparation of the fraction. Phytochemical screening was carried out using HPLC-DAD for determination and quantification of the secondary metabolites present in the fractions. Antibacterial and resistance-modulation assays were performed to determine minimum inhibitory concentration (MIC) using a microdilution assay. The data were subjected to statistical analysis with two-way ANOVA and Bonferroni posttests. Results of phytochemical prospecting and HPLC analysis of the fractions were in agreement with the literature. The natural products presented moderate antibacterial activity when considering the clinical relevance of a MIC of 256 µg/mL against Staphylococcus aureus, Escherichia coli and Pseudomonas aeruginosa, and 512 µg/mL against P. aeruginosa. However, when the fractions were combined with antibiotics we observed a synergic effect, as natural products enhanced the antibacterial effect of aminoglycosides, significantly decreasing the MIC of antibiotics at 12.5%-98.4%. We believe that the data obtained from phytochemical analysis and from antibacterial and resistance modulation assays of C. verbenacea extracts new can open perspectives in the search for new alternatives for the treatment of bacterial infections and stimulate the renewed use of antibiotics with reduced effectiveness due to resistance.
Asunto(s)
Aminoglicósidos/farmacología , Antibacterianos/farmacología , Productos Biológicos/farmacología , Cordia/química , Sinergismo Farmacológico , Fitoquímicos/farmacología , Antibacterianos/aislamiento & purificación , Productos Biológicos/aislamiento & purificación , Cromatografía Líquida de Alta Presión , Escherichia coli/efectos de los fármacos , Pruebas de Sensibilidad Microbiana , Fitoquímicos/análisis , Fitoquímicos/aislamiento & purificación , Hojas de la Planta/química , Pseudomonas aeruginosa/efectos de los fármacos , Staphylococcus aureus/efectos de los fármacosRESUMEN
CONTEXT: Murraya paniculata (Linn) JACK (Rutaceae) is used in traditional medicine in the treatment of diabetes, inflammation, and microbial disorders. OBJECTIVE: This study determined the polyphenol composition and antimicrobial and acute toxicological activity of the hydroethanolic extract of M. paniculata leaves (EEMp). MATERIALS AND METHODS: Chemical composition was evaluated by the Folin-Ciocalteu and AlCl3 assays and by HPLC-DAD. Antibacterial and modulatory activity was determined by the microdilution method. Toxicity was assessed with a single dose of EEMp administered orally at doses of 2000 and 5000 mg/kg body weight/day in male and female Swiss mice. RESULTS: Total phenolic content of the EEMp samples varied from 66.5 to 396.8 mg gallic acid equivalent/g of extract and flavonoid content varied from 0.3 to 31.1 mg quercetin equivalent/g of extract. The principal component identified by HPLC-DAD assay was ellagic acid. The results of oral acute toxicity showed no mortality, changes in hematological parameters, or CNS and ANS toxicities in rats. Biochemical analysis showed a significant increase in glucose and glutamic oxaloacetic transaminase activity and reduction in triglycerides and cholesterol for 5000 and 2000 mg/kg doses, respectively, when compared with the control group. Histopathological evaluation showed no significant microscopic changes. EEMp showed essentially no antimicrobial activity, but when aminoglycosides were combined with EEMp their MIC was reduced. CONCLUSIONS: Significant effects were observed in the acute toxicity assay, but they had no clinical relevance. The results suggest that M. paniculata could be used as a source of natural products with antibacterial resistance-modifying activity, with lower toxicity.
Asunto(s)
Antibacterianos/aislamiento & purificación , Farmacorresistencia Bacteriana/efectos de los fármacos , Flavonoides/aislamiento & purificación , Murraya/química , Extractos Vegetales/química , Animales , Antibacterianos/farmacología , Antibacterianos/toxicidad , Brasil , Relación Dosis-Respuesta a Droga , Femenino , Flavonoides/farmacología , Flavonoides/toxicidad , Masculino , Medicina Tradicional , Pruebas de Sensibilidad Microbiana , Hojas de la Planta/química , Ratas WistarRESUMEN
BACKGROUND: Multi-resistantmicroorganisms such as Escherichia coli, Staphylococcus aureus, Pseudomonas aeruginosa, Candida tropicalis e Candida krusei are the main causes of microbial infections. Padina sanctae-crucis is a seaweed often used to check the contamination of ecosystems by materials such as heavy metals, but studies of the antimicrobial activity of the same seaweed were not found. METHODS: The tests for the minimum inhibitory concentration and modulation of microbial resistance, with the use of ethanolic and methanolic extracts of Padina Sanctae-cruces combined with drugs of the class of aminoglycosides and antifungal were used to evaluate the activity against the cited microorganisms. RESULTS: Was observed a modulation of antibiotic activity between the natural products and the E. coli and S. aureus strains, indicating a synergism and antagonism respectively. CONCLUSIONS: The results showed a moderate modulatory effect against some microorganisms studied.
Asunto(s)
Antibacterianos/farmacología , Antifúngicos/farmacología , Bacterias/efectos de los fármacos , Hongos/efectos de los fármacos , Phaeophyceae/química , Extractos Vegetales/aislamiento & purificación , Etanol/química , Etanol/farmacología , Humanos , Metanol/química , Metanol/farmacología , Pruebas de Sensibilidad Microbiana , Extractos Vegetales/química , Extractos Vegetales/farmacología , Algas MarinasRESUMEN
A leishmaniose e a doença de Chagas tem sido um grande desafio, no que diz respeito à sua terapêutica. Devido à grande dificuldade de encontrar fármacos que garantam uma ação terapêutica eficiente e menos agressora à espécie humana, diferentes produtos naturais vêm sendo testados. Muitas espécies vegetais foram investigadas quanto à sua ação leishmanicida e tripanocida na expectativa de que seus compostos metabólicos possuam atividade antiparasitária e ausência ou baixa citotoxicidade. Neste estudo sobre bioatividade do a-pineno e carvacrol, avaliaram-se os potenciais leishmanicida e tripanocida. O carvacrol apresentou um percentual de inibição de 38,34% e 74,12% para as formas promastigotas e epimastigotas respectivamente, na concentração de 100µg/mL, apresentando uma citotoxicidade de 21,62%. O a-pineno apresentou 100% e 5,30% de inibição para as formas epimastigota e promastigota na concentração de 100 µg/mL, com citotoxicidade de 87,88%.
Leishmaniasis and Chagas Disease represent a great challenge against the modern therapeutics. Due the high difficult to find new drugs with therapeutic efficacy and low toxicity, several natural products had been screened. Many species of plants were investigated about their leishmanicidal and trypanocidal activities. Some phytocompounds are the a-pinene and carvacrol. In this work, we evaluated the bioactivities of a-pinene and carvacrol against Trypanosoma cruzi and Leishmania braziliensis cell lines. The carvacrol inhibited 38,34% and 74,12% of the promatigote and epimastigote forms, respectively at 100 µg/mL, showing a low cytotoxic activity (21,62%). The O a-pinene inhibited 100% and 5,30% against the epimastigote and promastigote forms respectively, at 100 µg/mL, showing a higher cytotoxic activity (87,88%).
Asunto(s)
Enfermedad de Chagas/tratamiento farmacológico , Leishmaniasis/tratamiento farmacológico , Tripanocidas/uso terapéutico , Tripanocidas/toxicidad , Antiparasitarios/toxicidad , Origanum , Pruebas de Toxicidad/métodosRESUMEN
CONTEXT: The combination of antibiotics with natural products has demonstrated promising synergistic effects in several therapeutic studies. OBJECTIVE: The aim of this study was to determine the effect of a combination of an ethanol extract of Myracrodruon urundeuva Fr. All. (Anacardiaceae) (aroeira plant) and its essential oil with six antimicrobial drugs against multiresistant strains of Staphylococcus aureus and Escherichia coli from clinical isolates. MATERIALS AND METHODS: After identification of the chemical components by GC-MS, the antibacterial activity of the natural products and antibiotics was assessed by determining the minimal inhibitory concentration (MIC) using the microdilution method and concentrations ranging 8-512 µg/mL and 0.0012-2.5 mg/mL, respectively. Assays were performed to test for a possible synergistic action between the plant products and the antimicrobials, using the extract and the oil at a sub-inhibitory concentration (128 µg/mL) and antibiotic at concentrations varying between 8 and 512 µg/mL. RESULTS: The GC-MS analysis identified the main compound as δ-carene (80.41%). The MIC of the natural products was >1024 µg/mL, except against S. aureus ATCC25923. Only the combinations of the natural products with gentamicin, amikacin and clindamycin were effective against S. aureus 358, enhancing the antibiotic activity by reducing the MIC. CONCLUSIONS: The extract from aroeira showed a higher antibacterial activity and the oil was more effective in potentiating the activity of conventional antibiotics.
Asunto(s)
Anacardiaceae/química , Antibacterianos/farmacología , Aceites Volátiles/farmacología , Extractos Vegetales/farmacología , Aceites de Plantas/farmacología , Terpenos/farmacología , Antibacterianos/administración & dosificación , Farmacorresistencia Bacteriana Múltiple/efectos de los fármacos , Sinergismo Farmacológico , Escherichia coli/efectos de los fármacos , Cromatografía de Gases y Espectrometría de Masas , Pruebas de Sensibilidad Microbiana , Aceites Volátiles/administración & dosificación , Aceites Volátiles/química , Aceites Volátiles/aislamiento & purificación , Extractos Vegetales/química , Extractos Vegetales/aislamiento & purificación , Hojas de la Planta/química , Aceites de Plantas/administración & dosificación , Aceites de Plantas/química , Aceites de Plantas/aislamiento & purificación , Staphylococcus aureus/efectos de los fármacos , Terpenos/administración & dosificación , Terpenos/química , Terpenos/aislamiento & purificaciónRESUMEN
Candidiasis is the most frequent infection by opportunistic fungi such as Candida albicans, Candida tropicalis, and Candida krusei. Ethanol extract from Eugenia uniflora was assayed, for its antifungal activity, either alone or combined with four selected chemotherapeutic antimicrobial agents, including anphotericin B, mebendazole, nistatin, and metronidazole against these strains. The obtained results indicated that the association of the extract of E. uniflora to metronidazole showed a potential antifungal activity against C. tropicalis. However, no synergistic activity against the other strains was observed, as observed when the extract was associated with the other, not enhancing their antifungal activity.
Asunto(s)
Antifúngicos/farmacología , Candida/efectos de los fármacos , Candidiasis/tratamiento farmacológico , Extractos Vegetales/farmacología , Syzygium/química , Candida/crecimiento & desarrollo , Candidiasis/microbiología , Combinación de Medicamentos , Sinergismo Farmacológico , Humanos , Pruebas de Sensibilidad MicrobianaRESUMEN
BACKGROUND & OBJECTIVES: Several chemical compounds isolated from natural sources have antibacterial activity and some enhance the antibacterial activity of antibiotics reversing the natural resistance of bacteria to certain antibiotics. In this study, the hexane and methanol extract of Cordia verbenaceae were assessed for antibacterial activity alone and combinated with norfloxacin against the Staphylococcus aureus strain SA1199B. METHODS: The minimum inhibitory concentration (MIC) of extracts was assayed using microdilution assay and the modulatory activity was evaluated using plate diffusion assay. RESULTS: The MIC observed varied between 256 to >1024 µg/ml. However, the antibiotic activity of norfloxacin was enhanced in the presence of subinhibitory concentrations of hexane extract of C. verbenaceae (HECV). INTERPRETATIONS & CONCLUSIONS: Our results indicate that Cordia verbenaceae DC. can be a source of plant derived products with antibiotic modifying activity.
Asunto(s)
Farmacorresistencia Bacteriana/genética , Extractos Vegetales/administración & dosificación , Infecciones Estafilocócicas/tratamiento farmacológico , Staphylococcus aureus/efectos de los fármacos , Antibacterianos/administración & dosificación , Cordia/química , Sinergismo Farmacológico , Hexanos/química , Humanos , Norfloxacino/administración & dosificación , Extractos Vegetales/química , Infecciones Estafilocócicas/genética , Infecciones Estafilocócicas/patología , Staphylococcus aureus/genética , Staphylococcus aureus/patogenicidadRESUMEN
The aim of this study was to verify the possible interactions between ethanol extracts of Amburana cearensis A. C. Smith and Anadenanthera macrocarpa (Benth.) Brenan, combined with six antimicrobial drugs against multiresistant strains of Staphylococcus aureus and Escherichia coli isolated from humans. The antibacterial activity of the extracts was determined using the minimum inhibitory concentration (MIC). The microdilution assay was performed to verify the interactions between the natural products and the antibiotics using a subinhibitory concentration. The activity of amikacin associated with the extract of Anadenanthera macrocarpa against EC 27 was enhanced, demonstrating an MIC reduction from 128 to 4 µg/mL. Among the ß-lactams, no potentiation on its activity was observed, with exception to the antagonism of the natural products with ampicillin against S. aureus 358.
Asunto(s)
Antibacterianos/farmacología , Fabaceae/química , Mimosa/química , Extractos Vegetales/farmacología , Amicacina/farmacología , Aminoglicósidos/farmacología , Ampicilina/farmacología , Farmacorresistencia Bacteriana , Escherichia coli/efectos de los fármacos , Pruebas de Sensibilidad Microbiana , Hojas de la Planta/química , Staphylococcus aureus/efectos de los fármacos , beta-Lactamas/farmacologíaRESUMEN
Chagas disease is caused by Trypanosoma cruzi, being considered a public health problem. An alternative to combat this pathogen is the use of natural products isolated from fruits such as Eugenia uniflora, a plant used by traditional communities as food and medicine due to its antimicrobial and biological activities. Ethanolic extract from E. uniflora was used to evaluate in vitro anti-epimastigote and cytotoxic activity. This is the first record of anti-Trypanosoma activity of E. uniflora, demonstrating that a concentration presenting 50% of activity (EC(50)) was 62.76 µg/mL. Minimum inhibitory concentration (MIC) was ≤ 1024 µg/mL. Our results indicate that E. uniflora could be a source of plant-derived natural products with anti-epimastigote activity with low toxicity.
Asunto(s)
Macrófagos/efectos de los fármacos , Extractos Vegetales/farmacología , Syzygium/química , Trypanosoma cruzi/efectos de los fármacos , Animales , Línea Celular , Supervivencia Celular/efectos de los fármacos , Colorimetría , Macrófagos/citología , Ratones , Extractos Vegetales/toxicidadRESUMEN
Tripanosomiasis or Chagas disease, caused by Trypanosoma cruzi, affect 10 million people in Latin America. Today, the chemotherapy is the only specific treatment against this disease, being the most used drugs the nifurtimox and benznidazole. Leishmaniasis is a disease caused by parasites of the genus Leishmania, mainly founded in regions with forests, as the Amazonia. Recent reports about the Leishmaniasis indicate a deficit of therapeutical drugs available against this disease and reinforce the necessity of the discovering of new drugs. An interesting approach against these diseases is the use of natural products, as the extracts of plants as Mentha arvensis and Turnera ulmifolia. For the in vitro assays against T. cruzi and Leishmania, was used the clone CL-B5 and promastigote forms, respectively. The cytotoxic assay was performed using fibroblasts. Our results indicated that M. arvensis was active against all strains assayed, inhibiting 65 e 47 percent of the assayed strains (IC50 = 192.3 and 531.9 ug/mL respectively), representing an interesting and alternative source of natural products with anti-kinetoplastida activity.
Doença de Chagas, causada por Trypanosoma cruzi, afeta cerca de 10 milhões de pessoas nas Américas. Atualmente, a quimioterapia é o único tratamento específico disponível para esta doença, onde os medicamentos utilizados são nifurtimox e benzonidazol. Leishmaniose tegumentar Americana no Brasil é causada por uma variedade de espécies de Leishmania e uma grande diversidade destes parasitos pode ser encontrada na Região Amazônica. Revisões recentes na quimioterapia de leishmaniose enfatizam as deficiências dos agentes terapêuticos atualmente disponíveis e mostram a necessidade urgente de novos candidatos. Uma alternativa para substituir esses medicamentos são extratos naturais de Mentha arvensis e Turnera ulmifolia. Foram preparados extratos etanólicos das folhas de M. arvensis e T. ulmifolia. Para os testes in vitro de T. cruzi, foi utilizado o clone CL-B5 e para Leishmania brasiliensis foram utilizadas formas promastigotas. O ensaio de citotoxicidade foi realizado com linhagens de fibroblastos. Nossos resultados indicam que M. arvensis foi eficaz contra as cepas de parasitos testadas apresentando 65 e 47 por cento de inibição em uma concentração de 500 ug/mL (respectivamente, CE50 = 192.3 e 531.9 ug/mL), sendo considerada uma fonte alternativa de produtos naturais com atividade contra T. cruzi e L. brasiliensis.
Asunto(s)
Antiparasitarios/farmacología , Extractos Vegetales/farmacología , Leishmania braziliensis , Mentha/química , Trypanosoma cruzi , Turnera/química , BrasilRESUMEN
CONTEXT: Chagas disease, caused by Trypanosoma cruzi, is a public health problem. Currently, chemotherapy is the only available treatment for this disease, and the drugs used, nifurtimox and benzonidazol, present high toxicity levels. An alternative for replacing these drugs are natural extracts from Momordica charantia L. (Cucurbitaceae) used in traditional medicine because of their antimicrobial and biological activities. OBJECTIVE: In this study, we evaluated the extract of M. charantia for its antiepimastigote, antifungal, and cytotoxic activities. MATERIALS AND METHODS: An ethanol extract of leaves from M. charantia was prepared. To research in vitro antiepimastigote activity, T. cruzi CL-B5 clone was used. Epimastigotes were inoculated at a concentration of 1 × 10(5) cells/mL in 200 µl tryptose-liver infusion. For the cytotoxicity assay, J774 macrophages were used. The antifungal activity was evaluated by microdilution using strains of Candida albicans, Candida tropicalis, and Candida krusei. RESULTS: The effective concentration capable of killing 50% of parasites (IC(50)) was 46.06 µg/mL. The minimum inhibitory concentration (MIC) was ≤ 1024 µg/mL. Metronidazole showed a potentiation of its antifungal effect when combined with an extract of M. charantia. CONCLUSIONS: Our results indicate that M. charantia could be a source of plant-derived natural products with antiepimastigote and antifungal-modifying activity with moderate toxicity.
Asunto(s)
Antifúngicos/farmacología , Momordica charantia/química , Extractos Vegetales/farmacología , Tripanocidas/farmacología , Animales , Antifúngicos/aislamiento & purificación , Antifúngicos/toxicidad , Candida/efectos de los fármacos , Línea Celular , Sinergismo Farmacológico , Concentración 50 Inhibidora , Macrófagos/efectos de los fármacos , Macrófagos/metabolismo , Medicina Tradicional , Metronidazol/administración & dosificación , Metronidazol/farmacología , Ratones , Pruebas de Sensibilidad Microbiana , Pruebas de Sensibilidad Parasitaria , Extractos Vegetales/administración & dosificación , Extractos Vegetales/toxicidad , Hojas de la Planta , Pruebas de Toxicidad , Tripanocidas/aislamiento & purificación , Tripanocidas/toxicidad , Trypanosoma cruzi/efectos de los fármacosRESUMEN
Chagas' disease, caused by Trypanosoma cruzi, is considered a public health problem. Nowadays, chemotherapy is the only available treatment for this disease, and the drugs currently used, nifurtimox and benzonidazole, present high toxicity levels. Alternatives for replacing these drugs are natural extracts from Eugenia jambolana, a plant used in traditional medicine because of its antimicrobial and biological activities. An ethanol extract from E. jambolana was prepared. To research in vitro anti-epimastigote activity, T. cruzi CL-B5 clone was used. Epimastigotes were inoculated at a concentration of 1×10(5)/mL in 200 µL of tryptose-liver infusion. For the cytotoxicity assay J774 macrophages were used. To examine antifungal activity, Candida albicans, Candida tropicalis, and Candida krusei were used. This is the first record of trypanocide activity for E. jambolana. The effective concentration capable of killing 50% of the parasites was 56.42 µg/mL. The minimum inhibitory concentration was ≤1,024 µg/mL. Metronidazole showed a potentiation of its antifungal effect when combined with the ethanol extract of E. jambolana. Thus our results indicate that E. jambolana could be a source of plant-derived natural products with anti-epimastigote and antifungal modifying activity with moderate toxicity.
Asunto(s)
Antifúngicos/uso terapéutico , Candida/efectos de los fármacos , Enfermedad de Chagas/tratamiento farmacológico , Extractos Vegetales/farmacología , Syzygium , Tripanocidas/farmacología , Trypanosoma cruzi/efectos de los fármacos , Animales , Antifúngicos/farmacología , Enfermedad de Chagas/microbiología , Citotoxinas/farmacología , Concentración 50 Inhibidora , Macrófagos/efectos de los fármacos , Metronidazol/farmacología , Ratones , Pruebas de Sensibilidad Microbiana , Extractos Vegetales/efectos adversos , Extractos Vegetales/uso terapéutico , Hojas de la Planta , Syzygium/efectos adversos , Tripanocidas/uso terapéuticoRESUMEN
Tropidurus hispidus and Tropidurus semitaeniatus are two lizard species utilized in traditional medicine in Northeast Brazil. Their medicinal use includes diseases related with bacterial infections such as tonsillitis and pharyngitis. They are used in the form of teas (decoctions) for the treatment of illnesses. In this work, we evaluated the antimicrobial activity of the decoctions of T. hispidus (DTH) and T. semitaeniatus (DTS) against bacterial strains, namely, standard and multiresistant Escherichia coli, Staphylococus aureus, and Pseudomonas aureuginosa, alone and in combination with aminoglycoside antibiotics. The decoctions were prepared using the whole body of the dried lizards, and the filtrate was frozen and lyophilized. When tested alone, the samples did not demonstrate any substantial inhibition of bacterial growth. However, in combination with antibiotics as aminoglycosides, decoctions reduced the minimal inhibitory concentration (MIC) of the assayed antibiotics against multiresistant strains of S. aureus and P. aureuginosa. Chemical prospecting tests revealed the presence of alkaloids in DTS. This is the first study evaluating the medicinal efficacy of T. hispidus and T. semitaeniatus and contributes to the list of new sources of medicines from natural products of animal origin.
RESUMEN
In this study, the methanol extracts of of Costus cf. arabicus L. were evaluated for antibacterial activity against multiresistant strains of Escherichia coli and Staphylococcus aureus. The antibacterial and modulatory activity of the extracts was assayed by microdilution. The light-enhanced antibacterial activity was assayed by light regimen. The growth of the bacteria tested was not inhibited by the extracts. The minimum inhibitory concentration (MIC) values ranged from 512 to ≥1024 µg·m L(-1). However, the antibiotic activity of the aminoglycosides was synergistically enhanced when these extracts were associated in sub-inhibitory concentrations with the antibiotics. Both extracts showed activity against at two standard bacterial strains. Because of this, we suggest that the ethanol extracts of the stems and leaves of Costus cf. arabicus L. show potential antibacterial, light-induced and synergistic antibiotic activity. With such results, these extracts are proven to be a promising source of antibacterial and modulatory agents.