Scytonemides A and B, cyclic peptides with 20S proteasome inhibitory activity from the cultured cyanobacterium Scytonema hofmanii.
J Nat Prod
; 73(11): 1927-32, 2010 Nov 29.
Article
em En
| MEDLINE
| ID: mdl-21058727
ABSTRACT
Two cyclic peptides, scytonemides A (1) and B (2), were isolated from the cultured fresh water cyanobacterium Scytonema hofmannii (UTEX 1834) by bioassay-guided fractionation using a proteasome inhibition assay. The planar structures of the compounds were determined by a combination of MS and 1D and 2D NMR spectroscopy. The advanced Marfey's method was used to determine the absolute configuration of both peptides. Scytonemide A possesses an unusual imino linkage, while scytonemide B is a depsipeptide containing 3-hydroxyoctanoic acid in the macrocycle. Both isolates were evaluated for their inhibition of the 20S proteasome, and scytonemide A displayed an IC(50) value of 96 nM, while scytonemide B was inactive at 50 µM.
Texto completo:
1
Coleções:
01-internacional
Base de dados:
MEDLINE
Assunto principal:
Cianobactérias
/
Depsipeptídeos
/
Inibidores de Proteassoma
/
Antineoplásicos
Limite:
Humans
Idioma:
En
Revista:
J Nat Prod
Ano de publicação:
2010
Tipo de documento:
Article