| Texto completo | |
| Autor(es): |
Monteiro, Jackson
;
Passero, Luiz Felipe D.
;
Jesus, Jessica A.
;
Laurenti, Marcia D.
;
Lago, Joao H. G.
;
Soares, Marisi G.
;
Batista, Andrea N. L.
;
Batista Jr, Joao M.
;
Sartorelli, Patricia
Número total de Autores: 9
|
| Tipo de documento: | Artigo Científico |
| Fonte: | CURRENT TOPICS IN MEDICINAL CHEMISTRY; v. 22, n. 19, p. 8-pg., 2022-01-01. |
| Resumo | |
Background: The fractionation of the n-hexane phase of the EtOH extract from the leaves of Duguetia lanceolata (Annonaceae) led to the identification of the sesquiterpene (-)-cyclocolorenone. Objectives: Chemical characterization, including determination of the absolute stereochemistry, and in vitro evaluation of antileishmanial activity of the sesquiterpene (-)-cyclocolorenone, isolated from D. lanceolata, were carried out. Methods: (-)-Cyclocolorenone was isolated from D. lanceolata leaves using different chromatographic steps and its structure was defined by analysis of NMR and ESI-HRMS data. Additionally, the absolute configuration of (-)-cyclocolorenone was ambiguously assigned by means of vibrational circular dichroism (VCD). Antileishmanial activity of (-)-cyclocolorenone was evaluated on promastigote and amastigote forms of Leishmania (Leishmania) amazonensis. The integrity of the cell membrane of L. (L.) amazonensis was analyzed using the SYTOX green probe. Results: (-)-(1R,6S,7R,10R)-Cyclocolorenone displayed activity against promastigotes and amastigotes forms of L. (L.) amazonensis with IC50 of 4.54 and 28.44 mu M, respectively. Furthermore, this compound was non-toxic in J774 macrophage cells (CC50 > 458.71 mu M) with a selectivity index > 100 (promastigotes) and > 32.2 (amastigotes). Additionally, (-)-cyclocolorenone was observed to target the parasite cell membrane. Conclusion: Obtained data suggested that (-)-cyclocolorenone, in which absolute configuration was determined, can be considered as a scaffold for the development of new drugs for the treatment of leishmaniasis. (AU) | |
| Processo FAPESP: | 18/24077-6 - Estudos pré-clínicos de tratamentos não invasivos nas leishmanioses |
| Beneficiário: | Luiz Felipe Domingues Passero |
| Modalidade de apoio: | Auxílio à Pesquisa - Regular |
| Processo FAPESP: | 21/02789-7 - Busca de metabólitos bioativos com ação antiparasitária em espécies vegetais de regiões de Mata Atlântica e Cerrado - uma abordagem química, fenotípica e metabolômica |
| Beneficiário: | João Henrique Ghilardi Lago |
| Modalidade de apoio: | Auxílio à Pesquisa - Programa BIOTA - Regular |
| Processo FAPESP: | 19/22319-5 - Marcadores espectrais de dicroísmo circular vibracional: facilitando o assinalamento da configuração absoluta de produtos naturais |
| Beneficiário: | João Marcos Batista Junior |
| Modalidade de apoio: | Auxílio à Pesquisa - Regular |
| Processo FAPESP: | 16/24985-4 - Estudo da composição química de fungos e plantas da Mata Atlântica visando o potencial antitumoral, antiparasitário e antimicrobiano |
| Beneficiário: | Patricia Sartorelli |
| Modalidade de apoio: | Auxílio à Pesquisa - Regular |