Farmacología de Terpenoides de Helianthus annuus L / Pharmacology of Terpenoids from Helianthus annuus L

Desde los albores de la humanidad, las plantas han sido fuente de interés porsus características nutricionales y medicinales. Por ello, se realizó un estudio farmacológicode terpenoides de Helianthus annuus L., optimizando un método deextracción, aislamiento y purificación de dichos metabolitos, para evaluar unaposible actividad farmacológica sobre modelos de inflamación. También se evaluóuna potencial actividad antiinflamatoria utilizando extractos (metanólico y acuoso)de la planta. Se aislaron tres diterpenos, dos kauranos y un traquilobano, mediantetécnicas cromatográficas, identificándose sus estructuras por RMN (1H, 13C) y evaluando su pureza por HPLC. Paralelamente se evaluó la variación estacional delácido grandiflorólico y de la mezcla de ácido kaurenoico y traquilobánico obtenida,en diferentes sumidades de la planta durante su desarrollo, con el fin de determinardónde y cuándo se produce una máxima acumulación del metabolito estudiado,para así obtener una extracción con un mayor rendimiento. Se encontrarondiferencias significativas útiles para el control de calidad de preparados a base deplantas medicinales que contengan algunos de estos metabolitos secundarios. Parael estudio de la actividad farmacológica de los terpenoides y de los extractos, setrabajó sobre dos modelos de inflamación (in vivo e in vitro). En el modelo in vivose evaluó la acción de los compuestos sobre el edema producido por aplicacióntópica de TPA en oreja de ratón, evaluando en paralelo la infiltración leucocitariaen términos de actividad mieloperoxidasa. En este modelo los ácidos kaurenoicoy traquilobánico demostraron actividad antiinflamatoria. En el modelo in vitro seutilizaron cultivos celulares de una línea de macrófagos, evaluando la actividad delos compuestos sobre la liberación de mediadores inflamatorios (NO, PGE2 y TNFa),y sobre la enzima COX, donde se observó que el ácido grandiflorólico y elextracto metanólico mostraron actividad inhibidora sobre la liberación de estosmediadores, además el ácido grandiflorólico mostró actividad inhibidora de laenzima COX. Sin embargo, no se descarta que en las actividades antiinflamatoriasde dichos compuestos estén implicados otros mediadores

Since the dawn of the humanity plants have been a source of interest becauseof their nutritional and medicinal characteristics. For that reason, a pharmacologicstudy of the terpenoids of Helianthus annuus L. was done, optimizing a method ofextraction, isolation and purification of these metabolites in order to evaluate apossible pharmacologic activity in inflammation models. Also, potentialantiinflammatory activity was evaluated using extracts (methanolic and watery) ofthe plant. Three diterpenes, two kauranes and a trachylobane were isolated, bymeans of chromatographic techniques; their structures were identified by RMN(1H, 13C) and their purity was evaluated by HPLC. Parallelly, the seasonal variationof grandiflorolic acid and kaurenoic and the trachylobanic acid mixture obtainedwas evaluated, in different above-ground parts from the plant during itsdevelopment, with the purpose of determining where and when the highestaccumulation of the studied metabolite occurs thus to obtain an extraction withthe greatest yield. Useful significant differences were found for the quality controlof preparations with medicinal plants that contain some of these secondarymetabolites. For the study of the pharmacologic activity of the terpenoids and theextracts, two models of inflammation (in vivo and in vitro) were worked on. In thein vivo model, the action of compounds was evaluated on edema produced by topical application of TPA in mouse ear, evaluating in parallel the leucocitaryinfiltration in terms of mieloperoxidase activity.In this model the kaurenoic and trachylobanic acids demonstratedantiinflammatory activity. In the in vitro model cellular cultures of a line ofmacrophages were used, the activity of compounds on the liberation ofinflammatory mediators (NO, PGE2 and TNF-a), and the COX enzyme wereevaluated, where it was observed that the grandiflorolic acid and the methanolicextract showed inhibiting activity on the liberation of these mediators. Also, thegrandiflorolic acid showed inhibiting activity on the COX enzyme. However, onedoes not rule out other mediators being implicated in the antiinflammatory activities of these said compounds

Comparação entre óleo de borragem e óleo de girassol quanto à eficácia no tratamento de mulheres com mastalgia cíclica / Comparison of borage oil and sunflower oil according to the efficacy for the treatment of women with cyclical mastalgia

A mastalgia cíclica constitui freqüente e exagerado processo fisiológico, recorrente na fase lútea do ciclo menstrual. Quando intensa, passa a comprometer a qualidade de vida da mulher, por interferir em suas atividades cotidianas. Com o objetivo de determinar, comparativamente, a efetividade e os possíveis efeitos dos óleos de borragem e de girassol, no tratamento da mastalgia cíclica moderada à intensa, foi realizado um estudo aleatório, duplo cego, tipo ensaio clínico, no período de fevereiro de 2001 a dezembro de 2002, envolvendo 111 mulheres. Mensalmente, a intensidade de dor mamária foi avaliada por escala visual analógica (EVA). As participantes foram subdivididas em dois grupos, segundo medicamento administrado, a saber, 56 em uso de cápsulas de óleo de borragem e 55 de óleo de girassol, ambos na dose de 1 cápsula ao dia, durante três meses. Ao final do tratamento, a evolução das intensidades de dor de cada paciente foi avaliada pelo Cardiff Breast Score, para determinação da responsividade terapêutica. A taxa de resposta terapêutica foi 71,4% e 76,4%, respectivamente para o óleo de borragem e de girassol, não havendo diferença, estatisticamente significativa, entre os medicamentos. A cefaléia, o estresse percebido e o edema mamário reduziram-se em ambos os grupos. Três mulheres do grupo do óleo de girassol apresentaram sangramento vaginal profuso. Concluiu-se que ambos os medicamentos foram eficazes no tratamento da mastalgia cíclica moderada à intensa. São necessários estudos adicionais para determinar a relação custo/benefício do óleo de girassol.

Cyclical mastalgia is a frequent condition and represents an exacerbation of the physiological process, recurring in the luteal phase of the menstrual cycle. When it is intense, it impairs a woman's quality of life, because if interferes on her daily activities. In order to make a comparative evaluation of the effectiveness and adverse effects of borage and sunflower oils in the treatment of moderate to severe cyclical mastalgia, a double-blind randomized study of clinical trial type was carried out between February 2001 and December 2002 involving 111 women. The intensity of breast pain was assessed on a monthly basis by means of the analogic visual scale. The participants were subdivided as follows into two groups according to the drug administered: 56 were given borage oil tablets and 55 sunflower oil, 1 tablet per day for both groups over a period of three months. At the end of the treatment, the evolution in the intensity of the pain of each patient was compared with the Cardiff Breast Score for an assessment of the responsiveness to treatment. The responsiveness rates were 71.4% and 76.4%, respectively for the borage and sunflower oil groups, no statistically significant differences being found. Although headache, perceived stress and mammary edema had reduzed in both groups; uterine bleeding occurred in three patients, as a serious side effect of sunflower oil. Further studies, however, are needed to determine the cost-benefit ratio of sunflower oil.