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Product name: Coptisine Chloride
Synonym name:
Catalogue No.: BP0391
Cas No.: 6020-18-4
Formula: C19H14ClNO4
Mol Weight: 355.774
Botanical Source: Coptidis rhizoma
Physical Description:
Type of Compound: Alkaloids
Purity: 95%~99%
Analysis Method: HPLC-DAD or/and HPLC-ELSD
Identification Method: Mass, NMR
Packing: Brown vial or HDPE plastic bottle
Storage: Store in a well closed container, protected from air and light. Put into refrigerate or freeze for long term storage.
Whenever possible, you should prepare and use solutions on the same day. However, if you need to make up stock solutions in advance, we recommend that you store the solution as aliquots in tightly sealed vials at -20℃. Generally, these will be useable for up to two weeks.
The product could be supplied from milligrams to grams
Inquire for bulk scale.
Chengdu Biopurify Phytochemicals Ltd. is a leading company in the research, development, manufacture and marketing of High Quality Phytochemicals and Extracts(especially Active Ingredients from Traditional Chinese Medicine，TCM), Natural Active Pharmaceutical Ingredients worldwide.
The main services:
A. Supply active ingredients and reference standards of TCM, from mgs to kgs scale
B. Custom extraction and purification, target Herb Active Ingredients
C. Custom synthesis and semi-synthesis for Natural Active Ingredients
D. CR(contract research), CM(contract manufacture) and PD(process development) services from lab scale, pilot scale to commercial scale(GMP is also available)
E. TCM compounds library for drug screen,more than 3000 compounds available, many of them are rare and unique.
HPLC of Coptisine Chloride
Storage conditions：Short-term storage at 2~8℃, long-term storage at -20 ~ -80℃
71.6900
.1900
.1900
High
No
No
Unknown
No
No
Negative
Coptisine Chloride (CAS No.: 6020-18-4) is a natural alkaloid isolated from the traditional Chinese medicinal herb Coptis chinensis Franch. and belongs to the isoquinoline alkaloid family. As one of the main active ingredients in Coptis chloride, coptisine hydrochloride has attracted much attention in recent years due to its multi-target and multifunctional pharmacological activity. It not only exhibits significant anti-antibacterial, antiviral, and antiviral biological activities, but also shows potential therapeutic value in regulating immune-related enzymes such as indole amine 2,3-dioxygenase (IDO). Especially in the fields of drug-resistant bacterial and viral infections, berberine hydrochloride has shown unique advantages as a novel drug candidate.
This review aims to systematically summarize the chemical structure and physicochemical properties of coptisine hydrochloride, plant origins and extraction methods, with a focus on evaluating its pharmacological activity and mechanism of action, analyzing its druggability and pharmacokinetic characteristics, exploring its potential and future development directions for clinical applications, and providing references for the fields of natural product pharmacology and new drug development.
The chemical formula of berberine hydrochloride is C19H14ClNO4, with a molecular weight of 355.77. Its structural core is a typical isoquiline framework, containing a polycyclic aromatic structure and multiple oxygen-containing functional groups. In terms of physicochemical properties, the LogP value of berberine hydrochloride is 0.19, indicating strong hydrophilicity and moderate lipid solubility, which is beneficial for distribution in the body. The polar surface area (TPSA) is 71.69 Ų, and the number of hydrogen bond acceptors is 6, indicating that its molecules have good water solubility and potential for binding to biomacromolecules.
Berberine hydrochloride has high blood-brain barrier permeability (BBB), and its "High" level of penetration provides a theoretical basis for its application in neurological diseases. Its hepatotoxicity, cardiotoxicity, and hERG channel inhibition effects remain unclear. Ames-induced mutagenesis tests were negative, indicating low genotoxicity risk and good safety potential.
Coptis hydrochloride is mainly found in Coptis species, especially the rhizome part of the classic Chinese medicine material Coptis (Coptis chinensis Franch.). As a traditional Chinese medicine, Coptis is widely used in treatments such as clearing heat and drying dampness, purging fire, and detoxifying. Berberine hydrochloride, as one of its main alkaloid components, is abundant and highly active.
Traditional methods for extracting berberine hydrochloride mostly involve extraction with acidic aqueous solutions or alcohol solvents, combined with liquid-liquid partitioning, column chromatography, and other techniques for separation and purification. Modern extraction technologies include ultrasound-assisted extraction, microwave-assisted extraction, and high-performance liquid chromatography (HPLC) separation, significantly improving extraction efficiency and purity. The typical process flow is: Coptis drying and pulverizing→ extracting with acidic water or ethanol→ coarse extract concentration→ silica gel column chromatography separation→ hydrochloride chloride to obtain coptisine hydrochloride. Purity typically exceeds 95%, meeting pharmaceutical and research needs.
Berberine hydrochloride has inhibitory effects on various bacteria, especially showing potential efficacy against drug-resistant strains. Its targets involve key enzymes such as bacterial DNA gyrase (GYRA) and dihydrofolate reductase (DHFR), which interfere with bacterial DNA replication and metabolism. Related studies show that berberine hydrochloride inhibits Gram-positive bacteria such as Staphylococcus aureus and Streptococcus pneumoniae, as well as some Gram-negative bacteria, and shows certain activity against drug-resistant strains such as methicillin-resistant Staphylococcus aureus (MRSA).
Berberine hydrochloride is an effective inhibitor of the H1N1 influenza virus neuraminidase (NA-1), with an IC50 of approximately 104.6 μg/mL. Neuraminidase is a key enzyme for the replication and release of influenza A virus; inhibiting its activity can interrupt the viral life cycle. Berberine hydrochloride reduces viral replication efficiency through non-competitive inhibition, demonstrates good antiviral activity, and holds potential for developing novel anti-influenza drugs.
Indole 2,3-dioxygenase (IDO) is a key enzyme in immune regulation, involved in tryptophan metabolism, immune tolerance, and tumor immune evasion. Berberine hydrochloride, as a non-competitive IDO inhibitor, had a Ki value of 5.8 μM and an IC50 of 6.3 μM, demonstrating significant enzyme inhibitory activity. By inhibiting IDOs, berberine hydrochloride can regulate the immune microenvironment and enhance anti-tumor immune responses, showing potential value in anti-tumor and immunotherapy.
In addition to the main activities mentioned above, berberine hydrochloride also exhibits various biological effects such as anti-inflammatory, antioxidant, and neuroprotective effects. By regulating signaling pathways such as NF-κB and MAPK, it inhibits the release of inflammatory factors and reduces tissue damage. In addition, berberine hydrochloride also has certain protective effects against neurological diseases such as Alzheimer's and Parkinson's disease, with related mechanisms being studied in depth.
The multi-target mechanism of berberine hydrochloride is the basis for its diverse pharmacological activity. Its main targets include:
Molecular docking and kinetic simulation studies further revealed the binding pattern between berberine hydrochloride and target proteins, providing a theoretical basis for structural optimization and enhanced pharmacogenital efficacy.
Berberine hydrochloride possesses excellent druggability parameters. Its molecular weight of 355.77 conforms to the Lipinski rule, and a LogP value of 0.19 indicates a moderate hydrophilic/lipophilic balance, which is beneficial for drug absorption and distribution. TPSA is 71.69 Ų, suitable for cell membrane penetration and target binding. With 6 hydrogen bond receptors, it supports stable hydrogen bond interactions between the molecule and target proteins.
Its high blood-brain barrier penetration capability suggests potential advantages in treating central nervous system diseases. In terms of safety, the Ames test for berberine hydrochloride was negative, indicating a low genotoxicity risk, but key safety indicators such as hepatotoxicity, cardiotoxicity, and hERG channel inhibition still require systematic evaluation.
In terms of pharmacokinetics, current research is relatively limited. The characteristics of absorption, distribution, metabolism, and excretion (ADME) in vivo require further elucidation. Preliminary data show that the oral bioavailability of berberine hydrochloride is moderate. Liver metabolism mainly occurs through the cytochrome P450 enzyme system, and metabolites and half-lives require in-depth study to guide clinical medication regimens.
As a multifunctional drug candidate molecule derived from natural products, berberine hydrochloride has broad clinical application potential. It offers new drug design ideas in the field of anti-drug-resistant bacterial infections, especially in the treatment of multidrug-resistant strains. Its anti-H1N1 influenza virus activity makes it a powerful supplement to the prevention and treatment of influenza virus infections, especially amid increasingly severe viral mutations and drug resistance.
The IDO inhibitory effect gives berberine hydrochloride its potential value in tumor immunotherapy, and in the future, it can be combined with immune checkpoint inhibitors to enhance anti-tumor efficacy. Additionally, its neuroprotective and anti-inflammatory activities offer potential for the treatment of neurodegenerative diseases and chronic inflammation-related conditions.
Future research directions include:
With advances in modern drug R&D technology, berberine hydrochloride is expected to become a model for natural product drug development, driving the modernization and internationalization of traditional Chinese medicine.
As an important alkaloid component in Coptis chinensis, berberine hydrochloride demonstrates potential in multiple applications such as resistance to drug-resistant bacterial infections, antiviral effects, immune regulation, and neuroprotection due to its unique chemical structure and multi-target pharmacological activity. Its excellent druggability parameters and safety foundation lay a solid foundation for new drug development. Although there are still shortcomings in pharmacokinetics and clinical research, with further research, berberine hydrochloride is expected to become an important breakthrough in the field of natural product pharmacology, providing new strategies and options for treating various diseases.
In the future, by integrating modern molecular biology, medicinal chemistry, and clinical pharmacology methods, research and development of berberine hydrochloride will further promote innovation and application of natural product drugs, supporting the advancement of human health.
Shenshuai
Wenjing
Hedandan
