The present invention provides a method for treating diabetes, hyperlipidemia or hepatic total lipids by using ergostatrien-3β-ol and its derivatives, as well as a method for decreasing blood glucose and HbA1c levels and reducing blood total cholesterol and triglyceride levels, whereas increasing blood HDL-C levels; and a method for decreasing hepatic total lipid and triacylglycerol levels; and increasing expression levels of membrane glucose transporter 4 (GLUT4) and phospho-Akt in skeletal muscle tissue, and phospho-AMPK in both skeletal muscle and liver tissue using ergostatrien-3β-ol and its derivatives.