Your browser doesn't support javascript.
loading
In vitro antiplasmodial activity and identification, using tandem LC-MS, of alkaloids from Aspidosperma excelsum, a plant used to treat malaria in Amazonia.
do Nascimento, Myrth Soares; Pina, Nayla di Paula Vieira; da Silva, Andressa Santa Brigida; Gomes, Luís Fabio Dos Santos; de Vasconcellos, Flávio; Brandão, Geraldo Célio; do Nascimento, Maria Fernanda Alves; de Oliveira, Alaíde Braga; Barbosa, Wagner Luiz Ramos.
Afiliação
  • do Nascimento MS; Graduate Program in Pharmaceutical Sciences, Federal University of Pará, R. Augusto Corrêa, 01, Guamá, CEP 66075-110 Belém, Pará, Brazil.
  • Pina NDPV; Graduate Program in Pharmaceutical Sciences, Federal University of Pará, R. Augusto Corrêa, 01, Guamá, CEP 66075-110 Belém, Pará, Brazil.
  • da Silva ASB; Graduate Program in Pharmaceutical Sciences, Federal University of Pará, R. Augusto Corrêa, 01, Guamá, CEP 66075-110 Belém, Pará, Brazil.
  • Gomes LFDS; Graduate Program in Pharmaceutical Sciences, Federal University of Pará, R. Augusto Corrêa, 01, Guamá, CEP 66075-110 Belém, Pará, Brazil.
  • de Vasconcellos F; Graduate Program in Pharmaceutical Sciences, Federal University of Pará, R. Augusto Corrêa, 01, Guamá, CEP 66075-110 Belém, Pará, Brazil.
  • Brandão GC; Faculty of Pharmacy, Federal University of Ouro Preto, R. Diogo de Vasconcelos, 122, Pilar, CEP 35400-000 Ouro Preto, Minas Gerais, Brazil.
  • do Nascimento MFA; Faculty of Pharmacy, Federal University of Minas Gerais, Av. Antônio Carlos, 6627, Pampulha, CEP 31270-901 Belo Horizonte, Minas Gerais, Brazil.
  • de Oliveira AB; Faculty of Pharmacy, Federal University of Minas Gerais, Av. Antônio Carlos, 6627, Pampulha, CEP 31270-901 Belo Horizonte, Minas Gerais, Brazil.
  • Barbosa WLR; Graduate Program in Pharmaceutical Sciences, Federal University of Pará, R. Augusto Corrêa, 01, Guamá, CEP 66075-110 Belém, Pará, Brazil; Faculty of Pharmacy, Institute of Health Sciences, Federal University of Pará, R. Augusto Corrêa, 01, Guamá, CEP 66075-110 Belém, Pará, Brazil. Electronic address
J Ethnopharmacol ; 228: 99-109, 2019 Jan 10.
Article em En | MEDLINE | ID: mdl-30201230
ETHNOPHARMACOLOGICAL RELEVANCE: Aspidosperma excelsum Benth. (Apocynaceae), a native tree in the Brazilian Amazonia, is traditionally used to treat various diseases, including malaria. AIM OF STUDY: To investigate the chemical constitution, antiplasmodial activity and cytotoxicity of samples obtained from A. excelsum trunk bark by different procedures aiming to evaluate their potential as an antimalarial phytomedicine. MATERIALS AND METHODS: A hydroethanolic extract and alkaloid extracts were prepared and assayed for antiplasmodial activity and cytotoxicity against chloroquine-resistant Plasmodium falciparum (W2 strain) and HepG2 cells, respectively. Taking into account the known occurrence and antimalarial activity of Aspidosperma monoterpene indole alkaloids (MIA), acid-base extractions were carried out and the fractions were assayed for antiplasmodial activity and cytotoxicity. All the samples were analysed by hyphenated chromatographic techniques, such as UPLC-DAD-ESI-MS/MS and HRMS (HPLC-MS MicroTOF), comparing their chemical composition to the literature data. RESULTS: The hydroethanolic extract disclosed a moderate in vitro activity against chloroquine-resistant Plasmodium falciparum (W2 strain) with IC50 23.68 ± 3.08 µg/mL), low cytotoxicity to HepG2 cells (> 250 µg/mL) and good SI (> 10.56). A total of 20 known monoterpene indole alkaloids were identified, seven of which are here firstly described for A. excelsum. Known highly active alkaloids, namely demethylaspidospermine, aspidocarpine, and ochrolifuanine are present in active alkaloid fractions and might contribute to their observed antiplasmodial effect. An alkaloid fraction (Ae-Alk2), obtained directly from trunk bark by extraction with dil. aqueous HCl, pointed out for its activity (IC50 8.75±2.26 µg/mL, CC50 185.14±1.97 µg/mL, SI 21.16) and should be highlighted as the most promising out of the assayed samples. CONCLUSION: The present results represent a preliminary support to the alleged antimalarial use of A. excelsum trunk bark and allowed to highlight alkaloid fractions as promising phytomedicines.
Assuntos
Palavras-chave

Texto completo: 1 Coleções: 01-internacional Base de dados: MEDLINE Assunto principal: Plasmodium falciparum / Aspidosperma / Alcaloides Indólicos / Antimaláricos Tipo de estudo: Diagnostic_studies Limite: Humans País/Região como assunto: America do sul / Brasil Idioma: En Revista: J Ethnopharmacol Ano de publicação: 2019 Tipo de documento: Article País de afiliação: Brasil País de publicação: Irlanda

Texto completo: 1 Coleções: 01-internacional Base de dados: MEDLINE Assunto principal: Plasmodium falciparum / Aspidosperma / Alcaloides Indólicos / Antimaláricos Tipo de estudo: Diagnostic_studies Limite: Humans País/Região como assunto: America do sul / Brasil Idioma: En Revista: J Ethnopharmacol Ano de publicação: 2019 Tipo de documento: Article País de afiliação: Brasil País de publicação: Irlanda