Western drugs and target medicines for disease treatment come with undesirable side effects that have limited their use in patients for an extended period of time. It is warranted to develop a treatment strategy with alternative medicines to reduce toxicity relating to drugs, in particular, cancer drugs. Thus, a combination therapy with herbal medicines provides a more effective treatment method for hard-to-treat diseases. The recent breakthroughs in naturally occurring small molecules from herbal medicines have provided experimental evidence and are clinically significant in treatment strategies.This unique volume presents the recent developments in the field of herbal medicines for the treatment of diseases and cancer. Recent progress on small molecules isolated from herbal medicines that exhibit therapeutic benefits in humans is highlighted. The book provides an overview of the significant discoveries and pioneering contributions of herbal medicines in combination with other drugs; the author’s evaluation of the combination therapy in cancer treatment; and a recent discovery of crocodile tissue extract with pharmacological properties.