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In this study we evaluated the in vitro effect of divaricatic acid against coupled worms of Schistosoma mansoni. The schistosomicidal effect was evaluated through the bioassay of motility and mortality, cellular viability of the worms and ultrastructural analysis through Scanning Electron Microscopy. To evaluate the cytotoxicity of divaricatic acid, a cell viability assay was performed with human peripheral blood mononuclear cells. Divaricatic acid proved effect against S. mansoni after 3 hours of exposure. At the end of 24 h the concentrations of 100 - 200 μM presented lethality to the worms. Motility changes were observed at sublethal concentrations. The IC50 obtained by the cell viability assay for S. mansoni was 100.6 μM (96.24 - 105.2 μM). Extensive damage to the worm's tegument was observed such as peeling, erosion, bubbles, edema, damage and loss of tubercles and spines, fissures and tissue ruptures. No cytotoxicity was observed in human peripheral blood mononuclear cells. This report provides data showing the schistosomicidal effect of divaricatic acid on S. mansoni, causing death, motile changes and ultrastructural damage to worms. In addition, divaricatic acid was shown to be non-toxic to human peripheral blood mononuclear cells at concentrations effective on S. mansoni.

Calotropis procera belongs to the Apocynaceae family and is found in the Northeast of Brazil. Several activities are attributed to this species, such as anti-inflammatory, antibacterial and anti-cancer activities. This research aimed to conduct a bioguided study of C. procera in order to isolate and identify triterpenes of the species and evaluate the cytotoxic activity of products of the plant species. The crude ethanolic extract (CEE) was obtained and partitioned. The hexanic phase was chromatographed giving the compound Cp-1, which was identified using spectroscopic techniques and thermal analysis. It was possible to identify Cp-1 as a triterpene called calotropenyl acetate, already reported in the literature. The cytotoxicity test was performed using the MTT technique and it was observed a good activity of CEE and hexanic phase against HL-60 and KS62 lines with an IC50 ranging between 26.8 ± 0.4 µg mL-1 and 47.0 ± 0.5 µg mL-1, besides no toxicity in normal lines, while Cp-1 showed no relevant activity against the tumor cells tested. The results indicated that the species contains in its chemical composition products with pharmacological interest, in addition to cytotoxic for leukemic cells, which can be further explored in complementary studies. Calotropis procera es una planta arbustiva perteneciente a la familia Apocynaceae, que se encuentra ampliamente en la región noreste de Brasil. A la especie se le atribuyen diversas actividades, como antiinflamatorias, antibacterianas y anticancerígenas, y el género Calotropis se caracteriza por presentar flavonoides, terpenos, taninos y compuestos fenólicos. Esta investigación tuvo como objetivo realizar un estudio bioguiado de C. procera con el fin de aislar e identificar triterpenos de la especie y evaluar la actividad citotóxica de productos de la especie vegetal. El extracto etanólico crudo (EEB) se obtuvo mediante maceración en etanol al 96% y se repartió con disolventes orgánicos, utilizando un gradiente de polaridad. La fase de hexano se cromatografió en columna con gel de sílice y se eluyó con disolventes orgánicos puros o en mezclas binarias dando lugar al compuesto codificado por Cp-1, que se identificó mediante técnicas espectroscópicas (RMN y IV) y análisis térmico. La evaluación de los datos del análisis espectroscópico y térmico permitió identificar al Cp-1 como un triterpeno denominado acetato de calotropenilo, ya reportado en la literatura. La prueba de citotoxicidad de productos obtenidos de la especie también se realizó mediante la técnica MTT. En la prueba de citotoxicidad, se observó una buena actividad de la EEB y de la fase hexano contra las cepas HL-60 y KS62 con un IC50 que varió de 26,8 ± 0,4 µg mL-1 a 47,0 ± 0,5 µg mL-1, además de ausencia de toxicidad en cepas normales, mientras que Cp-1 no mostró actividad relevante contra las células tumorales ensayadas. Los resultados indicaron que la especie contiene en su composición química productos con potencial fitoquímico para el aislamiento e identificación de compuestos por técnicas espectroscópicas y termoanalíticas, así como citotóxicos para células leucémicas, que pueden ser explorados con mayor profundidad en estudios complementarios. Calotropis procera é um vegetal arbustivo pertencente à família Apocynaceae, sendo amplamente encontrado na região Nordeste do Brasil. Diversas atividades são atribuídas a espécie, tais como as atividades anti-inflamatórias, antibacteriana e anticancerígena e o gênero Calotropis caracteriza-se por apresentar flavonoides, terpenos, taninos e compostos fenólicos. Esta pesquisa teve como objetivo realizar um estudo bioguiado de C. procera com o intuito de isolar e identificar triterpenos da espécie e avaliar a atividade citotóxica dos produtos da espécie vegetal. O extrato etanólico bruto (EEB) foi obtido por maceração em etanol a 96% e particionado com solventes orgânicos, utilizando um gradiente de polaridade. A fase hexânica foi cromatografada em coluna com gel de sílica e eluída com solventes orgânicos puros ou em misturas binárias dando origem ao composto codificado por Cp-1, que foi identificado utilizando técnicas espectroscópicas (RMN e IV) e de análise térmica. A avaliação dos dados espectroscópicos e de análise térmica permitiu identificar Cp-1 como sendo um triterpeno denominado acetato de calotropenil, já relatado na literatura. Também foi realizado o ensaio de citotoxicidade dos produtos obtidos da espécie utilizando a técnica de MTT. No ensaio de citotoxicidade observou-se uma boa atividade do EEB e da fase hexânica frente as linhagens HL-60 e KS62 com um IC50 variando entre 26.8 ± 0.4 µg mL-1 e 47.0 ± 0.5 µg mL-1, além de nenhuma toxicidade em linhagens normais, enquanto que Cp-1 não mostrou atividade relevante contra as células tumorais testadas. Os resultados indicaram que a espécie contém na sua composição química produtos com potencial fitoquímico para isolamento e identificação de compostos por técnicas espectroscópicas e termoanalíticas, além de citotóxico para células leucêmicas, que podem ser mais explorados em estudos complementares.

Schistosomiasis is one of the most significant neglected tropical diseases, affecting around 260 million people worldwide, and Praziquantel is currently the only available drug for the treatment of infected persons. Thus, the search for new schistosomicidal compounds is urgent. The objective of this study was to investigate of the schistosomicidal effect of barbatic acid, a lichen metabolite, on adult worms of Schistosoma mansoni. The in vitro schistosomicidal effect was evaluated through the assessment of motility and mortality, cellular viability of the worms and ultrastructural analysis through scanning electron microscopy. To evaluate the cytotoxicity of barbatic acid, a cell viability assay was performed with human peripheral blood mononuclear cells. Barbatic acid showed a schistosomicidal effect after 3 h of exposure. At the end of 24 h the concentrations of 50–200 μM presented lethality on the worms. Motility changes were observed at sublethal concentrations. The IC50 obtained by the cell viability assay for S. mansoni was 99.43 μM. Extensive damage to the worm's tegument was observed from 25 μM. No cytotoxicity was observed on human peripheral blood mononuclear cells. This report provides data showing the schistosomicidal effect of barbatic acid on S. mansoni, causing death, motility changes and ultrastructural damage to worms. In addition, barbatic acid was shown to be non-toxic to human peripheral blood mononuclear cells at concentrations that are effective against S. mansoni.

We report for the first time the in vitro effect of Potassium Salt, derived from Usnic Acid (PS-UA), isolated from the lichen Cladonia substellata Vanio, on couples of Schistosoma mansoni. As schistosomicide parameters, we evaluated mortality, motility, cell viability of the worms and tegument changes by scanning electron microscopy (SEM). Exposure to a concentration of 100 μM caused 75% mortality after 3 h. After 6 h, changes in motility in concentrations of 50 and 25 μM are evidenced. After 12 h and 24h, the concentrations of 50 and 100 μM caused 6.25% and 87.5% and 50% and 100% mortality, respectively. PS-UA reduced the cell viability of the worms by 27.36% and 52.82% at concentrations 50 and 100 μM, respectively. Through SEM we observed progressive dose-and time-dependent, alterations such as swelling, blisters, dorsoventral contraction, erosion until disintegration of the tubercles in the tegument of male and female. PS-UA did not alter the viability of human peripheral blood mononuclear cells and showed high selectivity indices (IC50 > 200 μM). Our results indicate that PS-UA represents a possible candidate for a new anthelmintic drug in the control of schistosomiasis.