Drug intelligence / Profile preview

5-demethylnobiletin

Development stage
Preclinical
Modality
Small Molecules
Administration
Oral
01

Overview

5-demethylnobiletin is a naturally occurring polymethoxyflavone, primarily found in citrus fruits, especially in their peels and as a metabolite of nobiletin formed during storage. It exhibits a range of **pharmacological activities**, including anti-inflammatory, anticancer, antioxidant, and neuroprotective effects. Mechanistically, 5-demethylnobiletin acts through regulation of multiple signaling pathways, including direct inhibition of 5-lipoxygenase (5-LOX), and modulation of MAPK/ERK, PKC, PKA, JAK2/STAT3, ROS-AKT/mTOR, and caspase-dependent apoptosis pathways. It induces cell cycle arrest and apoptosis in tumor cells (notably glioblastoma), suppresses inflammation by inhibiting iNOS and COX-2 expression, and has demonstrated activity against various cancers and inflammation-related diseases. Its metabolites often show stronger biological activities than the parent compound[1][2][3][5].

Other names
5-O-demethylnobiletin5-hydroxy Nob5DN5-demethylnobiletin-RM2-(3,4-dimethoxyphenyl)-5-hydroxy-6,7,8-trimethoxychromen-4-one5-dimethylnobiletin
02

Targets

ID1 (Inhibitor of DNA binding protein 1)

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