RESUMEN
The aim of this study was to evaluate the antifungal and modulatory potential of the Ziziphus joazeiro bark and leaf extracts, both in isolation and in association with fluconazole, against resistant species from the Candida genus. Antifungal assays were used to determine the half maximal inhibitory concentration (IC50) of the extract in isolation and in combination with fluconazole using the broth microdilution method and spectrophotometric readings, followed by verification of the minimum fungicidal concentration by solid medium subculture. According to the cell viability curve, both extracts inhibited fungal growth in a concentration dependent manner, in addition to showing inhibitory concentrations similar to fluconazole. However, the extracts behaved in a fungistatic manner with minimum inhibitory concentration > 8.19 mg/mL and IC50 values ranging from 0.450 mg/mL to 9 mg/mL. The minimum inhibitory concentration for both extracts decreased when in combination with fluconazole, with the AEL standing out against Candida albicans URM 4387, displaying an IC50 equal to that of fluconazole (0.002 mg/mL). Nevertheless, fluconazole antagonism was observed against the tested strains. Overall, the evaluation of both extracts against Candida spp. presented inhibitory concentration values greater than fluconazole. Moreover, despite these being chemically complex crude extracts, they did demonstrate antifungal effects and properties that concur with their ethno-biological aspect.
Asunto(s)
Antifúngicos/farmacología , Metaboloma , Fitoquímicos/farmacología , Ziziphus/metabolismo , Antifúngicos/química , Candida/efectos de los fármacos , Cromatografía Líquida de Alta Presión , Fluconazol/farmacología , Concentración 50 Inhibidora , Viabilidad Microbiana/efectos de los fármacos , Fitoquímicos/química , Extractos Vegetales/farmacología , AguaRESUMEN
In the search for new therapeutic agents against neglected diseases, both aqueous and hydroethanolic extracts from Psidium guajava L. and P. brownianum Mart ex DC leaves were investigated regarding their antiparasitic effect and cytotoxic potential. The extracts were tested at three concentrations (250, 500 and 1000⯵g/mL) against Trypanosoma cruzi epimastigote forms (Chagas, 1909), Leishmania braziliensis (Vianna, 1911) and L. infantum promastigotes forms (Nicolle, 1908), as well as against fibroblasts. P. guajava showed no activity against T. cruzi forms, while the hydroethanolic (PBHE), aqueous by decoction (PBAED) and aqueous by infusion (PBAEI) P. browninaum extracts were responsible, respectively, for inhibiting 100, 100 and 92.68% of T. cruzi epimastigote growth at the 1000⯵g/mL concentration. The P. brownianum hydroethanolic extract (PBHE) at the highest concentration caused 58.46% death in L. braziliensis, thus demonstrating moderate activity, however when tested against L. infantum, the PBHE inhibited their growth by 37.16%, revealing its low activity. As for the cytotoxicity assays, the P. brownianum aqueous extract by decoction (PBAED) obtained the highest death percentage when compared to the others, causing 90.85% fibroblast mortality at the 1000⯵g/mL concentration.
Asunto(s)
Antiparasitarios/farmacología , Leishmania braziliensis/efectos de los fármacos , Leishmania infantum/efectos de los fármacos , Extractos Vegetales/farmacología , Hojas de la Planta/química , Psidium/química , Trypanosoma cruzi/efectos de los fármacos , Animales , Línea Celular , RatonesRESUMEN
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
The aim of this work was to evaluate the interactions between gentamicin and the ethanol extract of the fern Lygodium venustum SW (EELV). The ethanol extract of L. venustum was obtained, the phytocompounds were identified and the EELV was assayed by the checkerboard method with gentamicin against two bacterial strains multiresistant to antibiotics. The antibiotic activity of gentamicin, when associated with the extract, was enhanced in an additive manner against both strains. The results indicated that L. venustum can be a source of secondary metabolites to be used in association with antibiotics as aminoglycosides in the antibiotic chemotherapy against resistant bacteria.
Asunto(s)
Antibacterianos/farmacología , Helechos/química , Gentamicinas/farmacología , Extractos Vegetales/farmacología , Antibacterianos/química , Evaluación Preclínica de Medicamentos/métodos , Farmacorresistencia Bacteriana Múltiple/efectos de los fármacos , Sinergismo Farmacológico , Escherichia coli/efectos de los fármacos , Etanol/química , Pruebas de Sensibilidad Microbiana , Extractos Vegetales/química , Staphylococcus aureus/efectos de los fármacosRESUMEN
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
The search for new therapeutic agents has been a constant for the treatment of diseases such as leishmaniasis and Chagas disease. Most drugs used have side effects, justifying the need to evaluate the cytotoxicity of the tested products for candidates to new drugs. In this study, the bioactivity of Lygodium venustum, a cosmopolitan fern of Lygodiaceae, was assessed about their leishmanicidal and trypanocidal potential. The better activity was observed using methanol fraction, with inhibition percentage of 63% and 68% for promastigotes and epimastigotes, respectively, at a concentration of 500 µg/mL. The ethyl acetate and methanol fractions demonstrated a higher cytotoxic potential. This was the first report of leishmanicidal, trypanocidal and cytotoxic activities to L. venustum.
Asunto(s)
Antiprotozoarios/farmacología , Helechos/química , Leishmania braziliensis/efectos de los fármacos , Extractos Vegetales/farmacología , Trypanosoma cruzi/efectos de los fármacos , Antiprotozoarios/química , Antiprotozoarios/aislamiento & purificación , Fenoles/análisis , Extractos Vegetales/química , Extractos Vegetales/aislamiento & purificación , Hojas de la Planta/química , Tripanocidas/química , Tripanocidas/aislamiento & purificación , Tripanocidas/farmacologíaRESUMEN
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
The genus Acinetobacter has gained importance in recent years due to involvement in serious infections and antimicrobial resistance. Many plants have been evaluated not only for direct antimicrobial activity, but also as resistance modifying agents. The Essential oil of Citrus limon (EOCL) addition at 156.25 µgmL(-1) (MIC/8) sub-inhibitory concentration in the growth medium led to MIC decrease for amikacin, imipenem and meropenem. The Essential oil of Cinnamomum zeylanicum (EOCZ) addition at 78.125 µg mL(-1) (MIC/8) sub-inhibitory concentrations in the growth medium caused drastic MIC reduction of amikacin. Results of combining antibiotics and essential oils had shown us a synergistic effect with both essential oils/amikacin combinations. An additive effect was observed with the combinations of both essential oils and gentamicin. The results of this study suggest that essential oil of C. limon and C. zeylanicum may suppress the growth of Acinetobacter species and could be a source of metabolites with antibacterial modifying activity.