Synonym name: (-)-Beta-Hydrastine
Catalogue No.: BP0744
Cas No.: 118-08-1
Formula: C₂₁H₂₁NO₆
Mol Weight: 383.4
Botanical Source: Alkaloid from Hydrastis canadensis and Berberis laurina (Papaveraceae, Berberidaceae)

Purity: 95%~99%
Analysis Method: HPLC-DAD or/and HPLC-ELSD
Identification Method: Mass, NMR
Packing: Brown vial or HDPE plastic bottle
Can be supplied from milligrams to grams.

For Reference Standard and R&D, Not for Human Use Directly.
Inquire for bulk scale.

HPLC of Hydrastine

Storage conditions：Short-term storage at 2~8℃, long-term storage at -20 ~ -80℃

Introduction/Overview

North American Coptis (Hydrastine, CAS No.: 118-08-1) is a type of alkaloid compound derived from natural plants, first derived from North American Coptis (Hydrastis canadensis). ) is separated to obtain the result. As a natural compound with multiple biological activities, North American berberine has attracted widespread attention in pharmacological research. Its unique molecular structure gives it multi-target properties, especially showing potential value in neurological diseases and antibacterial fields. In recent years, with in-depth research into Parkinson's disease (PD) and related neurodegenerative mechanisms, North American berberine has become an important tool molecule for studying dopaminergic neuron damage, as a selective competitive inhibitor of tyrosine hydroxylase (TH). Additionally, the inhibitory effect of North American berberine on the organic cation transporter (OCT1) provides new perspectives on its pharmacological activity. This paper will systematically review the chemical structure, plant origin, pharmacological activity, mechanism of action, druggability evaluation, and clinical application prospects of North American berberine, aiming to provide theoretical basis and reference for further research and development of this natural product.

Chemical structure and physicochemical properties

The chemical name of North American berberry is (-)-β-North American berberry, with the molecular formula C21H21NO5 and a molecular weight of 383.40. Its chemical structure features a polycyclic isoquinoline framework, with multiple hydroxyl and methoxy substituents, giving it certain polarity and water solubility. The LogP value of berberine in North America is 2.6144, indicating moderate lipid solubility, which helps penetrate cell membranes and the blood-brain barrier (BBB). Its topological pole surface area (TPSA) is 66.46 Ų, and combined with its high blood-brain barrier permeability, it indicates that North American berberine has significant distribution potential in the central nervous system (CNS). Low water solubility (0.0489 mg/mL) suggests possible solubility limits in vivo, requiring appropriate formulation techniques to improve bioavailability. Notably, North American berberine does not exhibit hERG channel inhibitory activity, reducing the risk of cardiotoxicity; The Ames-induced mutagenic test result was 0.6, indicating a low genotoxicity risk and a certain safety foundation.

Plant Origins and Extraction Methods

North American berthian is mainly found in Hydrastis canadensis, a plant belonging to the Ranunculaceae family, a perennial herb traditionally used to treat digestive system diseases and infections. The rhizome of North American Coptis is the main site of enrichment of North American coptis. The extraction method typically uses organic solvents (such as methanol, ethanol, or ethyl acetate) for reflux extraction of dried rhizomes, followed by purification through liquid-liquid partitioning, column chromatography, and other methods. In recent years, new technologies such as ultrasound-assisted extraction (UAE) and microwave-assisted extraction (MAE) have been applied to improve extraction efficiency and purity. In addition, countercurrent chromatography and high-performance liquid chromatography (HPLC) technologies are widely used for the separation and quantitative analysis of berberine in North America. Optimizing the extraction process not only improves yield but also lays the foundation for subsequent pharmacological research and formulation development.

Pharmacological activity research

Nervous system function

North American berberine, as a selective competitive tyrosine hydroxylase inhibitor, plays a key role in regulating dopamine biosynthesis. Tyrosine hydroxylase is a rate-limiting enzyme for dopamine synthesis, catalyzing the hydroxylation of tyrosine to dobutachol hydroxyphenylalanine (L-DOPA). North American berberine reduces dopamine synthesis by inhibiting the enzyme's activity (IC50=20.7 μM, PC12 cells), making it an important tool for studying dopaminergic neuron function and Parkinson's disease pathology. Its inhibition of the organic cation transporter OCT1 (IC50=6.6 μM) further affects neurotransmitter uptake and metabolism, potentially regulating neuronal homeostasis.

Neurotoxicity and apoptosis

Research shows that North American berberine may induce neuronal toxicity through mitochondrial dysfunction rather than oxidative stress pathways. When used in combination with L-DOPA, it can exacerbate apoptosis, suggesting that its potential synergistic toxicity should be carefully assessed in Parkinson's disease treatment. In addition, the influence of berberine in North America on mitochondrial membrane potentials and its regulatory mechanisms on cellular energy metabolism are becoming a hot topic in neurotoxicology research.

Antibacterial activity

North American berberine exhibits broad-spectrum antibacterial activity, targeting various key bacterial and fungal proteins, including DNA gyrase A (GYRA), red blood cell membrane protein (GYPB), bacterial cell division protein (FTSZ), fatty acid synthase (FABI), dihydrofolate reductase (DHFR), bacterial adhesion protein (MECA), penicillin-binding protein (PENA), and fungal cytochrome P450 14α-demethylase (ERG11/ CYP51A1) and fungal vent pumps (CDR1), etc. The diversity of these targets gives North American berberine potential application value in antimicrobial drug development, especially in the control of resistant strains.

Mechanism of action and molecular targets

The main mechanism of action of berberine in North America focuses on competitive inhibition of tyrosine hydroxylase. By binding to the enzyme's active site, it blocks the conversion of tyrosine to L-DOPA, reducing dopamine synthesis and thereby affecting the functional status of dopaminergic neurons. Additionally, the inhibitory effect of North American berberine on OCT1 may affect intracellular and extracellular transport of neurotransmitters, regulating the chemical environment within neurons. The induction mechanism of mitochondrial dysfunction is not yet fully understood, but evidence shows that North American berberine can interfere with mitochondrial membrane potentials and energy metabolism, inducing apoptosis signaling pathways, especially when combined with L-DOPA, showing synergistic toxicity.

In terms of antibacterial mechanisms, North American berberine inhibits key enzymes and proteins of bacteria and fungi through multi-target action, interfering with DNA replication, cell wall synthesis, fatty acid metabolism, and drug excretion, demonstrating strong antibacterial effects. This multi-target mechanism helps reduce the occurrence of resistance and enhances antibacterial efficacy.

Druggability evaluation and pharmacokinetics

North American berberine has a moderate molecular weight, and both its LogP value and TPSA indicators indicate good lipid solubility and suitable polarity, consistent with the pharmacokinetic characteristics of central nervous system drugs. Its high blood-brain barrier permeability gives it an advantage in the treatment of neurological diseases. Lower water solubility may limit oral bioavailability, so formulation optimization is needed to improve solubility and absorption rates.

In terms of safety, North American berberine does not inhibit hERG channels, reducing the risk of cardiotoxicity. Ames test results show low genotoxicity, providing a solid safety foundation. Current in vitro and in vivo pharmacokinetic studies show that berberine is widely distributed in the body, with metabolic pathways mainly involving hepatic enzyme systems and renal excretion. Its half-life and bioavailability require further systematic research to guide clinical dose design.

Prospects and outlooks for clinical applications

North American berberine is a versatile natural product with broad clinical application prospects. In the field of neurological diseases, as a selective inhibitor of tyrosine hydroxylase, it can be used for pathological mechanisms of Parkinson's disease and related dopaminergic neuron damage, and may even be developed as an adjunctive therapy to regulate dopamine metabolic balance. However, its potential neurotoxicity and synergistic effects with L-DOPA should be carefully evaluated to avoid adverse reactions.

In the antibacterial field, North American berberine inhibits key targets of various bacteria and fungi, offering new ideas for combating drug-resistant infections. In the future, structural optimization and drug design can enhance antibacterial activity and selectivity, enabling the development of novel antimicrobial drugs.

In addition, North American berberine has good druggability and a solid safety foundation, making it suitable for further preclinical pharmacokinetic and toxicological research. By combining modern drug delivery technologies, such as nanocarriers and sustained-release formulations, it is expected to overcome their insufficient water solubility and enhance clinical application potential.

Conclusion

North American berberine, a natural product with a unique structure and multiple pharmacological activities, demonstrates significant research value and application potential in neurological diseases and antibacterial fields. As a selective inhibitor of tyrosine hydroxylase, it provides an effective tool for studying dopaminergic neuron damage related to Parkinson's disease, and its multi-target antibacterial mechanism provides a theoretical basis for the development of novel anti-infective drugs. In the future, systematic research into its mechanism of action, pharmacokinetics, and safety should be strengthened, combined with modern drug development technologies, to promote the translation of berberine in North America into clinical application, benefiting patients.