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TNBG-5602, a novel derivative of quinoxaline, inhibits liver cancer growth via upregulating peroxisome proliferator-activated receptor γ in vitro and in vivo.

Authors
  • Hu, Xuelian1, 2
  • Wan, Chunmei1
  • Gan, Zongjie1
  • Liu, Rongxing3, 4
  • Chen, Yongjie1
  • Wang, Jing5
  • Gan, Linling1
  • Chen, Yuhang1
  • Li, Yingbo6
  • He, Baicheng3, 4
  • Yu, Yu1
  • 1 Department of Medical Chemistry, School of Pharmacy, Chongqing Medical University, Chongqing, China. , (China)
  • 2 Department of Pharmacy, Xinqiao Hospital, Chongqing, China. , (China)
  • 3 Department of Pharmacology, School of Pharmacy, Chongqing Medical University, Chongqing, China. , (China)
  • 4 Key Laboratory for Biochemistry and Molecular Pharmacology of Chongqing, Chongqing Medical University, Chongqing, China. , (China)
  • 5 Department of Blood Transfusion, The First Affiliate Hospital of Chongqing Medical University, Chongqing, China. , (China)
  • 6 Department of Physiology, Chongqing Medical University, Chongqing, China. , (China)
Type
Published Article
Journal
The Journal of pharmacy and pharmacology
Publication Date
Nov 01, 2019
Volume
71
Issue
11
Pages
1684–1694
Identifiers
DOI: 10.1111/jphp.13159
PMID: 31446646
Source
Medline
Keywords
Language
English
License
Unknown

Abstract

TNBG-5602 is a newly synthesized compound with an isoquinoline structure. In the present study, we demonstrated the anticancer effect of TNBG-5602 in in-vitro and in-vivo models and investigated its possible anticancer mechanism. The antiproliferation effect of TNBG-5602 in vitro was evaluated in human liver cancer cell line QGY-7701. The acute toxicity of TNBG-5602 was evaluated in mice. The anticancer activity of TNBG-5602 in vivo was assessed in a xenograft model of human liver cancer cell line QGY-7701. The results of CCK-8 assay showed that TNBG-5602 can effectively inhibit the proliferation of liver cancer cells in vitro. The acute toxicity test in mice showed that the LD50 of TNBG-5602 was 172 mg/kg. In a xenograft liver cancer model, TNBG-5602 could remarkably inhibit the growth of tumours. During in-vitro and in-vivo studies, we noted that TNBG-5602 could induce lipid accumulation in cancer cells and tissues. Further study indicated that the anticancer effect of TNBG-5602 may be exerted through activating peroxisome proliferator-activated receptor γ (PPARγ) and downregulating proliferating cell nuclear antigen (PCNA). Our results suggested that TNBG-5602 might exert potent anticancer activity through increasing the expression of PPARγ. © 2019 Royal Pharmaceutical Society.

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