Nobiletin, a naturally occurring polymethyl flavone (PMF) present in citrus fruits and 3',4'-didemethylnobiletin (DDMN), the major metabolite of nobiletin in mouse urine, have been shown to have a broad spectrum of beneficial attributes. This study focuses on the anti-carcinogenic and anti-inflammatory properties of these compounds. The results demonstrated that both nobiletin and DDMN were able to induce cytotoxicity, cell cycle arrest and apoptosis in COLO205 cancer cells. Nobiletin showed to be more effective in inducing apoptosis than its metabolite DDMN. In addition, in COLO205 cancer cells, treatment with nobiletin resulted in G1 phase cell cycle arrest, whereas DDMN caused G2/M phase arrest. In anti-inflammatory analysis, DDMN showed a greater degree of anti-inflammatory activity in nitrite assays. In addition, Western blotting analysis also indicated that DDMN is a better inhibitor of iNOS and COX-2. These results suggest that nobiletin and DDMN may exert different bioactivity by their targeting in different components.

Anti-carcinogenic and anti-inflammatory properties of nobiletin and 3',4'-didemethylnobiletin

241st National Meeting (2011)

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