A tremendous interest exists in the Western world in Traditional Chinese Medicine (TCM) with rapidly increasing export rates of TCM products from China to Europe and USA. This led to a national decision of the Chinese government to implement a "Plan for the Modernization of Chinese Medicine". Concerning the use of Chinese medicinal herbs, two major directions can be distinguished. One field is phytochemistry and pharmacognosy. Secondary metabolites isolated from Chinese plants can be easily subjected to pharmacological, molecular biological, and pharmacogenomic analyses using methods of modern cell and molecular biology as exemplified for camptothecin from Camptotheca acuminata in the present review. The second field of interest is phytomedicine. Standardized international quality guidelines help to improve quality, safety and efficacy of Chinese medicinal herbs. Sustainability of natural products from TCM can be reached by breeding high-yield varieties or by biotechnological approaches. In the long term, natural products from TCM can contribute to the development of molecular target-guided therapies and individualized treatment strategies.