The low success rate, despite a huge capital investment, has made the research and development of conventional drugs very costly.Over the past few decades, researchers have focused on drug discovery from herbal medicines or botanical sources.With a long history of herbal usage for the clinical management of a variety of diseases in indigenous cultures, the success rate of developing a new drug from herbal medicinal preparations should, in theory, be higher than that from chemical synthesis.While the endeavor for drug discovery from herbal medicines is experience-driven, the search for a therapeutically useful synthetic drug, like looking for a needle in a haystack, is a daunting task.In this article, we first illustrated various approaches of drug discovery from herbal medicines.Typical examples of successful drug discovery were given.In addition, problems in drug discovery from herbal medicines were described and possible solutions proposed.The prospect of drug discovery from herbal medicines in the post-genomic era was made with the provision of future directions in this area of drug development.