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Leishmania amazonensis response to artemisinin and derivatives.
Machín, Laura; Nápoles, Rachel; Gille, Lars; Monzote, Lianet.
Afiliação
  • Machín L; Department of Pharmacy, Institute of Pharmacy and Foods Sciences, University of Havana, Street 222, e/ 23 y 29, # 2317, La Coronela. La Lisa, Havana, Cuba.
  • Nápoles R; Department of Pharmacy, Institute of Pharmacy and Foods Sciences, University of Havana, Street 222, e/ 23 y 29, # 2317, La Coronela. La Lisa, Havana, Cuba.
  • Gille L; Institute of Pharmacology and Toxicology, Department of Biomedical Sciences, University of Veterinary Medicine, Veterinaerplatz 1, 1210 Vienna, Austria.
  • Monzote L; Parasitology Department, Institute of Tropical Medicine "Pedro Kouri", Autopista Novia del Mediodía Km 6 1/2. La Lisa, Havana, Cuba. Electronic address: monzote@ipk.sld.cu.
Parasitol Int ; 80: 102218, 2021 Feb.
Article em En | MEDLINE | ID: mdl-33137506
The worldwide presence of Leishmania parasites increases in the poorest regions. Current leishmaniasis treatments are unsatisfactory due to resistance development, side effects and cost. Herein, we describe the in vitro activity of artemisinin (ART), artemether (ATM), artesunate (ATS) and dihydroartemisinin (DHA) against Leishmania amazonensis. Selected compounds were assayed in the animal model of cutaneous leishmaniasis in BALB/c mice. On intracellular amastigotes, similar activity (p > 0.05) was observed for ART, ATM and ATS (IC50 = 15.0-19.2 µM), which were inferior (p < 0.05) respect to reference endoperoxide ascaridole (IC50 = 11.5 ±â€¯1.0 µM) and superior (p < 0.05) compared with reference drug Glucantime® (IC50 = 30.1 ±â€¯9.0 µM). In contrast, DHA (IC50 = 38.5 ±â€¯4.7 µM) showed higher IC50 values (p < 0.05) than other artemisinins and ascaridole, but similar (p > 0.05) than Glucantime®; while deoxyartemisinin caused smaller inhibition (IC50 = 88.9 ±â€¯5.2 µM). Selectivity indexes of >13, 6, 11 and 1 were obtained for ART, ATM, ATS and DHA, respectively. In addition, the potential effect of ART and ATS was also demonstrated in the murine model, causing a significant reduction (p < 0.05) of the lesion size and parasite load regarding untreated animals and treated with vehicle. Effects of both artemisinins were comparable (p > 0.05) with Glucantime® and ascaridole-treated mice. In particular, artemisinin is recommended to further studies, which could be an advantage over the ascaridole endoperoxide and could be useful in endemic areas of parasite resistance to antimonials.
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Texto completo: 1 Coleções: 01-internacional Base de dados: MEDLINE Assunto principal: Tripanossomicidas / Leishmania mexicana / Artemisininas / Carga Parasitária Limite: Animals Idioma: En Revista: Parasitol Int Assunto da revista: PARASITOLOGIA Ano de publicação: 2021 Tipo de documento: Article País de afiliação: Cuba País de publicação: Holanda
Texto completo
Adicionar na Minha BVS
Imprimir
XML
PubMed Links
Buscar no Google

Texto completo: 1 Coleções: 01-internacional Base de dados: MEDLINE Assunto principal: Tripanossomicidas / Leishmania mexicana / Artemisininas / Carga Parasitária Limite: Animals Idioma: En Revista: Parasitol Int Assunto da revista: PARASITOLOGIA Ano de publicação: 2021 Tipo de documento: Article País de afiliação: Cuba País de publicação: Holanda