5-Lipoxygenase inhibitors isolated from Gardeniae Fructus.

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Abstract
Five 5-lipoxygenase inhibitors chlorogenic acid (1), 6"-p-coumaroyl genipin gentiobioside (2), 3,4-di-O-caffeoylquinic acid (3), 3-O-caffeoyl-4-O-sinapoylquinic acid (4) and 3,5-di-O-caffeoyl-4-O-(3-hydroxy-3-methyl)glutaroylquinic acid (5), were isolated from Gardeniae Fructus. The structures of the new compounds (2, 4 and 5) were elucidated on the basis of spectral data and chemical evidence. These hydroxycinnamic acid derivatives inhibit 5-lipoxygenase activity, and 3 was the most potent inhibitor. The inhibitory effects were enhanced on methylation of the carboxyl group(s) of 1, 3, 4 and 5, and the ID50 values of the methyl esters of 3, 4 and 5 were of the order of 10-8 M.