The application of Chinese medicine to novel drug discovery.

Introduction: The apparent productivity crisis in the pharmaceutical industry and the economic and political rise of China have contributed to renewed interest in the application of Chinese medicine for drug discovery.

Areas Covered: The author presents an overview of the historical development and basic principles of theory and practice of Chinese herbal medicine, its materia medica and prescription formulas, and discusses the motivation for and rationale of its application to drug discovery. Furthermore, the author distinguishes the five main approaches to drug discovery from Chinese herbal medicine, based on the decreasing amount and detail of historical and clinical Chinese medicine knowledge that informed the research effort.

Expert Opinion: Many compounds that have been isolated from the Chinese materia medica exhibit pharmacological activities comparable to pharmaceutical drugs. With the exception of the antimalarial drug artemisinin, however, this knowledge has not led to the successful development of new drugs outside of China. The chance of success in a Chinese medicine-based drug discovery effort will be increased by consideration of the empirical knowledge that has been documented over many centuries in the historical materia medica and prescription literature. Most Chinese medicine-derived compounds affect more than one target and do not correspond to the one compound/one-target drug discovery paradigm. A new frontier is opening up with the development of drugs consisting of combinations of multiple compounds acting on multiple targets under the paradigm of network pharmacology. The ancient practice of combining multiple drugs in prescription formulas can serve as inspirational analogy and a practical guide.