Multi-Pharmacology of Berberine in Atherosclerosis and Metabolic Diseases: Potential Contribution of Gut Microbiota
Open accessAbstract
Atherosclerosis (AS), especially atherosclerotic cardiovascular diseases (ASCVDs), and metabolic diseases (such as diabetes, obesity, dyslipidemia, and nonalcoholic fatty liver disease) are major public health issues worldwide that seriously threaten human health. Exploring effective natural product-based drugs is a promising strategy for the treatment of AS and metabolic diseases. Berberine (BBR), an important isoquinoline alkaloid found in various medicinal plants, has been shown to have multiple pharmacological effects and therapeutic applications. In view of its low bioavailability, increasing evidence indicates that the gut microbiota may serve as a target for the multifunctional effects of BBR. Under the pathological conditions of AS and metabolic diseases, BBR improves intestinal barrier function and reduces inflammation induced by gut microbiota-derived lipopolysaccharide (LPS). Moreover, BBR reverses or induces structural and compositional alterations in the gut microbiota and regulates gut microbe-dependent metabolites as well as related downstream pathways; this improves glucose and lipid metabolism and energy homeostasis. These findings at least partly explain the effect of BBR on AS and metabolic diseases. In this review, we elaborate on the research progress of BBR and its mechanisms of action in the treatment of AS and metabolic diseases from the perspective of gut microbiota, to reveal the potential contribution of gut microbiota to the multifunctional biological effects of BBR.
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Because most of the berberine dose remains in the intestinal lumen, berberine remodels the composition of the microbiota and has broad-spectrum antimicrobial activity.
“Because most of the dose remains in the intestinal lumen, berberine remodels the composition of the microbiota and has broad-spectrum antimicrobial activity [95,96].”
From Berberine-Drug Interactions: Mechanisms, Clinical Relevance and Risk Stratification-A Narrative Review (2026) · cites this paper as [96]
The “Berberine Bioavailability and Gut Microbiota” section (page unavailable) reports poor intestinal absorption and oral bioavailability below 1% in rats. It also describes berberine-related changes in gut microbiota, including increased Akkermansia. The passages do not establish that most of the dose remains specifically in the intestinal lumen or that berberine has broad-spectrum antimicrobial activity. (LLM, conf=0.86)
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References 152 · Cited by 40
- Authors
- Yang, S., Li, D., Yu, Z., Li, Y., & Wu, M.
- Affiliations
- China Academy of Chinese Medical Sciences (CN)
- Xiyuan Hospital (CN)
- Corresponding author
- Wu, Min
- Venue
- Frontiers in Pharmacology
- Publisher
- Frontiers Media SA
- Published
- 2021-07-09
- Volume
- 12
- Pages
- 709629-709629
- ISSN
- 1663-9812 (ISSN-L)
- PMC
- PMC8299362
- OpenAlex
- W3181298887
- Cited by
- 40
- References
- 152
- Citations by year
- 2026: 8 · 2025: 6 · 2024: 7 · 2023: 10 · 2022: 7 · 2021: 2
- FWCI
- 0.82
- Type
- journal article
- Language
- en
- Open access
- gold
- doi.org
- Licence
- Locations
- Frontiers in Pharmacology (publishedVersion, cc-by)
- PubMed Central (publishedVersion, cc-by)
- PubMed (publishedVersion)
- DOAJ (DOAJ: Directory of Open Access Journals) (submittedVersion, cc-by-sa)
- Funders
- National Natural Science Foundation of China (81202805 82074254)
- Natural Science Foundation of Beijing Municipality (7172185)
- Topics
- Health Sciences › Medicine › Pharmacology › Berberine and alkaloids research
- Life Sciences › Biochemistry, Genetics and Molecular Biology › Molecular Biology › Gut microbiota and health
- Health Sciences › Medicine › Complementary and alternative medicine › Traditional Chinese Medicine Analysis
- Keywords
- berberine, atherosclerosis, atherosclerotic cardiovascular disease, metabolic disorders, gut microbiota, isoquinoline alkaloids, intestinal barrier function, lipopolysaccharide, inflammation, glucose metabolism, lipid metabolism, energy homeostasis, diabetes mellitus, obesity, dyslipidemia, non-alcoholic fatty liver disease
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