RESUMO
Species of Piperaceae are known by biological properties, including antiparasitic such as leishmanicidal, antimalarial and in the treatment of schistosomiasis. The aim of this work was to evaluate the antileishmania activity, cytotoxic effect, and macrophage activation patterns of the methanol (MeOH), hexane (HEX), dichloromethane (DCM) and ethyl acetate (EtOAc) extract fractions from the leaves of Piper cabralanum C.DC. The MeOH, HEX and DCM fractions inhibited Leishmanina amazonensis promastigote-like forms growth with a half maximal inhibitory concentration (IC50) of 144.54, 59.92, and 64.87 µg/mL, respectively. The EtOAc fraction did not show any relevant activity. The half maximal cytotoxic concentration (CC50) for macrophages were determined as 370.70, 83.99, 113.68 and 607 µg/mL for the MeOH, HEX and DCM fractions, respectively. The macrophage infectivity was concentration-dependent, especially for HEX and DCM. MeOH, HEX and DCM fractions showed activity against L. amazonensis with low cytotoxicity to murine macrophages and lowering infectivity by the parasite. Our results provide support for in vivo studies related to a potential application of P. cabralanum extract and fractions as a promising natural resource in the treatment of leishmaniasis.
Assuntos
Antiprotozoários/química , Piper/química , Extratos Vegetais/química , Animais , Antiprotozoários/isolamento & purificação , Antiprotozoários/farmacologia , Sobrevivência Celular/efeitos dos fármacos , Células Cultivadas , Feminino , Hexanos/química , Leishmania/efeitos dos fármacos , Leishmania/crescimento & desenvolvimento , Estágios do Ciclo de Vida/efeitos dos fármacos , Extração Líquido-Líquido , Macrófagos/citologia , Macrófagos/efeitos dos fármacos , Macrófagos/metabolismo , Masculino , Cloreto de Metileno/química , Camundongos , Camundongos Endogâmicos BALB C , Óxido Nítrico/metabolismo , Fagocitose/efeitos dos fármacos , Piper/metabolismo , Extratos Vegetais/isolamento & purificação , Extratos Vegetais/farmacologia , Folhas de Planta/química , Folhas de Planta/metabolismoRESUMO
The oral squamous cell carcinoma (OSCC) is the eighth more common cancer in men. The development of new and more efficient drugs is needed. Plants of the genus Piper are popularly used in the treatment of many diseases. This study evaluated the antitumor effect of extract, fraction and isolated compounds from leaves of P. rivinoides in oral cancer. The isolated compounds (conocarpan, eupomatenoid-5 and eupomatenoid-6) were effective in inducing cell death in OSCC cell lines (SCC4, SCC9 and SCC25) compared to the standard chemotherapeutic agent carboplatin, and this effect was time-dependent. Conocarpan was more selective and stable than eupomatenoid-5 and eupomatenoid-6, resembling the stability of carboplatin. There was a significant presence of pyknotic nuclei and active caspase-3 expression under conocarpan treatment, suggesting cell death through apoptosis. In conclusion, conocarpan was the most effective compound against OSCC cells and might be considered for future cancer studies.