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Updated: May 28, 2026
Preparation of Naringenin Solution for In Vivo Application
Published on: August 10, 2021
B-Ring-modified and/or 5-demethylated nobiletin congeners: inhibitory activity against pro-MMP-9 production
Tetsuta Oshitari1, Yuji Okuyama, Yoshiki Miyata
1School of Pharmaceutical Sciences, Teikyo University, 1091-1 Suarashi, Midori-ku, Sagamihara, Kanagawa 252-5195, Japan. ostr@pharm.teikyo-u.ac.jp
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.