Abstract: Diabetes mellitus can lead to various complications, such as cardiovascular disease, diabetic nephropathy, and nervous system disorders. These complications significantly burden patients' quality of life and socioeconomic. α-glucosidase, also known as glucosyltransferase, is responsible for breaking down carbohydrates into glucose, rendering it a critical target for diabetes prevention and treatment. Although clinical α-glucosidase inhibitors like acarbose exist, their long-term use often causes gastrointestinal side effects and liver damage. Therefore, there is an urgent need for new α-glucosidase inhibitors that are highly effective and less toxic. Chinese herbs have a good safety record in long-term clinical practice. Recent studies have shown that certain extracts and components of Chinese herbs can effectively inhibit α-glucosidase activity, offering potential avenues for blood sugar regulation and diabetes prevention and treatment. In this review, we place particular emphasis on the inhibition of α-glucosidase and provide a systematic overview of the inhibitory effects and underlying mechanisms of Chinese herbs and their chemical components. It also discusses the challenges faced in this field and prospects for future research and development of hypoglycemic drugs. All information contributes to the provision of new insights for the development of α-glucosidase inhibitors and hypoglycemic drugs from Chinese herbs.