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Tangeretin /603 SUPPLEMENT MONOGRAPHS TANGERETIN /603 carbon dioxide and methane; and lactate, pyruvate, succinate LITERATURE and formate. Acetate, propionate and butyrate that are not Collins MO, Gibson GR. Probiotics, prebiotics, and synbiotics: metabolized in colonocytes are absorbed from the colon and approaches for modulating the microbial ecology of the gut. Am transported via the portal circulation to the liver. These J Clin Nutr. 1999; 69(suppl): 10525-10575. short-chain fatty acids are extensively metabolized in hepato- Macfarlane GT, Cummings JH. Probiotics and prebiotics: can cytes. Acetate, propionate and butyrate that are not metabo- regulating the activities of intestinal bacteria benefit health? lized in hepatocytes are transported by the circulation to West J Med. 1999; 17:187-191. various tissues where they undergo further metabolism. Roberfroid MB. Prebiotics and synbiotics: concepts and Butyrate is an important respiratory fuel for colonocytes. nutritional properties. Br J Nutr. 1998; 80:5197-5202. INDICATIONS AND USAGE For additional Literature, see Prebiotics and Probiotics. Synbiotics are useful for the same indications as prebiotics and probiotics. Some may protect against intestinal patho- gens and ameliorate the severity of some inflammatory bowel diseases. Some may be helpful in antibiotic associated Tangeretin diarrhea, as well as some infectious and viral diarrheas. They may have some immune-enhancing, anticarcinogenic, anti- DESCRIPTION osteoporotic, glucose-modulating and lipid-modulating Tangeretin is a member of the polymethoxylated flavone, or effects. polymethoxyflavone, family of flavones. Flavones them- selves comprise a subclass of the large class of plant RESEARCH SUMMARY substances, the flavonoids. Polymethoxylated flavones See Probiotics and Prebiotics. (PMFs) exist almost exclusively in the Citrus genus, particularly in the peels and tissues of sweet oranges (Citrus CONTRAINDICATIONS, PRECAUTIONS, ADVERSE REACTIONS sinensis), the peels and tissues of bitter oranges (Citrus CONTRAINDICA TIONS Synbiotics are contraindicated in those who are hypersensi- aurantium L.) and, especially, in the peels and tissues of tive to any component of a synbiotic-containing supplement. tangerines (Citrus reticulata Blanco), including Dancy and Cleopatra tangerines and clementines. The two most com- PRECAUTIONS mon PMFs found in citrus peels and tissues are nobiletin (see Pregnant women and nursing mothers should only use Nobiletin) and tangeretin. Sinensetin is the third most synbiotic supplementation if prescribed by their physicians. common PMF found in the peels and tissues of citrus fruits. Only trace amounts of tangeretin, at best, are found in ADVERSE REACTIONS lemons (Citrus limon) and grapefruits (Citrus paradisi). The most common adverse reaction to synbiotics is flatulence. Tangeretin, like other flavonoids, is a plant secondary metabolite. Plant secondary metabolites comprise the de- INTERACTIONS fense system of plants against fungi, predators and pests, NUTRITIONAL SUPPLEMENTS among other things. Tangeretin possesses activity against Minerals (calcium, magnesium): Concomitant intake of certain fungal diseases, such as mal seco, an often fatal calcium or magnesium supplements and synbiotics may disease of horses in Argentina. However, tangere tin is not enhance the colonic absorption of these minerals. nearly as potent in this regard as is nobiletin (see Nobiletin). FOODS Tangeretin has been studied for its possible lipid-lowering Synbiotics, via their prebiotic oligosaccharides, may enhance activity, as well as for its possible anticancer activity. the colonic absorption of calcium and magnesium in foods. Tangeretin is chemically described as 5,6,7,8-tetramethoxy- DOSAGE AND ADMINISTRATION Synbiotic supplements that are currently available include 2-(4-methoxyphenyl)-4H-I-benzopyran-4-one. It is also combinations of bifidobacteria and fructo-oligosaccharides known as 4',5,6,7,8-pentamethoxyflavone, and ponkanetin (FOS), Lactobacillus GG and inulins and bifidobacteria and (ponkan is the conventional name for Citrus reticulata). Its lactobacilli and FOS or inulins. New combinations are CAS number is 48 I-53-8. Its empirical formula is C2oH2007 currently being developed. and its molecular weight is 372.37. The major chemical difference between tangeretin and nobiletin is the absence of Probiotic intake typically ranges from one to ten billion a 3'-methoxy group on the flavone skeleton in tangeretin and colony-forming units a few times a week. Doses of the presence of a 3'- methoxy group on the flavone skeleton prebiotics, in the form of synbiotics, are variable. in nobiletin. 604/TANGERETIN PDR FOR NUTRITIONAL SUPPLEMENTS The following chemical structures are described within this Antifungal: The antifungal mechanism of action of tangeretin monograph. is not entirely clear. Hypolipidemic: Apolipoprotein B (apoB) is the primary MeO apolipoprotein of low-density lipoprotein (LDL), which is responsible for carrying cholesterol to tissues. The role of tangeretin on the regulation of apoB and lipid metabolism MeO was studied in the human hepatoma cell line HepG2. It was OMeO found that tangeretin significantly lowered apoB secretion and decreased intracellular synthesis of cholesteryl esters, Tangeretin free cholesterol and triacylglycerol (TAG). The suppression of TAG synthesis went along with lowered activity of diacylglycerol (DAG) acyltransferase (DGAT) and micro- somal triglyceride transfer protein (MTP). Tangeretin was also found to activate the peroxisome proliferator-activated receptor (PPAR). PPAR is a transcription factor that has a o positive regulatory impact on fatty acid oxidation and TAG availability. Flavone Skeleton Citrus polymethoxylated flavones (PMFs), especially tanger- 4' etin, were found to significantly lower total cholesterol, very 7 3' low-density lipoprotein (VLDL) and LDL-cholesterol in hamsters with diet-induced hypercholesterolemia. The PMFs 6 reduced or tended to reduce serum triglyceride levels, as well. High-density lipoprotein cholesterol (HDL) was not affected. The mechanism of this lipid-lowering effect is Flavonoid Skeleton unclear. ACTIONS AND PHARMACOLOGY The hypolipidemic effect of tangeretin in human HepG2 ACTIONS cells along with its hypocholesterolemic effect in hamsters Tangeretin has antifungal activity against some citrus warrants further study as well as human trials to determine if pathogenic fungi. Tangeretin has possible anticancer and tangeretin might have a role in the management of hypolipidemic activities. hyperlipidemia. MECHANISM OF ACTION PHARMACOKINETICS Anticancer activity: Tangeretin was found to induce cell- The pharmacokinetics (PK) of tangeretin IS incomplete. cycle G I arrest in human colorectal carcinoma COLa 205 Almost all of the PK studies of tangeretin have been cells, inhibiting the growth of these cells. The polymethoxy- performed in animals. Tangeretin is absorbed across the lated flavone was demonstrated to inhibit the activities of small intestine to some degree. Tangeretin has very low cyclin-dependent kinases 2 (Cdk2) and 4 (Cdk4). In addition, solubility in water, but its permeability is quite high, which the Cdk inhibitors p21 and p27 were also shown to be ultimately contributes to fair bioavailability for this citrus elevated with the tangeretin treatment. Tangeretin possibly flavone. Tangeretin, following absorption, most likely enters exerted its growth inhibitory effect either via modulation of first into the lymphatics and is transported to the systemic the activities of several key G I regulatory proteins (Cdk2, circulation, which transports it to various tissues and organs, Cdk4) or via mediating the increase of Cdk inhibitors (p21, including the liver. It has been reported that tangeretin p27). More research is needed to understand this growth crosses the blood-brain barrier and, in a rat study, it was inhibitory effect of tangeretin. found in the hypothalamus, the striatum and the hippocam- pus. In contrast to polyphenolic flavonoids, tangeretin itself Tangeretin was demonstrated to inhibit the growth of human is not glucuronidated by UDP-glucuronosyltransferase to a mammary cells. In estradiol-primed human T47D mammary glucuronide. Nor does it get sulfated by sulfotransferases to a cancer cells, it was observed that tangeretin inhibited sulfate. This is because the hydroxyl groups are methylated. extracellular signal-regulated kinases 1/2 (ERK 1/2) phospho- rylation. It was thought that this kinase inhibitory action However, when the methoxy groups get demethylated, accounted, in part, for the inhibition of mammary cell phenolic hydroxyl groups open up, which can be glucuroni- growth. dated or sulfated. Metabolites of tangeretin that have been SUPPLEMENT MONOGRAPHS TANGERETIN /605 found in rat urine include monohydroxytetramethoxy fla- One group has reported that formulations containing citrus vone, dihydroxytrimethoxy flavone and glucuronide conju- PMFs, primarily tangeretin, show some promise as cholester- gates of the flavones. ol- and triacylglycerol-Iowering agents. These conclusions were based upon both in vitro and animal studies. One of the INDICATIONS AND USAGE same researchers, in collaboration with others, has also Clinical evidence in support of the claim that the citrus reported that PMFs ameliorate fructose-induced hyperglycer- flavonoid tangeretin is therapeutic in breast and some other idemia and other metabolic abnormalities associated with cancers is lacking. There is very preliminary nonclinical data insulin
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