Nobiletin is one of the citrus bioflavonoids. Limited laboratory and rodent studies indicate nobiletin to have antiinflammatory and antioxidnat properties.
Sytrinol has polymethoxylated flavones (PMFs) that decrease apoprotein B, a structural protein needed for endogenous synthesis of LKL cholesterol. PMFs (tangeritin and nobiletin) decrease diacylglycerol acetyl transferase, a liver enzyme needed for endogenous synthesis of triblycerides. Sytrinol is available as a supplement.
Nobiletin Research Update
Antagonistic effects of nobiletin, a polymethoxyflavonoid, on
eosinophilic airway inflammation of asthmatic rats and relevant
mechanisms.
Life Sci. 2005 Dec 7; Department of Pharmacology, Nanjing Medical
University, Nanjing, PR China.
Eosinophils are known to be the important effector cells in asthmatic
airway inflammation. The purpose of this study was to investigate the
effects of nobiletin, a polymethoxyflavonoid, on eosinophilic airway
inflammation of asthmatic rats, and explore its possible mechanisms.
Animals were actively sensitized by subcutaneous injection of ovalbumin
(OVA). The inflammation in lung tissues of asthmatic rats was observed by
hematoxylin and eosin (HE) staining. These results indicated that
nobiletin could inhibit the eosinophilic airway inflammation. Lowering the
levels of Eotaxin, relieving airway infiltration of eosinophils and
promoting apoptosis of eosinophils by enhancing expression of Fas mRNA may
be important mechanisms for nobiletin to antagonize eosinophilic airway
inflammation of asthmatic rats.
Characteristic rat tissue accumulation of nobiletin, a chemopreventive
polymethoxyflavonoid, in comparison with
luteolin.
Biofactors. 2002;16(3-4):73-82.
Nobiletin, a polymethoxyflavonoid, is an effective anti-inflammatory and
chemopreventive phytochemical found in citrus fruits. We compared the absorption
and metabolism characteristics of nobiletin with those of luteolin (LT) in male SD
rats. Each flavonoid (67.1 micromol/kg of body weight) was given separately by
gastric intubation, and then concentrations were measured at 1, 4, and 24 hours
after administration. In the digestive organs, Nobiletin showed a notable tendency for
localizing into the mucous membrane and muscularis from 1 to 4 hours, in
contrast to LT, though both nobiletin and LT were completely excreted within 24 hours.
Further, significant amounts of nobiletin were detected in the whole liver and kidney
specimens, whereas LT accumulation was slight. Although serum concentrations of
nobiletin from 1 to 4 hours were comparable to those of LT, urinary concentrations of
LT were significantly higher from 4 to 24 hours. Following glucuronidase/sulfatase
treatments of urinary materials, we detected 3 types of mono-demethylated
nobiletin,
including 3'-demethyl-NOB, and two di-demethylated types, as well as
3'-demethyl-NOB alone in serum samples using liquid chromatography-mass spectral
analysis. Our results suggest that the metabolic properties of
polymethoxyflavonoids are distinct from those of other general flavonoids,
because of their wide distribution and accumulation in tissue.
Novel anti-inflammatory actions of nobiletin, a citrus polymethoxy
flavonoid, on human synovial fibroblasts and mouse macrophages.
Biochem Pharmacol. 2003 Jun 15;65(12):2065-71.
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.
5-HTP
CoQ10
Vinpocetine
DMAE
Choline
Saw palmetto
Nobiletin as a tyrosinase inhibitor from the peel of Citrus fruit.
Biol Pharm Bull. 2002 Jun;25(6):806-8.
A tyrosinase inhibitor was isolated from the peel of Citrus fruit by
activity-guided fractionation, and identified as
3',4',5,6,7,8-hexamethoxyflavone (nobiletin) by comparison with reported
spectral data. Nobiletin exhibited more potency than Kojic acid used as a positive control, and it was found to
be potentially an effective inhibitor of the production of melanin.