RESUMO
Xylarianaphthol-1, a novel dinaphthofuran derivative, was isolated from a marine sponge-derived fungus of order Xylariales on the guidance of a bioassay using the transfected human osteosarcoma MG63 cells (MG63(luc+)). The chemical structure of xylarianaphthol-1 was determined from the (1)H and (13)C NMR analysis and was further confirmed by the total synthesis. Xylarianaphthol-1 activated p21 promoter stably transfected in MG63 cells dose-dependently. Expression of p21 protein in the wild-type MG63 cells was also increased by xylarianaphthol-1 treatment.
Assuntos
Benzofuranos/farmacologia , Inibidor de Quinase Dependente de Ciclina p21/metabolismo , Proteína Supressora de Tumor p53/metabolismo , Benzofuranos/química , Benzofuranos/isolamento & purificação , Linhagem Celular Tumoral , Inibidor de Quinase Dependente de Ciclina p21/genética , Relação Dose-Resposta a Droga , Humanos , Relação Estrutura-Atividade , Xylariales/química , Xylariales/metabolismoRESUMO
Three novel cytotoxic substances named prenylterphenyllin (1), 4''-deoxyprenylterphenyllin (2), and 4''-deoxyisoterprenin (3) were isolated from a cultured marine-derived fungus of Aspergillus candidus IF10 together with 4''-deoxyterprenin (4). Their chemical structures were elucidated on the basis of 2D NMR analysis. These compounds 1 approximately 4 showed cytotoxic activity against human epidermoid carcinoma KB cells (KB3-1) with IC(50) of 8.5, 3.0, 2.5, and 4.5 microg/ml, respectively.
