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Volume 13, Issue 5, Pages 310-317 (9 May 2006)


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Structure–activity relations of inhibitory effects of various flavonoids on lipopolysaccharide-induced prostaglandin E2 production in rat peritoneal macrophages: Comparison between subclasses of flavonoids

Y. Takano-IshikawaaCorresponding Author Informationemail address, M. Gotoa, K. Yamakiab

Received 13 January 2005; accepted 21 January 2005.

Abstract 

A study of the structure–activity relations of the inhibitory effect of flavonoids on lipopolysaccharide (LPS)-induced prostaglandin production was carried out via a comparative examination of 39 flavonoids and related compounds. A comparison of the subclasses showed that flavones were most effective, followed by flavanones. Flavonols were less effective than those two groups. These results suggest that the C2–C3 double-bond and 4-oxo functional group of the C-ring are important factors for the high inhibition activities. Flavonoids showed the strongest inhibitory effect on the expression of Cox-2 protein. These results help to explain part of the reason for the pharmacological efficacy of flavonoids as anti-inflammatory compounds.

a National Food Research Institute, Kannondai, Tsukuba, Ibaraki, Japan

b Japan International Research Center for Agricultural Sciences, 1-1 Ohwashi, Tsukuba, Ibaraki 305-8686, Japan

Corresponding Author InformationCorresponding author. Tel.: +81298388055; fax: +81298387996.

PII: S0944-7113(05)00171-6

doi:10.1016/j.phymed.2005.01.016


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