Target Screening and Validation of the Antitumor Effect of Saponin Extract From Holothuria leucospilota

ABSTRACT This paper aimed to isolate and characterize the saponins from Holothuria leucospilota and investigate their potential antitumor effects and antitumor targets using network pharmacology and bioinformatics. The purified saponins were analyzed using electrospray ionization–tandem mass spectrometry (ESI–MS/MS). Ten saponins were identified. The in vitro experiments demonstrated that H. leucospilota saponins exhibited significant dose‐dependent inhibition on HepG2, Panc02, and UM‐UC‐3 cell proliferation and differentiation. In addition, through network pharmacology, bioinformatics, and molecular docking, a total of 22 key tumor targets of H. leucospilota saponins were identified. Then, the reverse‐transcription quantitative polymerase chain reaction (RT‐qPCR) results showed that the saponins from H. leucospilota can inhibit the expression of target genes AURKB , BIRC5 , CHEK1 , PTGS2 , and MMP9 , and may affect the neuroactive ligand–receptor signaling pathway, thereby suppressing tumor proliferation and migration. In conclusion, we have demonstrated that the saponin extract from H. leucospilota has potential application value in tumor therapy.