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].
5-O-Demethylnobiletin 细胞实验
Cell Line
Concentration
Treated Time
Description
References
CL13 mouse lung cancer cells
5DN: 20 µM; M1: 1 µM; M2: 5 µM
24 hours
To investigate the effects of 5DN and its metabolites M1 and M2 on the cell cycle of CL13 mouse lung cancer cells. Results showed that 5DN and M1 significantly increased the proportion of cells in G2/M phase, while M2 slightly increased the proportion of cells in both G1/G0 and G2/M phases.
Food Funct. 2017 Mar 22;8(3):954-963
A549 human lung cancer cells
5DN: 20 µM; M1: 2 µM; M2: 10 µM
24 hours
To investigate the effects of 5DN and its metabolites M1 and M2 on the cell cycle of A549 human lung cancer cells. Results showed that 5DN and M2 significantly increased the proportion of cells in G1/G0 phase, while M1 significantly increased the proportion of cells in G2/M phase.
Food Funct. 2017 Mar 22;8(3):954-963
5-O-Demethylnobiletin 动物实验
Species
Animal Model
Administration
Dosage
Frequency
Description
References
Female A/J mice
NNK-induced lung tumor model
Dietary administration
0.025% or 0.05% (w/w) 5DN
16 weeks
To investigate the inhibitory effects of 5DN on NNK-induced lung tumorigenesis. Results showed that 5DN significantly reduced the number and volume of lung tumors and exhibited anti-proliferative effects.
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