title: Antitumour effects of tetrazanbigen against human hepatocellular carcinoma QGY-7701 through inducing lipid accumulation in vitro and in vivo.
abstract: OBJECTIVE
  Tetrazanbigen (TNBG) is a newly synthesized compound with an isoquinoline moiety, and its antitumour effects were evaluated in in-vitro and in-vivo models.
  
  
  METHODS
  3-[4, 5-dimethylthiazol-2-yl]-2,5-diphenyl tetrazolium bromide (MTT) assay was used to measure the antiproliferative activity of TNBG on cancer cell lines. Antitumour activity of TNGB in vivo was also assessed in a xenograft model of human hepatocellular carcinoma QGY-7701 cell line. Cell cycle and cell apoptosis analysis was performed.
  
  
  RESULTS
  TNBG exhibited strong antitumour efficacy against six human cancer cell lines with IC50 range of 2.13-8.01 μg/ml. The IC50 of TNBG on normal hepatic cells was 11.25 μg/ml. Lots of lipid droplets were observed in cytoplasm of human hepatocellular carcinoma QGY-7701 cells after treatment of TNBG. S phase arrest and apoptosis induction by TNBG were also found on QGY-7701 cells. Intraperitoneal injection of TNBG (1.5 mg/kg/day) resulted in significant decreases in tumour volume and tumour weight on nude mice bearing QGY-7701 cells xenografts. Results from pathological analysis in nude mice demonstrated that TNBG could induce lipid accumulation specifically in cancer tissue rather than in other normal organs, tissues and blood.
  
  
  CONCLUSIONS
  These results suggested that TNBG might exert potent antitumour activity through inducing lipid accumulation in cancer cell.
authors.affiliation: Department of Pharmacy, Chongqing Medical and Pharmaceutical College, Chongqing, China.
authors.forename: Xiaohong
authors.initials: X
authors.lastname: Zheng
authors.affiliation: Research Laboratory of Pharmaceutical Chemistry and Biological Materials, School of Pharmacy, Chongqing Medical University, Chongqing, China.
authors.forename: Wei
authors.initials: W
authors.lastname: Li
authors.affiliation: Department of Pharmacy, Chongqing Medical and Pharmaceutical College, Chongqing, China.
authors.forename: Zuoping
authors.initials: Z
authors.lastname: Lan
authors.affiliation: Research Laboratory of Pharmaceutical Chemistry and Biological Materials, School of Pharmacy, Chongqing Medical University, Chongqing, China.
authors.forename: Xiaolan
authors.initials: X
authors.lastname: Yang
authors.affiliation: Research Laboratory of Pharmaceutical Chemistry and Biological Materials, School of Pharmacy, Chongqing Medical University, Chongqing, China.
authors.forename: Longjiang
authors.initials: L
authors.lastname: Li
authors.affiliation: Department of Pharmacy, Children's Hospital of Chongqing Medical University, Chongqing, China.
authors.forename: Yonghua
authors.initials: Y
authors.lastname: Yuan
authors.affiliation: Department of Nuclear Medicine, The First Affiliated Hospital of Chongqing Medical University, Chongqing, China.
authors.forename: Zhu
authors.initials: Z
authors.lastname: Xia
authors.affiliation: Research Laboratory of Pharmaceutical Chemistry and Biological Materials, School of Pharmacy, Chongqing Medical University, Chongqing, China.
authors.forename: Xunguan
authors.initials: X
authors.lastname: Chen
authors.affiliation: Research Laboratory of Pharmaceutical Chemistry and Biological Materials, School of Pharmacy, Chongqing Medical University, Chongqing, China.
authors.forename: Xinyu
authors.initials: X
authors.lastname: Zhang
authors.affiliation: Research Laboratory of Pharmaceutical Chemistry and Biological Materials, School of Pharmacy, Chongqing Medical University, Chongqing, China.
authors.forename: Yu
authors.initials: Y
authors.lastname: Yu
mesh_terms: D000818:Animals; D000970:Antineoplastic Agents / Q000008:administration & dosage / Q000494:pharmacology*; D017209:Apoptosis / Q000187:drug effects; D001391:Azo Compounds / Q000008:administration & dosage / Q000494:pharmacology*; D006528:Carcinoma, Hepatocellular / Q000188:drug therapy* / Q000473:pathology; D002453:Cell Cycle / Q000187:drug effects; D045744:Cell Line, Tumor; D049109:Cell Proliferation / Q000187:drug effects; D005260:Female; D006067:Gonanes / Q000008:administration & dosage / Q000494:pharmacology*; D006801:Humans; D020128:Inhibitory Concentration 50; D008055:Lipids / Q000737:chemistry; D008113:Liver Neoplasms / Q000188:drug therapy* / Q000473:pathology; D051379:Mice; D008819:Mice, Nude; D009369:Neoplasms / Q000188:drug therapy / Q000473:pathology; D023041:Xenograft Model Antitumor Assays
chemical_list: D000970:Antineoplastic Agents; D001391:Azo Compounds; D006067:Gonanes; D008055:Lipids; C552897:tetrazanbigen
keywords: antitumour effect; human hepatocellular carcinoma; lipid accumulation; tetrazanbigen