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Updated: Jan 28, 2026

Seven Steps to Stellate Cells
Published on: May 10, 2011
Alogliptin alleviates liver fibrosis via suppression of activated hepatic stellate cell
Hanyan Zhang1, Dandan Sun2, Guanzhen Wang2
1School of Pharmacy, Nanchang University, 461 Bayi Road, Nanchang, 330006, China.
Abstract:
Liver fibrosis occurs in most types of chronic liver diseases. The understanding of the pathogenesis of liver fibrosis has grown considerably, but the effective treatments are still lacking. Alogliptin, a classical Dipeptidyl peptidase-4 (DPP4) inhibitor with great effects on type 2 diabetes, has shown the potential to protect liver, but its effects on the progression of liver fibrosis have not been clarified. Herein, we explored the anti-fibrosis effects of alogliptin. In vitro, we demonstrated that alogliptin suppressed the activation of LX-2 upon transforming growth factor-β (TGF-β) challenge. In vivo, chronic treatment with alogliptin alleviated hepatic steatosis and protected from the liver injury in ob/ob mice, which delayed the progression of liver fibrosis. Furthermore, alogliptin significantly relieved the hepatic fibrosis in CCl4-induced liver fibrosis mouse model. In conclusion, our results demonstrate that negatively modulation of alogliptin on hepatic stellate cell (HSC) activation might contribute to liver fibrosis alleviation. Our research provides the potential possibility of alogliptin on the application for liver fibrosis therapy and suggests that DPP4 may be a novel target for liver fibrosis therapy.
Insights
Alogliptin, a DPP4 inhibitor, shows potential in treating liver fibrosis by suppressing hepatic stellate cell activation. This study demonstrates its anti-fibrotic effects in vitro and in vivo, suggesting DPP4 as a novel therapeutic target.
Area of Science:
- Hepatology
- Pharmacology
- Cell Biology
Background:
- Liver fibrosis is a common consequence of chronic liver diseases with limited effective treatments.
- Dipeptidyl peptidase-4 (DPP4) inhibitors, like alogliptin, are used for type 2 diabetes and show potential liver-protective effects.
- The anti-fibrotic impact of alogliptin on liver fibrosis progression remains unclear.
Purpose of the Study:
- To investigate the anti-fibrosis effects of alogliptin.
- To explore alogliptin's mechanism in modulating hepatic stellate cell activation.
- To assess alogliptin's therapeutic potential for liver fibrosis.
Main Methods:
- In vitro: Assessed alogliptin's effect on LX-2 cells challenged with transforming growth factor-β (TGF-β).
- In vivo: Evaluated alogliptin's impact on liver injury, steatosis, and fibrosis in ob/ob and CCl4-induced mouse models.
Main Results:
- Alogliptin suppressed LX-2 cell activation in vitro.
- Chronic alogliptin treatment reduced hepatic steatosis and liver injury in ob/ob mice, delaying fibrosis progression.
- Alogliptin significantly alleviated liver fibrosis in a CCl4-induced mouse model.
Conclusions:
- Alogliptin negatively modulates hepatic stellate cell (HSC) activation, contributing to liver fibrosis alleviation.
- Alogliptin demonstrates therapeutic potential for liver fibrosis.
- DPP4 inhibition represents a novel therapeutic strategy for liver fibrosis.
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