The　rapid　screening　technology　was　used　to　investigate　the　transcriptional　regulation　effect　of　main　chemical　constituents　in　tubers　of　Polygonum　multiflorum,　including　2,　3,　5,　4＇-tetrahydroxystilbene-2-O-β-D-glucopyranoside(THSG)　and　anthraquinones　(such　as　rhein,　chrysophanol,　aloe-emodin,　emodin)　on　CYP3A4　drug　inducers　induced　by　human　pregnancy　X　receptor　(PXR).　The　effect　of　chemical　composition　on　the　cell　activity　was　detected　by　MTS　cell　viability　assay.　IC　50　was　calculated.　The　expression　vector　and　the　reporter　vector　were　co-transfected　into　HepG2　cells,　with　10　μmol·L　-1　rifampicin　(RIF)　as　a　positive　control,　and　10　μmol·L　-1　ketoconazole　(TKZ)　as　a　negative　control.　After　treated　with　different　concentrations　of　anthraquinones　(2.5,　5,　10　μmol·L　-1　)　for　24　h,　the　cells　were　tested　for　dual　luciferase　activity.　The　results　show　that　the　inhibitory　effect　of　THSG,　chrysophanol,　emodin,　rhein　and　aloe-emodin　on　CYP3A4　was　inhibited　by　co-transfection　of　pcDNA3.　1　and　pGL4.17-CYP3A4.　The　expressions　of　pcDNA3.14-PXR　and　pGL4.17-CYP3A4　were　induced　by　the　four　compounds.　Besides,　emodin　had　a　direct　inducing　effect.　In　conclusion,　the　four　anthraquinone　compounds　have　an　inducing　effect　on　CYP3A4　by　PXR,　but　emodin　can　directly　induce　CYP3A4.　THSG　can　inhibit　CYP3A4,　but　plasmid　can　induce　CYP3A4　after　intervened　with　PXR.　These　results　suggest　that　we　should　pay　attention　to　the　liver　function　and　avoid　liver　damage　in　the　combined　administration　of　drugs.　©　2017,　Editorial　Board　of　China　Journal　of　Chinese　Materia　Medica.　All　right　reserved.