Nature-based Drug Discovery - Past, Present, and Future

Sciences at the interface of chemistry and biology have led to increased opportunities for the identifying of lead molecules against various therapeutic targets. For centuries, natural products have served as key sources of therapeutic agents, and still many of current drugs are derived from medicinal plants. However, synthesis of natural products is still a challenging task due to various reasons, including structural and stereochemical complexities. These problems can circumvent with the help of biocatalysis and combinatorial biosynthesis, as enzymes have high selectivity and specificity and they can work under mild conditions in both organic and aqueous media.

During last four decades, our research has been focused on the discovery of chemical constituents from medicinal plants used in traditional medicines, as well as designing new biotransformed products with therapeutic potential. This has resulted in the identification of several novel drug leads against various therapeutic targets. Emphasis has been on the discovery of natural products and their analogs against chronic disorders, including cardiovascular, cancer, diabetes, and Alzheimer’s and Parkinson's diseases.

Novel analogues of existing drugs such as tibolones (postmenopausal osteoporosis), exemestane (anti-cancer drug), medrysone (anti-inflammatory agent) and many others were synthesized using biotransformation tools. Thus, potent anti-inflammatory, and cytotoxic agents were identified as lead molecules against breast cancer cell lines. Furthermore, inhibitors of key enzymes related to several diseases were also discovered.

During this presentation, some recent examples of our studies highlighting the translational potential of bioactive natural products, and biotransformation against non-communicable chronic diseases will be presented