title: [Silencing pyruvate kinase M2 sensitizes human prostate cancer PC3 cells to gambogic acid-induced apoptosis].
abstract: OBJECTIVE
  To study the effect of silencing pyruvate kinase M2 (PKM2) on gambogic acid (GA)-induced apoptosis of human prostate cancer PC3 cells.
  
  
  METHODS
  Three specific PKM2 siRNAs and one negative control siRNA (si-NC) were transfected into PC3 cells. The silencing effect of PKM2 siRNAs was determined by real-time fluorescence quantitative PCR (qRT-PCR) and Western blot, and the effects of PKM2 siRNA on the vitality and apoptosis of GA-stimulated PC3 cells detected by MTT and AO/EB double staining, respectively. The mRNA and protein levels of c-myc and cyclin D1 were analyzed by qRT-PCR and Western blot, respectively.
  
  
  RESULTS
  All the 3 PKM2 siRNAs effectively reduced the mRNA and protein expressions of PKM2, and PKM2 siRNA-1 exhibited the strongest silencing effect. At 24 h after transfection, the expression levels of PKM2 mRNA and protein were reduced by 70% and 85%, respectively (P < 0.05). Twenty-four hours of treatment with GA (0.5 micromol/L) following transfection with PKM2 siRNA-1 inhibited the vitality of the PC3 cells by 68%, increased their apoptosis, and significantly down-regulated the mRNA and protein levels of c-myc (50% and 35%) and cyclin D1 (60% and 20%) (P < 0.05).
  
  
  CONCLUSIONS
  Inhibition of PKM2 sensitized PC3 cells to GA-induced apoptosis, suggesting that PKM2 may be a potential therapeutic target for sensitizing human prostate cancer to GA.
authors: Department of Urology, Wuhan First Hospital, Wuhan, Hubei 430030, China.
authors: Lei
authors: L
authors: Lü
authors: Liang
authors: L
authors: Wang
authors: Guo-Song
authors: GS
authors: Jiang
authors: Chuan-Hua
authors: CH
authors: Zhang
authors: Fu-Qing
authors: FQ
authors: Zeng
mesh_terms: D017209:Apoptosis / Q000187:drug effects*; D002352:Carrier Proteins / Q000235:genetics* / Q000378:metabolism; D045744:Cell Line, Tumor; D006801:Humans; D008297:Male; D008565:Membrane Proteins / Q000235:genetics* / Q000378:metabolism; D011471:Prostatic Neoplasms / Q000235:genetics* / Q000378:metabolism / Q000473:pathology; D034622:RNA Interference; D034741:RNA, Small Interfering; D013963:Thyroid Hormones / Q000235:genetics* / Q000378:metabolism; D044004:Xanthones / Q000494:pharmacology*; D000097810:Thyroid Hormone-Binding Proteins
chemical_list: D002352:Carrier Proteins; D008565:Membrane Proteins; D034741:RNA, Small Interfering; D013963:Thyroid Hormones; D044004:Xanthones; D000097810:Thyroid Hormone-Binding Proteins; C052659:gambogic acid