School of Pharmacy, Tokyo University of Pharmacy and Life Sciences, 1432-1, Horinouchi, Hachioji, Tokyo 192-0392, Japan.
J Nat Med. 2012 Apr;66(2):394-9. doi: 10.1007/s11418-011-0593-z. Epub 2011 Oct 11.
Clove (Syzygium aromaticum flower buds) EtOH extract significantly suppressed an increase in blood glucose level in type 2 diabetic KK-A(y) mice. In-vitro evaluation showed the extract had human peroxisome proliferator-activated receptor (PPAR)-γ ligand-binding activity in a GAL4-PPAR-γ chimera assay. Bioassay-guided fractionation of the EtOH extract resulted in the isolation of eight compounds, of which dehydrodieugenol (2) and dehydrodieugenol B (3) had potent PPAR-γ ligand-binding activities, whereas oleanolic acid (4), a major constituent in the EtOH extract, had moderate activity. Furthermore, 2 and 3 were shown to stimulate 3T3-L1 preadipocyte differentiation through PPAR-γ activation. These results indicate that clove has potential as a functional food ingredient for the prevention of type 2 diabetes and that 2-4 mainly contribute to its hypoglycemic effects via PPAR-γ activation.
丁香(Syzygium aromaticum花蕾)乙醇提取物显著抑制 2 型糖尿病 KK-A(y)小鼠血糖水平的升高。体外评价表明,该提取物在 GAL4-PPAR-γ嵌合体测定中具有人过氧化物酶体增殖物激活受体(PPAR)-γ配体结合活性。乙醇提取物的生物活性指导分离得到 8 种化合物,其中脱氢二丁香酚(2)和脱氢二丁香酚 B(3)具有很强的 PPAR-γ配体结合活性,而乙醇提取物中的主要成分齐墩果酸(4)具有中等活性。此外,2 和 3 被证明通过 PPAR-γ 激活刺激 3T3-L1 前体脂肪细胞分化。这些结果表明,丁香具有作为预防 2 型糖尿病的功能性食品成分的潜力,并且 2-4 通过激活 PPAR-γ 主要有助于其降血糖作用。