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Baccharis trimera (Less.) DC leaf derivatives and eupatorin activities against Leishmania amazonensis.
Sahid, Esther Della Nina; Claudino, Josiane Clarice; Oda, Fernando Bombarda; Carvalho, Flávio Alexandre; Santos, André Gonzaga Dos; Graminha, Marcia A S; Clementino, Leandro da Costa.
Afiliação
  • Sahid EDN; Chemistry Institute, São Paulo State University (UNESP), Araraquara, Brazil.
  • Claudino JC; Chemistry Institute, São Paulo State University (UNESP), Araraquara, Brazil.
  • Oda FB; Chemistry Institute, São Paulo State University (UNESP), Araraquara, Brazil.
  • Carvalho FA; Chemistry Institute, São Paulo State University (UNESP), Araraquara, Brazil.
  • Santos AGD; Chemistry Institute, São Paulo State University (UNESP), Araraquara, Brazil.
  • Graminha MAS; School of Pharmaceutical Sciences, São Paulo State University (UNESP), Araraquara, Brazil.
  • Clementino LDC; Chemistry Institute, São Paulo State University (UNESP), Araraquara, Brazil.
Nat Prod Res ; 36(6): 1599-1603, 2022 Mar.
Article em En | MEDLINE | ID: mdl-33586545
Natural products have been largely explored as treatments for leishmaniasis, neglected diseases with few toxic therapeutic options, as scaffolds for the development of new drugs. Herein, derivatives from the aerial parts of Baccharis trimera (Less.) DC (extract and its fractions) were evaluated against Leishmania amazonensis and macrophage cells. The ethyl acetate extract was fractionated by solid-phase extraction, resulting in eight fractions (F1-F8). Fractions F3-4 were further separated into 149 subfractions; subfraction 148 (IC50-PRO = 1.56 ± 0.1 µg mL-1) was selected for purification and constituent(s) characterization by high-performance liquid chromatography, as well as 1H and 13C nuclear magnetic resonance spectroscopy. The flavonoid eupatorin (3',5-dihydroxy-4',6,7-trimethoxyflavone) was identified. This compound was 3.7 times more effective against intracellular amastigotes (IC50-AMA = 1.6 ± 0.1 µM) than amphotericin B and presented low cytotoxicity (CC50 > 100 µM), being almost 62 times more selective for the parasite, showing great potential in drug development for cutaneous leishmaniasis treatment.
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Texto completo: 1 Coleções: 01-internacional Base de dados: MEDLINE Assunto principal: Leishmania mexicana / Leishmaniose Cutânea / Baccharis / Antiprotozoários Idioma: En Revista: Nat Prod Res Ano de publicação: 2022 Tipo de documento: Article País de afiliação: Brasil País de publicação: Reino Unido
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: Leishmania mexicana / Leishmaniose Cutânea / Baccharis / Antiprotozoários Idioma: En Revista: Nat Prod Res Ano de publicação: 2022 Tipo de documento: Article País de afiliação: Brasil País de publicação: Reino Unido