Synonym name: Macelignan; Calophyn
Catalogue No.: BP0176
Cas No.: 107534-93-0
Formula: C20H24O4
Mol Weight: 328.408
Botanical Source: Myristica fragrans (nutmeg), bark of Kadsura longipedunculata and Schizandra sphenanthera
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 Anwuligan
Storage conditions：Short-term storage at 2~8℃, long-term storage at -20 ~ -80℃
Anwuligan, CAS number 107534-93-0, is a typical lignan natural product, mainly isolated from traditional Chinese medicinal materials such as Schisandra chinensis. As a natural compound with multiple biological activities, pentalipidin demonstrates significant pharmacological effects in antioxidant, anti-inflammatory, and metabolic regulation, attracting widespread attention in pharmacology and natural medicinal chemistry in recent years. Especially in adjunctive therapy for liver dysfunction and chemical liver injury, ampentadanin has shown good protective effects. Moreover, recent research suggests that amnpentalipin may participate in the pathological mechanisms of neurological diseases such as migraine disorders by regulating various molecular targets, offering new ideas and potential value for its clinical application. This paper aims to systematically review the chemical structure, plant origin, pharmacological activity, mechanism of action, druggability evaluation, and future clinical application prospects of pentalipidin, aiming to provide comprehensive and in-depth reference materials for researchers in related fields.
Anpentadin belongs to the lignan class of compounds with the molecular formula C20H24O4 and a molecular weight of 328.40. Its structural features are mainly the typical diphenylpropane backbone, featuring multiple hydroxyl substitutions and methoxy groups, which impart excellent antioxidant activity. In terms of physicochemical properties, the LogP value of pentadipidin is about 4.21, indicating good lipid solubility, which is beneficial for cell membrane penetration and bioavailability. The topological pole surface area (TPSA) is 55.12 Ų, and the number of hydrogen bond receptors is 4, indicating moderate polarity and hydrogen bond binding capability in drug design.
Blood-brain barrier (BBB) permeability assessment showed that pentadanin has a lower BBB penetration capacity, which may limit its direct role in central nervous system diseases but also reduces the risk of potential CNS toxicity. In terms of toxicological evaluation, pentafatin showed no hepatotoxicity, cardiotoxicity, or hERG channel inhibitory effects, demonstrating a good safety profile. Ames-induced mutagenic test data are not yet clear, and further tests are needed to verify its genotoxicity risk.
Anphthadanin is mainly isolated from Schisandra chinensis. Schisandra belongs to the Schisandaceae family, widely distributed in Northeast and North China, as well as the Korean Peninsula. It has long been used as a traditional Chinese medicine to regulate liver function, enhance immunity, and combat fatigue. Besides schisandra, some plants containing lignans can also detect pentadyne, but at lower levels.
The extraction process typically uses organic solvent extraction combined with column chromatography for separation and purification. The specific process includes:
1. Use ethanol or methanol as extractants to extract dried Schisandra fruit by reflux extraction;
2. Concentrate the extract by vacuum reduction;
3. Separation and purification using silica gel column chromatography and reversed-phase high-performance liquid chromatography (RP-HPLC);
4. Finally, the structure and purity are confirmed using technologies such as nuclear magnetic resonance (NMR) and mass spectrometry (MS).
In recent years, the application of ultrasound-assisted extraction and microwave-assisted extraction technologies has improved the extraction efficiency and purity of pentadan, and is more in line with green chemical principles.
Anpentalipidin exhibits significant antioxidant activity, effectively scavenging free radicals and inhibiting lipid peroxidation. In vitro DPPH radical scavenging experiments and cell models, ampentalipin significantly reduced oxidative stress indicators and enhanced intracellular antioxidant enzyme activity (such as superoxide dismutase SOD and glutathione peroxidase GSH-Px). Its antioxidant mechanism is closely related to the electron donor capacity of polyhydroxyl and methoxy groups in its structure.
Multiple in vivo and in vitro experiments have shown that pentalipidin can inhibit the production and release of inflammatory mediators. By downregulating the NF-κB signaling pathway, it reduces the expression of pro-inflammatory cytokines (such as TNF-α, IL-1β, IL-6), thereby alleviating inflammatory responses. In mouse models, ampentalipin significantly alleviated inflammatory liver injury and tissue edema, demonstrating good anti-inflammatory effects.
Anpentadanin regulates liver lipid metabolism and can improve hepatic steatosis and lipid accumulation. By activating the AMPK signaling pathway, it promotes fatty acid oxidation, inhibits lipid synthesis, and reduces hepatocyte fat deposition. Additionally, pentadipin affects glucose metabolism and demonstrates potential anti-diabetic effects.
Anpentadanin has shown significant protective effects in various liver injury models. In chemical liver injury (such as carbon tetrachloride and alcohol-induced models), pentadipin can lower serum transaminase (ALT, AST) levels, alleviate hepatocyte necrosis and inflammatory infiltration, and promote liver tissue repair. Its hepatoprotective effects are mainly attributed to multiple mechanisms including antioxidant, anti-inflammatory, and regulation of apoptosis.
Although pentalipidin has low blood-brain barrier permeability, it may have adjunctive therapeutic potential for migraine disorders by regulating the peripheral nervous system and inflammatory responses. Related studies indicate that ampentalipidin acts on multiple targets including ALOX15, BCHE, ACHE, EDNRA, DRD1, ADRA1A, TAAR1, EP300, and P2RX7, regulating inflammation, neurotransmitter metabolism, and vascular tone, thereby alleviating migraine symptoms.
The multi-target mechanism of pentafatin is the basis of its pharmacological activity. The main targets and related mechanisms are as follows:
Overall, Anpentadin regulates inflammatory responses, neurotransmitter metabolism, and vascular function through multi-target and multi-pathway synergistic effects, exerting its broad pharmacological effects.
The druggability evaluation of pentalipidin shows it has good potential for drug development. The molecular weight of 328.4 meets the Lipinski rule, and the LogP of 4.21 is moderate, indicating good membrane permeability and in vivo distribution characteristics. TPSA is 55.12 Ų, indicating moderate polarity and favorable for oral absorption.
Toxicological data indicate that pentafatin does not show significant hepatotoxicity, cardiotoxicity, or hERG channel inhibition, and is relatively safe. However, the lower permeability of the blood-brain barrier limits its direct role in central nervous system diseases but also reduces the risk of adverse reactions.
In terms of pharmacokinetics, current research is relatively limited. In vivo animal experiments show that pentadipin is absorbed orally relatively quickly, has a moderate plasma half-life, and is mainly metabolized by the liver, with excretion primarily via bile and urine. In the future, further systematic research on pharmacokinetics and metabolic kinetics is needed to clarify their in vivo behavior and metabolic activity products.
Based on the multiple pharmacological activities of Anpentaditin, especially its significant effects in liver protection, anti-inflammation, and metabolic regulation, it holds broad application prospects in adjunctive treatment of liver dysfunction, chemical liver injury, and metabolic syndrome. In recent years, with deeper understanding of migraine pathogenesis, Anpentazin has gained new ideas for treating migraine and other neurological diseases by regulating multiple targets to participate in neuroinflammation and vascular function regulation.
Future research focuses should include:
1. Systematic evaluation of the efficacy and safety of pentadipin in neurological diseases, especially its clinical efficacy verification for migraine;
2. Optimize extraction and synthesis processes to increase the yield and purity of Anpentalipin, and reduce production costs;
3. In-depth analysis of its molecular mechanisms to uncover more potential targets and signaling pathways;
4. Conduct pharmacokinetic, toxicological, and preclinical safety evaluations to lay the foundation for clinical trials;
5. Explore formulation development for pentalipidin, such as nanocarriers and sustained-release formulations, to improve its bioavailability and targeting.
In summary, pentafatin is a natural lignan compound with multi-target effects and possesses good pharmacological activity and safety, making it expected to become an important candidate for the treatment of liver and neurological diseases in the future.
Anpentalipin, as an important active ingredient in plants such as Schisandra, demonstrates broad research and application value in the field of natural product pharmacology due to its unique chemical structure and diverse biological activities. Its antioxidant, anti-inflammatory, and metabolic regulatory effects provide a theoretical basis and practical basis for liver protection and the treatment of neurological diseases. Although research on its pharmacokinetics and clinical applications is still in its early stages, with the continuous revelation of molecular target mechanisms and improvements in druggability evaluation, Anpentalipin is expected to become an important direction for future natural drug development. We look forward to more high-quality basic and clinical research to promote pentalipidin from the laboratory to clinical practice, bringing new treatment options for patients with related diseases.
