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(12) Patent Application Publication (10) Pub. No.: US 2013/0045289 A1 Cho Et Al

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(12) Patent Application Publication (10) Pub. No.: US 2013/0045289 A1 Cho Et Al US 2013 0045289A1 (19) United States (12) Patent Application Publication (10) Pub. No.: US 2013/0045289 A1 Cho et al. (43) Pub. Date: Feb. 21, 2013 (54) COMPOSITION FOR PROMOTING THE (30) Foreign Application Priority Data ACTIVITY OF PEROXSOME PROLIFERATOR-ACTIVATED Nov. 26, 2009 (KR) ........................ 10-2009-O115O24 RECEPTOR-DELTA Publication Classification (75) Inventors: Si Young Cho, Seoul (KR); Pil Joon (51) Int. Cl. Park, Yongin-si (KR); Ji Hae Lee, A61E36/282 (2006.01) Yongin-si (KR); Dae Bang Seo, A6IP 25/28 (2006.01) Yongin-si (KR); Sang Jun Lee, A6IP 25/6 (2006.01) Seongnam-si (KR) A6IP3/00 (2006.01) (73) Assignee: AMOREPACIFIC CORPORATION (52) U.S. Cl. ....................................................... 424/740 (57) ABSTRACT (21) Appl. No.: 13/511,964 Disclosed is a composition for promoting the activity of per oxisome proliferator-activated receptor-ö (PPAR-8), which (22) PCT Filed: Nov. 25, 2010 contains Artemisia vulgaris extracts or Artemisia capillaris extracts as active ingredients. The composition is effective in (86) PCT NO.: PCTAKR1O/O84O4. strengthening muscles, improving endurance and memory, S371 (c)(1), and preventing and alleviating the symptoms of dementia or (2), (4) Date: May 24, 2012 Parkinson's disease. Patent Application Publication Feb. 21, 2013 Sheet 1 of 4 US 2013/0045289 A1 Fig. 1 0.45 0.40 EC50: 7ppm 0.35 0.30 0.25 0.20 0.15 O. 10 0.05 0.00 0 0 (0.2 0.4 0.6 0.8 1 0 12 1.4 1, 6 1.8 Artemisia iWayOmogi extract ( ug/ml) Patent Application Publication Feb. 21, 2013 Sheet 2 of 4 US 2013/0045289 A1 Fig.2 600000 500000 400000 Y 300000 200000 100000 Patent Application Publication Feb. 21, 2013 Sheet 4 of 4 US 2013/0045289 A1 Fig. 4 2.5 1.5 0.5 Control Artemisia iWayOmogi US 2013/0045289 A1 Feb. 21, 2013 COMPOSITION FOR PROMOTING THE memory. The composition may be variously used in the field ACTIVITY OF PEROXSOME of food, health-food Supplements or pharmaceuticals. PROLIFERATOR-ACTIVATED RECEPTOR-DELTA DESCRIPTION OF DRAWINGS 0009 FIG. 1 shows fluorescence data showing PPAR-8- TECHNICAL FIELD LBD binding affinity of Artemisia iwayOmogi extract in a test 0001. The present disclosure relates to a composition tube: including Artemisia extract as an active ingredient. 0010 FIG. 2 shows expression level of the reporter gene luciferase as a result of PPAR-ö activation by Artemisia iway BACKGROUND ART Omogi extract; 0002 Peroxisome proliferator-activated receptors 0011 FIG. 3 shows expression level of the target genes of (PPARS) are ligand-activated transcription factors belonging PPAR-8, CPT1 Band PDK4, in muscle cells treated with 200 to the nuclear receptor Superfamily activated by fatty acids. ug/mL Artemisia iwayOmogi extract; and The PPAR family consists of PPAR-C, PPAR-B/8 and PPAR 0012 FIG. 4 shows fatty acid oxidation in muscle cells Y, which show different ligand specificity and tissue distribu promoted as a result of treating with 200 g/mL Artemisia tion. PPAR-C. is expressed the most in the liver and promotes iwayOmogi extract. fatty acid oxidation in peroxisomes and mitochondria. PPAR-Y is expressed in adipose tissues and regulates Storage BEST MODE of fats. The ligand of PPAR-C, fibrate, is used as hypolipi 0013. A composition according to an exemplary embodi demic agent, and the ligand of PPAR-Y, thiazolidinedione, is ment of the present disclosure comprises Artemisia extract as used in the treatment of diabetes mellitus type 2. an active ingredient. The composition comprising. Artemisia 0003 PPAR-8 is expressed in muscles, brown adipose extract promotes the activity of peroxisome proliferator-acti tissues, etc. This transcription factor shows anti-obesity effect vated receptor delta (PPAR-8) and is effective in promoting since fatty acid oxidation in adipocytes is promoted in mice in muscular metabolism and/or improving memory. which it is overexpressed (Wang Y X et al., Cell, 113, pp. 0014. In the present disclosure, Artemisia (ssuk, Artemisia 159-170, 2003). An activator of PPAR-8 promotes metabo princeps) collectively refers to dicotyledonous perennial lism in skeleton muscle cells, improves insulin sensitivity, grasses belonging to the family Asteraceae of the order reduces adipocytes and inhibits inflammatory response by Asterales. Artemisia grows naturally in the whole area of increasing expression of such proteins as carnitine palmitoyl Korea and has been widely used for food as Vegetable, Soup, transferase f (CPT1B) and pyruvate dehydrogenase kinase porridge, cake, etc. isozyme 4 (PDK4) (Barish G D et al., J. Clin. Invest., 116, pp. 0015. In an exemplary embodiment, the Artemisia extract 590-597, 2006, 116:590). When the ligand of PPAR-O, may be Artemisia iwayOmogi extract. Artemisia iwayOmogi is GW501516, was administered together with the AMP-acti a perennial grass belonging to the genus Artemisia of family vated protein kinase (AMPK) activator AICAR to a mouse, Asteraceae. It is also called Saengdang SSuk, aedang SSuk, the mouse showed strengthened muscles even without exer Sacheol SSuk, injincho, heat reliever, heuinsan SSuk or teolsan cise as well as anti-obesity effect (Vihang A Net al., Cell, 134, SSuk. In particular, the young leaves are called injin or heat pp. 1-11, 2008). reliever and traditionally have been used as food or folk 0004. However, activator or ligand of PPAR-8 with proven medicine owing to peculiar fragrance and medicinal effect. stability has not been found yet. The inventors of the present Injin, the young bud of sacheol SSuk which is a perennial grass disclosure have found out that Artemisia iwayOmogi extract belonging to the family Asteraceae, has been known from old contains a novel ligand capable of activating PPAR-8. times to be beneficial for the liver. Especially, it is known to be highly effective in jaundice. Injin promotes secretion of bile DISCLOSURE and clears the liver by excreting lumps, cholic acid and biliru bin in the bile. Also, it reduces blood pressure, relieves fever, Technical Problem and kills various germs including tubercle bacillus. In addi tion, it is effective in degrading lipids, dilating coronary arter 0005. An embodiment of the present disclosure is directed ies and promoting urination. to providing a composition including Artemisia extract. 0016. In an exemplary embodiment, the composition has 0006 Another embodiment of the present disclosure is the effect of regulating the expression of enzymes that pro directed to providing food, health-food Supplement and phar mote fat and Sugar metabolism in muscle cells. Specifically, maceutical compositions that include the composition the composition which comprises Artemisia princeps or Arte including Artemisia extract. misia iwayomogi extract as an active ingredient is effective in promoting the expression of proteins that promote fat and Technical Solution Sugar metabolism in muscles, as ligand activating PPAR-ö. In 0007. In one general aspect, the present disclosure pro an exemplary embodiment, the composition may be a com vides a composition including Artemisia princeps or Artemi position for strengthening muscles and/or improving endur ance. In another exemplary embodiment, the composition sia iwayOmogi extract as an active ingredient. may be a composition for preventing and/or alleviating the symptoms of dementia or Parkinson's disease. These effects Advantageous Effects may beachieved through promotion of the PPAR-8 activity. 0008. The composition according to the present disclosure 0017. In an exemplary embodiment, the composition may has the effect of promoting the activity of PPAR-8 and is comprise 1-100 wt %, specifically 1-80 wt % of the Artemisia effective in promoting muscular metabolism and improving princeps or Artemisia iwayOmogi extract based on the total US 2013/0045289 A1 Feb. 21, 2013 weight of the composition. More specifically, the Artemisia 0022. The pharmaceutical composition according to the princeps or Artemisia iwayOmogi extract may be included in present disclosure may be administered orally or parenterally, an amount of 10-60 wt % based on the total weight of the e.g. rectally, topically, transdermally, intravenously, intra composition. The above-described content of the Artemisia muscularly or Subcutaneously. princeps or Artemisia iwayOmogi extract is an effective con 0023. A pharmaceutically acceptable dosage, i.e. admin tent for activating PPAR-8. istration dosage, of the active ingredient will vary depending 0018. A process for preparing the Artemisia princeps or on the age, gender and body weight of the Subject, particular Artemisia iwayOmogi extract according to the present disclo disease or pathological condition to be treated, severity of the Sure is not particularly limited. The Artemisia princeps or disease or pathological condition, administration route and Artemisia iwayOmogi extract may be extracted using water or discretion of a diagnoser. Determination of the administration an organic solvent. The organic solvent may be selected from, dosage considering these factors is in the level of those skilled for example, a group consisting of ethanol, methanol, in the art. A general administration dosage may be 0.01-2000 butanol, ether, ethyl acetate, chloroform and a mixture of the mg/kg/day, specifically 1-100 mg/kg/day. However, this organic solvent with water. For example, the Artemisia prin administration dosage does not limit the scope of the present ceps or Artemisia iwayOmogi extract may be obtained by disclosure by any means. repeating a procedure of adding 70% ethanol (3 L) to Arte 0024. The composition according to the present disclosure misia princeps or Artemisia iwayOmogi (300g) and stirring at may be prepared into various types of composition for exter 70-80° C. for 3 hours 2 times. Thus obtained extract may be nal skin application, more specifically a cosmetic composi filtered through Whatman No. 1 filter paper and freeze dried tion. For example, it may be prepared into softening lotion, at -70° C. to obtain the Artemisia princeps or Artemisia astringent lotion, nourishing lotion, eye cream, nourishing iwayomogi extract in Solid form.
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