The present invention provides preparation methods of (+)-syringaresinol and (+)-epi-syringaresinol. The present invention also provides composition including (+)-syringaresinol and/or (+)-epi-syringaresinolhaving anti-cancer activity.本發明提供(+)-syringaresinol及(+)-epi-syringaresinol等化合物之製法、含(+)-syringaresinol及/或(+)-epi-syringaresinol之抗癌組成物以及該抗癌組成物之製法。