RESUMO
A major hallmark of Alzheimer's disease is the cerebral accumulation and resulting cytotoxicity of amyloid-ß peptides, particularly Aß42. In this study, we used an MTT assay to investigate the inhibitory activity of biflavonoids 1-22 against Aß42 cytotoxicity in PC-12 cell cultures. Cytoprotective effects were observed for the following amentoflavone type biflavonoids: podocarpusflavone B 8, isoginkgetin 10, sciadopitysin 13, and kayaflavone 15. These biflavonoids exhibited strong activity in tested compounds, with EC50 values of 5.18, 10.77, 9.84, and 5.29 µM, respectively. Cell viability tests of PC-12 cells revealed that biflavonoids 13 and 15 had stronger inhibitory activities than apigenin 23 and (-)-epigallocatechin gallate 24.
Assuntos
Peptídeos beta-Amiloides/toxicidade , Biflavonoides/química , Biflavonoides/farmacologia , Sobrevivência Celular/efeitos dos fármacos , Fragmentos de Peptídeos/toxicidade , Substâncias Protetoras/química , Substâncias Protetoras/farmacologia , Animais , Células PC12 , Ratos , Relação Estrutura-AtividadeRESUMO
Four novel benzo[j]fluoranthene derivatives, hypoxylonols C (3), D (4), E (5), and F (6), have been isolated from the mushroom Hypoxylon truncatum, together with two known benzo[j]fluoranthene derivatives, hypoxylonols A (1) and B (2). The structures were established by analysis of NMR spectroscopic data and X-ray diffraction data. Compounds 4 and 5 showed antiproliferative activity against HUVECs (human umbilical vein endothelial cells) and HUAECs (human umbilical artery endothelial cells).
Assuntos
Agaricales/química , Fluorenos/isolamento & purificação , Fluorenos/química , Fluorenos/farmacologia , Células Endoteliais da Veia Umbilical Humana/efeitos dos fármacos , Humanos , Estrutura Molecular , Ressonância Magnética Nuclear Biomolecular , Difração de Raios XRESUMO
Three new diterpenes, myrocin D (1), libertellenone E (2), and libertellenone F (3), and a new isocoumarin, decarboxyhydroxycitrinone (4), were isolated from the marine fungus Arthrinium sacchari, together with three known compounds (5-7). The structures of 1-4 were elucidated from spectroscopic data (NMR, MS, IR), and the absolute configurations of 1-3 were determined by X-ray diffraction analysis. The antiangiogenic activity of these compounds was evaluated by measuring their antiproliferation effects on human umbilical vein endothelial cells (HUVECs) and human umbilical artery endothelial cells (HUAECs). Compounds 4-7 showed inhibitory activity.
Assuntos
Inibidores da Angiogênese/isolamento & purificação , Ascomicetos/química , Diterpenos/isolamento & purificação , Isocumarinas/isolamento & purificação , Inibidores da Angiogênese/química , Inibidores da Angiogênese/farmacologia , Cristalografia por Raios X , Diterpenos/química , Diterpenos/farmacologia , Células Endoteliais/efeitos dos fármacos , Humanos , Isocumarinas/química , Isocumarinas/farmacologia , Biologia Marinha , Estrutura Molecular , Ressonância Magnética Nuclear Biomolecular , Cordão Umbilical/citologia , Cordão Umbilical/efeitos dos fármacosRESUMO
Three novel p-terphenyl compounds, named boletopsins A (1), B (2), and C (3), and four known analogues (4-7) were isolated from fruiting bodies of the mushroom Boletopsis leucomelas. Compounds 1-7 were tested for KDR kinase inhibitory activity, and boletopsin C (3) was found to have an IC(50) value of 70.7 microM. Compound 3 also showed inhibition of proliferation of human umbilical vein endothelial cells, with an IC(50) value of 9.04 microM.