ABSTRACT Pentavalent antimonials and amphotericin B remain as the main drugs to treat human leishmaniasis. However, the high toxicity and variable efficacy of treatment have stimulated the search for novel drug candidates. Naturally occurring alkaloids have a long history of antileishmanial activity. Here, we investigate the effects of the β-carboline-1-propionic acid alkaloid isolated from Quassia amara L., Simaroubaceae, against Leishmania amazonensis and Leishmania infatum. The alkaloid was isolated after liquid-liquid fractionation followed by chromatographic purification of the Q. amara methanol extract. The antileishmanial activity was evaluated by the microdilution method, using resazurin as the viability indicator. In addition, annexin and propidium iodide were used to detect parasites undergoing apoptosis. The anti-amastigote activity of the β-carboline-1-propionic acid alkaloid was determined by the infection of RAW 264.7 macrophages. The alkaloid displayed leishmanicidal activity against Leishmania amazonensis and L. infantum promastigotes and intracellular amastigotes with 50% inhibitory concentration ranging from 2.7 ± 0.82 to 9.4 ± 0.5 µg/ml and selectivity indexes >10. Moreover, apoptotic Leishmania amazonensis (19.5%) and L. infantum (40.4%) promastigotes were detected after 5 h incubation with the alkaloid. Finally, the β-carboline-1-propionic acid alkaloid inhibited the production of NO of infected macrophages, suggesting that the intracellular amastigote elimination occurs in a nitrosative stress-independent way. The results shown here suggest that the β-carboline-1-propionic acid alkaloid has potential as an antileishmanial agent.

O óleo essencial de folhas de Alpinia zerumbet (Pers.) B.L. Burtt & R.M. Sm., extraído por hidrodestilação, foi analisado por CG/DIC e CG/EM a fim de se determinar sua composição e atividade antimicrobiana. O óleo apresentou um elevado teor de monoterpenos oxigenados (52,5%): terpinen-4-ol, 1,8-cineol e γ-terpineno como principais constituintes. A atividade antimicrobiana do óleo foi analisada pelos testes de difusão em agar e ensaios de bioautografia. Através do teste de difusão em agar, todas as bactérias e fungos testados foram inibidos pelo óleo essencial. Placas preparativas de CCD (cromatografia em camada fina) foram eluídas em hexano: acetato de etila (70:20, v/v), e o óleo foi separado em três frações que foram raspadas, extraídas da sílica e identificadas por CG/EM. A análise bioautográfica permitiu detectar pronunciada inibição de Cryptococcus neoformans pelas frações F2 e F3, ambas ricas em monoterpenos oxigenados. A fração F2 apresentou 1,8 cineol (9,6%), linalol (3,7%) e óxido de cariofileno (5,4%), enquanto a fração F3 mostrou principalmente terpinen-4-ol (43,6%) e cerca de 32,7% de sesquiterpenos oxigenados. Os dados obtidos indicam os componentes do óleo de A. zerumbet envolvidos na atividade antimicrobiana.

Leaf oil prepared by hydrodistillation of Alpinia zerumbet Pers.) B.L. Burtt & R.M. Sm. was analyzed by GC/FID and GC/MS to determine the major compounds and it was also evaluated for antimicrobial activity. The oil presented a high content of oxygenated monoterpenes (52.5%), terpinen-4-ol, 1,8 cineole and γ-terpinene as the major constituents. The antimicrobial activity of leaf oil was tested by drop diffusion and bioauthography methods. Through drop test, all bacteria and fungi tested were inhibited by leaf oil. Preparative TLC (thin-layer chromatography) plates were developed using the mobile phase hexane: ethyl acetate (70:20, v/v) and fractions of the leaf oil were separated in three zones, scraped, extracted from silica and identified by GC/MS. The bioauthography method permitted to verify pronounced inhibition of Cryptococcus neoformans by fractions F2 and F3, both rich in oxygenated monoterpenes. The fraction F2 comprised 1,8 cineole (9.6%), linalool (3.7%) and caryophyllene oxide (5.4%), while fraction F3 showed mainly terpinen-4-ol (43.6%) and an amount of 32.7% oxygenated sesquiterpenes. The obtained data may be used to suggest the constituents of A. zerumbet leaf oil involved in antimicrobial activity.

A espécie Calceolaria chelidonioides (Scrophulariaceae), até então inédita nas citações científicas, foi estudada sob o ponto de vista farmacológico buscando-se identificar possíveis atividades antimicrobiana e antioxidante em metodologia in vitro. As partes aéreas dessa espécie demonstraram atividade antioxidante em modelo usando o radical livre DPPH. As flores de C. chelidonioides mostraram grande potencial antibacteriano frente à bactéria Staphylococcus aureus resistente a meticilina MRSA, um dos principais responsáveis em casos de infecção hospitalar.

The species Calceolaria chelidonioides (Scrophulariaceae), not scientific described so for, was studied in pharmacological aspects aiming to identify some anti-microbial and antioxidant activity. The aerial parts showed antioxidant activity using in vitro DPPH model. The flowers from C. chelidonioides showed strong antibacterial potential against meticiline resistant Staphylococcus aureus (MRSA) strains the main responsible for hospital infection complications.