γ-Mangostin from Garcinia Mangostana Pericarps as a Dual Agonist That Activates Both PPARα and PPARδ

被引:25
作者
Matsuura, Nobuyasu [1 ]
Gamo, Kanae [1 ,2 ]
Miyachi, Hiroyuki [2 ]
Iinuma, Munekazu [3 ]
Kawada, Teruo [4 ]
Takahashi, Nobuyuki [4 ]
Akao, Yukihiro [5 ]
Tosa, Hideki [6 ]
机构
[1] Okayama Univ Sci, Fac Sci, Dept Life Sci, Kita Ku, Okayama 7000005, Japan
[2] Okayama Univ, Grad Sch Med Dent & Pharmaceut Sci, Dept Pharmaceut Sci, Kita Ku, Okayama 7008530, Japan
[3] Gifu Pharmaceut Univ, Fac Pharmaceut Sci, Gifu 5011196, Japan
[4] Kyoto Univ, Grad Sch Agr, Div Food Sci & Biotechnol, Uji, Kyoto 6110011, Japan
[5] Gifu Univ, United Grad Sch Drug Discovery & Med Informat Sci, Gifu 5011193, Japan
[6] Field & Device Co, Osaka 5410045, Japan
关键词
dual agonist; Garcinia mangostana pericarp; PPAR alpha; PPAR delta; gamma-mangostin; LIPID-METABOLISM; GENE-EXPRESSION; 2; XANTHONES; ROOT BARK;
D O I
10.1271/bbb.130541
中图分类号
Q5 [生物化学]; Q7 [分子生物学];
学科分类号
071010 ; 081704 ;
摘要
We tested the peroxisome proliferator-activated receptor (PPAR)delta agonistic activity of a Garcinia mangostana pericarp extract to develop a treatment for the metabolic syndrome, and demonstrated gamma-mangostin to be an active compound on the basis of a luciferase reporter gene assay. gamma-Mangostin induced the expression of the uncoupling protein-3 (UCP-3) gene which is related to energy expenditure and fat metabolism in L6 cells. We showed that gamma-mangostin is a dual agonist that activates both PPAR delta and PPAR alpha. gamma-Mangostin also induced the expression of acyl-CoA synthase and carnitine palmitoyl-transferase 1A genes in HepG2 cells. These results suggest the potential of gamma-mangostin as a preventive agent of the metabolic syndrome.
引用
收藏
页码:2430 / 2435
页数:6
相关论文
共 18 条
[1]   Anti-cancer effects of xanthones from pericarps of mangosteen [J].
Akao, Yukihiro ;
Nakagawa, Yoshihito ;
Iinuma, Munekazu ;
Nozawa, Yoshinori .
INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES, 2008, 9 (03) :355-370
[2]   A XANTHONE FROM PERICARPS OF GARCINIA-MANGOSTANA [J].
ASAI, F ;
TOSA, H ;
TANAKA, T ;
IINUMA, M .
PHYTOCHEMISTRY, 1995, 39 (04) :943-944
[3]   PPAR dual agonists: Are they opening Pandora's box? [J].
Balakumar, Pitchal ;
Rose, Madhankumar ;
Ganti, Subrahmanya S. ;
Krishan, Pawan ;
Singh, Manjeet .
PHARMACOLOGICAL RESEARCH, 2007, 56 (02) :91-98
[4]   Pharmacotherapy for dyslipidaemia - current therapies and future agents [J].
Bays, H ;
Stein, EA .
EXPERT OPINION ON PHARMACOTHERAPY, 2003, 4 (11) :1901-1938
[5]   Peroxisome proliferator-activated receptors (PPARs): Nuclear receptors at the crossroads between lipid metabolism and inflammation [J].
Chinetti, G ;
Fruchart, JC ;
Staels, B .
INFLAMMATION RESEARCH, 2000, 49 (10) :497-505
[6]  
Coll Teresa, 2009, Curr Mol Pharmacol, V2, P46
[7]   Recent Insights into the Biosynthesis and Biological Activities of Natural Xanthones [J].
El-Seedi, H. R. ;
El-Barbary, M. A. ;
El-Ghorab, D. M. H. ;
Bohlin, L. ;
Borg-Karlson, Anna-Karin ;
Goransson, U. ;
Verpoorte, R. .
CURRENT MEDICINAL CHEMISTRY, 2010, 17 (09) :854-901
[8]   Effects of fibrates on serum metabolic parameters [J].
Elisaf, M .
CURRENT MEDICAL RESEARCH AND OPINION, 2002, 18 (05) :269-276
[9]   Phytol directly activates peroxisome proliferator-activated receptor α (PPARα) and regulates gene expression involved in lipid metabolism in PPARα-expressing HepG2 hepatocytes [J].
Goto, T ;
Takahashi, N ;
Kato, S ;
Egawa, K ;
Ebisu, S ;
Moriyama, T ;
Fushiki, T ;
Kawada, T .
BIOCHEMICAL AND BIOPHYSICAL RESEARCH COMMUNICATIONS, 2005, 337 (02) :440-445
[10]   Peroxisome proliferator-activated receptor δ (PPhRδ)-mediated regulation of preadipocyte proliferation and gene expression is dependent on cAMP signaling [J].
Hansen, JB ;
Zhang, HB ;
Rasmussen, TH ;
Petersen, RK ;
Flindt, EN ;
Kristiansen, K .
JOURNAL OF BIOLOGICAL CHEMISTRY, 2001, 276 (05) :3175-3182