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Licochalcone a Exhibits Leishmanicidal Activity in vitro and in Experimental Model of Leishmania (Leishmania) Infantum

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Autor(es):
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Souza, Julia M. [1] ; de Carvalho, Erica A. A. [1] ; Candido, Ana Carolina B. B. [1] ; de Mendonca, Rafael P. [2] ; Fernanda da Silva, Maria [2] ; Parreira, Renato L. T. [1] ; Dias, Fernanda G. G. [2] ; Ambrosio, Sergio R. [1] ; Arantes, Andrea T. [3] ; da Silva Filho, Ademar A. [4] ; Nascimento, Aline N. [5] ; Costa, Monique R. [5] ; Sairre, Mirela I. [5] ; Veneziani, Rodrigo C. S. [1] ; Magalhaes, Lizandra G. [1, 2]
Número total de Autores: 15
Afiliação do(s) autor(es):
[1] Univ Franca, Nucleo Pesquisa Ciencias Exatas & Tecnol, Franca, SP - Brazil
[2] Univ Franca, Pos Grad Ciencia Anim, Franca, SP - Brazil
[3] Ctr Tecnol Agr, Batatais - Brazil
[4] Univ Fed Juiz De Fora, Dept Ciencias Farmaceut, Juiz De Fora - Brazil
[5] Univ Fed ABC, Ctr Ciencias Nat & Humanas, Santo Andre, SP - Brazil
Número total de Afiliações: 5
Tipo de documento: Artigo Científico
Fonte: FRONTIERS IN VETERINARY SCIENCE; v. 7, DEC 10 2020.
Citações Web of Science: 0
Resumo

The efficacy of Licochalcone A (LicoA) and its two analogs were reported against Leishmania (Leishmania) amazonensis and Leishmania (Leishmania) infantum in vitro, and in experimental model of L. (L.) infantum in vitro. Initially, LicoA and its analogs were screened against promastigote forms of L. (L.) amazonensis. LicoA was the most active compound, with IC50 values of 20.26 and 3.88 mu M at 24 and 48 h, respectively. Against amastigote forms, the IC50 value of LicoA was 36.84 mu M at 48 h. In the next step, the effectivity of LicoA was evaluated in vitro against promastigote and amastigote forms of L. (L.) infantum. Results demonstrated that LicoA exhibited leishmanicidal activity in vitro against promastigote forms with IC50 values of 41.10 and 12.47 mu M at 24 and 48 h, respectively; against amastigote forms the IC50 value was 29.58 mu M at 48 h. Assessment of cytotoxicity demonstrated that LicoA exhibited moderate mammalian cytotoxicity against peritoneal murine macrophages; the CC50 value was 123.21 mu M at 48 h and showed about 30% of hemolytic activity at concentration of 400 mu M. L. (L.) infantum-infected hamsters and treated with LicoA at 50 mg/kg for eight consecutive days was able to significantly reduce the parasite burden in both liver and spleen in 43.67 and 39.81%, respectively, when compared with negative control group. These findings suggest that chalcone-type flavonoids can be a promising class of natural products to be considered in the search of new, safe, and effective compounds capable to treat canine visceral leishmaniosis (CVL). (AU)

Processo FAPESP: 13/11164-4 - Avaliação da indução da apoptose em vermes adultos de Schistosoma mansoni após exposição com curcumina
Beneficiário:Lizandra Guidi Magalhães
Modalidade de apoio: Auxílio à Pesquisa - Regular
Processo FAPESP: 16/18045-9 - Estudo da reação multicomponente de Hantzsch para a síntese de novos inibidores da dipeptidil peptidase 4 (DPP-4) para o tratamento de Diabetes tipo II
Beneficiário:Mirela Inês de Sairre
Modalidade de apoio: Auxílio à Pesquisa - Regular
Processo FAPESP: 16/24456-1 - Curcuminóides monocetônicos para o tratamento da esquistossomose: uma avaliação pré-clínica da atividade esquistossomicida
Beneficiário:Lizandra Guidi Magalhães
Modalidade de apoio: Auxílio à Pesquisa - Regular