Abstract
The natural glycosides with triterpenoid or spirostaneaglycones are the saponins, which are associated with a wide range of therapeutic activities, inclusive of gastrointestinal anticancer activities. To promote research and development of novel cytotoxic agents against GIT cancer, this chapter focused on the anticancer potentia l of the naturally occurring triterpenoid and steroidal saponins. The in vitro assays and in vivo studies authenticated the anticancer potential of these compounds through antiangiogenic, anti-proliferative, anti-metastatic and anti-multidrug resistance activities. The protein targets and signaling cascades behind the anticancer effect of these compounds in GIT cancer are also discussed in this chapter.