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Capilliposide B (CPS‐B), a novel oleanane triterpenoid saponin derived from Lysimachia capillipes Hemsl, is a potent anticancer agent. However, its anticancer mechanism remains elusive. In the present study, we demonstrated the potent anti‐tumor activity and molecular mechanism of CPS‐B both in vitro and in vivo. Proteomic analysis using isobaric tags for relative and absolute quantitation techniques...