title: Vitexicarpin induces apoptosis in human prostate carcinoma PC-3 cells through G2/M phase arrest.
abstract: Vitexicarpin (3', 5-dihydroxy-3, 4', 6, 7-tetramethoxyflavone), a polymethoxyflavone isolated from Viticis Fructus (Vitex rotundifolia Linne fil.), has long been used as an anti-inflammatory herb in traditional Chinese medicine. It has also been reported that vitexicarpin can inhibit the growth of various cancer cells. However, there is no report elucidating its effect on human prostate carcinoma cells. The aim of the present study was to examine the apoptotic induction activity of vitexicarpin on PC-3 cells and molecular mechanisms involved. MTT studies showed that vitexicarpin dose-dependently inhibited growth of PC-3 cells with an IC50~28.8 μM. Hoechst 33258 staining further revealed that vitexicarpin induced apoptotic cell death. The effect of vitexicarpin on PC-3 cells apoptosis was tested using prodium iodide (PI)/Annexin V-FITC double staining and flow cytometry. The results indicated that vitexicarpin induction of apoptotic cell death in PC-3 cells was accompanied by cell cycle arrest in the G2/M phase. Furthermore, our study demonstrated that vitexicarpin induction of PC-3 cell apoptosis was associated with upregulation of the proapoptotic protein Bax, and downregulation of antiapoptotic protein Bcl-2, release of Cytochrome c from mitochondria and decrease in mitochondrial membrane potential. Our findings suggested that vitexicarpin may become a potential leading drug in the therapy of prostate carcinoma.
authors: School of life sciences, Liaoning Provincial Key Laboratory of Biotechnology and Drug Discovery, Liaoning Normal University, Dalian, China.
authors: Fan-Min
authors: FM
authors: Meng
authors: Jing-Bo
authors: JB
authors: Yang
authors: Chun-Hui
authors: CH
authors: Yang
authors: Yu
authors: Y
authors: Jiang
authors: Yong-Feng
authors: YF
authors: Zhou
authors: Bo
authors: B
authors: Yu
authors: Hong
authors: H
authors: Yang
mesh_terms: D017209:Apoptosis / Q000187:drug effects* / Q000235:genetics; D002277:Carcinoma / Q000188:drug therapy* / Q000235:genetics; D059447:Cell Cycle Checkpoints / Q000187:drug effects* / Q000235:genetics; D016923:Cell Death / Q000187:drug effects / Q000235:genetics; D002455:Cell Division / Q000187:drug effects* / Q000235:genetics; D045744:Cell Line, Tumor; D045304:Cytochromes c / Q000235:genetics; D015536:Down-Regulation / Q000187:drug effects / Q000235:genetics; D005419:Flavonoids / Q000494:pharmacology*; D016195:G2 Phase / Q000187:drug effects* / Q000235:genetics; D006801:Humans; D008297:Male; D008516:Medicine, Chinese Traditional / Q000379:methods; D053078:Membrane Potential, Mitochondrial / Q000187:drug effects / Q000235:genetics; D008928:Mitochondria / Q000235:genetics; D010936:Plant Extracts / Q000494:pharmacology; D011471:Prostatic Neoplasms / Q000188:drug therapy* / Q000235:genetics; D019253:Proto-Oncogene Proteins c-bcl-2 / Q000235:genetics; D015854:Up-Regulation / Q000187:drug effects / Q000235:genetics; D051028:bcl-2-Associated X Protein / Q000235:genetics
chemical_list: D005419:Flavonoids; D010936:Plant Extracts; D019253:Proto-Oncogene Proteins c-bcl-2; D051028:bcl-2-Associated X Protein; C054133:casticin; D045304:Cytochromes c