85374-52-3Relevant articles and documents
B-Ring-modified and/or 5-demethylated nobiletin congeners: Inhibitory activity against pro-MMP-9 production
Oshitari, Tetsuta,Okuyama, Yuji,Miyata, Yoshiki,Kosano, Hiroshi,Takahashi, Hideyo,Natsugari, Hideaki
, p. 7085 - 7092 (2012/01/02)
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.