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

Objectives 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. Methods 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. Key findings 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). Conclusions Our results suggested that TNBG‐5602 might exert potent anticancer activity through increasing the expression of PPARγ.