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1.
J Nat Prod ; 80(10): 2684-2691, 2017 10 27.
Artigo em Inglês | MEDLINE | ID: mdl-28972755

RESUMO

With the aim of discovering new cytotoxic prenylated stilbenes of the schweinfurthin series, Macaranga tanarius was selected for detailed phytochemical investigation among 21 Macaranga species examined by using a molecular networking approach. From an ethanol extract of the fruits, seven new prenylated stilbenes, schweinfurthins K-Q (7-13), were isolated, along with vedelianin (1), schwenfurthins E-G (2-4), mappain (5), and methyl-mappain (6). The structures of the new compounds were established by spectroscopic data analysis. The relative configurations of compounds 8, 12, and 13 were determined based on ROESY NMR spectroscopic analysis. The cytotoxic activities of compounds 1-13 were evaluated against the human glioblastoma (U87) and lung (A549) cancer cell lines.


Assuntos
Antineoplásicos Fitogênicos/isolamento & purificação , Antineoplásicos Fitogênicos/farmacologia , Euphorbiaceae/química , Estilbenos/isolamento & purificação , Estilbenos/farmacologia , Antineoplásicos Fitogênicos/química , Ensaios de Seleção de Medicamentos Antitumorais , Flavonoides/química , Frutas/química , Humanos , Estrutura Molecular , Ressonância Magnética Nuclear Biomolecular , Folhas de Planta/química , Prenilação , Estilbenos/química , Vietnã
2.
J Med Chem ; 66(20): 14208-14220, 2023 10 26.
Artigo em Inglês | MEDLINE | ID: mdl-37795600

RESUMO

Schweinfurthins (SWs) are naturally occurring prenylated stilbenes with promising anticancer properties. They act through a novel mechanism of action similar to that of other families of natural compounds. Their known target, oxysterol-binding protein (OSBP), plays a crucial role in controlling the intracellular distribution of cholesterol. We synthesized 15 analogues of SWs and demonstrated for the first time that their cytotoxicity as well as that of natural derivatives correlates with their affinity for OSBP. Through this extensive SAR study, we selected one synthetic analogue obtained in one step from SW-G. Using its fluorescence properties, we showed that this compound recapitulates the effect of natural SW-G in cells and confirmed that it leads to cell death via the same mechanism. Finally, after pilot PK experiments, we provided the first evidence of its in vivo efficacy in combination with temozolomide in a patient-derived glioblastoma xenograft model.


Assuntos
Oxisteróis , Receptores de Esteroides , Humanos , Receptores de Esteroides/metabolismo , Colesterol/metabolismo
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