| Bufadienolides, extracted from Venenum Bufonis, a traditional Chinese medicine, was reported to possess anticancer activities in vivo and in vitro. Bufadienolides lipid microsphere (BULM) is a new strategy for intravenous delivery system of bufadienolides. This study was done to investigate the effect of BULM on the proliferation of human cancer cell lines and human peripheral blood mononuclear cell (PBMC), as well as the underlying mechanisms.The cancer cell lines were exposed to different concentrations of BULM (8×10-4μg/ml, 8×10-3μg/ml, 8×10-2μg/ml, 8×10-1μg/ml, 8μg/ml) for 24, 48, 72h, respectively, and PBMC were incubated with BULM for 24h only. The viability, cell cycle distribution, and p53 expression were determined by MTT assay, flow cytometry, and immunocytochemistry method, respectively.BULM inhibited the proliferation of p53-positive Hep G2, HGC-27, HL-60 and A549 cells in a concentration- and time-dependent manner with IC50 of 5.50, 4.43, 3.20 and 2.15μg/m for 48-hour treatment, respectively, and presented minor cytotoxicity against PBMC, while did not demonstrate antiproliferation effect on the p53-negtive Hep 3B cell, Moreover, BULM induced cell cycle arrest in G2/M phase in HGC-27 while induced an accumulation of Hep G2 in sub-G1 phase, which has been considered the marker of cell death. Both of the two cell lines showed an increase of P53 expression after BULM treatment.It was suggested that BULM has a selective antitumor activity, which was associate with the p53 expression, and less side effects on normal human cells. These evidence indicated it might be a candidate for liver and gastric cancer therapy.
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