RRC ID 64155
Author Nakamura K, Yang JH, Sato E, Miura N, Wu YX.
Title Effects of Hydroxy Groups in the A-Ring on the Anti-proteasome Activity of Flavone.
Journal Biol Pharm Bull
Abstract The ubiquitin-proteasome pathway plays an important role in regulating apoptosis and the cell cycle. Recently, proteasome inhibitors have been shown to have antitumor effects and have been used in anticancer therapy for several cancers such as multiple myeloma. Although some flavones, such as apigenin, chrysin and luteolin, have a specific role in the inhibition of proteasome activity and induced apoptosis in some reports, these findings did not address all flavone types. To further investigate the proteasome-inhibitory mechanism of flavonoids, we examined the inhibitory activity of 5,6,7-trihydroxyflavone, baicalein and 5,6,7,4'-tetrahydroxyflavone, scutellarein on extracted proteasomes from mice and cancer cells. Unlike the other flavones, baicalein and scutellarein did not inhibit proteasome activity or accumulate levels of ubiquitinated proteins. These results indicate that flavones with hydroxy groups at positions 5, 6 and 7 of the A-ring lack the anti-proteasome function.
Volume 38(6)
Pages 935-40
Published 2015-1-1
DOI 10.1248/bpb.b15-00018
PMID 25810454
MeSH Animals Antineoplastic Agents / chemistry Antineoplastic Agents / pharmacology* Antineoplastic Agents, Phytogenic / chemistry Antineoplastic Agents, Phytogenic / pharmacology* Apigenin / chemistry Apigenin / pharmacology Apoptosis Flavanones / chemistry Flavanones / pharmacology Flavones / chemistry Flavones / pharmacology* HCT116 Cells Humans Jurkat Cells Molecular Structure Neoplasms / metabolism* Phytotherapy Plant Extracts / chemistry Plant Extracts / pharmacology* Proteasome Endopeptidase Complex / metabolism* Proteasome Inhibitors / chemistry Proteasome Inhibitors / pharmacology* Rabbits Structure-Activity Relationship
IF 1.863
Human and Animal Cells Jurkat