Background: Dipyrithione (PTS2) is widely used as a bactericide and fungicide. Here, we investigated whether PTS2\r\nhas broad-spectrum antitumor activity by studying its cytotoxicity and proapoptotic effects in four cancer cell lines.\r\nMethods: We used MTT assays and trypan blue staining to test the viability of cancer cell lines. Hoechst 33258 and\r\nDAPI staining were used to observe cell apoptosis. Cell-cycle percentages were analyzed by flow cytometry.\r\nApoptosis was assayed using caspase-3 and poly (ADP-ribose) polymerase (PARP) combined with Western blotting.\r\nStudent�s t-test was used for statistical analysis.\r\nResults: PTS2 inhibited proliferation in four cancer cell lines in a dose-dependent manner. Treated cells showed\r\nshrinkage, irregular fragments, condensed and dispersed blue fluorescent particles compared with control cells.\r\nPTS2 induced cycle-arrest and death. Cleavage of caspase-9, caspase-3, and PARP were detected in PTS2-treated\r\ncells. Antitumor activity of PTS2 was more effective against widely used cancer drugs and its precursor.\r\nConclusions: PTS2 appears to have novel cytotoxicity and potent broad-spectrum antitumor activity, which\r\nsuggests its potential as the basis of an anticancer drug.
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