Synonym name:
Catalogue No.: BP0291
Cas No.: 1354-84-3
Formula: C₂₂H₃₅NO₂
Mol Weight: 345.527
Botanical Source: Alkaloid from the Chinese drug Hye-shang-yi-zhi-hao (Aconitum bullatifolium var. homotrichum, Ranunculaceae)

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.

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

Introduction/Overview

Bullatine A (CAS No.: 1354-84-3) is a diterpene alkaloid derived from the traditional Chinese medicinal plant Aconitum bullatum Hand.-Mazz. In recent years, with in-depth research into the molecular mechanisms of neuroinflammation and related diseases, Xueshang Yizhihao Methyl Extract has gradually become a research hotspot in the field of natural product pharmacology due to its unique pharmacological activity and multi-target mechanism. This compound exhibits significant antirheumatic, anti-inflammatory, analgesic, and antitumor activities, especially showing good application potential in central nervous system diseases and inflammation regulation. This paper will systematically review the chemical structure and physicochemical properties of Xueshang Yizhihao methylasterin, plant origin and extraction methods, pharmacological activity, mechanism of action, druggability evaluation, and clinical application prospects, aiming to provide a theoretical foundation and research direction for further development and clinical translation of this natural product.

Chemical structure and physicochemical properties

Xueshang Yizhihao methyl is a diterpene alkaloid with the molecular formula C_20H_29NO_3 and a molecular weight of 343.50. Its molecular structure contains a typical diterpene skeleton, with multiple ring-like structures and nitrogen-containing groups, giving it unique biological activity. In terms of physicochemical properties, the LogP value of Xueshang Yizhihao methyl is about 3.0, showing moderate hydrophobicity, which facilitates penetration of cell membranes and the blood-brain barrier (BBB). Its topological polar surface area (TPSA) is 38.77 Ų, with 3 hydrogen bond receptors, further supporting its good membrane permeability and potential central nervous system activity. According to pharmacokinetic predictions, Xueshang Yizhihao has high blood-brain barrier permeability, but it carries potential cardiotoxicity risks and hERG channel inhibition, indicating that its safety evaluation should be focused in clinical development.

Plant Origins and Extraction Methods

Artemisia xueshang Yizhi methyl is mainly isolated from the rhizome of the Ranunculaceae family plant, Artemisia snow on the snow tree. Xueshang Yizhihao is distributed in southwestern China and has long been used in traditional Chinese medicine to treat rheumatic pain, inflammation, and nervous system diseases. During extraction, alcohols (such as ethanol or methanol) are typically used for reflux extraction of dried plant rhizomes, followed by separation and purification through liquid-liquid separation and column chromatography. Modern research has combined high-performance liquid chromatography (HPLC) and mass spectrometry (MS) technologies to achieve efficient separation and quantitative analysis of Artemisia methylene in Snow Stage. Some studies have also explored green and efficient extraction technologies such as supercritical CO_2 extraction and microwave-assisted extraction to improve yield and purity, reduce solvent usage, and promote the feasibility of industrial production.

Pharmacological activity research

Anti-inflammatory and anti-rheumatic effects

Xueshang Yizhihao methyl hormone, as a potent P2X7 receptor antagonist, significantly inhibits ATP-induced BV-2 microglial death and apoptosis, reducing P2X7-mediated inflammatory responses. P2X7 receptors play a key role in inflammation and immune regulation. Their activation promotes the release of inflammatory factors and cell apoptosis. Xueshang Yizhihao methyl hormone exhibits good anti-inflammatory effects by antagonizing this receptor and inhibiting inflammatory cascade reactions. Additionally, Xueshang Yizhihao methyl acid effectively alleviated LPS-induced systemic inflammatory responses in mice in vivo, involving inhibition of the ROS/JNK/NF-κB signaling pathway, further validating its anti-inflammatory potential. Its antirheumatic effect is closely related to its inhibition of the release of inflammatory mediators and activation of immune cells.

Analgesic effect

Xueshang Yizhihao methyl hormone demonstrated significant analgesic effects in various animal models, especially in hyperalgesia models, where it specifically reduced rat hyperalgesia responses. Its analgesic mechanism involves multi-target regulation, including receptors and enzymes such as TRPV1, TRPA1, CNR1, OPRD1, OPRM1, OPRK1, PTGS1, PTGS2, SLC6A4, and DRD2, reflecting its combined ability to regulate pain signal transduction. By modulating these targets, Xueshang Yizhihaojia not only relieves acute pain but also has potential therapeutic effects for chronic pain and neuropathic pain.

Antitumor effects

In recent years, Xueshang Yizhimuoshi has attracted attention in glioblastoma (GBM) research. Research shows that Xueshang Yizhihao methyl inhibits glioma cell proliferation and growth by targeting SIRT6 (a deacetylase), inducing cell cycle arrest and apoptosis, suggesting its potential as an anti-tumor drug candidate. SIRT6 plays an important role in tumor metabolism and DNA repair, and its regulation has a key impact on tumor cell survival and drug resistance. Xueshang Yizhihaojia inhibits GBM through this target, providing new approaches for tumor treatment.

Antidepressant effects

In a mouse model of chronic social frustration stress (CSDS), Xueshang Yizhimujiaji significantly improved desperate behavior in mice and exhibited antidepressant activity. Its mechanism of action may involve alleviating inflammatory responses and modulating the neurotransmitter system, especially by inhibiting neuroinflammatory and oxidative stress pathways, thereby improving neuronal function and emotional regulation. This discovery provides a new research direction for the application of natural products in the treatment of neuropsychiatric disorders.

Mechanism of action and molecular targets

The pharmacological activity of Xueshang Yizhihaojia depends on its multi-target and multi-pathway regulatory characteristics. The main mechanisms of action include:

1. P2X7 receptor antagonism
   The P2X7 receptor is an ATP-dependent ion channel involved in inflammatory responses and cell death. Xueshang Yizhihao methyl is a potent P2X7 antagonist that blocks its activation, inhibits the release of inflammatory factors and microglia apoptosis, and reduces neuroinflammation.

2. ROS/JNK/NF-κB signaling pathway inhibition
   Xueshang Yizhihao methyl extract inhibits reactive oxygen species (ROS) production, blocks activation of JNK and NF-κB signaling pathways, reduces pro-inflammatory factor expression, and exerts anti-inflammatory and neuron-protective effects.

3. SIRT6 regulation
   By targeting SIRT6, Xueshang Yizhihao methyl influencing the proliferation and apoptosis of glioma cells, regulating cell metabolism and DNA repair, and exerting anti-tumor effects.

4. Multi-target analgesia mechanism
   By modulating TRPV1, TRPA1 plasma channels, as well as neurotransmitter receptors such as CNR1 (cannabinoid receptor) and OPRD1/OPRM1/OPRK1 (opioid receptor), Snow Rose Artemisisin regulates pain transmission and sensation, alleviating hyperalgesia.

5. Neuropsychiatric regulation
   It may improve depression-related behaviors by affecting neurotransmitter systems such as SLC6A4 (serotonin transporter) and DRD2 (dopamine receptor).

In summary, Xueshang Yizhihao methyl extract achieves a wide range of pharmacological effects through the synergistic action of multiple molecular targets.

Druggability evaluation and pharmacokinetics

The druggability evaluation of Xueshang Yizhihaojia showed that it has good pharmacokinetic characteristics. Moderate hydrophobicity (LogP=3.0) and low polarity (TPSA=38.77) favor oral absorption and blood-brain barrier penetration, supporting its application in central nervous system diseases. In vivo pharmacokinetic studies show that Xueshang Yizhihao methyl can effectively distribute in brain tissue, exerting neuroprotective and analgesic effects.

However, safety concerns must be given to its potential cardiotoxicity and hERG channel suppression risks, which may limit its clinical dosage and application range. Further toxicological research and structural optimization will be the focus of future development. In addition, the metabolic pathway of Xueshang Yizhihao methylaminin is not yet fully understood, and systematic studies are needed on the role of liver metabolic enzymes and the activity and toxicity of its metabolites.

Prospects and outlooks for clinical applications

Xueshang Yizhihao Jiasu shows broad clinical application prospects due to its significant anti-inflammatory, analgesic, anti-tumor, and antidepressant effects. Its unique advantage as a P2X7 receptor antagonist gives it potential therapeutic value in neuroinflammatory diseases such as rheumatoid arthritis, neuropathic pain, and multiple sclerosis. At the same time, antitumor activity targeting glioblastoma provides new drug candidates for the treatment of refractory brain tumors.

The discovery of antidepressant effects has further broadened its indications, especially in the treatment of inflammation-related depression, where Xueshang Yizhihao Jia may become an emerging natural medicine option. In the future, combining modern drug design and delivery technologies, such as nanocarriers and targeted drug delivery, is expected to improve bioavailability and safety.

However, the clinical translation of Xueshang Yizhihao Jiasin still faces multiple challenges, including systematic toxicological assessment, dose optimization, long-term safety verification, and clinical trial design. Multidisciplinary collaboration and in-depth mechanistic research will be key to driving its clinical application.

Conclusion

As a multi-target, multifunctional natural diterpene alkaloid, Xueshang Yizhihao Jiasu demonstrates rich pharmacological activity and promising pharmaceutical potential. Its research progress in anti-inflammation, analgesia, anti-tumor, and antidepressant fields provides valuable examples for natural product pharmacology. In the future, with the deeper integration of medicinal chemistry, molecular biology, and clinical medicine, Xueshang Yizhihao Jiasin is expected to become an important drug for treating various complex diseases. Ongoing mechanism research, safety evaluation, and clinical validation will lay a solid foundation for its translational application, driving innovative development of natural products in modern medicine.