Abstract: Alzheimer's disease (AD) is a neurodegenerative disorder with a variety of etiological hypotheses, among which the cholinergic hypothesis is one of the primary theories. Natural inhibitors of acetylcholinesterase (AChE), such as galantamine and rivastigmine, are clinically approved for the treatment of AD. Biologically active molecules like sesquiterpenoids exhibit significant structural diversity and are an important class of terpenoids with a wide range of biological activities. Previous studies have demonstrated the potential of various sesquiterpenoids to improve cholinergic transmission through inhibiting AChE. This review summarizes the research progress on the activity of various sesquiterpenoids against AChE over the past five years. Through analysis, it was found that several sesquiterpenoids possess AChE inhibitory activity to varying degrees, demonstrating their potential as candidate medicines for the treatment of AD.