In recent years, research on the chemical constituents and pharmacological effects of Atractylodis macrocephalae Rhizoma, a traditional and commonly used Chinese medicinal herb, has made a series of important advances. This review systematically summarizes the newly discovered bioactive components of Atractylodis macrocephalae Rhizoma, including volatile oils, sesquiterpene lactones, polysaccharides, and polyacetylenes. It particularly highlights the multi-target and network-integrated pharmacological actions of representative active substances such as Atractylodis macrocephalae Rhizoma polysaccharides, atractylenolides Ⅰ/Ⅲ, and atractylon. This actions include dual-directional regulation of gastrointestinal function, immunoenhancement, antioxidant activity, anti-aging effects, amelioration of Alzheimer's disease, relaxation of uterine smooth muscle, and bone protection. By synthesizing the current research findings, this review aims to comprehensively present the current state of knowledge regarding the pharmacological activities of Atractylodis macrocephalae Rhizoma, with the goal of providing useful references for the development of novel Chinese medicine formulations based on Atractylodis macrocephalae Rhizoma and its rational clinical application.

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