Department of Pharmacology, Chungnam National University College of Pharmacy, Daejeon 305-764, Republic of Korea.
J Agric Food Chem. 2012 Aug 8;60(31):7652-8. doi: 10.1021/jf300601z. Epub 2012 Jul 31.
Eriodictyol [2-(3,4-dihydroxyphenyl)-5,7-dihydroxy-2,3-dihydrochromen-4-one] is a flavonoid with anti-inflammatory and antioxidant activities. Because inflammation and oxidative stress play critical roles in the pathogenesis of diabetes mellitus, the present study was designed to explore whether eriodictyol has therapeutic potential for the treatment of type 2 diabetes. The results show that eriodictyol increased insulin-stimulated glucose uptake in both human hepatocellular liver carcinoma cells (HepG2) and differentiated 3T3-L1 adipocytes under high-glucose conditions. Eriodictyol also up-regulated the mRNA expression of peroxisome proliferator-activated receptor γ2 (PPARγ2) and adipocyte-specific fatty acid-binding protein (aP2) as well as the protein levels of PPARγ2 in differentiated 3T3-L1 adipocytes. Furthermore, it reactivated Akt in HepG2 cells with high-glucose-induced insulin resistance. This response was strongly inhibited by pretreatment with the phosphatidylinositol 3-kinase (PI3K) inhibitor LY294002, indicating that eriodictyol increased Akt phosphorylation by activating the PI3K/Akt pathway. These results imply that eriodictyol can increase glucose uptake and improve insulin resistance, suggesting that it may possess antidiabetic properties.
圣草次苷[2-(3,4-二羟基苯基)-5,7-二羟基-2,3-二氢色原酮-4-酮]是一种具有抗炎和抗氧化活性的类黄酮。由于炎症和氧化应激在糖尿病的发病机制中起着关键作用，本研究旨在探讨圣草次苷是否具有治疗 2 型糖尿病的潜力。结果表明，圣草次苷在高糖条件下增加了人肝癌细胞（HepG2）和分化的 3T3-L1 脂肪细胞中胰岛素刺激的葡萄糖摄取。圣草次苷还上调了分化的 3T3-L1 脂肪细胞中过氧化物酶体增殖物激活受体γ2（PPARγ2）和脂肪细胞特异性脂肪酸结合蛋白（aP2）的 mRNA 表达以及 PPARγ2 的蛋白水平。此外，它在高糖诱导胰岛素抵抗的 HepG2 细胞中重新激活 Akt。这种反应被磷脂酰肌醇 3-激酶（PI3K）抑制剂 LY294002 的预处理强烈抑制，表明圣草次苷通过激活 PI3K/Akt 通路增加 Akt 磷酸化。这些结果表明，圣草次苷可以增加葡萄糖摄取并改善胰岛素抵抗，表明它可能具有抗糖尿病特性。
