Berberine hydrochloride: mechanism of action and side effect

General Description

Berberine hydrochloride activates AMP-activated protein kinase, a key regulator of cellular energy metabolism, leading to increased glucose uptake, improved insulin sensitivity, and regulation of lipid metabolism. It also modulates the gut microbiota, promoting gut health and impacting metabolic processes. Berberine hydrochloride inhibits enzymes involved in carbohydrate metabolism, helping to control blood glucose levels. Furthermore, it exhibits anti-inflammatory effects by suppressing pro-inflammatory cytokines. Common side effects of berberine hydrochloride include gastrointestinal disturbances, while rare cases may experience more severe effects like low blood pressure or liver toxicity. It is important to use berberine hydrochloride under the guidance of a healthcare professional and disclose any medications you are taking to prevent potential interactions.

Figure 1. Berberine hydrochloride

Mechanism of action

Activation of AMP-activated protein kinase

Berberine hydrochloride activates the enzyme AMP-activated protein kinase a critical regulator of cellular energy metabolism. This activation leads to several beneficial effects, including increased glucose uptake, improved insulin sensitivity, and regulation of lipid metabolism. By activating AMP-activated protein kinase, berberine hydrochloride promotes the uptake of glucose into cells, enhances the responsiveness of cells to insulin, and helps regulate the breakdown and utilization of lipids within cells. These actions contribute to improved energy balance, glucose control, and lipid metabolism regulation. ¹

Modulation of gut microbiota

Studies have demonstrated that berberine hydrochloride possesses antimicrobial properties and has the capacity to modulate the composition and diversity of the gut microbiota. This modulation of the gut microbiota can have positive effects on gut health, reducing inflammation and influencing various metabolic processes. Berberine hydrochloride's antimicrobial properties allow it to inhibit the growth of certain microorganisms, promoting a healthier balance of gut bacteria. This, in turn, can contribute to improved gastrointestinal function, reduced inflammation, and an impact on metabolic processes such as nutrient absorption, energy metabolism, and hormone regulation within the body. ²

Inhibition of enzymes

Berberine hydrochloride exhibits inhibitory effects on various enzymes involved in carbohydrate metabolism, including alpha-glucosidase and dipeptidyl peptidase-4. Through the inhibition of these enzymes, berberine hydrochloride effectively retards the process of carbohydrate digestion and absorption. This mechanism plays a crucial role in promoting better control over blood glucose levels. By slowing down the breakdown of complex carbohydrates into simpler sugars and reducing the activity of dipeptidyl peptidase-4, berberine hydrochloride helps regulate postprandial blood sugar spikes and contributes to improved glycemic control. ³

Anti-inflammatory effects

Berberine hydrochloride displays notable anti-inflammatory properties by effectively suppressing the activity of pro-inflammatory cytokines and modulating key signaling pathways involved in inflammation. Through its actions, berberine hydrochloride has the potential to mitigate chronic low-grade inflammation, which has been implicated in the development and progression of various metabolic disorders. By downregulating the production of inflammatory mediators and inhibiting the activation of inflammatory signaling cascades, berberine hydrochloride exerts its anti-inflammatory effects, thereby contributing to the maintenance of a balanced and healthier inflammatory response within the body. ⁴

Side effect

While berberine hydrochloride is generally considered safe for short-term use, it may cause some side effects in certain individuals. Common side effects of berberine hydrochloride include gastrointestinal disturbances such as diarrhea, constipation, flatulence, stomach cramps, and nausea. These symptoms are usually mild and resolve on their own as the body adjusts to the medication. In rare cases, high doses or prolonged use of berberine hydrochloride may lead to more severe side effects, including low blood pressure, heart rhythm disturbances, allergic reactions, and liver toxicity. It is important to use berberine hydrochloride under the guidance of a healthcare professional and follow the recommended dosage and duration of treatment. Furthermore, berberine may interact with certain medications, such as anticoagulants, antiplatelet drugs, and hypoglycemic agents, potentially increasing the risk of bleeding or affecting blood glucose levels. Therefore, it is crucial to inform your healthcare provider about any medications you are taking before starting berberine hydrochloride.

Reference

1. Ge Y, Zhang Y, Li R, Chen W, Li Y, Chen G. Berberine regulated Gck, G6pc, Pck1 and Srebp-1c expression and activated AMP-activated protein kinase in primary rat hepatocytes. Int J Biol Sci, 2011, 7(5):673-684.

2. Cao J, Chen M, Xu R, Guo M. Therapeutic Mechanisms of Berberine to Improve the Intestinal Barrier Function via Modulating Gut Microbiota, TLR4/NF-κ B/MTORC Pathway and Autophagy in Cats. Front Microbiol, 2022, 13:961885.

3. Ye F, Zhou Q, Tian L, Lei F, Feng D. The protective effect of berberine hydrochloride on LPS‑induced osteoclastogenesis through inhibiting TRAF6‑Ca2+‑calcineurin‑NFATcl signaling pathway. Mol Med Rep, 2017, 16(5):6228-6233.

4. Wang X, Feng S, Ding N, et al. Anti-Inflammatory Effects of Berberine Hydrochloride in an LPS-Induced Murine Model of Mastitis. Evid Based Complement Alternat Med, 2018, 2018:5164314.

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