Anti-inflammatory property of the urinary metabolites of nobiletin in mouse

Anti-inflammatory property of the urinary metabolites of nobiletin in mouse
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DOI:
10.1016/j.bmcl.2007.06.096
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发表时间:
2007-09-15
影响因子:
2.7
通讯作者:
Ho, Chi-Tang
Ho, Chi-Tang
中科院分区:
医学4区
文献类型:
--
作者:
Li, Shiming;Sang, Shengmin;Ho, Chi-Tang

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诺比莱汀是柑橘类水果中多甲氧基黄酮的主要成分,具有广泛的有益健康特性,包括抗炎和抗癌活性。对小鼠尿中nobiletin代谢产物的鉴定表明,nobiletin经历了单脱甲基(3‘-和4’-去甲基nobiletin)和二脱甲基(3‘,4’-didemthylnobiletin)的代谢途径。诺比林及其代谢物的生物筛选表明,这些代谢物比它们的母体化合物具有更强的抗炎活性。因此,本文报道了nobiletin代谢产物的鉴定及其对内毒素诱导的巨噬细胞NO产生和iNOS、COX-2蛋白表达的抗炎作用。(C)2007爱思唯尔有限公司。保留所有权利。
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.