The classical drug discovery approach to defining bioactive constituents of botanicals

In this review, several recently identified biologically active principles of selected botanical dietary supplement ingredients are described, and were isolated using classical phytochemical chromatographic methods, with various spectroscopic procedures used for their isolation and structure elucidation. A central component of such an approach is “activity-guided fractionation” to monitor the compound purification process. In vitro assays germane to cancer chemoprevention were used to facilitate the work performed. Bioactive compounds, including several new substances, were characterized from açai (Euterpe oleracea), baobab (Adansonia digitata), licorice (Glycyrrhiza glabra), mangosteen (Garcinia mangostana), and noni (Morinda citrifolia). Many of these compounds exhibited quite potent biological activity, but tended to be present in their plant of origin only at low concentration levels.