Antileishmanial activity of Melampodium divaricatum and Casearia sylvestris essential oils on Leishmania amazonensis.

Leishmaniasis is a disease that affects millions of people and it is an important public health problem. The drugs currently used for the treatment of leishmaniasis present undesirable side effects and low efficacy. In this study, we evaluated the in vitro activity of Melampodium divaricatum (MD-EO) and Casearia sylvestris (CS-EO) essential oils (EO) against promastigote and amastigote forms of Leishmania amazonensis. Sesquiterpenes E-caryophyllene (56.0%), germacrene D (12.7%) and bicyclogermacrene (9.2%) were identified as the main components of MD-EO, whereas E-caryophyllene (22.2%), germacrene D (19.6%) and bicyclogermacrene (12.2%) were the main constituents of CS-EO. CS-EO and E-caryophyllene were active against promastigote forms of L. amazonensis (IC50 24.2, 29.8 and 49.9 µg/mL, respectively). However, MD-EO, CS-EO and E-caryophyllene were more active against amastigote forms, with IC50 values of 10.7, 14.0, and 10.7 µg/mL, respectively. E-caryophyllene presented lower cytotoxicity against macrophages J774-A1 (CC50 of 62.1 µg/mL) than the EO. The EOs and E-caryophyllene should be further studied for the development of new antileishmanial drugs.

Sucupira as a Potential Plant for Arthritis Treatment and Other Diseases.

Trees of the genus Pterodon, commonly known as "sucupira-branca" or "faveira," are native to central Brazil. The Pterodon fruits are traditionally used in ethnomedicine as an infusion, in small doses, and at regular time intervals as an antirheumatic, anti-inflammatory, tonic, and depurative agent. The various compounds present in the Pterodon class are, generally, water-insoluble and derived from the fusion of high-molecular weight pentacarbonate units. Scientific research has shown that the major compounds isolated from Pterodon species are linear and/or tetracyclic diterpenes with vouacapane skeletons that partly underlie the pharmacological activities of the fruit-derived oil. Material from Pterodon species has several biological properties, such as analgesic, anti-inflammatory, and anticancer effects. Therefore, recent studies have sought to microencapsulate these extracts to protect them from potential chemical degradation and improve their water solubility, ensuring greater stability and quality of the end products. This review presents a succinct overview of the available scientific evidence of the biological activity and toxicity of Pterodon species in addition to other important aspects, including phytochemical and technological features.

Inhibitory Effect of the Hexane Fraction of the Ethanolic Extract of the Fruits of Pterodon pubescens Benth in Acute and Chronic Inflammation.

Fruits of Pterodon pubescens Benth have been used traditionally for the treatment of rheumatism, sore throat, and respiratory disorders, and also as anti-inflammatory, analgesic, depurative, tonic, and hypoglycemic agent. The study was aimed at evaluating the anti-inflammatory activity of the hexane fraction of an ethanolic extract of P. pubescens fruits. The oil from P. pubescens fruits was extracted with ethanol and partitioned with hexane. The anti-inflammatory activity was measured with increasing doses of the hexane fraction (FHPp) by using a carrageenan-induced rat model of pleurisy and a rat model of complete Freund's adjuvant-induced arthritis by using an FHPp dose of 250 mg/kg for 21 days. Treatment with an FHPp resulted in anti-inflammatory activity in both models. The results of biochemical, hematological, and histological analyses indicated a significant decrease in glucose, cholesterol, and triglycerides levels (18.32%, 34.20%, and 41.70%, resp.) and reduction in the numbers of total leukocytes and mononuclear cells. The FHPp dose of 1000 mg/kg induced no changes in behavioral parameters, and no animal died. The results of this study extend the findings of previous reports that have shown that administration of extracts and fractions obtained from species of the genus Pterodon exhibits anti-inflammatory activity and lacks toxicity.

Preparation and characterization of microcapsules of Pterodon pubescens Benth. by using natural polymers

An oleaginous fraction obtained from an alcohol extract of the fruit of Pterodon pubescens Benth. (FHPp) was microencapsulated in polymeric systems. These systems were developed using a complex coacervation method and consisted of alginate/medium-molecular-weight chitosan (F1-MC), alginate/chitosan with greater than 75% deacetylation (F2-MC), and alginate/low-molecular-weight chitosan (F3-MC). These developed systems have the potential to both mask the taste of the extract, and to protect its constituents against possible chemical degradation. The influence of the formulation parameters and process were determined by chemical profiling and measurement of the microencapsulation efficiency of the oleaginous fraction, and by assessment of microcapsule morphology. The obtained formulations were slightly yellow, odorless, and had a pleasant taste. The average diameters of the microcapsules were 0.4679 µm (F2-MC), 0.5885 µm (F3-MC), and 0.9033 µm (F1-MC). The best formulation was F3-MC, with FHPp microencapsulation efficiency of 61.01 ± 2.00% and an in vitro release profile of 75.88 ± 0.45%; the content of vouacapans 3-4 was 99.49 ± 2.80%. The best model to describe the release kinetics for F1-MC and F3-MC was that proposed by Higuchi; however, F2-MC release displayed first-order kinetics; the release mechanism was of the supercase II type for all formulations.

Uma fração oleaginosa obtida do extrato etanólico de frutos de Pterodon pubescens Benth (FHPp) foi microencapsulada em um sistema polimérico. Estes sistemas foram desenvolvidos utilizando o método de coacervação complexa, constituído de alginato/quitosana massa molecular média (F1-MC), alginato/quitosana com desacetilação superior a 75% (F2-MC) e alginato/quitosana de massa molecular baixa (F3-MC). Estes sistemas desenvolvidos têm o potencial tanto de mascarar o sabor do extrato, quanto de protegê-lo de possível degradação química. A influência dos parâmetros de formulação e processo foram determinadas por caracterização química, determinação da eficiência de microencapsulação da fração oleaginosa e por avaliação morfológica da microcápsula. As formulações mostraram-se ligeiramente amareladas, inodoras e com sabor agradável. Os diâmetros médios das microcápsulas foram de 0,4679 µm (F2-MC), 0,5885 µm (F3-MC) e 0,9033 µm (F1-MC). A melhor formulação foi F3-MC, considerando-se que apresentou eficiência de encapsulação de 61,01 ± 2,00%, e perfil de liberação in vitro de 75,88 ± 0,45%; o conteúdo dos vouacapanos 3-4 foi 99,49 ± 2,80%. O melhor modelo para descrever a cinética de liberação foi o modelo proposto por Higuchi para F1-MC e F3-MC, entretanto, para F2-MC foi o modelo de primeira ordem, e o mecanismo de liberação foi do tipo super caso II para todas as formulações.

Spectrophotometric determination of tannins and caffeine in preparations from Paullinia cupana var. sorbilis

The present work was designed to quantify the caffeine and total polyphenols in the extractive solution and the granulated form from the seeds of Paullinia cupana var. sorbilis, by the spectrophotometric method. The method showed linearity for the caffeine and polyphenols in the range of 5-25 µg/ml and 2.4-5.6 µg/ml respectively. The solutions of the semipurified fraction (EPA) and granulated form (GRA) showed linear responses in the range of 0.288-0.672 and 0.4-1.2 µg/ml, respectively. The precision and accuracy were determined for the EPA solution at a concentration of 100 µg/ml. The spectrophotometric method performed well in quantifying the caffeine and total polyphenols.

A qualidade de preparações fitofarmacêuticas deve ser avaliada de acordo com os requisitos estabelecidos pela Agência Nacional de Vigilancia Sanitária na RDC n. 48 (ANVISA-BRASIL). As análises para avaliar a integridade dos produtos da droga vegetal incluem a quantificação de substâncias marcadoras através de métodos validados. O trabalho objetivou quantificar cafeína e polifenóis totais em soluções extrativas e no granulado obtidos das sementes de P. cupana var. sorbilis através de método espectrofotométrico. O método apresentou linearidade para a cafeína e polifenóis no intervalo de 5-25 µg/ml e 2,4-5,6 µg/ml, respectivamente. Soluções da fração semipurificada (EPA) e do granulado (GRA) mostraram resposta linear no intervalo de 0,288-0,672 µg/ml e 0,4-1,2 µg/ml respectivamente. A precisão e exatidão foram determinadas para a solução de EPA na concentração de 100 µg/ml. O método espectrofotométrico obteve um bom desempenho na quantificação de cafeína e polifenóis totais, uma vez que a presença de interferentes foi previamente avaliada.

Avaliação farmacológica de um extrato de Passiflora edulis variedade flavicarpa / Pharmacological evaluation of a Passiflora edulis variety flavicarpa extract

A produção de fitoterápicos requer critérios técnicos de qualidade e avaliação de seus efeitos. Este estudo visa à avaliação de efeitos comportamentais de um extrato padronizado de Passiflora edulis. O extrato foi obtido de folhas por percolação. Em sua padronização determinou-se: a) teor de flavonóides totais (droga e extrato), b) resíduo seco, c) pH, d) densidade e e) teor alcoólico. Os efeitos farmacológicos da P. edulis foram avaliados sobre os seguintes parâmetros: 1) atividade exploratória, 2) tempo de sono induzido pelo pentobarbital e 3) catatonia. O extrato padronizado apresentou as seguintes propriedades: a) 3,83± 0,10g por cento (n=3) e 9,50± 0,27g por cento (n=3), respectivamente; b) 6,7± 0,30 por cento (n=6); c) 5,5 (n=3), d) 0,94± 0,01 g/mL (n=3); e) 50 °GL (n=3). O extrato de P. edullis exerceu efeitos dose-dependentes sobre os vários parâmetros analisados: 1) reduziu as atividades de comportamento exploratório (deambulação e autolimpeza: P<0,01) e, qualitativamente, diminuiu os comportamentos de levantamento ("rearing") e salto ("jumping"); 2) aumentou o tempo de hipnose induzida pelo pentobarbital (P<0,01); e 3) induziu catatonia (P<0,0001 extrato 80 mg/kg vs veículo). Através das investigações farmacológicas realizadas, o extrato de P. edulis demonstrou ser depressor do sistema nervoso central, sugerindo uma ação calmante tipo tranqüilizante maior.