An unprecedented chlorine-containing piperamide from Piper pseudoarboreum as potential leishmanicidal agent.

A phytochemical investigation of the ethanolic extract of leaves from Piper pseudoarboreum led to the isolation of 3-chlorosintenpyridone 1, an unprecedented chlorinated piperamide, together with the known compounds 2-12. Their structures were established based on 1D and 2D (COSY, ROESY, HMQC, and HMBC) NMR spectroscopy, in addition to high resolution mass spectrometry. The proposed biosynthetic pathway of compound 1 is discussed. Compounds 1-12 were tested in vitro for their leishmanicidal potential against promastigote stages of Leishmania amazonensis, L braziliensis, L. guyanensis and L. infantum. Two compounds from this series, the alkamide 1 (IC50 3.4-5.2 µM) and the fatty acid 9 (IC50 18.7-29.6 µM) displayed higher or similar potency to Miltefosine, used as the reference drug.

Productos naturales con actividad leishmanicida y tripanocida / Natural products with leishmanicidal and trypanocidal activity

Las enfermedades parasitarias constituyen un importante problema de salud, y muchas de ellas están emergiendo en países donde se consideraban erradicadas. La leishmaniasis, la enfermedad del sueño y la enfermedad de Chagas, causadas por los parásitos Leishmania spp, Trypanosoma brucei y Trypanosoma cruzi, respectivamente, se encuentran entre las enfermedades parasitarias más prevalentes. La principal alternativa para tratarlas es la quimioterapia. Sin embargo, los tratamientos actuales se encuentran lejos de ser satisfactorios. La toxicidad de los fármacos, la vía de administración, la duración de los tratamientos y la aparición de resistencias hacen necesario el desarrollo de nuevas moléculas activas, más seguras y eficaces. Estudios recientes ponen de manifiesto la actividad leishmanicida y tripanocida in vivo de una amplia variedad de compuestos fenólicos, alcaloides y terpenos. En este artículo se revisan los productos naturales activos frente a leishmaniasis, enfermedad del sueño y enfermedad de Chagas (AU)

Diseases caused by protozoan parasites are still an important human health problem, since many of them are becoming “emerging” infectious sickness in geographical areas where they were considered eradicated. Leishmaniasis, African sleeping sickness and Chagas disease, caused by the parasites Leishmania spp, Trypanosoma brucei and Trypanosoma cruzi, respectively, are among the most important parasitic diseases. The main alternative to control such parasitosis is chemotherapy. Nevertheless, the current drug treatments are far from being satisfactory. Toxic side effects, route of administration, long-term treatments and the apparition of resistance, highlight the urgent need of developing new active molecules, more safe and effective. Recent studies report the leishmanicidal and trypanocidal activities of a wide variety of phenolic compounds, alkaloids and terpenes that have shown activity in vivo. This review outlines the current understanding of natural products against leishmaniasis, African sleeping sickness and Chagas disease (AU)