The plant Cecropia pachystachya Trécul is widely used in Brazilian ethnomedicine to treat hypertension, asthma, and diabetes. Arginase is an enzyme with levels that are elevated in these disorders, and it is central to Leishmania polyamine biosynthesis. The aims of this study were to evaluate antileishmanial activity and inhibition of the arginase enzyme by C. pachystachya extracts, and to study changes in cellular organization using electron microscopy. The ethanol extract of C. pachystachya was tested on Leishmania (Leishmania) amazonensis promastigote survival/proliferation and arginase activity in vitro. Qualitative ultrastructural analysis was also used to observe changes in cell organization. The major bioactive molecules of the ethanol extract were characterized using liquid chromatography-electrospray ionization-mass spectrometry (LC-ESI-MS). The ethyl acetate fraction of the ethanol extract diminished promastigote axenic growth/survival, inhibited arginase activity, and altered a mitochondrial kinetoplast DNA (K-DNA) array. The bioactive compounds of C. pachystachya were characterized as glucoside flavonoids. Orientin (9) (luteolin-8-C-glucoside) was the main component of the methanol-soluble ethyl acetate fraction obtained from the ethanol extract and is an arginase inhibitor (IC50 15.9 μM). The ethyl acetate fraction was not cytotoxic to splenocytes at a concentration of 200 μg/mL. In conclusion, C. pachystachya contains bioactive compounds that reduce the growth of L. (L.) amazonensis promastigotes, altering mitochondrial K-DNA arrangement and inhibiting arginase.
Among the plant species studied, C. americana proved to be effective against microorganisms, especially as an antifungal. The results will help in the search for alternative drugs to be used in pharmacotherapy, and will contribute to establish safe and effective use of phytomedicines in the treatment of infectious diseases.
Works on antiviral compounds date back to the 1950s, but for several reasons, only a couple of drugs were approved for clinical use about a decade later. To date, many antiviral drugs have been developed after extensive research and demanding trials, some of them with selective mechanisms against viral replication. 1) Although the primary focus has been on synthetic products, the number of natural compounds with antiviral action for different DNA and RNA viruses that are being studied is increasing. Many phytochemical compounds are being investigated based primarily on ethnopharmacologic knowledge and have been considered of great importance in new drug development. 2)Extracts of many plant species, such as Tridax procumbens, Carissa carandas, Mallotus philippensis, Streblus aspere, Terminatta alata, Macaranga pustulata, Sibbaldia micropetala, Hypericum cordifolium, H. uralum and Maesa macrophylla were found to be active against the replication of poliovirus and herpes simplex-1 (HSV-1), with some of them also active against Sindbis virus.3,4) A methanol extract of Annona muricata and aqueous extract of Petunia myctaginiflora were shown to inhibit HSV-1 cytopathic effect in Vero cells, at a concentration of 1 mg/ml. 5)Methanol extracts of Indonesian plants were tested for cytotoxicity and antiviral activity (HSV-1 and poliovirus) in murine and human cell lines. Piper aduncum was found to be active on poliovirus, while Elytranthe tubaeflora and Melastoma malabathricum inhibited HSV-1. 6) Dengue virus was inhibited by an aqueous extract of Azadirachta indica when assayed in mice. 7)Stem bark of Stryphnodendron adstringens (MART.) COV-ILLE, Leguminosae, popularly known in our country as barbatimão, has been empirically used as wound healing, astringent, antimicrobial, antifungal, antidiarrheal and hypoglycemic agents.8) Similarly, Guazuma ulmifolia LAM., Sterculiaceae, popularly known as mutamba, is known to have medicinal properties, such as wound healing, antiulcerogenic, hypoglycemic and antimicrobial. 9) G. ulmifolia aqueous and methanol fractions were found to inhibit HSV-1 replication, respectively, by 16.8% and 4.5%, at a concentration of 100 mg/ml, in a study of various plants. Those showing antiviral activity in vitro were also tested in HSV-1 infected mice. Melaleuca leucadendron and Nephelium lappaceum reduced mortality and delayed the appearance of lesions. 10)Among plant antiviral compounds, anthraquinones found in Aloe barbadensis inhibited HSV-1, HSV-2, varicela-zoster, pseudorabies and influenza.11) Stevia rebaudiana polysaccharides inhibited adsorption of human rotavirus in MA-104 cells.12) Flavonoids present in Troillius chinensis flowers also inhibited parainfluenza in HEp-2 cells.13) Quassia africana extracts were tested for HSV-1, coxsackie B2, polio-1, measles, Semliki Forest virus and vesicular stomatitis virus, where simalikalactone D was found to be responsible for the antiviral effect.14) Anagyrine, oxymatrine, sophoranol, wogonin and oroxylin found in Sophora flavescens and Scutellaria b...
We report the effect of Stryphnodendron adstringens on the trypanosomatid Herpetomonas samuelpessoai. The parasites were grown at 28ºC in a chemically defined medium containing crude extract and fractions at concentrations from 100 to 5000 µg/ml obtained from S. adstringens. Concentrations of 500, 1000, 2500, and 5000 µg/ml both crude extract and semi-purified fraction progressively inhibited the protozoans' growth. At a concentration of 100 µg/ml, crude extract or a semi-purified (F3)
Um método de separação e quantificação por cromatografia líquida de alta eficiência (CLAE) em fase reversa foi desenvolvido usando água (0,05% de TFA):acetonitrila (0,05% de TFA) como fase móvel, em sistema gradiente para a análise dos flavan-3-óis presentes em extrato semipurificado das cascas de Stryphnodendron adstringens, Stryphnodendron polyphyllum e Stryphnodendron obovatum. A CLAE foi realizada com a fração acetato de etila (FAE) sendo submetida à extração em fase sólida (cartucho C18-E) com metanol:água (2:8), filtrada por membrana de porosidade 0,5 µm; a pré-coluna e coluna empregadas foram Phenomenex ® Gemini C-18 (5 µm), com esta última mantida a 30 ºC, com vazão de 0,8 mL/min e detecção a 210 nm. Utilizaram-se soluções dos padrões de ácido gálico e galocatequina para a obtenção da curva analítica. O método proposto foi validado de acordo com a resolução RE n° 899/2003 da ANVISA. A análise quantitativa da FAE das três espécies mostrou que existe similaridade no teor de galocatequina. S. adstringens possui ácido gálico em uma proporção superior a 60% em relação às outras duas espécies. A metodologia desenvolvida mostrou-se viável à aplicação em plantas ricas em taninos, como nos casos de S. adstringens, S. polyphyllum e S. obovatum. Unitermos: Stryphnodendron adstringens. Stryphnodendron polyphyllum. Stryphnodendron obovatum.Cromatografia líquida de alta eficiência. Taninos/determinação quantitativa. Análise quantitativa.A method of separation and quantification by reverse-phase high-performance liquid chromatography (HPLC) was developed, using water (0.05% TFA):acetonitrile (0.05% TFA) as the mobile phase in a gradient system. Flavan-3-ols present in a semipurified extract from the stem bark of Stryphnodendron adstringens, Stryphnodendron polyphyllum and Stryphnodendron obovatum were analyzed. The HPLC was performed with the ethyl-acetate fraction (EAF) using a solid-phase extraction on cartridges C18-E with methanol:water (2:8), filtered through a membrane of 0.5 μm pore size; the column was Phenomenex INTRODUÇÃOStryphnodendron adstringens (Mart.) Coville, Stryphnodendron polyphyllum Mart. e Stryphnodendron obovatum Benth. são plantas medicinais que crescem abundantemente nas regiões de cerrado do Brasil, e pertencem à família Leguminosae (Occhioni, 1990). Popularmente são conhecidas como "barbatimão", sendo extensamente empregadas pela população nativa no trata-
The ethnomedicinal plant Curatella americana L. (Dilleniaceae) is a common shrub in the Brazilian cerrado, in which crude extract showed antifungal activity in a preliminary study. In this work, the antifungal and cytotoxic properties of the crude extract, fractions, and isolated compounds from C. americana were evaluated against the standard yeast strains Candida albicans, C. tropicalis, and C. parapsilosis, clinical isolates, and fluconazole-resistant strains. The combinatory effects between subfractions and isolated compounds and effects on cell morphology, virulence factors, and exogenous ergosterol were also evaluated. The MIC obtained against the Candida species including fluconazole-resistant strain ranged from 15.3 to 31.3 µg/mL for crude extract, 3.9 to 15.6 µg/mL for ethyl acetate fraction, and 7.8 to 31.3 µg/mL for subfractions. The isolated compounds identified as 4′-O-methyl-catechin, epicatechin-3-O-gallate, and 4′-O-methyl-catechin-3-O-gallate showed lower antifungal activity than the crude extract and fractions (MIC ranging from 31.3 to 125.0 µg/mL). The addition of exogenous ergosterol to yeast culture did not interfere in the antifungal activity of the extract and its fractions. Synergistic antifungal activity was observed between subfractions and isolated compounds. The effects on virulence factors and the different mechanisms of action compared to fluconazole and nystatin suggest that this ethnomedicinal plant may be an effective alternative treatment for candidiasis.
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