This is about a type of Piper laetispicum C.DC. extract and the preparation method thereof as well as the application of the extract in preparing drugs, healthcare products and food additives for treating and/or preventing diseases related to monoamine transmitters such as 5-hydroxytryptamine, noradrenaline and dopamine. The extract is obtained through impregnating or percolating at normal temperature or ≤70°C, or is obtained through supercritical fluid extraction method, and in comparison with the existing reflux method, it has higher alkaloid content and higher biological activity.