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Icariin promotes osteogenic differentiation by upregulating alpha-enolase expression

Osteogenic differentiation is a crucial biological process for maintaining bone remodelling. Aerobic glycolysis is the main source of energy for osteogenic differentiation. Alpha-enolase (Eno1), a glycolytic enzyme, is a therapeutic target for numerous diseases. Icariin, a principal active component of the traditional Chinese medicine Epimedium grandiflorum, can stimulate osteogenic differentiation. Here, we aimed to determine if icariin promotes osteogenic differentiation via Eno1. Icariin (1 μM) significantly promoted osteogenic differentiation of MC3T3-E1 cells. Icariin upregulated Eno1 protein and gene expressions during osteogenic differentiation. Moreover, ENOblock, a specific inhibitor of Eno1, markedly inhibited icariin-induced osteogenic differentiation. Futhermore, western blot assay showed that Eno1 might mediate osteogenic differentiation through the BMP/Smad4 signalling pathway. Collectively, Eno1 could be a promising drug target for icariin to regulate osteogenic differentiation.

 

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The passage describes a study conducted to investigate the effects of icariin, a compound found in the traditional Chinese medicine Epimedium grandiflorum, on osteogenic differentiation. Osteogenic differentiation is an important biological process involved in maintaining bone remodeling.

The study found that icariin at a concentration of 1 μM significantly promoted the osteogenic differentiation of MC3T3-E1 cells. This suggests that icariin has a positive effect on the formation of bone cells. Additionally, icariin was found to upregulate the expression of alpha-enolase (Eno1), which is a glycolytic enzyme.

To further understand the role of Eno1 in icariin-induced osteogenic differentiation, the researchers used ENOblock, a specific inhibitor of Eno1. They found that ENOblock markedly inhibited the osteogenic differentiation induced by icariin. This indicates that Eno1 is involved in mediating the effects of icariin on osteogenic differentiation.

Furthermore, the study explored the potential signaling pathway through which Eno1 mediates osteogenic differentiation. The researchers conducted a western blot assay and found that Eno1 may exert its effects through the BMP/Smad4 signaling pathway. This pathway is known to play a crucial role in regulating bone formation and remodeling.

Based on these findings, the study suggests that Eno1 could be a promising therapeutic target for icariin to regulate osteogenic differentiation. By targeting Eno1, icariin may modulate the BMP/Smad4 signaling pathway and promote the formation of bone cells. This research provides valuable insights into the potential mechanisms underlying the osteogenic effects of icariin and highlights Eno1 as a potential target for therapeutic intervention in bone-related diseases.

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S7443 AP-III-a4 (ENOblock) AP-III-a4 (ENOblock) is the first nonsubstrate analogue inhibitor of enolase with IC50 of 0.576 μM.

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