| Summary: | The fructus of Kadsura coccinea known as 'Bu-Fu-Na' is an emerging internet-famous fruit. For deep processing of 'Bu-Fu-Na' related products, an approach combining LC-MS analysis, network pharmacological prediction, and experimental validation was adopted to explore phytochemicals and biological functions of K. coccinea pericarpium (KCP) for the first time. In total, 9 lignans and 11 triterpenoids in KCP chloroform extract were identified by HPLC-Q-TOF/MS, and these chemicals acted on their key targets through multiple signaling pathways to achieve various biofunctions according to the constructed compound-target-pathway-disease network. Further experimental validation indicated that the four high-content lanostane-type triterpenoid acids in KCP strongly decreased 4T1 breast cancer cell viability in vitro, and the KCP chloroform extract had a good safety profile in 4T1 tumor-bearing mice and achieved anti-tumor efficacy by modulating immunity and activating the MAPK signal pathway. The obtained results provided comprehensive phytochemical and bioactive information for developing high value-added products of 'Bu-Fu-Na'.
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