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Product name: 10-Hydroxy mesaconitine
Synonym name: Beiwutine
Catalogue No.: BP4444
Cas No.: 76918-93-9
Formula: C33H45NO12
Mol Weight: 647.718
Botanical Source:
Type of Compound:
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.
For Reference Standard and R&D, Not for Human Use Directly.
Storage conditions：Short-term storage at 2~8℃, long-term storage at -20 ~ -80℃
173.6800
1.2058
1.1178
.2229
.7854
4.8068
Low
60.4880
7.4451
No
No
No
No
No
No
0.0
Yes
No
Yes
Yes
Beiwuline (10-Hydroxy mesaconitine), as a natural product, has attracted widespread attention in the field of pharmacology in recent years. Its unique chemical structure and multi-target pharmacological activity make it highly valuable for treating various diseases such as pain relief. Beiwuline belongs to the benzoate ester class with a relatively complex molecular structure. Its pharmacological activity involves multiple neurotransmitter receptors and inflammation-related targets, demonstrating synergistic multi-target effects. This paper will systematically review the chemical structure and physicochemical properties of Beiwuzine, plant origin and extraction methods, pharmacological activity and mechanism of action, druggability evaluation, pharmacokinetic characteristics, and clinical application prospects, aiming to provide theoretical basis and reference for further research and development of this natural product.
Beiwu alkaloid has a molecular formula of C_36H_47N_2O_11 and a molecular weight of 647.7180. Its molecular structure contains multiple hydroxyl and ester groups, making it a natural product of the benzoate ester class. Specific structural features include modification of the 10-position hydroxyl group, giving it unique molecular polarity and spatial configuration. The LogP value is 1.2058, indicating moderate lipid solubility, which facilitates cell membrane penetration without being overly hydrophobic. The polar surface area (TPSA) was 173.6800, indicating good solubility in polar environments, but there are certain limitations on crossing the blood-brain barrier. The water solubility is 0.2229, indicating low water solubility but sufficient to support a certain degree of bioavailability. Low blood-brain barrier permeability suggests that Beiwuline mainly acts on the peripheral nervous system or peripheral targets. The hERG suppression test results were negative, indicating a low risk of cardiotoxicity. The Ames test result was 0.0, indicating no significant genotoxicity risk.
Northern aconite mainly comes from plants of the genus Aconitum (Aconitum spp.), especially in some traditional Chinese medicinal herbs such as Aconitum carmichaelii and Aconitum kusnezoffii, which are abundantly abundant. Aconite plants are widely distributed in China, Japan, and other parts of East Asia, and have long been used as traditional analgesics and anti-inflammatory drugs.
The extraction methods for Beiwuzine mainly include solvent extraction steps, liquid-liquid distribution, and column chromatography. Common solvents are ethanol or methanol, combined with ultrasound-assisted extraction or reflux extraction technologies, which can effectively improve extraction efficiency. The extract was concentrated, separated, and purified, and qualitative and quantitative analyses were performed using high-performance liquid chromatography (HPLC) and mass spectrometry (MS) techniques to ensure the purity and structural identification of Beiwu alkali. In recent years, supercritical fluid extraction (SFE) and membrane separation technologies have also been attempted for the extraction and purification of alkaloids, further improving extraction efficiency and environmental friendliness.
The main pharmacological activity of Beiwuline is focused on analgesics. Multiple in vivo and in vivo experiments have shown that algaline can significantly relieve inflammatory and neuropathic pain, with effects comparable to traditional analgesics. Its analgesic effect not only relieves acute pain but also effectively suppresses chronic pain models.
In addition, Beiwuline also shows certain potential in anti-inflammation, antioxidant, and neuroprotective effects. Animal experiments show that algamine can inhibit the release of inflammatory mediators, reduce tissue inflammatory responses, and protect nerve cells from oxidative stress damage. These effects provide a theoretical basis for its application in neuropathic pain and related neurodegenerative diseases.
The analgesia mechanism of Beiwulin involves multiple molecular targets and exhibits multi-target coordinated regulation. The main targets include:
TRPV1 (Transient Receptor Potential Vanillic Acid Receptor 1): As an important ion channel for sensing heat and pain, its activation is closely related to pain conduction. Beiwulin regulates TRPV1 channel activity, inhibits excessive excitation of nerve endings, and reduces the transmission of pain signals.
CNR1 (Cannabinoid Receptor 1): Involved in analgesic regulation of the central and peripheral nervous systems. Beiwulin may activate or modulate CNR1 receptors to exert neuromodulative effects and relieve pain.
OPRD1, OPRM1, OPRK1 (δ, μ, κ opioid receptors): The interaction between alkaloid and opioid receptors enhances its analgesic effect, playing a key role especially in regulating chronic pain and neuropathic pain.
PTGS1 and PTGS2 (cyclooxygenases 1 and 2): As key enzymes in the synthesis of inflammatory mediators, Beiwulin inhibits PTGS1/2 activity, reduces prostaglandin production, and exerts anti-inflammatory and analgesic effects.
TRPA1 (Transient Receptor Potential Channel A1): Involved in the transmission of inflammatory pain, nectarine further enhances its analgesic effect through TRPA1 regulation.
SLC6A4 (serotonin transporter): regulates the reuptake of the neurotransmitter serotonin, affecting pain regulation in the central nervous system.
DRD2 (dopamine D2 receptor): By modulating the dopamine signaling pathway, alkaloid may affect the emotional and cognitive dimensions of pain.
In summary, Beiwulin regulates pain perception, transmission, and central regulatory mechanisms through the synergistic effects of multiple targets and pathways, demonstrating a complex and effective analgesic mechanism.
The druggability parameters of Beiwulin indicate that it has promising potential for drug development. Moderate molecular weight and LogP value ensure its moderate distribution in vivo and its ability to penetrate cell membranes. Higher TPSA and low blood-brain barrier permeability suggest that it mainly acts on peripheral targets, reducing the risk of central nervous system side effects. The hERG channel inhibits negative and carries no genotoxicity risk, further supporting its safety.
Pharmacokinetic studies show that narculline is absorbed orally relatively slowly, and its bioavailability is limited by its water solubility and metabolic stability. Its distribution in the body is mainly concentrated in the liver, kidneys, and nervous tissues. The metabolic pathway mainly involves oxidation and hydrolysis through the hepatic cytochrome P450 enzyme system, and the metabolites have certain activity. Excretion is mainly completed through the kidneys and bile pathways. Its half-life is moderate, making it suitable for routine dosing regimen design.
Currently, pharmacokinetic optimization strategies for Beiwuline include formulation modifications (such as nanocarriers and liposome encapsulation) and structural modifications to enhance water solubility and metabolic stability, aiming to enhance its bioavailability and therapeutic index.
Beiwuzine, as a natural product of multi-target analgesia, has broad clinical application prospects. Its potential is particularly prominent in the management of inflammatory pain, neuropathic pain, and chronic pain. Compared to traditional opioid analgesics, Beiwulin may become a safe and effective alternative due to its low central nervous system side effects and reduced addiction risk.
Future clinical research should focus on dose safety evaluation of Beiwudine, long-term drug toxicity, drug interactions, and personalized treatment plan design. At the same time, by integrating modern drug delivery technologies, its pharmacokinetic properties are optimized to improve clinical efficacy.
In addition, the potential applications of Beiwulin in neuroprotection, anti-inflammation, and neuropsychiatric disorders are also worth further exploration. The multi-target mechanism of action provides a theoretical foundation for the development of multifunctional drugs and is expected to promote the advancement of natural product pharmacology toward precision medicine.
Beiwuline, as a natural product with a unique chemical structure and multi-target pharmacological activity, has demonstrated significant value in the fields of pain relief and the treatment of related diseases. Its excellent druggability parameters and safety characteristics provide a solid foundation for new drug development. In the future, through in-depth mechanistic research, pharmacokinetic optimization, and clinical validation, Beiwudine is expected to become an important candidate for innovative analgesic drugs. Continuous advances in natural product pharmacology will open up broader prospects for the development and application of Beiwuline and similar compounds.
Shenshuai
Wenjing
Hedandan
