©　2017,　Editorial　Office　of　Chinese　Traditional　and　Herbal　Drugs.　All　right　reserved.　Objective　To　analyze　inhibitory　effect　of　taspine　derivative　TasD1-6　on　human　liver　cancer　cells　of　Hep3B,　HepG2,　and　BEL7402,　and　to　study　their　preliminary　mechanism　of　anticancer　action.　Methods　Effect　of　TasD1-6　on　cell　growth　of　Hep3B,　HepG2,　and　BEL7402　were　determined　by　3-(4,5-dimethyl-2-thiazolyl)-2,5-diphenyl-2-H-tetrazolium　bromide　(MTT)　and　real-time　cellular　analysis　(RTCA)　assay.　Effect　of　TasD1-6　on　Hep3B　cell　morphology　was　investigated　with　crystal　violet　staining.　Next,　Hep3B　cell　apoptosis　was　analyzed　by　Annexin　V　FITC/PI　and　Hoechst　33258　staining.　Flow　cytometry　was　used　to　determine　Hep3B　cell　cycle.　Effect　of　TasD1-6　on　cell　apoptosis　protein　expression　in　Hep3B　cell　was　determined　by　Western　blotting.　Results　MTT　and　RTCA　assay　demonstrated　that　TasD1-6　significantly　inhibited　the　growth　of　Hep3B　cell　and　the　IC50　was　(11.3　±　1.6)　μmol/L.　Hep3B　cell　morphology　indicated　the　shrinkage　and　obvious　morphology　changes.　And　TasD1-6　induced　the　Hep3B　cell　apoptosis　in　dose-dependent　manner.　Cell　was　stopped　as　G1　phase　by　TasD1-6.　Western　blotting　analysis　showed　TasD1-6　could　upregulate　the　protein　expression　of　p53　and　Bax　and　downregulate　Mcl-1　protein　expression　(P　＜　0.05).　Conclusion　Taspine　derivative　TasD1-6　shows　better　inhibitory　action　on　the　growth　of　human　liver　cancer　Hep3B　cell　than　HepG2　and　BEL7402　cells.　At　the　same　time,　TasD1-6　can　change　cell　cycle　and　induce　cell　apoptosis,　which　probably　related　to　upregulation　of　p53　and　Bax　protein　expression　and　downregulation　of　Mcl-1　protein　expression.