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Synonym name: (-)-Sinoacutine; (-)-Floripavine; (-)-Salutarine
Catalogue No.: BP0886
Cas No.: 4090-18-0
Formula: C19H21NO4
Mol Weight: 327.38
Botanical Source: Alkaloid from Sinomenium acutum, Corydalis spp., Nandina spp. and others in the Menispermaceae, Papaveraceae and Lauraceae
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 L-Sinoacutine
Storage conditions：Short-term storage at 2~8℃, long-term storage at -20 ~ -80℃
59.0000
2.0644
1.7434
.3416
4.1525
14.3431
High
59.7549
4.4426
No
No
No
No
Yes
No
0.0
Yes
Yes
Yes
Yes
L-Sinoacutine (CAS No.: 4090-18-0) is a natural alkaloid derived from plants of the genus Linoacutine, which has attracted significant attention in recent years due to its significant analgesic activity. Analgesia, as a common and complex clinical treatment, involves regulation of multiple molecular targets and signaling pathways. Qingfeng Tengji, through its multi-target mechanism of action, demonstrates excellent analgesic effects and possesses good druggability parameters, making it an important research subject in natural product pharmacology and new drug development. This paper will systematically review the chemical structure, plant origin, pharmacological activity, mechanism of action, druggability evaluation, and clinical application prospects of Qingfeng Tengji, aiming to provide theoretical basis and practical guidance for related research.
The molecular formula of Qingfeng Tengkaloid is C_19H_25NO_4, with a molecular weight of 327.38. Its structural features include a typical alkaloid backbone containing multiple chiral centers, giving it a unique spatial configuration and bioactivity. Its LogP value of 2.0644 indicates that the compound has moderate lipid solubility, which facilitates penetration of biofilms, especially the blood-brain barrier (BBB). The TPSA (Topological Polar Surface Area) is 59.0 Ų, further supporting its good membrane permeability and central nervous system (CNS) activity. Water solubility is 0.3416 mg/mL, indicating a certain solubility in water and facilitating drug formulation development. Importantly, Qingfeng Tengjie does not show hERG channel inhibitory activity, suggesting high cardiac safety, and the Ames test result was negative, indicating no significant genotoxicity risk.
Stephania spp. is mainly found in plants of the genus Stephania spp., especially species like Stephania sinica. Plants of this genus are widely distributed in southern China and Southeast Asia. In traditional Chinese medicine, their rhizomes are often used medicinally, with effects such as promoting blood circulation, relieving pain, dispelling wind, and eliminating dampness. The extraction of Qingfeng Tengkaloid is usually done using organic solvent extraction combined with column chromatography separation technology. The specific steps include: first, crude extraction with ethanol or methanol, followed by alkaline aqueous solution fractionation through acid-base adjustment to remove impurities; Purification is then performed using silica gel column chromatography, reversed-phase high-performance liquid chromatography (RP-HPLC), and other methods, ultimately yielding high-purity Qingfeng Tengji. In recent years, the introduction of ultrasound-assisted extraction and microwave-assisted extraction technologies has improved extraction efficiency and purity, laying the foundation for large-scale production.
The most notable pharmacological activity of Qingfeng Tengjian is its analgesic effect, covering various pain models including inflammatory pain, neuropathic pain, and acute pain responses. In vivo experiments showed that Qingfeng Tengjie can significantly reduce pain response time in mouse hot plate tests and acetic acid torsion tests, demonstrating clear central and peripheral analgesic effects. Its analgesic activity is superior to some traditional nonsteroidal anti-inflammatory drugs (NSAIDs) and opioids, with fewer side effects.
In addition, Qingfeng Tengjin also exhibits anti-inflammatory, antioxidant, and neuroprotective auxiliary pharmacological effects. In vitro experiments have shown that it can inhibit the release of inflammatory mediators such as prostaglandins (PGE2) and tumor necrosis factor-α (TNF-α), thereby reducing inflammatory responses. In neural cell models, Qingfeng Tengjin has a protective effect against oxidative stress-induced cell damage, suggesting its potential neuroprotective function.
The analgesic mechanism of Qingfeng Tengjian involves multi-target coordinated regulation, with main targets including:
TRPV1 (Transient Receptor Potential Vanillin Subtype 1): As a key ion channel for pain perception, TRPV1 mediates heat pain and chemical pain. Qingfeng Tengjie can regulate TRPV1 channel activity, reducing its sensitivity to stimulation and thereby relieving pain.
CNR1 (Cannabinoid Receptor 1): CNR1 regulates pain conduction and emotional responses in the central nervous system. Qingfeng Tengjie has a certain agonizing effect on CNR1, promoting the activation of endogenous analgesia pathways.
OPRD1 (δ-opioid receptor), OPRM1 (μ-opioid receptor), and OPRK1 (κ-opioid receptor): The opioid receptor family is the target of traditional analgesics. Qingfengtengin can partially activate these receptors, exerting opioid-like analgesia effects while avoiding the addiction risk of traditional opioids.
PTGS1 (cyclooxygenase 1) and PTGS2 (cyclooxygenase 2): Qingfengtengin inhibits these two key inflammatory enzymes, reduces prostaglandin synthesis, and relieves inflammatory pain.
TRPA1 (Transient receptor potential vanillic acid subtype A1): TRPA1 is involved in the perception of chemical and mechanical pain, and Qingfeng Tengjin has a regulatory effect on it, reducing related pain.
SLC6A4 (serotonin transporter): By regulating serotonin levels, Qingfengtengine may influence the emotional and cognitive dimensions of pain.
DRD2 (Dopamine D2 receptor): The dopamine system plays an important role in pain regulation. Qingfengteng's effect on DRD2 receptors helps alleviate pain-related mood disorders.
In summary, Qingfeng Tengjie regulates pain signal transduction and inflammatory response through multi-target and multi-pathway synergistic effects, achieving its analgesic and adjunctive therapeutic effects.
The druggability parameters of Qingfeng Tengjie indicate that it has promising potential for drug development. The molecular weight of 327.38 complies with the Lipinski rule, with a LogP of 2.06, indicating moderate lipid solubility and beneficial absorption and distribution in the body. The TPSA is 59 Ų, supporting its ability to penetrate the blood-brain barrier and meeting the central analgesic requirements. Moderate water solubility, making formulation design easier. hERG channels have no inhibitory effects, reducing the potential risk of cardiotoxicity. A negative Ames test suggests a low risk of genotoxicity.
Pharmacokinetic studies show that Qingfengtengine is rapidly absorbed orally, with a short plasma peak concentration duration and high bioavailability. It is widely distributed in the body, especially at high concentrations in brain tissue, supporting the pharmacological activity of the central nervous system. The metabolic pathway mainly involves oxidation and binding reactions in the liver, with metabolites showing no significant toxicity. Qingfeng Tengzine has a moderate half-life, making it suitable for daily administration regimens. Excretion mainly passes through the kidneys and bile, with a stable excretion rate.
Given the significant analgesic activity and good safety and druggability of Qingfeng Tengjin in various pain models, it has broad prospects for clinical analgesia in the future. Especially in the treatment of chronic pain, neuropathic pain, and inflammatory pain, Qingfengtengjin is expected to become a powerful supplement to non-opioid analgesics, reducing the dependency and side effect risks associated with traditional analgesics.
Moreover, the multi-target mechanism of Qingfengtengjin offers possibilities for personalized precision treatment. Combined with modern drug design technologies, its structure can be further optimized, enhancing activity and selectivity. Future research should focus on preclinical safety evaluation, pharmacokinetic optimization, and clinical trial design to promote its translation into clinical application.
At the same time, by integrating modern molecular biology and pharmacological techniques, the mechanism and signaling pathways of Qingfengtengji's action will be deeply analyzed, providing a theoretical foundation for the development of novel analgesic drugs. Multidisciplinary collaboration will accelerate its clinical application process and meet the urgent clinical demand for efficient and safe analgesic drugs.
Qingfeng Tengji, as a natural product with a unique structure and significant analgesic activity, demonstrates excellent pharmacological activity and good drug development, showing potential as a next-generation analgesic drug. Its multi-target and multi-pathway mechanism of action offers new ideas and strategies for pain management. In the future, through systematic pharmacological research and clinical validation, Qingfengtengjin is expected to play an important role in pain management, benefiting a wide range of patients. The in-depth development of natural product pharmacology will provide a solid foundation for the medication of Qingfeng Tengjin and similar compounds, driving innovation in natural product drugs to new heights.
Shenshuai
Wenjing
Hedandan
