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J Nat Prod ; 85(1): 63-69, 2022 01 28.
Artigo em Inglês | MEDLINE | ID: mdl-34949088

RESUMO

A recently discovered secondary metabolism regulator, NPD938, was used to alter the secondary metabolite profile in Fusarium sp. RK97-94. Three lucilactaene analogues were detected via UPLC-ESI-MS analysis in NPD938-treated culture. The three metabolites were successfully purified and identified as dihydroNG391 (1), dihydrolucilactaene (2), and 13α-hydroxylucilactaene (3) via extensive spectroscopic analyses. DihydroNG391 (1) exhibited weak in vitro antimalarial activity (IC50 = 62 µM). In contrast, dihydrolucilactaene (2) and 13α-hydroxylucilactaene (3) showed very potent antimalarial activity (IC50 = 0.0015 and 0.68 µM, respectively). These findings provide insight into the structure-activity relationship of lucilactaene and its analogues as antimalarial lead compounds.


Assuntos
Antimaláricos/farmacologia , Fusarium/química , Antimaláricos/química , Antimaláricos/isolamento & purificação , Cromatografia/métodos , Humanos , Metabolismo Secundário , Análise Espectral/métodos , Relação Estrutura-Atividade
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