Berberine

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Cat Number

PIPE-0569

CAS Number

2086-83-1

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CAS Number

2086-83-1

EINECS

218-229-1

Storage

Store at room temperature

Synonyms

Umbellatine; Berberin; Berbericine; Majarine; Thalsine; Umbellatin

Molecular Formula

C20H18NO4

Molecular Weight

336.4

Smiles

COC1=C(C2=C[N+]3=C(C=C2C=C1)C4=CC5=C(C=C4CC3)OCO5)OC

Appearance

White to yellow crystals

Melting Point

204-206°C

Boiling Point

486.8°C

Relative Density

1.17

General Description

Berberine (BBR) is a plant-derived isoquinoline alkaloid. It is a small molecule with a broad range of pharmacological activities and multi-targeted mechanisms of action. BBR has demonstrated therapeutic potential across multiple organ systems, including digestive, metabolic, cardiovascular, and neurological.

Mechanism of Action

Berberine's mechanisms are multifaceted. A primary pathway involves activating the AMPK (AMP-activated protein kinase) pathway, which enhances insulin sensitivity, regulates glucose metabolism, and improves lipid profiles. It also inhibits the NLRP3 inflammasome activation and has anti-inflammatory and antioxidant effects. Additionally, berberine modulates the gut microbiota by suppressing pathogenic bacteria while restoring beneficial ratios, and it enhances the intestinal barrier to reduce endotoxin entry into the bloodstream.

Application

Berberine is widely studied for its clinical applications in managing type 2 diabetes mellitus (T2DM), improving blood glucose levels, and reducing lipid profiles. It is also being investigated for its protective effects against diabetic complications and its role in treating cardiovascular diseases, digestive disorders, and neurological conditions. It has shown potential in treating cancer, with research examining its pharmacological mechanisms and therapeutic applications.

This review summarizes the pharmacologic effects of berberine on animals and humans through regulation of the gastrointestinal microbiota. Berberine has been used to treat obesity, diabetes, atherosclerosis, and metabolic diseases, with clinical trials ongoing for cardiovascular, gastrointestinal, and endocrine conditions. Its lipid‑lowering and insulin‑sensitizing effects are partially attributed to microbiota modulation. The review highlights the incompletely understood mechanisms linking berberine, gut microbes, and metabolic benefits.

Fig. 1 Effects of berberine on diseases by regulating intestinal flora. (Zhang L, et al., 2021)

References

Zhang L, et al. Effects of Berberine on the Gastrointestinal Microbiota. Front Cell Infect Microbiol. 2021;10:588517.

Oral berberine (BBR) acts as an agonist of tyrosine hydroxylase (TH) in gut bacteria (e.g., Enterococcus faecalis, E. faecium). BBR supplies H• via reduced dihydroberberine, promoting BH₄ production from dihydrobiopterin, which enhances TH activity and accelerates L‑dopa production by gut bacteria. L‑dopa enters the brain and converts to dopamine. In Parkinson’s disease mice, Enterococcus transplantation increased brain dopamine and ameliorated symptoms; BBR strengthened this effect. In 28 hyperlipidemic patients, oral BBR increased blood/fecal L‑dopa. BBR improves brain function via vitamin‑like upregulation of gut microbial L‑dopa biosynthesis.

Fig. 2 Dopa/dopamine might be the chemical link for the crosstalk between gut and brain. (Wang Y, et al., 2021)

References

Wang Y, et al. Oral berberine improves brain dopa/dopamine levels to ameliorate Parkinson's disease by regulating gut microbiota. Signal Transduct Target Ther. 2021;6(1):77.

Does Berberine require protection from light during storage?

Yes, it is photosensitive. UV light can cause photodegradation and discoloration (yellow to brown). Store in light-resistant containers, preferably amber glass.

What is the recommended storage temperature for Berberine?

Store at controlled room temperature (15-25°C). Avoid excessive heat above 30°C, which can accelerate oxidation of the isoquinoline ring.

Is Berberine stable under high-humidity conditions?

It is not hygroscopic and shows good stability. However, store in tightly sealed containers to prevent any potential surface effects.

How is the impurity berberrubine (a demethylated degradation product) monitored?

This degradation product is quantified using a stability-indicating HPLC method with fluorescence detection, ensuring it remains below pharmacopoeial limits.