Potent antidiabetic effects of rivoglitazone, a novel peroxisome proliferator-activated receptor-γ agonist, in obese diabetic rodent models

DOI Web Site PubMed 被引用文献4件 参考文献65件 オープンアクセス
  • Kanda Shoichi
    Biological Research Laboratories II, Daiichi Sankyo Co., Ltd., Japan
  • Nakashima Ryutaro
    Biological Research Laboratories II, Daiichi Sankyo Co., Ltd., Japan
  • Takahashi Kanako
    Biological Research Laboratories II, Daiichi Sankyo Co., Ltd., Japan
  • Tanaka Jun
    Biological Research Laboratories II, Daiichi Sankyo Co., Ltd., Japan
  • Ogawa Junko
    Biological Research Laboratories II, Daiichi Sankyo Co., Ltd., Japan
  • Ogata Tsuneaki
    Biological Research Laboratories II, Daiichi Sankyo Co., Ltd., Japan
  • Yachi Makoto
    Pharmacology Research Laboratories, Daiichi Sankyo Co., Ltd., Japan
  • Araki Kazushi
    Biological Research Laboratories II, Daiichi Sankyo Co., Ltd., Japan
  • Ohsumi Jun
    Biological Research Laboratories II, Daiichi Sankyo Co., Ltd., Japan

書誌事項

タイトル別名
  • Potent Antidiabetic Effects of Rivoglitazone, a Novel Peroxisome Proliferator-Activated Receptor-.GAMMA. Agonist, in Obese Diabetic Rodent Models
  • Potent antidiabetic effects of rivoglitazone a novel peroxisome proliferator activated receptor g agonist in obese diabetic rodent models
公開日
2009
DOI
  • 10.1254/jphs.09084fp
公開者
公益社団法人 日本薬理学会

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説明

The pharmacological effects of rivoglitazone, a novel thiazolidinedione-derivative peroxisome proliferator–activated receptor (PPAR)-γ agonist, were characterized in vitro and in vivo. Rivoglitazone activated human PPARγ more potently compared with rosiglitazone and pioglitazone and had little effect on PPARα and PPARδ activity in luciferase reporter assays. In Zucker diabetic fatty (ZDF) rats, 14-day administration of rivoglitazone decreased the plasma glucose and triglyceride (TG) levels in a dose-dependent manner. The glucose-lowering effect of rivoglitazone was much more potent than those of pioglitazone (ED50: 0.19 vs. 34 mg/kg) and rosiglitazone (ED50: 0.20 vs. 28 mg/kg). In addition, rivoglitazone showed potent antidiabetic effects in diabetic db/db mice. In Zucker fatty rats, rivoglitazone at a dose of 0.1 mg/kg clearly ameliorated insulin resistance and lowered plasma TG levels by accelerating the clearance of plasma TG. Gene expression analysis in the liver and heart of ZDF rats treated with rivoglitazone for 14 days suggested that rivoglitazone may reduce hepatic glucose production and modulate the balance of the cardiac glucose/fatty acid metabolism in diabetic animals. In summary, we showed that rivoglitazone is a potent and selective PPARγ agonist and has a potent glucose-lowering effect via improvement of the insulin resistance in diabetic animal models.<br>

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