Active components from traditional Chinese medicine (TCM) are the material basis for disease treatment. Extraction, identification, and transformation are the critical processes to analyze and use the active components of TCM. Botanic TCM takes up 90 % of total Chinese crude drugs. Some active components are complex and of lower level; moreover, most of them are enveloped under plant cell wall. Traditional extraction methods such as lixiviate method, decoction, and others are often hindered by cell wall, leading to low extraction efficiency, low clearance of impurity, and other problems, which have restricted the development of TCM. This paper reviews both domestically and internationally published literatures in recent years on application of enzymatic methods in the extraction and transformation of active ingredients from TCM. Principles of enzymatic method and its application in extraction and transformation of active ingredients and in dreg recycles of TCM are introduced in detail. With the development of TCM modernization, enzymatic method applied in the domain of TCM has achieved prominent benefits, not only improving the extraction and separation rate of active ingredients from TCM and elevating the transformation level and production, but also reducing costs in the transformation of active ingredients.