Evaluation of Boldine Activity against Intracellular Amastigotes of Leishmania amazonensis

Abstract

Leishmaniasis is a neglected and endemic disease that affects poorest population mainly in developing countries. A lack of adequate and definitive chemotherapeutic agents to fight against this infection has led to the investigation of numerous compounds. The aim of this study was to investigate in vitro activity of boldine against Leishmania amazonensis murine cell infection. Boldine ((S)-2,9-dihydroxy-1,10-dimethoxy-aporphine) is an aporphine alkaloid found abundantly in the leaves/bark of boldo (Peumus boldus Molina), a widely distributed tree native to Chile. The in vitro system consisted of murine macrophage infection with amastigotes of L. amazonensis treated with different concentrations from 50 to 600 μg/ml of boldine for 24 hr. Intracellular parasite destruction was assessed by morphological examination and boldine cytotoxicity to macrophages was tested by the MTT viability assay. When cells were treated with 100 μg/ml of boldine the reduction of parasite infection was 81% compared with untreated cultures cells. Interestingly, boldine-treatment caused a concentration-dependent decrease of macrophage infection that culminated with 96% of reduction when cells were submitted to 600 μg/ml of boldine. Cell cultures exposed to 100 μg/ml of boldine and 300 μg/ml of Glucantime® during 24 hr showed a significant reduction of 50% in parasitized cells compared with cell cultures exposed just to Glucantime®. The study showed that treatment with boldine produces a better effect than treatment with the reference antimonial drug, glucantime, in L. amazonensis infected macrophage. Our results suggest that boldine is a potentially useful agent for the treatment of leishmaniasis.

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“…It showed that, reduction of parasite infection in treated cells by 81% using 100 μg/ml of boldine. Besides, a concentrationdependent decrease in macrophage infection culminated with a 96% of reduction when cells were incubated with 600 μg/ml [48].…”

“…Leishmania amazonensis murine cell infection using MTT viability assay 100-600 μg/ml ↓parasite infection in treated cells [48].…”

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“…The development of alternative control strategies that rely less on the use of synthetic drugs is being driven by rising drug resistance in livestock parasites that reside in the gastrointestinal tract as well as worries about chemical residues in animal products and the environment (21). The use of bioactive forages with antiparasitic properties as food for animals or as possible sources of the novel, natural parasiticides is a strategy that is being studied more and more (21). The anti-Leishmanial effect of boldine isolated from boldo leaves was investigated using an MTT viability assay (21).…”

“…The use of bioactive forages with antiparasitic properties as food for animals or as possible sources of the novel, natural parasiticides is a strategy that is being studied more and more (21). The anti-Leishmanial effect of boldine isolated from boldo leaves was investigated using an MTT viability assay (21). Results showed that boldine reduces this parasitic infection and had a potent activity in the treatment of leishmaniasis infection (21).…”

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“…IC 50 for the two strains and the clone were 110, 115, and 120 μΜ, respectively [ 61 ]. Boldine at concentrations of 100 and 600 μg/mL was also able to reduce the infection to 81 and 96%, respectively, of the amastigotes of Leishmania amazonensis in a murine macrophage model [ 62 ]. Finally, boldine at 100 and 50 μΜ was able to inhibit the replication of human deficiency virus (HΙV-1 NL4-3 ) on CEM-GXR cells and hepatitis C virus (HCV) on Hun-7.5 cells, respectively [ 63 ].…”