Abstract
The treatment of leishmaniasis includes pentavalent antimony drugs but, because of the side effects, toxicity and cases of treatment failure or resistance, the search of new antileishmanial compounds are necessary. The aims of this study were to evaluate and compare the in vitro antileishmanial activity of four green tea catechins, and to assess the efficacy of topical (−)-epigallocatechin gallate in a cutaneous leishmaniasis model. The antileishmanial activity of green tea catechins was evaluated against intracellular amastigotes, and cytotoxicity was performed with human monocytic cell line. BALB/c mice were infected in the ear dermis with Leishmania (Leishmania) amazonensis and treated with topical 15% (−)-epigallocatechin gallate, intraperitoneal Glucantime, and control group. The efficacy of treatments was evaluated by quantifying the parasite burden and by measuring the lesions size. (−)-Epigallocatechin gallate and (−)-epigallocatechin were the most active compounds with IC50 values <59.6 µg/mL and with a selectivity index >1. Topical treatment with (−)-epigallocatechin gallate decreased significantly both lesion size and parasite burden (80.4% inhibition) compared to control group (p < 0.05), and moreover (−)-epigallocatechin gallate showed a similar efficacy to Glucantime (85.1% inhibition), the reference drug for leishmaniasis treatment.
Highlights
Cutaneous leishmaniasis (CL) is a widespread tropical infection caused by a protozoa parasite of Leishmania genus which is transmitted to humans by the bite of an infected sand fly [1]
We investigated the activity of four green tea catechins (GTC) against intracellular amastigotes
These compounds showed antileishmanial activity in macrophages infected with L. (L.) amazonensis after 48 h of incubation, epigallocatechin gallate (EGCG) and EGC being the most active with IC50 values
Summary
Cutaneous leishmaniasis (CL) is a widespread tropical infection caused by a protozoa parasite of Leishmania genus which is transmitted to humans by the bite of an infected sand fly [1]. CL is characterized by an ulcerative lesion (single or multiple), and depending of Leishmania species, the disease can progress to more severe manifestations such us mucocutaneous, diffuse leishmaniasis, disseminated leishmaniasis, and leishmaniasis recidivans [1]. The antimonials, sodium stibogluconate (Pentostam) or meglumine antimoniate (Glucantime), are the first choice for the treatment of all forms of leishmaniasis, but because of their toxicity, high cost and prolonged treatment regimens, are not satisfactory as an ideal drug. Molecules 2020, 25, 1741 showed a low efficacy against Leishmania Viannia species [2]. There is a need for new Molecules 2020, 25, x FOR PEER REVIEW antileishmanial drugs
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