Abstract
Anti-proliferative and apoptosis-inducing effects of 2,4,3′,4′-tetramethoxy-biphenyl (TMBP) on human gastric cancer MGC-803 cells were investigated. The molecular mechanisms of TMBP-mediated tumor cell death were detected by clonogenic assay, staining with Hoechst 33258, DNA fragmentation assay, Western blot analysis and flow cytometry assay. Studies on MGC-803 cells treated with TMBP showed that TMBP inhibited the proliferation of MGC-803 cells in a time- and dose-dependent manner. The induction of apoptosis by TMBP was accompanied by the loss of mitochondrial membrane potential (ΔΨm), cytochrome C release and activation of caspase cascade, resulting in the cleavage of some specific substrates for caspase-3 such as poly (ADP-ribose) polymerase (PARP). In conclusion, these findings showed that TMBP may induce the apoptosis of MGC-803 through a mitochondrial/caspase pathway, suggesting its possible use for treating human cancers.
Highlights
Gastric cancer is the fourth most common cancer, after lung, breast and colorectal cancer, and the second leading cause of cancer death worldwide
The results showed that TMBP induced apoptotic cell death at various concentrations, which the effect of 100 μM is stronger than others (Figure 2B)
Twelve intermediates biphenyl compounds were produced in the course of the synthesis of protosappanin A
Summary
Gastric cancer is the fourth most common cancer, after lung, breast and colorectal cancer, and the second leading cause of cancer death worldwide. For this reason, it is necessary to determine an effective gastric cancer therapy strategy. Apoptosis can be initiated via either an extrinsic pathway or intrinsic pathway, with the extrinsic pathway being initiated by cell surface receptors and the intrinsic pathway being initiated by a mitochondriamediated death signaling cascade (Hengartner, 2000; Harada and Grant, 2000; Ghobrial et al, 2005; Fulda and Debatin, 2006). It has been reported previously that biphenyl compounds have biological activity including anti-oxidant and anticancer (Shen and Du, 2008). This article discloses our efforts to evaluate the biological activity of our structurally novel compounds I-XII (Table I)
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