Mechanochemical extraction technique was explored for efficient and selective extraction of magnolol from Magnolia officinalis. This process was carried out using a high intensive activator, AGO-2. The yield of magnolol via mechanochemical method was maximized under the following conditions: milling with Na2CO3 (2.0 wt%) for 7 min; extraction by water at 40 degrees C and liquid/solid ratio of 25:1 mL/g for 20 min; precipitation at pH 3.5. The results from scanning electron micrographs, infra-red spectrum and nuclear magnetic resonance indicate that mechanochemical action could result in the disruption of cell walls and the transformation of magnolol into a water-soluble salt form with the addition of sodium carbonate. Compared with superfine grinding extraction and heat-reflux extraction, mechanochemical extraction method reduced both extraction time and temperature, and also achieved a higher magnolol yield and content in the crude extracts. (C) 2011 Elsevier B.V. All rights reserved.