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Liraglutide attenuates the osteoblastic differentiation of MC3T3‑E1 cells by modulating AMPK/mTOR signaling.

Mol Med Rep · 2016

Last updated 2026-05-28

In lab tests, the diabetes/obesity drug liraglutide reduced bone-forming cell activity in a dose-dependent way, lowering markers linked to bone growth by up to 50%. The effect appears tied to changes in two cell-signaling pathways: liraglutide boosted one pathway (AMPK) while lowering another (mTOR) and a growth factor (TGF-β). Blocking the AMPK pathway or activating mTOR reversed liraglutide’s effects, suggesting these pathways are key to its action.

AI summary of the abstract below.

JournalMol Med Rep, 2016
Citations24
Relative citation ratio0.91
NIH percentile47
Molecules liraglutide

Abstract

Liraglutide, a synthetic analogue of glucagon-like peptide‑1, is utilized in the treatment of type 2 diabetes and obesity. Liraglutide has been previously demonstrated to prevent osteoblastic differentiation of human vascular smooth muscle cells, resulting in the slowing of arterial calcification, however, its effect on bone formation remains unclear. The present study investigated the effect of liraglutide on osteoblastic differentiation using Alizarin Red S staining, and examined the molecular mechanisms underlying the regulatory effect by western blot analysis. The present study demonstrated that protein expression levels of phosphorylated adenosine monophosphate‑activated protein kinase (p‑AMPK) were downregulated in MC3T3‑E1 cells during osteoblastic differentiation in commercial osteogenic differentiation medium, whereas protein expression levels of transforming growth factor‑β (TGF‑β) and phosphorylated mammalian target of rapamycin (p‑mTOR) increased. Liraglutide was subsequently demonstrated to dose‑dependently attenuate the osteoblastic differentiation of MC3T3‑E1 cells, to upregulate p‑AMPK, and downregulate p‑mTOR and TGF‑β protein expression levels. Treatment with an AMPK‑specific inhibitor, Compound C, eradicated the effect of liraglutide on osteoblastic differentiation, and p‑mTOR and TGF‑β downregulation. An mTOR activator, MHY1485, also abolished the inhibitory effect of liraglutide on osteoblastic differentiation, and resulted in p‑mTOR and TGF‑β downregulation, but did not attenuate the liraglutide‑induced increase in p‑AMPK protein expression levels. The results of the present study demonstrate that liraglutide attenuates osteoblastic differentiation of MC3T3‑E1 cells via modulation of AMPK/mTOR signaling. The present study revealed a novel function of liraglutide, which contributes to the understanding of its pharmacological and physiological effects in clinical settings.

Verbatim abstract via PubMed 27600753 ↗

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