Journal
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
Volume 17, Issue 18, Pages 5177-5181Publisher
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2007.06.096
Keywords
nobiletin; nobiletin metabolites; demethylnobiletin; 3',4'-didemethylnobiletin; anti-inflammatory activity
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Nobiletin, a major component of polymethoxyflavones in citrus fruits, has a broad spectrum of health beneficial properties including anti-inflammatory and anti-carcinogenic activities. The metabolite identification of nobiletin in mouse urine has concluded that it undergoes mono-demethylation (3 '- and 4 '-deinethylnobiletin) and di-demethylation (3 ',4 '-didemethylnobiletin) metabolic pathway. Biological screening of nobiletin and its metabolites has revealed that the metabolites possess more potent anti-inflammatory activity than their parent compound. Therefore, this letter reports the identification of nobiletin metabolites and their anti-inflammatory activity against LPS-induced NO production and iNOS, COX-2 protein expression in RAW264.7 macrophage. (c) 2007 Elsevier Ltd. All rights reserved.
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