This thesis described a proof-of-concept to translate ancient traditional Chinese medicines to modern drugs. Taking TCMs targeting neurodegenerative diseases, the thesis presented a data mining of ancient literature, physicochemical analysis of known drugs and TCM compounds, and chemical analysis, and phenotypic screening of TCM extracts, fractions and compounds, and early development of a target identification method. Chapter 1 started with an introduction of traditional Chinese medicines and neurodegenerative diseases. It pointed out that the formula is the essence of TCM, and that herb pairs are a starting point of many formulas. It summarized the natural products used for the treatment of neurodegenerative diseases. It presented an unmet medical need that required new therapeutics. It provided a foundation for the further investigations.