[Show abstract][Hide abstract] ABSTRACT: About 1.5 million new cases of cutaneous leishmaniasis and 500,000 new cases of visceral leishmaniasis occur each year around the world. For over half a century, the clinical forms of the disease have been treated almost exclusively with pentavalent antimonial compounds. In this review, we describe the arsenal available for treating Leishmania infections, as well as recent advances from research on plants and synthetic compounds as source drugs for treating the disease. We also review some new drug-delivery systems for the development of novel chemotherapeutics. We observe that the pharmaceutical industry should employ its modern technologies, which could lead to better use of plants and their extracts, as well as to the development of synthetic and semi-synthetic compounds. New studies have highlighted some biopharmaceutical technologies in the design of the delivery strategy, such as nanoparticles, liposomes, cochleates, and non-specific lipid transfer proteins. These observations serve as a basis to indicate novel routes for the development and design of effective anti-Leishmania drugs.
International journal of infectious diseases: IJID: official publication of the International Society for Infectious Diseases 05/2011; 15(8):e525-32. DOI:10.1016/j.ijid.2011.03.021 · 1.86 Impact Factor
[Show abstract][Hide abstract] ABSTRACT: Copaiba oil has been used in folk medicine since the 19th century. The use of copaiba oils to treat leishmaniasis is cited in several ethnopharmacological studies. Nevertheless, the potential antileishmania of copaiba oils had not been studied.
Eight different kinds of Brazilian copaiba oils were screened for antileishmanial activity.
The antiproliferative effect of copaiba oil on promastigote and amastigote axenic were determined. To determine the survival index peritoneal macrophage were infected with promastigotes of Leishmania amazonensis and treated with copaiba oil. The cytotoxic effect of copaiba oil was assessed on macrophage strain J774G8 by assay of sulforhodamine B.
Copaiba oils showed variable levels of activity against promastigote forms with IC(50) values in the range between 5 and 22microg/mL. The most active oil was that from Copaifera reticulata (collected in Pará State, Brazil) with IC(50) values of 5, 15, and 20microg/mL for promastigote, axenic amastigote and intracellular amastigote forms, respectively. Amphotericin B showed IC(50) of 0.058 and 0.231microg/mL against promastigote and amastigote forms, respectively. Cytotoxicity assay showed that this copaiba oil obtained from Copaifera reticulata showed low cytotoxicity against J774G8 macrophages.
Copaiba oils showed significant activity against the parasite Leishmania amazonensis.
Journal of Ethnopharmacology 09/2008; 120(2):204-8. DOI:10.1016/j.jep.2008.08.007 · 3.00 Impact Factor
[Show abstract][Hide abstract] ABSTRACT: Biological activity of the crude extract and several fractions obtained from Piper regnellii var. pallescens was assessed on Leishmania amazonensis. This study included the extraction process and bioassay-guided fractionation by the adsorption chromatography method. A progressive increase in the antileishmanial effect was observed in the course of the purification process. The hydroalcoholic extract water soluble (EBA) had a 50% inhibitory concentration (IC50) at 167 µg/mL whereas the hydroalcoholic extract acetate soluble (EBAcOEt) showed an IC50 of 30 µg/mL against the growth of promastigote forms after 48 h of culturing. The hexan fraction (FHex) showed an antileishmanial activity greater than EBAcOEt with IC50 at 21.5 µg/mL. Analysis of cytotoxicity indicated that the toxic concentrations of the EBA, EBAcOEt, and fractions were higher for J774G8 macrophages than for the protozoans.
Revista Brasileira de Farmacognosia 03/2006; 16(1):61-66. DOI:10.1590/S0102-695X2006000100011 · 0.83 Impact Factor