Traditional Chinese medicine (TCM) is a medical practice that originated in ancient China. Based on its ancient philosophical concepts, it features unique diagnostic and therapeutic approaches that have been evolved from extensive observation and clinical experience gained over more than 2000 years. Chinese herbal medicine (CHM) is the cornerstone and principal form of TCM practice. In recent years, phytochemicals and other natural compounds have been receiving attention from researchers to develop more potent and less toxic treatments. Although still underdeveloped, various studies have been conducted to uncover the complexity of CHM and obtain evidence for its efficacy and toxicity as interpreted from the aspects of biomedical science. In this thesis, four CHM formulas are presented as examples to illustrate the advancement of such research.