5-O-Demethylnobiletin reduced the oedema formation, cell infiltration, and tissue damage in the inflammation induced by TPA (12- O-tetradecanoylphorbol 13-acetate) in mouse ears, along with the acute oedema induced by carrageenan in mouse paws and the acute PLA (2)-induced (phospholipase A (2)) oedema in mouse paws[2]. 5-Demethylnobiletin and gardenin A (10 - 20 μM) potently induce neurite outgrowth in PC12 cells, accompanied by the expression of neuronal differentiation and synapse formation marker proteins, growth-associated protein-43 (GAP-43), and synaptophysin[3]. Three novel metabolites were identified in mice after oral administration of 5-demethylniobiletin. These metabolites exhibited strong inhibitory effects against human colon cancer cells. For example, metabolites (2 - 4) showed IC50 of 0.12, 5.5, and 4.2 μM in SW620 cells, respectively, while 5-demethylnobiletin at 10 μM only caused 37% inhibition after 72 h of treatment[4].
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