Nobiletin
Nobiletin is a polymethoxylated flavone derived from the peel of citrus fruits. Nobiletin displays anti-inflammatory, anticancer, antioxidative, neuroprotective, cognition enhancing, antidepressant, and anti-obesity properties. In vitro, Nobiletin decreases iNOS expression and levels of NO and also inhibits NF-κB activity. In a variety of cancer cell lines, Nobiletin induces cell cycle arrest and inhibits cellular proliferation through several mechanisms, including inhibition of Ras and MAPK/ERK signaling, downregulation of Bcl-2 and COX-2 levels, upregulation of Bax and caspase-3 expression, and downregulation of matrix metalloproteinase 2 and CXCR4 expression. In aged mice and animal models of Alzheimer’s disease, nobiletin increased glutathione peroxidase and superoxide dismutase activity and decreased phosphorylation of tau, attenuating learning and memory impairments. In other animal models, this compound displays potential use as an antidepressant, attenuating stress-induced deficits in BDNF, TrkB, and synapsin I in the hippocampus. Additionally, nobiletin displays anti-obesity effects in vivo, increasing levels of PPARα/γ, GLUT4, adiponectin, fatty acid synthase, and other enzymes, resulting in decreased body weight gain in overweight animals. Nobiletin may act as a positive allosteric modulator at AMPA receptors by increasing phosphorylation of the GluR1 subunit.
References PubMed ID：:http://www.ncbi.nlm.nih.gov/pubmed/18949484
| Cas No. |
478-01-3 |
|---|---|
| Purity |
≥97% |
| Formula |
C21H22O8 |
| Formula Wt. |
402.39 |
| IUPAC Name |
2-(3,4-dimethoxyphenyl)-5,6,7,8-tetramethoxychromen-4-one |
| Appearance |
White to off white powder |
Yoshigai E, Machida T, Okuyama T, et al. Citrus nobiletin suppresses inducible nitric oxide synthase gene expression in interleukin-1β-treated hepatocytes. Biochem Biophys Res Commun. 2013 Sep 13;439(1):54-9. PMID: 23958298.
Nakajima A, Aoyama Y, Nguyen TT, et al. Nobiletin, a citrus flavonoid, ameliorates cognitive impairment, oxidative burden, and hyperphosphorylation of tau in senescence-accelerated mouse. Behav Brain Res. 2013 Aug 1;250:351-60. PMID: 23714077.
Ma X, Jin S, Zhang Y, et al. Inhibitory Effects of Nobiletin on Hepatocellular Carcinoma In Vitro and In Vivo. Phytother Res. 2013 Jul 1. [Epub ahead of print]. PMID: 23818450.
Aoki K, Yokosuka A, Mimaki Y, et al. Nobiletin induces inhibitions of Ras activity and mitogen-activated protein kinase kinase/extracellular signal-regulated kinase signaling to suppress cell proliferation in C6 rat glioma cells. Biol Pharm Bull. 2013;36(4):540-7. PMID: 23546290.
Lee YS, Cha BY, Choi SS, et al. Nobiletin improves obesity and insulin resistance in high-fat diet-induced obese mice. J Nutr Biochem. 2013 Jan;24(1):156-62. PMID: 22898571.
Baek SH, Kim SM, Nam D, et al. Antimetastatic effect of nobiletin through the down-regulation of CXC chemokine receptor type 4 and matrix metallopeptidase-9. Pharm Biol. 2012 Oct;50(10):1210-8. PMID: 22853317.
