Abstract: Moutan Cortex is widely used in clinical practice of traditional Chinese medicine for its efficacy in clearing heat from the heart, kidney, and liver, as well as activating blood circulation to resolve stasis. Paeonol, as the core active monomer of Moutan Cortex, has become a research hotspot in natural medicine due to its multi-target biological activities. Pharmacological studies have indicated that paeonol demonstrates multi-dimensional therapeutic potential in anti-inflammation, neuroprotection, cardiovascular protection, and anti-tumor effects by regulating inflammatory mediators, cyclins, and oxidative stress pathways. At the same time, its pharmacokinetic characteristics are also gradually being revealed. Based on relevant domestic and international research, this article systematically summarizes the research progress in pharmacological effects and pharmacokinetics of paeonol, aiming to provide a theoretical basis and new perspectives for its further investigation and clinical application.