ABSTRACT Tithonia diversifolia (Hemsl.) A. Gray, Asteraceae, commonly known as Mexican sunflower, is a wide distributed invasive species encountered around the world. We proposed herein to establish the relationship between different abiotic environmental factors and the variation in the production of volatile compounds in T. diversifolia, during a period of one year. Samples of leaf and inflorescence volatile oils obtained from individuals located at two different regions of Brazil were analyzed by GC–MS and the data were submitted to chemometric analysis. Based on the main constituents, the analysis allowed us to classify the volatile oils into two chemotypes, according to their geographical origin. The influence of soil nutrients, mainly Ca and P, was also observed in the composition of the volatile oils. Climate also seems to affect the constituents of the volatile oils, mainly the contents of leaf sesquiterpenes of individuals growing in areas with higher average temperatures and solar radiation levels. We can therefore highlight that the appropriate multivariate statistical analysis allowed us to propose for the first time the existence of chemotypes for the volatile oils of T. diversifolia, as well as reporting the main abiotic environmental factors related to the accumulation of the discriminant compounds in these oils.

ABSTRACT Sesquiterpene lactones (SLs) are the active constituents of a variety of medicinal plants used in traditional medicine for the treatment of inflammatory diseases and other ailments. Objective In this study, we evaluated whether budlein A modulates the activation of innate and adaptive immune cells such as neutrophils and lymphocytes. Material and Methods Our research group has investigated several plant species and several compounds have been isolated, identified, and their medical potential evaluated. Budlein A is a SL isolated from the species Aldama buddlejiformis and A. robusta (Asteraceae) and shows anti-inflammatory and anti-nociceptive activities. Advances in understanding how plant-derived substances modulate the activation of innate and adaptive immune cells have led to the development of new therapies for human diseases. Results Budlein A inhibited MPO activity, IL-6, CXCL8, IL-10, and IL-12 production and induces neutrophil apoptosis. In contrast, budlein A inhibited lymphocyte proliferation and IL-2, IL-10, TGF-β, and IFN-γ production, but it did not lead to cell death. Conclusions Collectively, our results indicate that budlein A shows distinct immunomodulatory effects on immune cells.

Tanacetum parthenium (tanaceto) é uma planta medicinal comercializada no mundo todo para tratamento de enxaqueca. Seu efeito farmacológico é creditado principalmente à lactona sesquiterpênica partenolídeo e flavonóides. Até o momento não existem estudos sobre a padronização de pré-formulações ou o desenvolvimento de fitoterápicos com tanaceto. Logo, o objetivo deste trabalho foi obter comprimidos de revestimento entérico a partir de extrato seco e padronizado de tanaceto. Neste trabalho, o extrato seco do tanaceto obtido pelo método de spray drying foi avaliado quanto ao teor de partenolídeo, presença da santina, teor de flavonóides totais, solubilidade do partenolídeo, tamanho de partícula, ângulo de repouso, densidade, análise higroscópica e teor de umidade. A partir do extrato seco obtiveram-se comprimidos que foram revestidos em leito de jorro. Os comprimidos revestidos foram avaliados com relação ao peso médio, friabilidade, dureza e desintegração. O teor de flavonóides totais e de partenolídeo no extrato seco foram 1,31% e 0,76% (p/p), respectivamente. O extrato seco apresentou características farmacotécnicas satisfatórias permitindo a obtenção de comprimidos pelo método de compressão direta. As propriedades dos comprimidos revestidos estão de acordo com as especificações da literatura. Os procedimentos utilizados nesse trabalho podem ser utilizados para obter extrato seco e fitoterápicos de T. parthenium com alto padrão de qualidade.

Tanacetum parthenium (feverfew) is an herb that is commercialized worldwide as a therapeutic treatment for migraine. Its pharmacological effect is mainly due to the presence of the sesquiterpene lactone parthenolide as well as of flavonoids. So far, there are no studies on standardization of pre-formulations or phytomedicines containing this herb. The present study aimed at developing a pre-formulation using a standardized spray-dried extract of feverfew and further designing and standardizing enteric coated tablets. In this work, the spray-dried extract of feverfew was evaluated for its parthenolide, santin and total flavonoid content, parthenolide solubility, particle size, tapped density, hygroscopicity, angle of repose and moisture content. Tablets containing the spray-dried extract were tested for their average weight, friability, hardness, and disintegration time. The total flavonoid and parthenolide contents in the spray-dried extract were 1.31 % and 0.76% w/w, respectively. The spray-dried extract presented consistent pharmacotechnical properties and allowed its tableting by direct compression. Tablet properties were in accordance with the proposed specifications. The procedures described herein can be used to prepare and evaluate pre-formulations of feverfew with adequate properties for the development of a high-quality phytomedicine.

Neste trabalho, é apresentada uma proposta para o controle de qualidade físico e químico do pó de T. parthenium (tanaceto) e do seu extrato hidroalcoólico obtido por percolação. A lactona sesquiterpênica partenolídeo, o principal componente ativo da espécie, foi quantificada por CLAE e seu teor foi de 0,49% no pó e 1,06% no extrato. O teor de flavonóides totais foi determinado por espectroscopia no UV e foi de 0,54% no pó e 1,05% no extrato hidroalcoólico. A santina, principal flavonóide da espécie, foi isolada e posteriormente identificada no extrato por CLAE. Uma vez que o partenolídeo também pode ser encontrado em outras espécies de Asteraceae, a análise da santina é importante para certificar a autenticidade do material vegetal. Os resultados obtidos neste trabalho confirmam a autenticidade do material e a eficiência do processo extrativo.

In this study, we present a proposal for the physical and chemical quality control of the powder of the species T. parthenium (feverfew) and its hydroalcoholic extract obtained by percolation. The sesquiterpene lactone parthenolide, the main active compound of this plant, was quantified by HPLC and its content was found to be 0.49% in the powder and 1.06% in the extract. The total content of flavonoids, determined by UV spectroscopy, was found to be 0.54% in the powder and 1.05% in the hydroalcoholic extract. Santin, the main flavonoid of this species, was isolated and further identified in the extract by HPLC. Since parthenolide can also be found in other Asteraceae species, the analysis of santin is important to certify the authenticity of the plant material. The results confirmed the authenticity of the plant material and the efficiency of the extraction procedure.

The development of new tools for chemoinformatics, allied to the use of different algorithms and computer programmes for structure elucidation of organic compounds, is growing fast worldwide. Massive efforts in research and development are currently being pursued both by academia and the so-called chemistry software development companies. The demystification of this environment provoked by the availability of software packages and a vast array of publications exert a positive impact on chemistry. In this work, an overview concerning the more classical approaches as well as new strategies on computer-based tools for structure elucidation of organic compounds is presented. Historical background is also taken into account since these techniques began to develop around four decades ago. Attention will be paid to companies which develop, distribute or commercialize software as well as web-based and open access tools which are currently available to chemists.

Neste trabalho 12 flavonóides foram detectados nos tricomas glandulares de duas espécies de Chromolaena através do emprego da técnica de microamostragem de tricomas glandulares, associada à análise por CLAE. Esta é a primeira vez que se relata o acúmulo de flavonóides em tricomas glandulares no gênero. Com base nos resultados obtidos, podemos sugerir que esta técnica pode ser uma ferramenta útil na busca de substâncias com propriedades medicinais e em estudos quimiotaxonômicos de Eupatorieae.

In this work, twelve flavonoids were detected in glandular trichomes of two species of Chromolaena through the glandular microsampling technique and HPLC-UV-DAD analysis. This is the first time that the accumulation of flavonoids in glandular trichomes of the genus Chromolaena is reported. Based on the results, we suggest that this technique can be an useful tool in the search of new compounds with medicinal properties as well as in chemotaxonomic studies of Eupatorieae.