To stabilize the basal extraction conditions of Leonuri herbal products, three kinds of Leonurus sibiricus water extracts were prepared with different extraction conditions (boiling extraction (I), high thermal process & boiling extraction (II), and wet grinding & boiling extraction (III)), and their physiological properties were investigated. The extraction yields of the L. sibiricus water extracts were from 13.02 to 15.90%, with no significant difference among them. The polyphenol contents were significantly high in extracts (II) and (III) than in extract (I). The IC50 for the electron-donating ability was the smallest in extracts (II), (III) and (I) in ascending order. The ABTS radical scavenging ability was significantly higher in extracts (II) and (III) than in extract (I). Also, the ACE in hibition ability for 5 mg/mL of each extract was high in extracts (II) and (III), but there was no significant difference among the three extracts in terms of their nitrite scavenging abilities. Extraction processes (II) and (III) were shown to be useful for preparing Leonurus sibiricus water extracts with healthful properties.