Berberine clearing plaque from arteries

Unlock Heart Health: Can Berberine Help Fight Cholesterol and Inflammation?

Mira Elwood in Health & Wellness December 2025 • 5 min read.

"Explore how berberine, a natural compound, could offer new hope in the battle against oxidized LDL-induced macrophage activation, a key factor in heart disease."

In the ongoing effort to combat heart disease, researchers are constantly exploring new avenues for prevention and treatment. While modern medicine has made significant strides with interventions like stents and medications, the incidence of issues like neoatherosclerosis and in-stent restenosis after percutaneous coronary intervention (PCI) remains a concern. This has prompted a deeper look into the underlying mechanisms and potential alternative therapies.

One area of particular interest is the role of inflammation in these processes. Macrophage activation, a key component of the immune response, plays a significant role in the development of atherosclerosis. These immune cells, when overly activated by factors like oxidized low-density lipoprotein (ox-LDL), contribute to the buildup of plaque in arteries. Galectin-3, a protein mainly expressed on macrophages, amplifies inflammation in atherosclerotic progression. Therefore, controlling macrophage activation and galectin-3 expression represents a promising target for heart health.

Berberine (BBR), a natural compound with a long history in traditional medicine, has emerged as a potential player in this arena. Found in various plants, berberine has been investigated for its diverse health benefits, including its ability to improve insulin resistance, inhibit inflammation, and combat atherosclerosis. This article delves into the latest research exploring how berberine could alleviate ox-LDL-induced macrophage activation by downregulating galectin-3, offering a new perspective on natural heart health strategies.

How Does Berberine Help Lower Cholesterol and Reduce Inflammation?

Recent research has shed light on how berberine tackles the complex processes that lead to heart disease. A study published in Phytotherapy Research investigated the effects of berberine on macrophage activation and galectin-3 expression. Here’s a breakdown of the key findings:

The study focused on the impact of berberine (BBR) on oxidized low-density lipoprotein (ox-LDL)-induced macrophage activation and galectin-3 expression and their underlying mechanisms. THP-1-derived macrophages were pretreated with BBR prior to stimulation with ox-LDL. Galectin-3 expression was measured by real-time PCR, Western blotting, and confocal microscopy. Macrophage activation was assessed by lipid accumulation, expression of inflammatory cytokines, and CD11b and CD86. Plasma galectin-3 levels were measured in patients undergoing PCI at baseline and after BBR treatment for 3 months.

Reduced Galectin-3 and Macrophage Activation: Berberine was found to suppress ox-LDL-induced upregulation of galectin-3 and macrophage activation. This is crucial because galectin-3 amplifies inflammation, and reducing its levels can help to calm the inflammatory response in arteries.
AMPK Activation and NF-κB Inhibition: Berberine activates phospho-AMPK and inhibits phospho-NF-кВ р65 nuclear translocation. AMPK inhibition and NF-KB activation abolished the inhibitory effects of BBR on galectin-3 expression and macrophage activation. These pathways are central to regulating inflammation and cellular stress. By modulating them, berberine helps to create a more balanced cellular environment.
Synergistic Effects with Rosuvastatin: Combination of BBR and rosuvastatin exerted greater effects than BBR or rosuvastatin alone. However, BBR treatment did not further reduce plasma galectin-3 after PCI in patients receiving standard therapy. This is particularly interesting as it suggests that berberine could complement conventional treatments, potentially enhancing their effectiveness.

These findings suggest that berberine alleviates ox-LDL-induced macrophage activation by downregulating galectin-3 via the NF-kB and AMPK signaling pathways. This means berberine can directly influence the key processes that drive inflammation and plaque formation in atherosclerosis. By activating AMPK and inhibiting NF-kB, berberine helps to reduce the inflammatory burden on the arteries, making it a potential therapeutic agent for maintaining heart health.

The Future of Berberine in Heart Health

While these findings are promising, it’s important to remember that research is ongoing. Larger clinical trials are needed to fully understand the long-term effects of berberine on heart health and to determine the optimal dosage and administration methods. However, the evidence so far suggests that berberine holds significant potential as a natural adjunct to conventional heart disease treatments, offering a holistic approach to cardiovascular wellness.

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This article is based on research published under:

DOI-LINK: 10.1002/ptr.6217, Alternate LINK

Title: Berberine Alleviates Oxidized Low-Density Lipoprotein-Induced Macrophage Activation By Downregulating Galectin-3 Via The Nf-Κb And Ampk Signaling Pathways

Subject: Pharmacology

Journal: Phytotherapy Research

Publisher: Wiley

Authors: Chongzhe Pei, Yi Zhang, Ping Wang, Beijian Zhang, Lu Fang, Bo Liu, Shu Meng

Published: 2018-11-06

Everything You Need To Know

What is berberine and how is it being explored in the context of heart health?

Berberine (BBR) is a natural compound found in various plants, recognized for its potential health benefits, including improving insulin resistance, inhibiting inflammation, and combating atherosclerosis. Researchers are investigating berberine as a possible therapeutic agent for heart health, focusing on its ability to address oxidized low-density lipoprotein (ox-LDL)-induced macrophage activation, a key factor in the development of atherosclerosis. This research aims to explore how berberine can help alleviate the inflammatory processes that contribute to heart disease, offering a natural approach to cardiovascular wellness.

How does berberine impact the inflammatory response related to heart disease?

Berberine (BBR) impacts the inflammatory response by several mechanisms. Studies show that berberine suppresses ox-LDL-induced upregulation of galectin-3 and macrophage activation. Galectin-3, which amplifies inflammation, is reduced by berberine. BBR activates phospho-AMPK and inhibits phospho-NF-кВ р65 nuclear translocation. The AMPK and NF-KB pathways are central to regulating inflammation and cellular stress. By modulating these pathways, berberine helps reduce the inflammatory burden on the arteries, contributing to potential therapeutic benefits for maintaining heart health.

What role do macrophages play in heart disease, and how does berberine interact with them?

Macrophages are immune cells that play a significant role in the development of atherosclerosis. When overly activated by factors like oxidized low-density lipoprotein (ox-LDL), macrophages contribute to the buildup of plaque in arteries. Berberine (BBR) interacts with macrophages by suppressing ox-LDL-induced macrophage activation. This is achieved through the downregulation of galectin-3 expression, which reduces the inflammatory response within the arteries. By modulating the activation of macrophages, berberine may help prevent plaque formation and slow the progression of atherosclerosis.

Can berberine be used with existing treatments like rosuvastatin? What are the implications of this combination?

Yes, berberine can be used in combination with other treatments, such as rosuvastatin. The research indicates that the combination of berberine (BBR) and rosuvastatin exerted greater effects than either BBR or rosuvastatin alone. While berberine treatment did not further reduce plasma galectin-3 after PCI in patients already receiving standard therapy, the synergistic effects suggest that berberine could potentially complement conventional treatments, enhancing their effectiveness. This implies that berberine could be integrated into existing treatment strategies to improve outcomes in heart health, but this needs further evaluation.

What are the future directions for berberine in heart health, and what should be considered?

The future of berberine in heart health involves larger clinical trials to fully understand its long-term effects and determine the optimal dosage and administration methods. While the initial findings on berberine are promising, particularly in its ability to reduce galectin-3 expression, macrophage activation, and potentially complement existing treatments, more comprehensive research is needed. This includes establishing the specific benefits, identifying potential side effects, and defining the appropriate patient populations who may benefit most. The goal is to validate berberine as a natural adjunct to conventional heart disease treatments, offering a holistic approach to cardiovascular wellness.