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Abstract Trichilia catigua A. Juss., Meliaceae, known as "catuaba" in Brazil, has been popularly used as a tonic for fatigue, impotence and memory deficits. Previously, we have demonstrated that T. catigua ethyl-acetate fraction exerted antidepressive-like effects in mice. Affective-like symptoms are also well recognized outcome of cerebral ischemia in clinical and preclinical settings. Therefore, here we evaluated the effects of ethyl-acetate fraction on the emotional outcomes and its relation with hippocampal neurogenesis in ischemic mice. Male Swiss mice were subject to the bilateral common carotid occlusion during 20 min. The animals received ethyl-acetate fraction (400 mg/kg, orally) 30 min before and once per day during 7 days after reperfusion. Emotional outcomes were assessed using the open field test, elevated zero maze, and the tail suspension test. After the behavioral testing, the animals were sacrificed and their brains were processed to immunohistochemistry and Nissl staining. Ischemic mice exhibited anxiogenic-like behaviors in the elevated zero maze, hippocampal neurodegeneration and decreased hippocampal neurogenesis. The anxiogenic-like effect was counteracted by ethyl-acetate fraction administration. Furthermore, ethyl-acetate fraction restored the number of newborn neurons in the dentate gyrus of hippocampus of ischemic mice. In conclusion, T. catigua ethyl-acetate fraction promoted functional recovery and restored hippocampal neurogenesis in ischemic mice.
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Abstract Trichilia catigua A. Juss., Meliaceae, known as catuaba in Brazil, is traditionally used for the treatment of stress, sexual impotence and memory deficits. To our knowledge, there is no analytical method described in literature for simultaneous quantification of catuaba extract marker substances in biological matrices. The aim of this study was to develop and validate a bioanalytical method by LC-MS/MS to quantify epicatechin and procyanidin B2 in rat plasma after administration of standardized extract of T. catigua. Chromatographic separation was achieved with a C18 column, methanol and 0.1% aqueous formic acid at a flow rate of 0.25 ml/min. Detection was performed using electrospray ionization in negative mode. The lower limits of quantification were 5 ng/ml and 12.5 ng/ml for procyanidin B2 and epicatechin, respectively. Intra- and inter-day assays variability were less than 15%. The extraction recovery was 104% for epicatechin and 74% for procyanidin B2 using one-step liquid-liquid extraction with ethyl acetate. Epicatechin and PB2 were detected in plasma up to 300 min after oral administration of 400 mg/kg of standardized extract of T. catigua in rats. This rapid and sensitive method for the analysis of the epicatechin and procyanidin B2 in rat plasma can be applied to pharmacokinetic studies.
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ABSTRACT Medicinal plants play an important role in human health care. It is estimated that about 25–30% of all drugs are evaluated as therapeutic agents derived from natural products. Research in the pharmaceutical industry has demonstrated that for complex diseases, natural products still represent a valuable source for the production of new chemical compounds, since they possess privileged structures. Among Brazilian biodiversity, "catuaba" is popularly used as a tonic to treat fatigue, stress, impotence, memory deficits, and digestive disorders. Studies show antibacterial, trypanocidal, antioxidant, antiarrhythmic, antidepressant, improvement of memory, anti-inflammatory and antinociceptive activities, as well as phytocosmetic activity in cellulite treatment and in anti-ageing. The Brazilian plants known and used as catuaba are represented by more than twenty different species; however, the plant most commonly found in Brazil as "catuaba" is the species Trichilia catigua A. Juss., Meliaceae. Thus, the aim of this paper is to present a review of T. catigua, with emphasis on biological activities, chemical and analytical development and formulations in order to provide a broader and deeper insight, seeking a herbal medicine and/or phytocosmetic as well as future prospects for commercial exploitation and directions for future studies.
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AbstractGuaraná (Paullinia cupana Kunth, Sapindaceae) is well known for its dietary and pharmaceutical potential, and the semipurified extract of guaraná shows antidepressant and panicolytic effects. However, the low solubility, bioavailability and stability of the semipurified extract limit its use as a component of pharmaceutical agents. Delivery of the semipurified extract in a microparticle form could help to optimize its stability. In this study, microparticles containing semipurified extract of guaraná were obtained by the spray-drying technique, using a combination of maltodextrin and gum arabic. The raw materials and microparticles produced were characterized by particle size analysis, differential scanning calorimetry, thermogravimetric analysis, and scanning electron microscopy. The drug content and antioxidant capacity were also evaluated. In vitrodissolution tests using flow cell dissolution apparatus, were carried out to investigate the influence of formulation parameters on the release of semipurified extract of guaraná from the microparticles. The spray-drying technique and the processing conditions selected gave satisfactory encapsulation efficiency (80–110%) and product yield (55–60%). The mean diameter of microparticles was around 4.5 µm. The DPPH radical scavenging capacity demonstrated that microparticles can protect the semipurified extract of guaraná from the effect of high temperatures during the process maintained the antioxidant capacity. Differential scanning calorimetry results indicated an interaction between semipurified extract of guaraná and gum arabic: maltodextrin in the microparticles, and thermogravimetric analysis indicate that the profile curves of the microparticles are similar to the adjuvants used in drying, probably due to the higher proportion of adjuvants compared to semipurified extract of guaraná. In vitro dissolution tests demonstrate that all formulations complete dissolution within 60 min. Microencapsulation improved the technological characteristics of the powders and preserved the antioxidant properties. The study demonstrated the feasibility of producing these microparticles for a one-step process using spray drying. The composition of each formulation influenced the physical and chemical characteristics. This spray-drying technique can be used as an efficient and economical approach to produce semipurified extract of guaraná microparticles.
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The flowers of Tagetes patula L., Asteraceae, commonly known as French marigold, are used in folk medicine as an antiseptic, diuretic, blood purifier and insect repellent. This study was conducted to optimize the extraction process through the biomonitoring of flavonoids, using a statistical mixture simplex-centroid design, to evaluate the effect of the solvents water, ethanol and acetone, as well as mixtures of these solvents, assessed by the total flavonoid content. The extracts were tested for dry residue, radical scavenging activity, chromatographic profile, and larvicidal activity. The acetone extract had the highest total flavonoid content, 25.13 ± 1.02% (4.07%); and the best radical scavenging activity, with IC50 of 15.74 μg/ml ± 1.09 (6.92%), but with lower dry residue, 6.62 ± 1.33% (20.10%). The water extracts showed higher levels of dry residue, but lower total flavonoid content and radical scavenging activity than the acetone extract. The positive correlation between the total flavonoid content and radical scavenging activity of the extracts showed that flavonoids contribute significantly to the antioxidant capacity. The statistical mixture design allowed us to optimize the extraction of flavonoids from flowers of T. patula, with acetone as the best extraction solvent. Preliminary studies on the biological activity of the optimized extracts demonstrated a larvicidal effect of the acetone extract on Aedes aegypti mosquitoes.
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This study evaluated the technological feasibility of producing a semipurified extract of guaraná (Paullinia cupana Kunth, Sapindaceae) in tablet form, using a direct-compression process. Maltodextrin and gum arabic were used to produce the extract microparticles, in order to protect the microparticles against such factors as temperature, oxidation, and humidity. Using pharmacopoeial methodologies, technological and physicochemistry tests (determination of residual moisture, of bulk and tapped density, Hausner ratio, compressibility and compactibility index, appearance, mean weight, hardness, friability, disintegration time, determination of EPA amount in tablets and in vitro release profile) were conducted. The formulation containing 200 mg of microparticles, 170 mg microcrystalline cellulose, and 10 mg lactose gave the best results in terms of hardness (116 N), friabilility (0.28%), mean weight (0.3821 g), and disintegration time (25 min) for a tablet designed for oral administration. The results met pharmacopoeial specifications, and the tablets are suitable for oral administration.
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A própolis é uma resina coletada das árvores pelas abelhas Apis mellifera L., que contém inúmeras substâncias, dentre elas os flavonóides. Devido a grande variedade de sua composição química, apresenta várias ações farmacológicas, destacando-se as ações antiinflamatória, cicatrizante, antitumoral e antimicrobiana, principalmente a antifúngica. Esta ação foi testada frente a leveduras isoladas de onicomicoses, que são infecções de difícil e longo tratamento que causam efeitos indesejáveis ao paciente. A própolis surge como uma eficiente opção de tratamento, pois é de baixa toxicidade e pode ser de uso tópico. Este trabalho objetivou avaliar a otimização do processo extrativo da própolis através de parâmetros físico-químicos e demonstração da atividade antifúngica.
Propolis is a resin collected by the bees Apis mellifera L., which contains several substances including the flavonoids. Due to a diversified chemical composition propolis presents some pharmacological actions, being distinguished the anti-inflammatory, healing, antitumoral and antimicrobial properties and, in particular, its antifungal action. This action has been tested against yeasts obtained from onychomycosis, which are infections of difficult and long treatment and they can manifest intolerable effects on the patient. The propolis appears as an efficient therapy option, as it has low toxicity and should be of dermal use. The aim of the present study was to evaluate the optimization of the propolis extractive process through physiochemical parameters and antifungal activity demonstration.
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Abejas , Antifúngicos/farmacología , Onicomicosis , Optimización de Procesos/métodos , PrópolisRESUMEN
The aim of this study was to determine the in vitro activity of propolis extract against 67 yeasts isolated from onychomycosis in patients attending at the Teaching and Research Laboratory of Clinical Analysis of the State University of Maringá. The method used was an adaptation made from the protocol approved by the National Committee for Clinical Laboratory Standards. The yeasts tested were: Candida parapsilosis 35 percent, C. tropicalis 23 percent, C. albicans 13 percent, and other species 29 percent. The propolis extract showed excellent performance regarding its antifungal activity: the concentration capable of inhibiting the all of the yeasts was 5 Î 10-2 mg/ml of flavonoids and 2 Î 10-2 mg/ml of flavonoids stimulated their cellular death. Trichosporon sp. were the most sensitive species, showing MIC50 and MIC90 of 1.25 Î 10-2 mg/ml of flavonoids, and C. tropicalis was the most resistant, with CFM50 of 5 Î 10-2 mg/ml of flavonoids and MFC90 of 10 Î 10-2 mg/ml. In view of the fact that propolis is a natural, low cost, non-toxic product with proven antifungal activity, it should be considered as another option in the onychomycosis treatment.