As natural products continue to play a major role in drug discovery, especially at the early stage, our laboratory has focused on advancing the frontier which would ultimately lead to the discovery of natural products with novel skeletons, endless potential, and uncharted utilization. Despite traditional clinical use, the composition in herbal medicines has not been clearly identified. This has prompted our team to undertake systematic chemotaxonomic approach to elucidate the structures of bioactive compounds, some of which have warranted further investigations and development into drug-like candidates for their direct use or templates for structural modifications.