Biotransformations of Bioactive Natural Products with Complicated Structures

Since natural products usually possess complicated structures, it is very difficult to modify their structure efficiently by traditional chemical methods because of poor selectivity. However, biotransformation is an enzymatic reaction with higher selectivity and efficiency and various other advantages over chemical synthesis, so biotransformation can carry out reactions that cannot be successfully dealt with by chemical methods. Therefore, biotransformation is a powerful alternative to chemical modification and plays an important role in the structural optimization of natural products for the discovery of novel drug leads/candidates. In this presentation, the biotransformations of a number of bioactive natural products, such as taxanes, (-)-huperzine A, ginsenosides and the discovery of drug leads/candidates, are introduced. In addition, the directed glycosyl hydrolysis of 7-xylosyl-taxanes and ginsenosides and prenylation of flavonoids are introduced. Finally, recent progress in the prenyl transferase genes cloning, heterogenous expression and functional characterization from fungus and plants in our group will be reported.

Acknowledgements: This work was supported by the National Natural Science Foundation of China (Grant Nos., 30572243, 30772736), the Program for New Century Excellent Talents in University (Grant No., NCET-06–0155) and the National Science & Technology Major Project “Key New Drug Creation and Manufacturing Program”, China (No. 2009ZX09103–033).