Berberine on the prevention and management of cardiometabolic disease: clinical applications and mechanisms of action
Abstract
Berberine is an alkaloid from several medicinal plants originally used to treat diarrhea and dysentery as a traditional Chinese herbal medicine. In recent years, berberine has been discovered to exhibit a wide spectrum of biological activities in the treatment of diverse diseases ranging from cancer and neurological dysfunctions to metabolic disorders and heart diseases. This review article summarizes the clinical practice and laboratory exploration of berberine for the treatment of cardiometabolic and heart diseases, with a focus on the novel insights and recent advances of the underlying mechanisms recognized in the past decade. Berberine was found to display pleiotropic therapeutic effects against dyslipidemia, hyperglycemia, hypertension, arrhythmia, and heart failure. The mechanisms of berberine for the treatment of cardiometabolic disease involve combating inflammation and oxidative stress such as inhibiting proprotein convertase subtilisin/kexin 9 (PCSK9) activation, regulating electrical signals and ionic channels such as targeting human ether-a-go-go related gene (hERG) currents, promoting energy metabolism such as activating adenosine monophosphate-activated protein kinase (AMPK) signaling pathway, modifying gut microbiota to promote transforming of berberine into its intestine-absorbable form, and interacting with non-coding RNAs via targeting multiple signaling pathways such as AMPK, mechanistic target of rapamycin (mTOR), etc. Collectively, berberine appears to be safe and well-tolerated in clinical practice, especially for those who are intolerant to statins. Knowledge from this field may pave the way for future development of more effective pharmaceutical approaches for managing cardiometabolic risk factors and preventing heart diseases.
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Berberine may be more effective in short-term treatment lasting ≤90 days, possibly due to drug tolerance or metabolic adaptation with extended treatment.
“These findings support that berberine may be more effective in short-term treatment lasting ≤90 days, possibly due to drug tolerance or metabolic adaptation with extended treatment (Cao et al., 2021).”
From Efficacy and safety of berberine on the components of metabolic syndrome: a systematic review and meta-analysis of randomized placebo-controlled trials (2025) · cites this paper as Cao et al., 2021
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- Authors
- Cao, R. Y., Zheng, Y., Zhang, Y., Jiang, L., Li, Q., Sun, W., Gu, W., Cao, W., Zhou, L., Zheng, H., & Yang, J.
- Affiliations
- Fudan University (CN)
- Department of Rehabilitation, Shanghai Xuhui Fengling Community Healthcare Service Center, Shanghai 200032, P. R. China
- Department of Rehabilitation, Shanghai Xuhui Caohejing Community Healthcare Service Center, Shanghai 200235, P. R. China
- Venue
- The American Journal of Chinese Medicine
- Publisher
- World Scientific Pub Co Pte Ltd
- Published
- 2021-01
- Volume
- 49
- Issue
- 07
- Pages
- 1645-1666
- ISSN
- 0090-2942 (ISSN-L)
- 0192-415X
- 1793-6853
- OpenAlex
- W3196530787
- Cited by
- 31
- References
- 97
- Citations by year
- 2026: 6 · 2025: 8 · 2024: 9 · 2023: 4 · 2022: 3 · 2021: 1
- FWCI
- 0.54
- Type
- journal article
- Language
- en
- Open access
- closed
- Locations
- The American Journal of Chinese Medicine (publishedVersion)
- PubMed (publishedVersion)
- Funders
- National Natural Science Foundation of China (81973612)
- Shanghai Municipal Health Commission (ZK2019A11, ZK2019A10)
- Topics
- Health Sciences › Medicine › Pharmacology › Berberine and alkaloids research
- Health Sciences › Medicine › Complementary and alternative medicine › Traditional Chinese Medicine Analysis
- Life Sciences › Biochemistry, Genetics and Molecular Biology › Molecular Biology › Metabolism, Diabetes, and Cancer
- Keywords
- berberine, cardiometabolic disease, heart failure, dyslipidemia, hyperglycemia, hypertension, cardiac arrhythmias, inflammation, oxidative stress, PCSK9, AMPK signaling, gut microbiota, non-coding RNA, mTOR signaling, statin intolerance, traditional Chinese medicine, alkaloids
- MeSH terms
- Berberine, Cardiovascular Diseases, Humans, Medicine, Chinese Traditional, Molecular Structure
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