Nobiletin (NOB), a polymethoxyflavone, has a few pharmacological activities, including anti-inflammation and anti-cancer effects. Nobiletin, up to 100 μM without cytotoxicity, significantly decreased motility, migration and invasion as well as enzymatic activities, protein levels and mRNA expressions of matrix metalloproteinase (MMP)-2 and MMP-9 in U2OS and HOS cells[3]. NOB significantly improves metabolic fitness in naturally aged mice fed with a regular diet (RD). Furthermore, NOB enhances healthy aging in mice fed with a high-fat diet (HF)[4]. Nobiletin plays a modulatory role in adipocytes via induction of browning in 3T3-L1 white adipocytes and activation of HIB1B brown adipocytes combined with amelioration of stress in adipocytes[5]. Nobiletin improved cognitive deficits and the pathological features of AD, such as Aβ pathology, hyperphosphorylation of tau, and oxidative stress, in animal models of AD. In addition, nobiletin improved motor and cognitive deficits in PD animal models[6].
Nobiletin/川陈皮素 细胞实验
Cell Line
Concentration
Treated Time
Description
References
Primary rat astrocytes
5, 10, 20, 40 µM
24 hours
NOB alone did not produce any cytotoxic effects and protected cells against Aβ42-induced cytotoxicity in a concentration-dependent manner
Redox Biol. 2024 Jul;73:103197.
Primary rat astrocytes
20, 40 µM
24 hours
NOB significantly reduced the Aβ42-induced mRNA expression levels of pro-inflammatory markers
Redox Biol. 2024 Jul;73:103197.
Enteric neural stem cells (ENSCs)
20, 40, 80, 100 µM
24, 48, 72 hours
Nobiletin at 40 and 80 μM significantly promoted PA-induced ENSC proliferation and significantly decreased caspase3/7 activity, indicating that Nobiletin protected against PA-induced ENSC damage by promoting proliferation and inhibiting apoptosis.
Mol Med. 2024 Aug 2;30(1):113.
Nobiletin/川陈皮素 动物实验
Species
Animal Model
Administration
Dosage
Frequency
Description
References
C57BL/6J mice
High-fat diet-induced obesity model
Gastric gavage
100 mg/kg/d and 200 mg/kg/d
Once daily for 4 weeks
Nobiletin improved obesity-related indices and abnormal glucose tolerance in HFD-fed mice, reduced colonic lipid accumulation and peroxidation, promoted enteric nerve regeneration, and regulated enteric nerve cell proliferation through the GDNF/AKT/FOXO3a/P21 pathway.
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