The flavonoid content and antiproliferative, hypoglycaemic, anti-inflammatory and free radical scavenging activities of Annona dioica St. Hill.

BACKGROUND: Annona dioica St. Hill (Annonacaeae) is a Brazilian plant used in folk medicine for the treatment of several types of rheumatisms and diarrhoea. The focus of this work was to evaluate the in vitro antiproliferative and antioxidant activity and the in vivo hypoglycaemic and anti-inflammatory activity of A. dioica and identify the principal constituents of this plant. METHODS: The crude methanol extract (EAD) and hexane (HF), chloroform (CF), ethyl acetate (EAF) and hydromethanol fractions (HMF) were evaluated for free radical scavenging activity using the DPPH assay. The EAD and EAF were assayed for hypoglycaemic activity in rats. The EAD was tested in an antiproliferation assay and for anti-inflammatory effects in paw oedema, in addition to myeloperoxidase activity induced by carrageenan (Cg) in mice. The EAF was assayed using chromatographic methods. RESULTS: The fractionation of the EAF through chromatographic methods identified derivatives of the flavonoids quercetin and kaempferol. Among all the tested fractions, the ethyl acetate and hydromethanol fractions were the most potent, exhibiting an IC50 of 8.53 and 10.57 µg/mL, respectively, which is comparable to that of the commercial antioxidant butylated hydroxytoluene (BHT). The oral administration of the EAD (100 mg/kg) and EAF (15 mg/kg) inhibited the increase of glucose levels, resulting in a hypoglycaemic effect. The EAD (30 to 300 mg/kg) exhibited an anti-oedematogenic effect in Cg-induced paw oedema in a time- and dose-dependent manner. The results showed a reduction of MPO activity by A. dioica 6 h after the induction of paw oedema at all doses tested with maximal inhibition at 300 mg/kg. CONCLUSIONS: Our results reveal for the first time that compounds contained in the A. dioica leaves exert anti-inflammatory, hypoglycaemic, antiproliferative, and antioxidant effects. The antioxidant activity may be associated with the presence of flavonoids.

Levantamento de fitoterápicos manipulados em farmácias magistrais de Dourados-MS / Survey of herbal compounding pharmacies handled in Dourados-MS

Este trabalho teve como objetivo realizar o levantamento dos fitoterápicos manipulados em duas farmácias magistrais de Dourados, enfatizando a constituição das fórmulas (matéria-prima e forma farmacêutica), a possível indicação terapêutica, a origem das drogas vegetais utilizadas na manipulação dos fitocomplexos e a confirmação da existência ou não de artigos científicos que comprovem a utilização das cinco matérias-primas mais manipuladas nas farmácias. Para isso, foram analisados os cadastros ou fichas de pesagem, após a autorização das farmacêuticas responsáveis, do período correspondente a 21 de dezembro de 2006 a 21 de março de 2007. Concluiu-se que: 1. As matérias-primas mais utilizadas, nas duas farmácias, foram Ginkgo biloba e Hypericum perforatum, coincidentemente, com as maiores demandas e as mesmas concentrações. 2. A credibilidade nos fitoterápicos, por parte da população e dos médicos prescritores, pode ser considerada como baixa, uma vez que apenas 4,1 por cento das fórmulas manipuladas nas duas farmácias magistrais em estudo corresponderam aos fitoterápicos. 3. Em relação às formas farmacêuticas, houve prevalência de cápsulas gelatinosas, provavelmente, porque a indicação terapêutica das fórmulas tenha sido para uso interno. 4. Dentre as cinco plantas medicinais mais manipuladas, apenas Hoodia gordonii não apresentou comprovação científica e 5. As plantas medicinais mais utilizadas na manipulação dos fitocomplexos estiveram relacionadas com a perda de peso.

The aim of this work was to carry out the survey of the phytotherapics manipulated in two magistral drugstores from Dourados, emphasizing the constitution of formulas (raw materials and pharmaceutical form), the possible therapeutic indication, the origin of the vegetal drugs utilized in manipulation of phytocomplexes and the confirmation of the existence or not of scientific articles demonstrating the use of the five most manipulated raw materials in drugstores. Thus, the registration or files weighing were analyzed, with the approval of responsible pharmacists, from the period of 21st December 2006 to 21st March 2007. It was concluded that: 1. Raw materials most utilized in both drugstores were Ginkgo biloba and Hypericum perforatum, coincidentally both showed the highest demands and the same concentrations. 2. The credibility of the phytotherapics, by the public and prescribers, can be considered low, since just 4.1 percent of the manipulated formulas from both magistral drugstores studied corresponded to the phytotherapics. 3. In relation to the pharmaceutical formulas, there was a prevalence of gelatin capsules, probably because the therapeutic indication of formulas had been designed for internal use. 4. Among the five most manipulated medicinal plants, only Hoodia gordonii did not show scientific proof and 5. The medicinal plants most utilized in the manipulation of phytocomplexes were related to weight loss.