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(Referência obtida automaticamente do Web of Science, por meio da informação sobre o financiamento pela FAPESP e o número do processo correspondente, incluída na publicação pelos autores.)

Antitrypanosomal activity and effect in plasma membrane permeability of (-)-bornyl p-coumarate isolated from Piper cernuum (Piperaceae)

Texto completo
Autor(es):
Morais, Thiago R. [1] ; Costa-Silva, Thais A. [2] ; Ferreira, Daiane D. [3] ; Novais, Bianca J. [1] ; Torrecilhas, Ana Claudia T. [1] ; Tempone, Andre G. [3] ; Lago, Joao Henrique G. [2]
Número total de Autores: 7
Afiliação do(s) autor(es):
[1] Univ Fed Sao Paulo, Inst Environm Chem & Pharmaceut Sci, BR-09972270 Sao Paulo - Brazil
[2] Univ Fed ABC, Ctr Nat Sci & Humanities, BR-09210580 Santo Andre, SP - Brazil
[3] Adolfo Lutz Inst, Ctr Parasitol & Mycol, BR-01246000 Sao Paulo, SP - Brazil
Número total de Afiliações: 3
Tipo de documento: Artigo Científico
Fonte: BIOORGANIC CHEMISTRY; v. 89, AUG 2019.
Citações Web of Science: 1
Resumo

This work describes the isolation of six metabolites from leaves and branches of Piper cernuum (Piperaceae): ( - )-cubebin (1), ( - )-hinokinin (2), ( - )-kusunokinin (3), trans-dehydroagarofuran (4), 11-hydroxi-4,5-secoeudesmane-4,5-dione (5), and ( - )-bornyl p-coumarate (6). Antitrypanosomal activity and toxicity of purified compounds were performed in vitro against trypomastigote forms of Trypanosoma cruzi and NCTC cells, respectively. Compounds 2, 3 and 5 showed moderate activities with IC50, values of 33.1, 31.8 and 45.9 mu M, respectively, while compounds 1 and 4 were inactive (IC50 > 100 mu M). On the other hand, compound 6 displayed an IC50 value of 2.1 mu M, a selectivity index (SI) of 18 and induced a considerable interference in the plasma membrane permeability (87%) in trypomastigotes of T. cruzi. Additionally, the lethal effect of compound 6 in T. cruzi could be associated to the plasma membrane permeability. Finally, experiments using scanning electron microscopy (SEM) confirmed the obtained results in which was possible to observe total alteration parasites topography after treatment with compound 6 in comparison to untreated parasites. These data indicated that the lethal action of compound 6 is directly related to structural disruption of the membrane. (AU)

Processo FAPESP: 18/10279-6 - Seleção e otimização de novos candidatos a fármacos para Leishmaniose e Doença de Chagas
Beneficiário:André Gustavo Tempone Cardoso
Linha de fomento: Auxílio à Pesquisa - Regular
Processo FAPESP: 18/07885-1 - Biomoléculas oriundas de espécies vegetais de áreas remanescentes da Mata Atlântica e do Cerrado para tratamento de doenças tropicais negligenciadas - aspectos químicos e farmacológicos
Beneficiário:João Henrique Ghilardi Lago
Linha de fomento: Auxílio à Pesquisa - Programa BIOTA - Regular