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[I. Chemical biology and drug discovery-22]



                   Anticancer activity of violacein against hepatocellular


                                                carcinoma cells




                                     Hee Jeong Shin¹, Ye Seul Choi¹˙, Hye Jin Jung¹˙*

          ¹Department of Pharmaceutical Engineering & Biotechnology, Sun Moon University, Asan 336-708, Republic of

                                                          Korea




        Violacein is a deep violet indole derivative produced by a limited number of gram-negative bacteria species and
        exhibits  several  biological  properties  such  as  antitumoral,  antibacterial,  and  antioxidant  activities.  However,  the

        therapeutic effect and anticancer mechanism of violacein against hepatocellular carcinoma (HCC) cells have not

        been studied.  In this  study, we  investigated the inhibitory  effect  of  violacein  on  the  growth  of  HCC  cells.  The
        compound dose-dependently inhibited the growth of three different human HCC cells, including HepG2, Hep3B,
        and Huh7. Moreover, violacein caused apoptosis by activating caspase‑9, caspase-3, PARP, and death receptor 5 in

        Huh7  cells.  Furthermore,  we  evaluated  the  effects  of  violacein  on ROS generation, nuclear fragmentation,
        mitochondrial membrane potential, and expression of Bcl-2 family and cell cycle regulators. In addition, violacein

        downregulated the c-Met signaling pathway that has been implicated in HCC tumorigenesis and progression. These
        results suggest that violacein might be a promising anticancer agent for HCC treatment.
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