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Verbascoside Inhibits Promastigote Growth and Arginase Activity of Leishmania amazonensis.
Maquiaveli, Claudia C; Lucon-Júnior, João F; Brogi, Simone; Campiani, Giuseppe; Gemma, Sandra; Vieira, Paulo C; Silva, Edson R.
Afiliação
  • Maquiaveli CC; Department of Chemistry, Universidade Federal de São Carlos , Rod. Washington Luís, Km 235, 13565-905 São Carlos, SP, Brazil.
  • Lucon-Júnior JF; Department of Veterinary Medicine, Universidade de São Paulo , Avenida Duque de Caxias Norte, 225, 13635-900 Pirassununga, SP, Brazil.
  • Brogi S; European Research Centre for Drug Discovery and Development (NatSynDrugs) and Department of Biotechnology, Chemistry, and Pharmacy, Università degli Studi di Siena , Via Aldo Moro 2, 53100 Siena, Italy.
  • Campiani G; European Research Centre for Drug Discovery and Development (NatSynDrugs) and Department of Biotechnology, Chemistry, and Pharmacy, Università degli Studi di Siena , Via Aldo Moro 2, 53100 Siena, Italy.
  • Gemma S; European Research Centre for Drug Discovery and Development (NatSynDrugs) and Department of Biotechnology, Chemistry, and Pharmacy, Università degli Studi di Siena , Via Aldo Moro 2, 53100 Siena, Italy.
  • Vieira PC; Department of Chemistry, Universidade Federal de São Carlos , Rod. Washington Luís, Km 235, 13565-905 São Carlos, SP, Brazil.
  • Silva ER; Department of Veterinary Medicine, Universidade de São Paulo , Avenida Duque de Caxias Norte, 225, 13635-900 Pirassununga, SP, Brazil.
J Nat Prod ; 79(5): 1459-63, 2016 05 27.
Article em En | MEDLINE | ID: mdl-27096224
Verbascoside (1) is a phenylethanoid glycoside that has antileishmanial activity against Leishmania infantum and Leishmania donovani. In this study, we verified the activity of 1 on Leishmania amazonensis and arginase inhibition. Compound 1 showed an EC50 of 19 µM against L. amazonensis promastigotes and is a competitive arginase inhibitor (Ki = 0.7 µM). Docking studies were performed to assess the interaction of 1 with arginase at the molecular level. Arginase is an enzyme of the polyamine biosynthesis pathway that is important to parasite infectivity, and the results of our study suggest that 1 could be useful to develop new approaches for treating leishmaniasis.
Assuntos

Texto completo: 1 Bases de dados: MEDLINE Assunto principal: Fenóis / Arginase / Leishmaniose / Glucosídeos / Leishmania Limite: Animals Idioma: En Revista: J Nat Prod Ano de publicação: 2016 Tipo de documento: Article País de afiliação: Brasil

Texto completo: 1 Bases de dados: MEDLINE Assunto principal: Fenóis / Arginase / Leishmaniose / Glucosídeos / Leishmania Limite: Animals Idioma: En Revista: J Nat Prod Ano de publicação: 2016 Tipo de documento: Article País de afiliação: Brasil