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Cytotoxicity and anti-Leishmania amazonensis activity of Citrus sinensis leaf extracts.
Garcia, Andreza R; Amaral, Ana Claudia F; Azevedo, Mariana M B; Corte-Real, Suzana; Lopes, Rosana C; Alviano, Celuta S; Pinheiro, Anderson S; Vermelho, Alane B; Rodrigues, Igor A.
Afiliação
  • Garcia AR; a Graduate Program in Pharmaceutical Sciences, School of Pharmacy , Federal University of Rio de Janeiro , RJ , Brazil.
  • Amaral ACF; b Department of Natural Products , Farmanguinhos, FIOCRUZ , RJ , Brazil.
  • Azevedo MMB; c Department of General Microbiology , Institute of Microbiology Paulo de Góes, Federal University of Rio de Janeiro , RJ , Brazil.
  • Corte-Real S; d Laboratory of Structural Biology and Electron Microscopy Platform Rudolf Barth , Oswaldo Cruz Institute (IOC) , RJ , Brazil.
  • Lopes RC; e Department of Botany , Institute of Biology, Federal University of Rio de Janeiro , RJ , Brazil.
  • Alviano CS; c Department of General Microbiology , Institute of Microbiology Paulo de Góes, Federal University of Rio de Janeiro , RJ , Brazil.
  • Pinheiro AS; f Department of Biochemistry , Institute of Chemistry, Federal University of Rio de Janeiro , RJ , Brazil.
  • Vermelho AB; c Department of General Microbiology , Institute of Microbiology Paulo de Góes, Federal University of Rio de Janeiro , RJ , Brazil.
  • Rodrigues IA; a Graduate Program in Pharmaceutical Sciences, School of Pharmacy , Federal University of Rio de Janeiro , RJ , Brazil.
Pharm Biol ; 55(1): 1780-1786, 2017 Dec.
Article em En | MEDLINE | ID: mdl-28524774
CONTEXT: Leishmania amazonensis is the main agent of diffuse cutaneous leishmaniasis, a disease characterized by lesional polymorphism and the commitment of skin surface. Previous reports demonstrated that the Citrus genus possess antimicrobial activity. OBJECTIVE: This study evaluated the anti-L. amazonensis activity of Citrus sinensis (L.) Osbeck (Rutaceae) extracts. MATERIALS AND METHODS: Citrus sinensis dried leaves were subjected to maceration with hexane (CH), ethyl acetate (CEA), dichloromethane/ethanol (CD/Et - 1:1) or ethanol/water (CEt/W - 7:3). Leishmania amazonensis promastigotes were treated with C. sinensis extracts (1-525 µg/mL) for 120 h at 27 °C. Ultrastructure alterations of treated parasites were evaluated by transmission electron microscopy. Cytotoxicity of the extracts was assessed on RAW 264.7 and J774.G8 macrophages after 48-h treatment at 37 °C using the tetrazolium assay. In addition, Leishmania-infected macrophages were treated with CH and CD/Et (10-80 µg/mL). RESULTS: CH, CD/Et and CEA displayed antileishmanial activity with 50% inhibitory activity (IC50) of 25.91 ± 4.87, 54.23 ± 3.78 and 62.74 ± 5.04 µg/mL, respectively. Parasites treated with CD/Et (131.2 µg/mL) presented severe alterations including mitochondrial swelling, lipid body formation and intense cytoplasmic vacuolization. CH and CD/Et demonstrated cytotoxic effects similar to that of amphotericin B in the anti-amastigote assays (SI of 2.16, 1.98 and 1.35, respectively). Triterpene amyrins were the main substances in CH and CD/Et extracts. In addition, 80 µg/mL of CD/Et reduced the number of intracellular amastigotes and the percentage of infected macrophages in 63% and 36%, respectively. CONCLUSION: The results presented here highlight C. sinensis as a promising source of antileishmanial agents.
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Texto completo: 1 Coleções: 01-internacional Base de dados: MEDLINE Assunto principal: Extratos Vegetais / Folhas de Planta / Citrus sinensis / Leishmania / Macrófagos / Antiprotozoários Limite: Animals Idioma: En Revista: Pharm Biol Ano de publicação: 2017 Tipo de documento: Article País de afiliação: Brasil País de publicação: Reino Unido

Texto completo: 1 Coleções: 01-internacional Base de dados: MEDLINE Assunto principal: Extratos Vegetais / Folhas de Planta / Citrus sinensis / Leishmania / Macrófagos / Antiprotozoários Limite: Animals Idioma: En Revista: Pharm Biol Ano de publicação: 2017 Tipo de documento: Article País de afiliação: Brasil País de publicação: Reino Unido