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CAS No.: 10236-47-2

Synonyms: 3',4',5,6,7,8-hexamethoxyflavone

Melting Point: 137 - 138degree C

Appearance£ºColorless Needle


Anti-cancer, Anti- epiphyte,Anti-inflammation,Anti-allergic, Anticholinesterase(cholinergic agonist,Alzheimer's disease)Anti-histamic, Fungicide.


1. Inhibitory Effect of Citrus Nobiletin on Phorbol Ester-induced Skin Inflammation, Oxidative Stress, and Tumor Promotion in Mice

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The intake of citrus fruits has been suggested as a way to prevent the development of some types of human cancer. Nitric oxide (NO) is closely associated with the processes of epithelial carcinogenesis. We attempted a search for NO generation inhibitors in Citrus unshiu . The active constituent was traced by an activity-guiding separation. NO and superoxide (O 2 - ) generation was induced by a combination of lipopolysaccharide and IFN- in mouse macrophage RAW 264.7 cells, and by 12- O -tetradecanoylphorbol-13-acetate (TPA) in differentiated human promyelocyte HL-60, respectively. Expression of inducible NO synthase and cyclooxygenase 2 proteins were detected by Western blotting. The in vivo anti-inflammatory and antitumor promoting activities were evaluated by topical TPA application to ICR mouse skin with measurement of edema formation, epidermal thickness, leukocyte infiltration, hydrogen peroxide production, and the rate of proliferating cell nuclear antigen-stained cells. As a result, nobiletin, a polymethoxyflavonoid, was identified as an inhibitor of both NO and O 2 - generation. Nobiletin significantly inhibited two distinct stages of skin inflammation induced by double TPA application [first stage priming (leukocyte infiltration) and second stage activation (oxidative insult by leukocytes)] by decreasing the inflammatory parameters. It also suppressed the expression of cyclooxygenase-2 and inducible NO synthase proteins and prostaglandin E 2 release. Nobiletin inhibited dimethylbenz[ a ]anthracene (0.19 ¦Ìmol)/TPA (1.6 nmol)-induced skin tumor formation at doses of 160 and 320 nmol by reducing the number of tumors per mouse by 61.2% ( P < 0.001) and 75.7% ( P < 0.001), respectively. The present study suggests that nobiletin is a functionally novel and possible chemopreventive agent in inflammation-associated tumorigenesis.

2. Novel anti-inflammatory actions of nobiletin, a citrus polymethoxy flavonoid, on human synovial fibroblasts and mouse macrophages. Click here for detail, ¡ï¡ï

We previously reported that nobiletin (5,6,7,8,3',4'-hexamethoxy flavone), a citrus polymethoxy flavonoid, effectively interferes with the production of promatrix metalloproteinase (proMMP)-9/progelatinase B in rabbit synovial fibroblasts [J. Rheumatol. 27 (2000) 20]. In this paper, we further examine the effects of nobiletin on the production of cyclooxygenases (COXs), prostaglandin (PG) E(2), and proinflammatory cytokines in human synovial fibroblasts and the mouse macrophage J774A.1 cell line. Nobiletin suppressed the interleukin (IL)-1-induced production of PGE(2) in human synovial cells in a dose-dependent manner (<64 microM). Additionally, it selectively downregulated COX-2, but not COX-1 mRNA expression. Nobiletin also interfered with the lipopolysaccharide-induced production of PGE(2) and the gene expression of proinflammatory cytokines including IL-1alpha, IL-1beta, TNF-alpha and IL-6 in mouse J774A.1 macrophages. In addition, nobiletin downregulated the IL-1-induced gene expression and production of proMMP-1/procollagenase-1 and proMMP-3/prostromelysin-1 in human synovial fibroblasts. In contrast, production of the endogenous MMP inhibitor, TIMP-1, was augmented by nobiletin. These anti-inflammatory actions of nobiletin are very similar to those of anti-inflammatory steroids such as dexamethasone, and the upregulation of TIMP-1 production is a unique action of nobiletin. Therefore, these results further support the notion that nobiletin is likely to be a candidate for characterization as a novel immunomodulatory and anti-inflammatory drug.

3. Citrus nobiletin inhibits azoxymethane-induced large bowel carcinogenesis in rats, Click here for detail, ¡ï¡ï

The inhibitory effects of dietary feeding of citrus nobiletin on azoxymethane (AOM)-induced rat colon carcinogenesis using a long-term bioassay were investigated. Five-week old male F344 rats were initiated with two weekly subcutaneous injections of AOM (20 mg/kg bw) to induce colonic tumors. They were also given the diets containing 0.01% or 0.05% nobiletin for 34 weeks, starting one week after the last dosing of AOM. At the end of the study, the incidence of colonic adenocarcinoma were 67% in the AOM alone group, 55% in the AOM¡ú0.01% nobiletin group, 35% (p < 0.05) in the AOM¡ú0.05% nobiletin group. Also, nobiletin feeding reduced the cell-proliferation activity, increased the apoptotic index, and decreased the prostaglandin E _{2} content in colonic adenocarcinoma and/or colonic mucosa. These findings might suggest that citrus nobiletin has chemopreventive ability against AOM-induced rat colon carcinogenesis.

4. Nobiletin: efficient and large quantity isolation from orange peel extract, Click here for detail, ¡ï¡ï

It is known that nobiletin possesses anticancer, antiviral and anti-inflammatory activities. Recently, the demand for nobiletin in large quantities and high purity has increased. However, conventional normal-phase silica gel chromatography and C 18 -reverse-phase separation methods cannot satisfy the requirement of pure and gram scale nobiletin in a timely manner. In exploring the composition and the biological activities of polymethoxyflavones from sweet orange ( Citrus sinensis ) peel, we developed an efficient isolation method for nobiletin. By employing this methodology, pure nobiletin, in gram quantities, was obtained in only one purification cycle. The orange peel extract was loaded onto a silica gel flash column and eluted by a mixed solvent system of ethyl acetate and hexanes, and the fractions collected. Upon combination of the eluted fractions, mainly containing nobiletin and 5,6,7,4 -tetramethoxyflavone, and concentration under reduced pressure, the resultant residue was loaded onto a Regis chiral column. Gram amounts of nobiletin and 5,6,7,4 -tetramethoxyflavone were then eluted with ethanol and hexanes, respectively. Copyright ? 2005 John Wiley & Sons, Ltd.

5. Inhibition of cell proliferation by nobiletin, a dietary phytochemical, associated with apoptosis and characteristic gene expression, but lack of effect on early rat hepatocarcinogenesis in vivo, Click here for detail, ¡ï¡ï

Dietary phytochemicals can inhibit the development of certain types of tumors. We here investigated the effects of nobiletin (Nob), garcinol (Gar), auraptene (Aur), ¦Â-cryptoxanthin- and hes-peridine-rich pulp (CHRP) and 1,1'-acetoxychavicol acetate (ACA) on hepatocarcinogenesis in a rat medium-term liver bioassay, and also examined their influence on cell proliferation, cell cycle kinetics, apoptosis and cell invasion of rat and human hepatocellular carcinoma (HCC) cells, MH1C1 and HepG2, respectively. While there were no obvious suppressive effects on the development of putative preneoplastic liver lesions, inhibition of hepatocarcinoma cell proliferation was evident in the Nob group. Nob also caused G2/M cell cycle arrest and apoptosis. Microarray analysis identified a set of genes specifically regulated by Nob, and these are likely to be involved in the observed growth suppression of HCC cells. These results suggest that phytochemicals might have chemopreventive potential in late stages of hepatocarcinogenesis.