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OBJECTIVE To study the potential approach in the development of saponins as new anticancer drugs.METHODS The extraction,isolation and structural elucidation on the saponin constituents from three species of starfishes (Culcita novaeguineae,Anthenea chinensis and Pentaceraster chinensis),five species of sea cucumbers (Holothuria fuscocinerea,Pseudocolochirus violaceus,Pentacta quadrangularis,Bohadschia marmorata and Hoiothuria (Microthele)axiloga) and eight species of plants (Ardisia pusilla,Bolbostemma paniculatum,Clematis argentilucida,Anemone taipaiensis,Anemone rivularis vat.flore-minore,Anemone tomentosa,Clematis tangutica and Ardisia brevicaulis) were carried out.The antitumor,especially anti-glioblastoma effects in vitro and in vivo,as well as the mechanisms of these saponins were studied.RESULTS One hundred and seventy-four saponins were identified,and 88 are new compounds,among which most possessed relative rare structural features.Most of them showed in vitro cytotoxicity against tumor cells,especially glioblastoma cells.Several saponins exhibited significant aniti-glioblastoma effects in vivo by in situ administration (interstitial chemotherapy) and their haemolytic side effects were avoided in the tests.Multiple mechanisms of action,such as inducing apoptosis,promoting stabilization of microtubule,as well as several signal transduction pathways,were involved in their anticancer effects.CONCLUSION These studies provided valuable leads for pursuing new anti-glioblastoma drugs,and established a homebase for further development of these organisms.The success of the approach to administrate saponins in situ conquered the bottleneck in the development of saponins as new drugs—haemolytic effects.The studies indicated that saponins may be developed as potential chemotherapeutic agents in pursuing new anti-glioblastoma drugs.