Basic Study
Copyright ©The Author(s) 2022. Published by Baishideng Publishing Group Inc. All rights reserved.
World J Gastrointest Oncol. Apr 15, 2022; 14(4): 842-857
Published online Apr 15, 2022. doi: 10.4251/wjgo.v14.i4.842
Berberine retarded the growth of gastric cancer xenograft tumors by targeting hepatocyte nuclear factor 4α
Ling-Li Li, Ze Peng, Qian Hu, Li-Jun Xu, Xin Zou, Dong-Mei Huang, Ping Yi
Ling-Li Li, Ze Peng, Li-Jun Xu, Xin Zou, Dong-Mei Huang, Ping Yi, Department of Integrated Traditional Chinese and Western Medicine, Tongji Hospital, Tongji Medical College, Huazhong University of Science and Technology, Wuhan 430045, Hubei Province, China
Qian Hu, Department of Integrated Traditional Chinese and Western Medicine, West China Hospital of Sichuan University, Chengdu 610041, Sichuan Province, China
Author contributions: Yi P designed the research; Li LL, Peng Z, Xu LJ and Zou X performed the research; Xu LJ, and Zou X contributed analytic tools; Li LL and Peng Z analyzed the data; Li LL wrote the manuscript; Yi P, Hu Q and Huang DM revised the manuscript.
Supported by the National Natural Science Foundation of China, No. 81673757 and No. 81573787.
Institutional review board statement: The study was reviewed and approved by the Huazhong University of Science and Technology Institutional Animal Care and Use Committee.
Conflict-of-interest statement: The authors declare no conflicts of interest regarding the publication of this paper.
Data sharing statement: the data is available from the corresponding author at pyi219@163.com.
Open-Access: This article is an open-access article that was selected by an in-house editor and fully peer-reviewed by external reviewers. It is distributed in accordance with the Creative Commons Attribution NonCommercial (CC BY-NC 4.0) license, which permits others to distribute, remix, adapt, build upon this work non-commercially, and license their derivative works on different terms, provided the original work is properly cited and the use is non-commercial. See: http://creativecommons.org/Licenses/by-nc/4.0/
Corresponding author: Ping Yi, PhD, MD, Department of Integrated Traditional Chinese and Western Medicine, Tongji Hospital, Tongji Medical College, Huazhong University of Science and Technology, No. 1095 Jiefang Avenue, Wuhan 430045, Hubei Province, China. pyi219@163.com
Received: March 1, 2021
Peer-review started: March 2, 2021
First decision: October 3, 2021
Revised: October 15, 2021
Accepted: February 23, 2022
Article in press: February 23, 2022
Published online: April 15, 2022
Processing time: 409 Days and 21.8 Hours
Abstract
BACKGROUND

Gastric cancer is the third deadliest cancer in the world and ranks second in incidence and mortality of cancers in China. Despite advances in prevention, diagnosis, and therapy, the absolute number of cases is increasing every year due to aging and the growth of high-risk populations, and gastric cancer is still a leading cause of cancer-related death. Gastric cancer is a consequence of the complex interaction of microbial agents, with environmental and host factors, resulting in the dysregulation of multiple oncogenic and tumor-suppressing signaling pathways. Global efforts have been made to investigate in detail the genomic and epigenomic heterogeneity of this disease, resulting in the identification of new specific and sensitive predictive and prognostic biomarkers. Trastuzumab, a monoclonal antibody against the HER2 receptor, is approved in the first-line treatment of patients with HER2+ tumors, which accounts for 13%-23% of the gastric cancer population. Ramucirumab, a monoclonal antibody against VEGFR2, is currently recommended in patients progressing after first-line treatment. Several clinical trials have also tested novel agents for advanced gastric cancer but mostly with disappointing results, such as anti-EGFR and anti-MET monoclonal antibodies. Therefore, it is still of great significance to screen specific molecular targets for gastric cancer and drugs directed against the molecular targets.

AIM

To investigate the effect and mechanism of berberine against tumor growth in gastric cancer xenograft models and to explore the role of hepatocyte nuclear factor 4α (HNF4α)-WNT5a/β-catenin pathways played in the antitumor effects of berberine.

METHODS

MGC803 and SGC7901 subcutaneous xenograft models were established. The control group was intragastrically administrated with normal saline, and the berberine group was administrated intragastrically with 100 mg/kg/d berberine. The body weight of nude mice during the experiment was measured to assess whether berberine has any adverse reaction. The volume of subcutaneous tumors during this experiment was recorded to evaluate the inhibitory effect of berberine on the growth of MGC803 and SGC7901 subcutaneous transplantation tumors. Polymerase chain reaction assays were conducted to evaluate the alteration of transcriptional expression of HNF4α, WNT5a and β-catenin in tumor tissues and liver tissues from the MGC803 and SGC7901 xenograft models. Western blotting and IHC were performed to assess the protein expression of HNF4α, WNT5a and β-catenin in tumor tissues and liver tissues from the MGC803 and SGC7901 xenograft models.

RESULTS

In the both MGC803 and SGC7901 xenograft tumor models, berberine significantly reduced tumor volume and weight and thus retarded the growth rate of tumors. In the SGC7901 and MGC803 subcutaneously transplanted tumor models, berberine down-regulated the expression of HNF4α, WNT5a and β-catenin in tumor tissues from both transcription and protein levels. Besides, berberine also suppressed the protein expression of HNF4α, WNT5a and β-catenin in liver tissues.

CONCLUSION

Berberine retarded the growth of MGC803 and SGC7901 xenograft model tumors, and the mechanism behind these anti-growth effects might be the downregulation of the expression of HNF4α-WNT5a/β-catenin signaling pathways both in tumor tissues and liver tissues of the xenograft models.

Keywords: Berberine; Gastric cancer; Xenograft models; Hepatocyte nuclear factor 4α; WNT5a

Core Tip: Hepatocyte nuclear factor 4α (HNF4α) is a member of the nuclear receptor transcription factor family, which is at the center of a complex transcriptional regulatory network and regulates the biological effects of different pathways via transcriptional regulation of differential target genes. The role of HNF4α in gastric cancer is poorly understood, so the study of the berberine targeting HNF4α in gastric cancer cell xenograft models is of great significance. In this study, we showed that the inhibition of HNF4α genes/proteins by berberine was correlated with the tumor inhibition in gastric cancer xenografts. Further experiments also indicated that berberine downregulated HNF4a to exert its antineoplastic activity in vivo.