Nowadays, resulting from disordered glucose and lipid metabolism, metabolic diseases (e.g., hyperglycemia, type 2 diabetes, and obesity) are among the most serious health issues facing humans worldwide. Increasing evidence has confirmed that dietary intervention (with healthy foods) is effective at regulating the metabolic syndrome. Whole grain rice (WGR) rich in dietary fiber and many bioactive compounds (e.g., γ-amino butyric acid, γ-oryzanol, and polyphenols) can not only inhibit starch digestion and prevent rapid increase in the blood glucose level, but also reduce oxidative stress and damage to the liver, thereby regulating glucose and lipid metabolism. The rate of starch digestion is directly related to the blood glucose level in the organism after WGR intake. Therefore, the effects of different factors (e.g., additives, cooking, germination, and physical treatments) on WGR starch digestibility are examined in this review. In addition, the mechanisms from human and animal experiments regarding the correlation between the intake of WGR or its products and the lowered blood glucose and lipid levels and the reduced incidence of diabetes and obesity are discussed. Moreover, information on developing WGR products with the health benefits is provided.