• Title/Summary/Keyword: PPAR ${\alpha}$ and ${\gamma}$ dual agonist

Search Result 2, Processing Time 0.014 seconds

Design and Synthesis of Oxime Ethers of β-Oxo-γ-phenylbutanoic Acids as PPAR α and -γ Dual Agonists

  • Han, Hee-Oon;Koh, Jong-Sung;Kim, Seung-Hae;Park, Ok-Ku;Kim, Kyoung-Hee;Jeon, Sang-Kweon;Hur, Gwong-Cheung;Yim, Hyeon-Joo;Kim, Geun-Tae
    • Bulletin of the Korean Chemical Society
    • /
    • v.33 no.6
    • /
    • pp.1979-1982
    • /
    • 2012
  • Oxime ethers of ${\beta}$-oxo-${\gamma}$-phenylbutanoic acids were prepared to develop more effective PPAR ${\alpha}$ and ${\gamma}$ dual agonists. Among them, compound 11k exhibited potent $in$ $vitro$ activities with $EC_{50}$ of 2.5 nM and 3.3 nM in PPAR ${\alpha}$ and ${\gamma}$, respectively. It showed better glucose lowering effects than rosiglitazone 1 and improved the lipid profile like plasma triglyceride in db/db mice model.

The Hypoglycemic Effect of Complex of Chinese Traditional Herbs (CTH) and Macelignan in Type 2 Diabetic Animal Model (레이저 제2형 당뇨동물모델에서 macelignan과 한약제 열수 추출물의 병용효과)

  • Yeo, Ji-Young;Cho, Soo-In;Jung, Myeong-Ho
    • Journal of Life Science
    • /
    • v.20 no.7
    • /
    • pp.1113-1120
    • /
    • 2010
  • This study investigated the efficacy of macelignan and hot water with Chinese traditional herb (CTH) extract on altering severe diabetic conditions in C57BL/KsJ-db/db mice. Previously, the anti-diabetic effects of macelignan were partly reported as a PPAR $\alpha/\gamma$-dual agonist. Here, we futher studied whether a combination of macelignan and CTH had more beneficial effects or not. The macelignan and CTH compound significantly decreased fasting blood glucose and HbA1c compared to macelignan-treated mice, and also significantly improved postprandial glucose, insulin sensitivity, and plasma lipid profiles (FFA, and TG). On the other hand, insulin levels were not significantly changed compared to the diabetic control group. There were no significant changes in the concentrations of total cholesterol and HDL-cholesterol, but there were changes in HTR and AI. These results suggest that the macelignan and CTH compound ameliorates hyperglycemia and efficiently improves postprandial glucose, insulin sensitivity, and hyperlipidemia compared with macelignan in db/db mice. Moreover, the macelignan and CTH compound seems to be more potent in affecting diabetic complications than macelignan.