Berberine is an active compound found in many plants, and humans have long used it in folk medicine. People claim it is beneficial for diabetes, high cholesterol, and parasitic infections. This article describes all the benefits of berberine known to science.
What is berberine?
Berberine is a plant isoquinoline alkaloid found in a variety of plants, including barberry (
Berberis vulgaris ), Oregon grape (
Mahonia aquifolium ), goldenseal (
Hydrastis canadensis ), and Chinese coptis (Coptis
chinensis ). It has a 3,000-year history of use in traditional Chinese and Indian medicine, particularly to relieve diarrhea due to its antimicrobial effects.
Berberine has been studied by researchers for heart failure, diarrhea, infections, and other conditions. However, according to the National Center for Complementary and Integrative Health (
NCCIH , USA), oral
berberine is poorly absorbed from the gut. As a result, many of the findings from berberine studies may not meet the “gold standard” for proving its benefits and effectiveness.
Berberine itself has many potential benefits. It is often used to treat diabetes or high cholesterol, and there is some evidence to support this. However, there have been few high-quality, large-scale human studies of berberine to date.
Alkaloids – substances for plant protection
In their natural habitat, plants are surrounded by a variety of enemies, including a wide range of viruses, bacteria, fungi, nematodes, insects and other herbivores, which are responsible for detrimental reductions in plant growth and production.
Plants protect themselves by producing a variety of compounds called secondary metabolites, including terpenes, phenols, sulfur compounds, saponins, and alkaloids.
Alkaloids are a diverse group of nitrogen-containing natural products consisting of more than 20 different classes, including pyrrolidines, pyrrolizidines, quinolizidines, tropanes, piperidines, pyridines, and others.
Most alkaloids are thought to function as nitrogen storage reservoirs, protection against predators, especially animals, vertebrates, insects, as well as arthropods due to their general toxicity and deterrence, and growth regulators, as some alkaloids have structures similar to known plant growth regulators.
Furthermore, many alkaloids have been used as a source of medicines for thousands of years due to their structure-activity relationship, and this area of interest is still a major one in organic chemistry and the pharmaceutical industry. For example,
quinine , obtained from the bark of the tropical cinchona tree, was used by South American Indians to treat fever, and later proved to be an indispensable drug against malaria.
Benefits of Berberine
Be sure to consult your doctor before taking berberine. It should never be used as a substitute for standard medical therapy. It should only be used as an adjunct to treatment and empowerment.
The most proven and effective properties of berberine
Choleretic action
Berberine consumption increases
the conversion of cholesterol into bile acids , which helps lower blood cholesterol levels, as bile acid synthesis is the main way to remove cholesterol from the body.
This lipid-lowering (
cholesterol ) effect was confirmed in a meta-analysis of 27 clinical trials, making berberine an attractive alternative for patients with dyslipidemia who cannot take statins due to side effects.
However, keep in mind that berberine is not a drug and is not regulated as strictly as prescription drugs. Furthermore, the mechanism of action of this substance (increased secretion of bile acids into the digestive tract) is generally associated with negative physiological effects, including an increased risk of colorectal cancer.
Mouth ulcers (stomatitis)
Topical application of gelatin with berberine (5 mg/g) 4 times daily for 5 days reduced pain and ulcer size in 84 people with recurrent aphthous stomatitis, without apparent side effects.
Type 2 diabetes
According to one meta-analysis, berberine may be beneficial for people with type 2 diabetes
. However, the authors of this article emphasized that the evidence is generally weak, as the included studies were few, of poor methodological quality, had small sample sizes, and were at unknown risk of bias.
In one study, berberine (0.5 g, taken 3 times daily for 3 months)
was as effective as metformin (a diabetes medication) in reducing glycated hemoglobin A1C (HbA1c), fasting blood glucose, postprandial blood glucose, and triglyceride levels in 36 patients with type 2 diabetes.
A study of 48 patients with type 2 diabetes treated with berberine showed similar results, with
plasma insulin levels also decreasing . Total cholesterol and LDL (“bad cholesterol”) levels were also reduced.
In another study, berberine, taken at 1 g per day, reduced fasting and postprandial blood glucose, glycated hemoglobin HbA1c, triglycerides, total cholesterol, and LDL cholesterol (in 116 patients with type 2 diabetes).
In rats, berberine increased insulin production, regeneration of pancreatic beta cells (cells that produce insulin), antioxidant activity, and reduced lipid peroxidation, which resulted in reduced oxidative stress.
Proposed mechanisms of action of berberine in diabetes
Scientists have put forward a number of hypotheses about how berberine may help diabetes at the cellular level, including:
- By directly increasing AMPK (5'AMP-activated protein kinase), which promotes glucose uptake into muscle cells and helps balance high blood sugar levels (studies in rats and cells)
- Delaying the breakdown of carbohydrates into simple sugars (rat study)
- Increased glucagon secretion (rat study)
- Mimics the action of insulin by increasing the body's ability to absorb glucose (cell study)
- Reduced volume of glucose moving through the intestinal lining (cell study)
- Increase in adiponectin, a protein that helps regulate blood sugar levels (via AMPK) (cell study)
- Activation of glucose transporter 1 (GLUT1) in the blood by sugar transport activity (cell assay)
- Activation of GPR40 fatty acid receptor (cell-based assay)
- Protection of pancreatic beta cells from cell death
- Inhibition of hepatic glucose production (rat study)
- Improved intestinal microflora composition (rat study)
- Inhibition of the NF-kB inflammatory pathway (cell-based assay)
- Insulin receptor increase (cell study)
However, larger studies are needed to test the effectiveness of berberine in people with type 2 diabetes.
High cholesterol
Berberine and a multi-ingredient supplement (berberine, policosanol, red yeast extract, folic acid, and astaxanthin), taken daily for 4 weeks, reduced total cholesterol, LDL cholesterol, and triglycerides, and increased HDL "good" cholesterol (40 patients with moderate cholesterol problems).
In another study involving 32 patients with high cholesterol, berberine supplements for 3 months significantly reduced cholesterol, triglycerides, and LDL levels.
Berberine supplementation (500 mg berberine, 10 mg policosanol, 200 mg red yeast rice, 0.2 mg folic acid, 2.0 mg coenzyme Q10, and 0.5 mg astaxanthin) reduced total cholesterol, LDL, and insulin resistance, but had no effect on HDL (80 patients with cholesterol problems). This cholesterol-lowering effect has also been studied in mice.
Although plausible, the overall evidence for its positive effects on cholesterol is still weak. Further large-scale studies are needed.
Based on laboratory experiments, scientists believe that
berberine can reduce LDL cholesterol levels :
- Increased LDL receptor activity in the liver
- Decreased hepatocyte nuclear factor 1alpha activity
- Inhibition of lipid synthesis by activation of AMPK
Hypertension
According to a large meta-analysis of clinical trials, berberine supplementation combined with conventional treatment (the drug Amlodipine, a 3rd generation slow-acting calcium channel blocker) reduces systolic blood pressure after 2 months of supplementation.
This combination of the drug and berberine reduced systolic blood pressure by 5 mmHg. and diastolic blood pressure by 2 mm Hg. Art. compared to treatment alone.
Cardiovascular diseases
Despite some promising results, there is no scientific evidence to support the use of berberine in people with cardiovascular disease. Large-scale clinical trials are needed.
Berberine (1.2–2.0 g/day) in combination with several conventional treatments improved quality of life (physical activity and reduced fatigue) and reduced mortality in 156 patients with
chronic congestive heart failure .
Studies in rats have shown that berberine may improve aspects of cardiovascular health. It has been investigated for its potential protective effects on heart muscle cells damaged by the return of blood flow after a blood flow restriction (such as after a stroke).
Polycystic ovary syndrome (PCOS)
Some evidence suggests that berberine may improve metabolism in women with polycystic ovary syndrome (PCOS) and insulin resistance.
In clinical trials, berberine taken for 3 months prior to ovarian stimulation for in vitro fertilization (IVF) reduced fasting blood sugar, insulin resistance, total cholesterol, LDL cholesterol, triglycerides, testosterone, and waist-to-hip ratio.
Berberine also increased HDL “good cholesterol” and sex hormone binding globulin (SHBG) values in women with PCOS and insulin resistance compared to placebo.
Berberine also appears
to improve lipid status (e.g., LDL and total cholesterol) compared to metformin, the standard drug of choice for PCOS.
However, it is still unclear whether berberine increases the chance of pregnancy in women with PCOS who are trying to conceive.
In another study, it was as effective as metformin but had fewer side effects. In another study, it did not improve results when added to a new ovulation-inducing drug (letrozole). Further research is needed to explain these mixed findings.
Berberine Dosage
Berberine is available in tablet or capsule form. Although there is no set dosage, most
studies have used a dosage of 1,000–1,500 mg (1–1.5 g) per day.
Berberine may cause some side effects, which we will discuss in more detail below. People may want to start taking a lower dose of berberine to monitor for potential side effects and gradually increase the dose to 1,500 mg per day.
To maintain stable levels of this substance in the body, berberine is often recommended to be taken in multiple doses, such as 500 mg three times a day.
Side effects of berberine
During studies with berberine, some patients experienced minor adverse digestive effects, such as
abdominal discomfort (nausea, bloating, diarrhea).
Pregnant or breastfeeding women should not take berberine without consulting a doctor. Although studies have not shown that berberine harms a developing fetus or infant, only further research can provide definitive evidence that it is safe.
Berberine drug interactions
Berberine can cause a number of side effects, including adverse interactions with prescription medications. The fact is that this substance reduces the effectiveness of medications.
Berberine inhibits (inhibits) the enzymes CYP2D6 and CYP3A4, which are involved in the metabolism of endogenous (internal) substances and xenobiotics (those not produced by the body), including many drugs.
For example, it may interfere with the absorption of
tetracycline and related antibiotics.
Plants containing berberine may
enhance the effects of oral medications
that lower blood sugar levels due to its multiple antidiabetic effects. People taking oral hypoglycemic medications should monitor glucose levels while taking berberine. Dosage adjustments may be necessary.
