School of Life Sciences, South-Central University for Nationalities, Wuhan, China.
School of Pharmaceutical Sciences, South-Central University for Nationalities, Wuhan, China.
Mol Nutr Food Res. 2018 Feb;62(3). doi: 10.1002/mnfr.201700444. Epub 2018 Jan 9.
The number of people with diabetes is increasing rapidly in the world. In the present study, the hypoglycemic activity and potential mechanism of ergosterol (ERG), a phytosterol derived from the edible mushroom Pleurotus ostreatus are investigated in vitro and in vivo.
ERG is isolated from Pleurotus ostreatus and identified by NMR spectra. The effects of ERG on the glucose uptake, glucose transporter 4 (GLUT4) translocation, GLUT4 expression, and the phosphorylation of AMPK, Akt and PKC in L6 cells are evaluated. ERG enhances glucose uptake and displays a GLUT4 translocation activity with up-regulating GLUT4 expression and phosphorylation of Akt and PKC in L6 cells. In vivo, antidiabetic activity of ERG is examined. The phosphorylation of Akt and PKC in different tissues from KK-A mice is assessed. ERG significantly improves insulin resistance and blood lipid indices while reducing fasting blood glucose levels and protecting pancreas and liver in the mice. Moreover, the phosphorylation of Akt and PKC is increased in different tissues.
The results suggest that ERG may be a potential hypoglycemic agent for the treatment of T2DM with the probable mechanism of stimulating GLUT4 translocation and expression modulated by the PI3K/Akt pathway and PKC pathway.
世界范围内糖尿病患者的数量正在迅速增加。在本研究中，从食用蘑菇平菇中提取的植物固醇麦角甾醇（ERG）在体外和体内进行了降血糖活性和潜在机制的研究。
从平菇中分离出 ERG，并通过 NMR 谱进行鉴定。评估 ERG 对 L6 细胞葡萄糖摄取、葡萄糖转运蛋白 4（GLUT4）易位、GLUT4 表达以及 AMPK、Akt 和 PKC 磷酸化的影响。ERG 增强葡萄糖摄取，并显示 GLUT4 易位活性，上调 L6 细胞中 GLUT4 的表达和磷酸化 Akt 和 PKC。在体内，研究了 ERG 的抗糖尿病活性。评估 KK-A 小鼠不同组织中 Akt 和 PKC 的磷酸化。ERG 可显著改善胰岛素抵抗和血脂指标，同时降低空腹血糖水平，保护小鼠的胰腺和肝脏。此外，不同组织中 Akt 和 PKC 的磷酸化增加。
研究结果表明，ERG 可能是一种潜在的治疗 2 型糖尿病的降血糖药物，其作用机制可能是通过 PI3K/Akt 途径和 PKC 途径刺激 GLUT4 易位和表达。
