ABSTRACT
Chagas disease, a worldwide public health concern, is a chronic infection caused by Trypanosoma cruzi. Considering T. cruzi chronic persistence correlates with CD4+ and CD8+ T cell dysfunction and the safety and efficacy profiles of Benznidazol and Nifurtimox, the two drugs currently used for its etiological treatment, are far from ideal, the search of new trypanocidal treatment options is a highly relevant issue. Therefore, the objective of this work was to evaluate the trypanocidal effect and cytokine production induction of three extracts (hexane, dichloromethane and hydroalcoholic) obtained from Clethra fimbriata, a plant traditionally used as a febrifuge in Colombia. Additionally, the extracts' major components with the highest trypanocidal activity were determined. It was evidenced C. fimbriata hexane extract exhibited the highest activity capable of inhibiting the three parasite developmental stages with an IC50/EC50 of 153.9 ± 29.5 (epimastigotes), 39.3 ± 7.2 (trypomastigotes), and 45.6 ± 10.5 (amastigotes) µg/mL, presenting a low cytotoxicity in VERO cells with a selectivity index ranging from 6.49 to 25.4. Moreover, this extract induced trypomastigote apoptotic death and inhibited parasite cell infection. The extract also induced IFN-γ and TNF production in CD4+ and CD8+ T cells, as well as de novo production of the cytotoxic molecules granzyme B and perforin in CD8+ T cells from healthy donors. Fatty acids and terpenes represented C. fimbriata key compounds. Thus, the trypanocidal activity and cytokine production induction of the hexane extract may be associated with terpene presence, particularly, triterpenes.
ABSTRACT
Introduction: Sida cordifolia L. (Malvaceae) is a weed about which not much is known in Colombia. This plant is used in folk medicine to treat oral mucosa, blennorrhea, asthma and bronchitis.In Brazil it finds application as an anti-inflammatory,while in Colombia its "baba" is used for treating hair loss, constipation and internal fever, among other ailments. Objectives: to quantify the saponoside content and evaluate its antioxidant and antifungal functionality. Methods: we prepared organic, aqueous and hydroalcoholic extracts from the aerial section of the plant. The saponoside material was quantified by the DNS and p-anisaldehyde methods. The most concentrated extracts were selected for antioxidant and antifungal assays. Results: it was found that Sida cordifolia, collected in Ibague-Colombia, is a good source of saponins with diverse chemical structures, mainly of steroidal nature, some of which may be hecogenin, diosgenin or a homologue. Conclusions: these factors may contribute, at least in part, to the antioxidant and antifungal functionality of Sida cordifolia L., but this capacity may be modified if these saponins act independently or together with some other metabolites of the plant such as tannins, flavonoids steroids, and alkaloids among others.
Introducción: Sida cordifolia L. (Malvaceae) es una hierba de la cual se tiene un conocimiento limitado en Colombia. Se utiliza en la medicina popular para el tratamiento de la mucosa oral, la blenorragia, el asma y la bronquitis. En Brasil encuentra aplicación como antiinflamatorio, mientras que en Colombia su "baba" se utiliza para tratar la pérdida del cabello, el estreñimiento, y la fiebre interna, entre otros padecimientos. Objetivos: cuantificar el contenido saponósido y evaluar sus propiedades antioxidantes y funcionalidad antifúngica. Métodos: se prepararon extractos orgánicos, acuosos e hidroalcohólicos de la parte aérea de la planta. El material de saponósidos se cuantificó por los métodos del DNS (dinitrosalicylic acid reagent) y de p-anisaldehído. Los extractos más concentrados se seleccionaron para los ensayos antioxidante y antifúngico. Resultados: estos mostraron que Sida cordifolia, colectada en Ibague-Colombia, es una buena fuente de saponinas con diversas estructuras químicas, principalmente de naturaleza esteroidal, algunas de las cuales pueden ser hecogenina, diosgenina o un homólogo. Conclusiones: estos factores pueden contribuir, al menos en parte, en la funcionalidad antioxidante y antifúngica de Sida cordifolia L., pero su capacidad se puede modificar si esas saponinas actúan de forma independiente o en conjunto con otros metabolitos de la planta, como taninos, esteroides flavonoides, alcaloides, entre otros.
