Synonym name: 6,6'-Di-O-methyldauricoline
Catalogue No.: BP0452
Cas No.: 524-17-4
Formula: C₃₈H₄₄N₂O₆
Mol Weight: 624.778
Botanical Source: Alkaloid from the rhizomes of Menispermum dauricum, the subterranean parts of Menispermum canadense, and from Polyalthia nitidissima and Sinomenium acutum

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.

NMR of Dauricine

HPLC of Dauricine

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

Introduction/Overview

Dauricine, also known as bat kudzu alkaloid, is a typical biphenylisoquinoline alkaloid, mainly found in the traditional Chinese medicinal material Menispermum (Menispermum dauricum DC.). As an important active ingredient in traditional Chinese medicine, Ergosan root alkaloid has attracted widespread attention due to its diverse pharmacological activities, especially showing significant potential in anti-inflammatory, anti-tumor, and anti-arrhythmic fields. In recent years, with advances in molecular biology and pharmacological techniques, the mechanism of action of salimine has gradually been clarified, especially in research on regulating cell signaling pathways, ion channel function, and cell cycle regulation, making significant progress.

This paper will systematically review the chemical structure and physicochemical properties, plant origin, and extraction methods of Physicalsin, focusing on its pharmacological activity and mechanism of action. Combined with druggability evaluation and pharmacokinetic data, it explores its clinical application prospects and development directions, aiming to provide theoretical basis and reference for pharmacological research of natural products and related new drug development.

Chemical structure and physicochemical properties

Dauricine (CAS No.: 524-17-4) belongs to the biphenylisoquinoline alkaloids, with a molecular formula of C38H44N2O6 and a molecular weight of 620.78. Its structural feature is that two isoquiline units are connected by double bonds, forming a relatively complex three-dimensional conformation. This structure gives it strong lipophilicity, with a LogP value of about 4.57, indicating good lipid solubility, which facilitates penetration of cell membranes, but may also affect its water solubility and bioavailability.

The polar surface area (TPSA) of Erphan root alkaloid is 88.38 Ų, and the number of hydrogen bond receptors is 8, suggesting that it possesses certain hydrophilicity and binding ability in intermolecular interactions. Despite its large molecular weight, a reasonable polarity distribution helps it bind to biological macromolecule targets. According to existing data, Ergophylline is not easily crossed the blood-brain barrier (BBB), which may limit potential side effects on the central nervous system, but could also restrict its application in central nervous system diseases.

Plant Origins and Extraction Methods

Physicalum mainly comes from the plant Menispermum dauricum DC., a perennial vine widely distributed in Northeast Asia. In traditional Chinese medicine, this plant is used as a detoxifying, anti-inflammatory, and anti-rheumatic herb. Wild bean root alkaloids, as its main alkaloid component, are usually concentrated in the rhizomes.

The main extraction methods for Physomaline include solvent extraction, liquid-liquid distribution, and column chromatography purification. Traditional extraction mostly uses ethanol or methanol as solvents, with crude extracts obtained by reflux, followed by pH adjustment by acid-base methods to separate alkaloids. Further purification of commonly used technologies such as silica gel column chromatography and reversed-phase high-performance liquid chromatography (RP-HPLC) is performed to obtain high-purity S.A. root alkaloids.

In recent years, emerging technologies such as ultrasound-assisted extraction and microwave-assisted extraction have also been applied to the extraction of Phylin alkaloids, significantly improving extraction efficiency and purity. In addition, synthetic methods for soutine have also been reported, making large-scale production possible.

Pharmacological activity research

Anti-inflammatory activity

Physaline shows significant anti-inflammatory effects. Both in vitro and in vivo studies have shown that sand root root sinine can significantly inhibit the expression of inflammatory factors such as TNF-α, IL-6, and IL-1β. Its anti-inflammatory mechanism mainly works by inhibiting activation of the nuclear factor κB (NF-κB) signaling pathway, reducing the transcription of pro-inflammatory genes and thereby alleviating inflammatory responses.

In models of inflammatory diseases such as colitis, sand root root can reduce infiltration of inflammatory cells, lessen tissue damage, and demonstrate good protective effects. Moreover, its antioxidant activity helps alleviate inflammatory damage related to oxidative stress.

Antitumor activity

Physalmine has demonstrated the ability to inhibit cell proliferation and induce apoptosis across various tumor cell lines. Especially in colon cancer cells, sinophylline exhibits dose-dependent anticancer effects by inhibiting NF-κB activation, blocking cell cycle progression, and suppressing cell invasion and migration.

Mechanistic studies have shown that Physophylline can regulate multiple signaling pathways, including MAPK, PI3K/Akt, and mitochondrial pathways, promoting the expression of apoptosis-related proteins such as Bax upregulation, Bcl-2 downregulation, and activation of caspase family proteins. In addition, sand root root aline can inhibit tumor angiogenesis, block tumor nutrient supply, and further enhance its anti-tumor effect.

Antiarrhythmic activity

As a potential antiarrhythmic drug, Ergon root aline mainly targets various cardiac ion channels, including KCNH2 (hERG), KCNQ1, SCN5A, CACNA1C, KCNE1, KCNE2, and RYR2. By regulating the functions of these ion channels, Eric root aline can stabilize the electrophysiological state of myocardial cells, preventing and correcting arrhythmias.

In vitro electrophysiology experiments show that scopine regulates potassium and sodium channels, can extend the duration of action potentials, suppress abnormal autonomic discharges, and reduce the frequency of arrhythmias. Animal model studies further confirm its potential in arrhythmia prevention and treatment.

Mechanism of action and molecular targets

The multi-target mechanism of Sand bean root alkaloid forms the basis for its pharmacological diversity. Its main mechanisms of action include:

1. Inhibition of NF-κB signaling pathway: NF-κB is a key transcription factor regulating inflammation and tumor development. Phylinine exerts anti-inflammatory and antitumor effects by blocking the degradation of IκBα, inhibiting nuclear translocation of NF-κB, and reducing the expression of pro-inflammatory and anti-apoptotic genes.

2. Regulating ion channel function: Physine directly or indirectly acts on cardiac potassium channels (such as hERG/KCNH2, KCNQ1), sodium channels (SCN5A), and calcium channels (CACNA1C), modulating the action potentials of myocardial cells and stabilizing heart rhythm.

3. Induction of apoptosis: By regulating the expression of Bcl-2 family proteins and the caspase cascade, Physophylline promotes tumor cell apoptosis, blocks the cell cycle, and inhibits cell proliferation.

4. Antioxidant effect: Physalmine can eliminate free radicals, reduce oxidative stress, and protect cells from damage.

In addition, sandazine may also affect other signaling pathways such as MAPK and PI3K/Akt, regulating the balance between cell survival and death. Specific molecular targets and their interactions still require further in-depth study.

Druggability evaluation and pharmacokinetics

The druggability parameters of Shandongine showed a relatively large molecular weight (620.78 Da) and a LogP value of 4.57, indicating good lipid solubility, but possibly challenges in bioavailability and solubility. TPSA is 88.38 Ų, with 8 hydrogen bond receptors, indicating moderate molecular polarity that facilitates binding to target proteins.

Currently, data on the hepatotoxicity, cardiotoxicity, and hERG channel inhibitory effects of sandrogine remain unclear, and systematic safety evaluation is urgently needed to ensure its clinical safety. The Ames test results are unknown and require further genotoxicity assessment.

Pharmacokinetics, orally alkaloid is absorbed slowly, and its bioavailability is limited. In the body, it is mainly metabolized by the liver, and its metabolic pathways and metabolic products have not yet been fully understood. Because it does not easily cross the blood-brain barrier, its distribution in the central nervous system is limited, which may reduce the risk of central nervous system side effects.

Future research should focus on optimizing its pharmacokinetic properties, such as improving solubility, bioavailability, and targeting through structural modification and nanocarrier systems.

Prospects and outlooks for clinical applications

As a multifunctional natural product, Ergophylline has broad clinical application potential. Its anti-inflammatory and anti-tumor activities offer new ideas for the treatment of inflammatory diseases and tumors, especially promising applications in digestive system tumors such as colon cancer. At the same time, its ability to regulate cardiac ion channels gives it a unique advantage in the field of antiarrhythmia.

However, the clinical translation of sandozozine-shanti still faces many challenges, including poor pharmacokinetic properties, lack of safety data, and dosage optimization issues. In the future, in-depth research into its pharmacological mechanisms should be strengthened, safety evaluations improved, and systematic preclinical and clinical studies should be conducted.

In addition, by integrating modern drug design concepts and using chemical modifications, formulation improvements, and combination drug strategies, the efficacy and safety of Ergophylline will be enhanced, promoting its development as a new drug with clinical value.

Conclusion

As a typical biphenylisoquinoline alkaloid, Erphine Root alkaloid shows broad application prospects in anti-inflammation, anti-tumor, and anti-arrhythmia fields due to its multi-target and multi-mechanism pharmacological properties. Although there are still some shortcomings in terms of druggability and safety, with deeper research and technological advancements, Erandine is expected to become an important candidate molecule in the development of natural product drugs.

Future research should focus on systematic elucidation of its molecular mechanisms, optimization of pharmacokinetics, and scientific validation of clinical applications, laying a solid foundation for transforming it into safe and effective clinical drugs. Research on Physophyllum not only enriches the theoretical framework of natural product pharmacology, but also provides new strategies and ideas for the treatment of related diseases.