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.
This is an Open Access article that uses a funding model which does not charge readers or their institutions for access and distributed under the terms of the Creative Commons Attribution License (http://creativecommons.org/licenses/by/4.0) and the Budapest Open Access Initiative (http://www.budapestopenaccessinitiative.org/read), which permit unrestricted use, distribution, and reproduction in any medium, provided the original work is properly credited..
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
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