Medicinal herbs have been used to treat human diseases in China for thousands of years. There has been great interest in the research and development of bioactive components from herbal medicines. Significant pharmacological properties have been demonstrated for many herbs over recent decades. Not only important in China, herbal preparations are becoming increasingly popular in Europe and North America as complementary therapeutics. Traditional Chinese Medicine (TCM) is usually a mixture of herbal plants or extracts which comprise hundreds of different constituents with widely differing physiochemical properties. The qualification and quantitative analysis of active constituents from this mixture is often a challenging task especially when the relevant compounds might be present in minute amounts only. Additional challenge is batch-to-batch inconsistency of constituents due to the natural variability of the herbal plants. Thus, there is a substantial need to use modern bioassay and analytical techniques, including developing high throughput and sensitive technologies, to determine active constituents and to monitor the quality control of herbal medicines. The rapid growth in proteomics, genomics and metabonomics provides a lot of new tools for the integration of traditional Chinese medicine with modern technology and systems biology. This special issue aims at providing the readers of CCHTS with a perspective of the technology developments and their applications in the rapid progress of up-to-date research in TCM. I would like to express my thanks to all the contributors for their valuable articles and to the referees for their constructive comments as well as to Professor Rathnam Chaguturu, the Editor-in-Chief, for his continuing support during the preparation of this issue.