Tropical Journal of Pharmaceutical Research

Original Research Article | OPEN ACCESS

Azaindole inhibits liver cancer cell proliferation in vitro and in vivo by targeting the expression of kinesin family member C1

Zhen You¹, Bei Li¹, Jun Gao², Jiong Lu¹, Ruihua Xu¹

¹Department of Biliary Surgery, Westchina Hospital of Sichuan University; ²Department of Toxicological Inspection, Sichuan Centre for Disease Prevention and Control, Chengdu, Sichuan 610041, China.

For correspondence:- Ruihua Xu Email: ruihuaxuo41@gmail.com Tel:+862885422114

Accepted: 23 January 2021 Published: 28 February 2021

Citation: You Z, Li B, Gao J, Lu J, Xu R. Azaindole inhibits liver cancer cell proliferation in vitro and in vivo by targeting the expression of kinesin family member C1. Trop J Pharm Res 2021; 20(2):359-364 doi: 10.4314/tjpr.v20i2.20

© 2021 The authors.
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Abstract

Purpose: To investigate the effect of azaindole on proliferation of liver cancer cells, as well as the underlying mechanism.

Methods: Colony forming and 3?(4,5?dimethylthiazole?2?yl)?2,5?biphenyl tetrazolium bromide (MTT) assays were used to determine the effect of azaindole on cell proliferation. A tumor model was established through subcutaneous administration of HEPG2 cells to rats. Thereafter, in vivo tumor development was measured using Vernier caliper.

Results: The proliferation potential of HEPG2 and SNU-398 cells was markedly and dose-dependently suppressed by treatment with azaindole at doses of 2, 4, 8, 16 and 20 µM (p < 0.05). The expression levels of Ki67 and PCNA levels were significantly down-regulated in HEPG2 and SNU-398 cells on treatment with 20 µM azaindole. Moreover, azaindole significantly suppressed mRNA and protein expressions of KIFC1 in HEPG2 and SNU-398 cells (p < 0.05). Tumor volume in azaindole-treated rats on day 21 was greatly reduced, while KIFC1 expression in azaindole-treated rat tumor tissue was significantly down-regulated, when compared to the model group (p < 0.05).

Conclusion: Azaindole targets proliferation of liver cancer cells in vitro and inhibits tumor growth in vivo through a mechanism involving down-regulation of KIFCI expression. Thus, azaindole is a potential therapeutic candidate for liver cancer.

Keywords: Liver cancer, Azaindole, Malignant tumor, Kinesin, Antartic sponge