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Inhibition of lipid synthesis through activation of AMP kinase: an additional mechanism for the hypolipidemic effects of berberine
Open accessAbstract
The alkaloid drug berberine (BBR) was recently described to decrease plasma cholesterol and triglycerides (TGs) in hypercholesterolemic patients by increasing expression of the hepatic low density lipoprotein receptor (LDLR). Using HepG2 human hepatoma cells, we found that BBR inhibits cholesterol and TG synthesis in a similar manner to the AMP-activated protein kinase (AMPK) activator 5-aminoimidazole-4-carboxamide 1-beta-ribofuranoside (AICAR). Significant increases in AMPK phosphorylation and AMPK activity were observed when the cells were incubated with BBR. Activation of AMPK was also demonstrated by measuring the phosphorylation of acetyl-CoA carboxylase, a substrate of AMPK, correlated with a subsequent increase in fatty acid oxidation. All of these effects were abolished by the mitogen-activated protein kinase kinase inhibitor PD98059. Treatment of hyperlipidemic hamsters with BBR decreased plasma LDL cholesterol and strongly reduced fat storage in the liver. These findings indicate that BBR, in addition to upregulating the LDLR, inhibits lipid synthesis in human hepatocytes through the activation of AMPK. These effects could account for the strong reduction of plasma TGs observed with this drug in clinical trials.
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AMP kinase and malonyl-CoA: targets for therapy of the metabolic syndrome
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Efficacy of berberine in patients with type 2 diabetes mellitus
Yin, J., Xing, H., & Ye, J. (2008) · Metabolism · doi:10.1016/j.metabol.2008.01.013 · Cited by 801
Turner, N., Li, J.-Y., Gosby, A., To, S. W. C., Cheng, Z., Miyoshi, H., Taketo, M. M., Cooney, G. J., Kraegen, E. W., James, D. E., et al. (2008) · Diabetes · doi:10.2337/db07-1552 · Cited by 535
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Gomes, A. P., Duarte, F. V., Nunes, P., Hubbard, B. P., Teodoro, J. S., Varela, A. T., Jones, J. G., Sinclair, D. A., Palmeira, C. M., & Rolo, A. P. (2012) · Biochimica et Biophysica Acta (BBA) - Molecular Basis of Disease · doi:10.1016/j.bbadis.2011.10.008 · Cited by 159
Metadata
- Authors
- Brusq, J.-M., Ancellin, N., Grondin, P., Guillard, R., Martin, S., Saintillan, Y., & Issandou, M.
- Venue
- Journal of Lipid Research
- Publisher
- Elsevier BV
- Published
- 2006-06
- Volume
- 47
- Issue
- 6
- Pages
- 1281-1288
- ISSN
- 0022-2275 (ISSN-L)
- OpenAlex
- W1984985876
- Cited by
- 343
- References
- 6
- FWCI
- 9.06
- Type
- journal article
- Language
- en
- Open access
- hybrid
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- CoChat. (2026). Citation check: Inhibition of lipid synthesis through activation of AMP kinase: an additional mechanism for the hypolipidemic effects of berberine. https://app.cochat.ai/papers/10.1194/jlr.m600020-jlr200
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- Brusq, J.-M., Ancellin, N., Grondin, P., Guillard, R., Martin, S., Saintillan, Y., & Issandou, M. (2006). Inhibition of lipid synthesis through activation of AMP kinase: an additional mechanism for the hypolipidemic effects of berberine. Journal of Lipid Research. https://doi.org/10.1194/jlr.m600020-jlr200
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Bibliographic data: Semantic Scholar, OpenAlex, Crossref.
Contains information from the Semantic Scholar Academic Graph Datasets, made available under the ODC Attribution License (ODC-BY 1.0).
Semantic Scholar’s data is described in: Kinney, R., et al. (2023). The Semantic Scholar Open Data Platform. arXiv:2301.10140.
