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Background:Apoptosis is a programmed cell death with distinct biochemical and genetic features essential for development, tissue homeostasis and immunity.Defective apoptosis and over proliferation is implicated in initiation and progression of various cancer types, which are characterized by impaired intrinsic and extrinsic apoptotic signaling.Compound Bieshe Kang'ai (CBK) is a traditional Chinese medicinal formula widely used in China for the treatment of various solid cancers, with underlying mechanism to be illuminated.Materials and methods:Human colorectal cancer cells HCT116 were treated with ethanol extract of CBK, followed by determination of the cell proliferation with MTT assay, the activities of caspase-9 and caspase-3 and the protein expression of Bcl-2 (B-cell lymphoma 2) and BAX (Bcl-2-associated X protein) of HCT116 cells, and observation of morphological alterations ofHCT116 cells with Hoechst 33342 staining.Results:CBK suppressed the proliferation of HCT 116 cells in dose-and time-dependent patterns, elevated the activities of caspase-9 and caspase-3, mitigated Bc1-2 expression and augmented BAX expression of HCT116 cells in dose-dependent fashion, and induced cell shrinkage, chromatin condensation and nuclear fragmentation.Conclusions:This study suggests that CBK may protect against cancers potentially by retardation of proliferation and induction of apoptosis of cancer cells.