Phytochemical characterization of the Ziziphus joazeiro Mart. metabolites by UPLC-QTOF and antifungal activity evaluation.

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.

Serine protease inhibition and modulatory-antibiotic activity of the proteic extract and fractions from Amburana cearensis.

This study investigated the inhibitory activity of serine protease, as well as antibacterial and antibiotic modifying activities of the crude extract and fractions of A. cearensis seeds. Microdilution assay was used to evaluate the antibacterial activity and the antibiotic resistance-modulating effects of samples against multiresistant bacteria Staphylococcus aureus (SA10) and Escherichia coli (EC06). In the inhibition test for serine protease, all the samples showed inhibition of enzymatic activity. Crude extract and fractions of A. cearensis seeds showed a Minimum Inhibitory Concentration ≥1024 µg/mL for all microorganisms tested. However, the samples acted as resistance modifying agent, presenting synergism when associated with gentamicin, norfloxacin and penicillin. The present study provides data indicating a possible use of the seeds extract of A. cearensis in association with antibiotics in the fight against bacterial infections.

Additive effect of Lygodium venustum SW. in association with gentamicin.

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.

Avaliação da atividade citotóxica e potencial antiparasitário in vitro do a-pineno e carvacrol / Cytotoxic and antiparasitic in vitro activities of a-pinene and carvacrol

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%).

Chemical composition and evaluation of modulatory of the antibiotic activity from extract and essential oil of Myracrodruon urundeuva.

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.

Citotocixidade e atividade antiparasitária de Lygodium venustum SW / Cytotoxic and antiparasitic activity of Lygodium venustum SW

. Doenças parasitárias infecciosas como leishmaniose e doença de Chagas tem se difundido nas últimas décadas a locais onde antes não se observava sua ocorrência. São consideradas negligenciadas por assolarem países pobres e serem marginalizadas farmacologicamente. O tratamento não apresenta muitas opções de fármacos e estes demonstram relevante toxicidade contribuindo para o aparecimento de diversos efeitos colaterais. A pesquisa com produtos naturais tem se mostrado uma interessante alternativa para a procura por novos fármacos. Lygodium venustum é uma samambaia cosmopolita de hábito lianescente encontrada na encosta na Chapada do Araripe, considerada por algumas populações americanas como planta medicinal para o tratamento de dermatoses, infecções, micoses e tricomoníases. Neste estudo foi avaliada sua atividade anti-parasitária contra Leishmania brasiliensis e Trypanosoma cruzi, bem como sua citotoxicidade através de ensaios n vitro. Foram testadas a fração hexânica e o extrato etanólico obtido das folhas de Lygodium venustum em diferentes concentrações. 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 fbroblastos. L. venustum não apresentou atividade antiparasitária clinicamente relevante na forma de extrato etanólico bruto nem como fração hexânica contra Leishmania. A fração hexânica apresentou uma atividade intermediária contra T. cruzi, porém a concentração de efeito moderado possui citotoxicidade máxima tornando-se inviável para aplicação clínica. Entretanto, a citoxicicidade apresentada poderá ser útil em pesquisas sobre atividade antineoplásica em células tumorais.

Infectious and parasitic diseases like leishmaniasis and Chagas disease have spreading recent decades to places not observed before. They are considered neglected by desolating poor countries and marginalized pharmacologically. There are not many options for the treatment and these drugs have shown signifcant toxicity contributing to the appearance of several side effects. Research on natural products has been shown to be an interesting alternative to the search for new drugs. Lygodium venustum is a cosmopolitan fern with latescence habit found on the Chapada do Araripe, considered by some American popula-tions as a medicinal plant for the treatment of skin diseases, infections, fungal infections and trichomoniasis. This study evaluated its antiparasitic activity against Trypanosoma cruzi and Leishmania brasiliensis, as well as its cytotoxicity through trials in vitro. We tested the ethanolic extract and hexane fraction obtained from the leaves of L. venustum at different concentrations. For in vitro tests of T. cruzi, we used the clone CL-B5 and for L. brasiliensis we used promastigotes. The cytotoxicity assay was performed with strains of fbroblasts. L.venustum showed no antiparasitic activity clinically relevant in the form of crude ethanolic extractor as the hexane fraction against Leishmania. The hexane fraction showed an intermediate activity against T.cruzi, but the concentration of moderate effect has maximum cytotoxicity becoming unfeasible for clinical application. However, the cytotoxicity presented may be useful in research on antineoplastic activity in tumor cells.

Phenol composition, cytotoxic and anti-kinetoplastidae activities of Lygodium venustum SW. (Lygodiaceae).

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.

Evaluation of the Antimicrobial Activity of the Decoction of Tropidurus hispidus (Spix, 1825) and Tropidurus semitaeniatus (Spix, 1825) Used by the Traditional Medicine.

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.