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ID: ALA1926519

Journal: Bioorg Med Chem

Title: B-Ring-modified and/or 5-demethylated nobiletin congeners: inhibitory activity against pro-MMP-9 production.

Authors: Oshitari T, Okuyama Y, Miyata Y, Kosano H, Takahashi H, Natsugari H.

Abstract: Three metabolites and 12 analogues of nobiletin (1) were synthesized. Whereas nobiletin derivatives 2-4 inhibited pro-MMP-9 production similarly in both PMA- and TNF-α-stimulated human lens epithelial cells, the 2'-hydroxylated analogue 5a exerted marked inhibitory effects (IC(50): 0.4 μM) on PMA-treated cells, which were 170-fold more potent than those on TNF-α-treated cells. This activity may be closely related to PKC-mediated transcriptional regulation of pro-MMP-9.

CiteXplore: 22047798

DOI: 10.1016/j.bmc.2011.10.001