The antitumor activities of ethyl acetate extracts from Selaginella doederleinii Hieron (SD extracts) in vitro and in vivo and its\npossible mechanism were investigated. HPLC method was developed for chemical analysis. SD extracts were submitted to 3-(4,5-\ndimethylthiazol-2-yl)-2,5-diphenyl tetrazolium bromide (MTT) assay on different cells, flow cytometry, and RT-PCR analysis using\nHepG2 cell and antitumor activity in vivo using H-22 xenograft tumor mice. Six biflavonoids from SD extracts were submitted to\nmolecular docking assay. The results showed that SD extracts had considerable antitumor activity in vitro and in vivo without\nobvious toxicity on normal cells and could induce cell apoptosis.The mechanisms of tumorigenesis and cell apoptosis induced by\nSD extracts may be associated with decreasing the ratio of bcl-2 and bax mRNA level, activating caspase-3, suppressing survivin,\nand decreasing the gene expression of COX-2, 5-LOX, FLAP, and 12-LOX mRNA. The main active component in SD extracts is\nbiflavonoids and some exhibited strong interactions with COX-2, 5-LOX, 12-LOX, and 15-LOX.These results offering evidence of\npossible mechanisms of SD extracts suppress cell proliferation and promote apoptosis and provide the molecular theoretical basis\nof clinical application of S. doederleinii for cancer therapy.
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