Development of New Target-Based Anticancer Agents from Higher Plants

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The objective of this research is to develop new target-based anticancer agents with apoptosis inducing activity from higher plants. The chemical constituents of Bulbinella floribunda (Liliaceae), Agave utahensis (Agavaceae), Tacca chantrieri (Taccaceae), Helleborus orientalis (Ranunculaceae), Helleborus niger (Ranunculaceae), Curculigo orchioides (Hypoxidaceae), and Tithonia diversifolia (Compositae) have been investigated. New phenylanthraquinone derivatives, new steroidal glycosides, cardeotonic glycosides, phytoecdysones, triterpenes with the cycloartane skeleton, and flavonoids and sesquiterpenoids were isolated from B.floribunda, A.utahensis, H.orientalis, H.niger, C.orchioides, and T.diversifolia, respectively, as cytotoxic and antitumor compounds, and their chemical structures were determined on the basis of the spectroscopic data and chemical evidence. Since the cytotoxic compounds isolated from the same plants are structurally related each other, the structure-activity relationships were established. In a panel-screening using a variety of cultured tumor cells, a phytoecdysone from H.niger, a cycloartane triterpene from C.orchioides, and a sesquiterpene from T.diversifolia showed differential cytotoxicity. Some 5β-spirostanol glycosides from A.utahensis caused the death of HL-60 cells through the apoptotic process.