Biotransformation of Bioactive Natural Products for Pharmaceutical Lead Compounds

Biotransfomation has been increasingly utilized as a tool to generate pharmaceutical lead compounds from natural products in recent years. A wide variety of natural pruducts including aromatics, steroids, alkaloids, coumarins, flavonoids and terpenoids can be biotransformed by fungi, yeasts, bacteria, plant cells and enzymes derived from these sources. The biochemical reactions occurring in microorganisms and plant cells are typically regio- and stereo-selective, which is difficult to be achieved by chemical methods. In this review we describe important biotransformations used for the generation of lead compounds with pharmaceutical utilities and further structural diversification of complex natural products, especially those from traditional Chinese medicines. Such approach will ultimately benefit the advancement of biotransformation and potential therapeutics.