Hedyosulide, a novel trypanosomicidal sesterterpene lactone from Hedyosmum brasiliense Mart. ex Miq

Autor(es):Mostrar menos -

Murakami, Cynthia ^[1] ; Cabral, Rodrigo Sant'Ana ^[1] ; Gomes, Kaio S. ^[2] ; Costa-Silva, Thais A. ^[2] ; Amaral, Maiara ^[3] ; Romanelli, Maiara ^[3] ; Tempone, Andre G. ^[3] ; Lago, Joao Henrique G. ^[2] ; Bolzani, Vanderlan da S. ^[4] ; Moreno, Paulo Roberto H. ^[5] ; Young, Maria Claudia M. ^[1]

Afiliação do(s) autor(es)

^[1] Inst Bot Sao Paulo, Nucleo Pesquisa Fisiol & Bioquim, Ave Miguel Stefano 3687, Sao Paulo - Brazil

^[2] Univ Fed ABC, Ctr Ciencias Nat & Humanas, Ave Estados 5001, Santo Andre - Brazil

^[3] Adolfo Lutz Inst, Ctr Parasitol & Micol, Av Dr Arnaldo 351, Sao Paulo, SP - Brazil

^[4] Univ Estadual Paulista, Inst Quim, Ave Prof Francisco Degni 55, Araraquara - Brazil

^[5] Univ Sao Paulo, Inst Quim, Av Lineu Prestes 748, Cidade Univ, Sao Paulo - Brazil

• Tipo de documento: Artigo Científico
• Fonte: PHYTOCHEMISTRY LETTERS; v. 33, p. 6-11, OCT 2019.
• Citações Web of Science: 0

Resumo

A new sesterterpene lactone, Hedyosulide, together with five previously described sesquiterpene lactones were isolated from the leaves of Hedyosmum brasiliense Mart. ex Miq. (Chloranthaceae). Their structures were established by NMR analysis and HRESIMS data. The isolated compounds were evaluated for antiprotozoal activity against trypomastigote and amastigote forms of Trypanosoma cruzi. Hedyosulide displayed the highest activity against the amastigote forms, in which the parasite takes in the vertebrate host, with IC50 of 21.6 mu mol/L with a selectivity index (SI) higher than 9. Oxyonoseriolide showed moderate activity against the intracellular form with IC50 of 60.2 mu mol/L and a weak SI (2.7), while the four other sesquiterpene lactones were inactive. Therefore, sesterterpene lactones, a relatively rare group of terpenoids, might be considered as a scaffold for developing new trypanosomicidal agents that are effective against T. cruzi. Also, this work brings an important contribution on the chemical/biological aspects of H. brasiliense due to the isolation of a sesterterpene lactone selectively active against both clinical forms of T. cruzi. (AU)

• Processo FAPESP: 14/17561-8 - Diversidade química e potencial farmacológico de Hedyosmum brasiliense Mart. ex Miq
• Beneficiário: Cynthia Murakami
• Linha de fomento: Bolsas no Brasil - Doutorado
• Processo FAPESP: 14/15299-4 - Diversidade química e potencial biológico de espécies selecionadas da flora paulista
• Beneficiário: Maria Claudia Marx Young
• Linha de fomento: Auxílio à Pesquisa - Regular