ABSTRACT
Chemical substances derived from natural products such as plants, animals, and microbes have been invaluable as a source of therapeutic agents for all kinds of diseases since the dawn of medicine.1-5 Even now, natural products still play a dominant role in the discovery of leads to drugs for the treatment of human disease. During the period 1981-2002, of the 877 small molecule New Chemical Entities introduced, nearly half (49%) were natural products, semisynthetic natural product analogues, or synthetic compounds based on natural-product pharmacophores.6 Traditional Chinese
medicines (TCMs), as an important group of natural remedies, are gaining increased attention in drug lead discovery. TCMs have a long history dating back several thousands of years.7 The origin of TCMs was associated with the legendary testing of many herbs for their medicinal properties by the folk hero Shen Nong.8 His experience and work in these areas was eventually recorded in Shen Nong Ben Cao Jing (The Herbal Classic of the Divine Plowman) in about 2700 BCE. Up until the second and rst centuries BCE, the establishment of the “Yin and Yang” doctrine under the in uence of Confucius helped to reinforce the use of herbal materials for relieving illnesses and the rst major medical text, Huang Di Nei Jing (Yellow Thearchy’s Inner Canon), appeared in China. With the development of theory and clinical practice, China accumulated a rich body of empirical knowledge about the use of medicinal plants for the treatment of various diseases. In the Ming Dynasty (1368-1644), a major medical literature Ben Cao Gang Mu (The Comprehensive Herbal Foundation) written by Li Shi-Zhen in 1590 discussed 1892 medicinal substances and contained over 1000 illustrations and over 10,000 medicinal formulas, which indicates that the contemporary Chinese had grasped comprehensive pharmaceutical knowledge and clinical experience. So far, there have been 12,806 medical resources discovered in China, including 11,145 medicinal plants, 1581 medicinal animals, and 80 medicinal minerals.9 The clinic medicinal experience of more than 4000 years and a modern integrated theory system for diagnosis and treatment open a potential shortcut for discovering new bioactive compounds from these natural products.
