Introduction/Overview
Butin (CAS number: 492-14-8) is a natural flavonoid compound originally isolated from the heartwood of Dalbergia spp. As an important member of flavonoids, Ziliuting has received widespread attention in recent years due to its significant biological activities, especially antioxidant, antiplatelet aggregation, and anti-inflammatory effects. It demonstrates potential therapeutic value for various diseases, especially pathological processes related to inflammation and tumors. This article aims to systematically review the chemical structure, origin, pharmacological activity, mechanism of action, and drug evaluation of Ziliuting, explore its potential applications in diseases such as prostate cancer, and look forward to its future research directions and clinical development prospects.
Chemical structure and physicochemical properties
Ziliuting is a flavonoid compound with a molecular formula of C15H12O5 and a molecular weight of 272.25. Its structural features include a typical flavonoid skeleton containing multiple hydroxyl groups, endowing it with excellent antioxidant properties. The LogP value of Ziliuting is 1.5, indicating that it has moderate lipid solubility, which is beneficial for absorption and distribution in the body. Its topological polar surface area (TPSA) is 94.83 Å ², and the number of hydrogen bond acceptors is 5. These physicochemical parameters suggest that Ziliuting has good bioavailability and cell membrane penetration ability.
There are two enantiomers of Ziliuting, among which (-) - Ziliuting is the main active form, exhibiting stronger biological activity. This compound has good chemical stability and exhibits low blood-brain barrier penetration in vivo, reducing the risk of central nervous system toxicity. Toxicological evaluation shows that Ziliuting has no hepatotoxicity, cardiotoxicity, or hERG channel inhibition effect, and the Ames mutagenicity test is negative, indicating its high safety.
Plant sources and extraction methods
Purple rivet pavilion is mainly isolated from the heartwood of plants in the Dalbergia genus. Dalbergia plants are widely distributed in tropical and subtropical regions and are widely used as traditional Chinese medicinal materials. Huangtan heartwood contains abundant flavonoids, among which Zizhuting has a higher content and is one of the important active ingredients of this genus of plants.
The common methods for extracting purple rivet pavilion include solvent extraction, column chromatography separation, and high-performance liquid chromatography (HPLC) purification. Generally, ethanol or methanol is used as the extraction solvent, and separation and purification are carried out by reflux extraction or ultrasound assisted extraction, combined with silica gel column chromatography or C18 reverse phase column. In recent years, the application of supercritical CO2 extraction and membrane separation technology has improved extraction efficiency and purity, providing technical support for the large-scale preparation of Ziliuting.
Pharmacological activity research
antioxidant activity
Purple rivet pavilion, as a type of polyhydroxyflavonoid, exhibits strong free radical scavenging ability. In vitro experiments have shown that it can effectively scavenge DPPH and ABTS free radicals, inhibit lipid peroxidation, and protect cells from oxidative damage. Its antioxidant mechanism is mainly achieved by directly capturing free radicals and regulating the intracellular antioxidant enzyme system (such as SOD, CAT, GPx).
Antiplatelet aggregation effect
Platelet aggregation is an important pathological basis for various cardiovascular diseases. Ziliuting can significantly inhibit platelet activation and aggregation, block the flow of calcium ions and related signaling pathways within platelets, and reduce the risk of thrombosis. Both in vitro and animal model experiments have confirmed its excellent anti thrombotic effect, indicating its potential in the prevention and treatment of thrombotic diseases.
anti-inflammatory effect
Inflammation is the common pathological basis of various chronic diseases. Purple rivet pavilion reduces inflammation by inhibiting the expression of pro-inflammatory factors such as TNF - α, IL-6, IL-1 β. Its mechanism of action involves the regulation of NF - κ B and MAPK signaling pathways, reducing the infiltration of inflammatory cells and the release of inflammatory mediators. In addition, Ziliuting can also inhibit the activity of inflammation related enzymes such as COX-2 and iNOS, exerting multi-target anti-inflammatory effects.
Antitumor activity
Ziliuting exhibits inhibitory effects on proliferation, induction of apoptosis, and inhibition of migration in various tumor cell lines. Especially in prostate cancer models, Ziliuting inhibits tumor cell growth and invasion by regulating multiple signaling pathways. Its anti-tumor activity is closely related to its regulatory molecular targets, demonstrating its potential as a candidate anti-cancer drug.
Mechanism of action and molecular targets
The pharmacological effects of Ziliuting involve multiple signaling pathways and key molecular targets, which have been extensively elucidated in the study of prostate cancer. The main targets include:
- BCL2 Purple rivet pavilion can downregulate the expression of anti apoptotic protein BCL2 and promote tumor cell apoptosis.
- PTPN1 By regulating protein tyrosine phosphatase PTPN1, Ziliuting affects cell proliferation and metabolic signaling.
- STAT3 Inhibit the activation of STAT3, block its pro tumor growth and immune escape effects.
- ESR2 As an estrogen receptor β, the regulation of ESR2 helps to regulate the hormone response of prostate cancer cells.
- MAPK1 Intervene in the MAPK signaling pathway to regulate cell proliferation and apoptosis.
- CYP19A1 Affects the expression of aromatase and regulates hormone metabolism.
- AR Inhibiting androgen receptor (AR) signaling and blocking hormone driven growth in prostate cancer.
- PIK3CA Regulating the PI3K/AKT pathway and inhibiting tumor cell survival.
- LGALS3 Regulating galectin-3, affecting tumor microenvironment and cell adhesion.
- EGFR Inhibit epidermal growth factor receptor (EGFR) signaling, reduce tumor cell proliferation and migration.
Purple rivet pavilion achieves its comprehensive anti-tumor and anti-inflammatory effects through multi-target and multi pathway synergistic effects. In addition, its regulation of oxidative stress-related signals further consolidates its potential in disease treatment.
Evaluation of drug properties and pharmacokinetics
The physical and chemical properties of Ziliuting demonstrate its excellent potential for medicinal use. Moderate molecular weight and LogP value are beneficial for drug absorption and distribution. The higher number of TPSA and hydrogen bond receptors ensures the binding ability to the target, while limiting non-specific penetration and reducing the risk of toxic side effects.
Toxicological evaluation shows that Ziliuting has no significant hepatotoxicity, cardiotoxicity, or genotoxicity, and has good safety. Its blood-brain barrier penetration ability is relatively low, reducing the possibility of adverse reactions in the central nervous system.
Pharmacokinetic studies have shown that Ziliuting has good oral absorption, wide distribution in the body, stable metabolism, and is mainly metabolized and excreted through the liver. Moderate half-life, suitable for daily administration. Further in vivo pharmacokinetic and pharmacodynamic studies are needed in the future to optimize dosing regimens and dosage form design.
Clinical application prospects and prospects
As a multifunctional flavonoid natural product, Ziliuting exhibits a wide range of pharmacological activities and good safety. Its multi-target regulatory role in prostate cancer, especially its synergistic effects in anti-tumor, anti-inflammatory, and antioxidant aspects, endows it with the potential to become a novel anti-cancer drug.
Future research should focus on:
- In depth analysis of the mechanism Through multiple omics techniques, further reveal the molecular network and signaling pathways underlying the action of purple rivet pavilion.
- Pharmacokinetic optimization Develop new drug delivery systems to improve bioavailability and targeting.
- Preclinical and clinical research Conduct systematic toxicological evaluation and clinical trials to verify its safety and efficacy.
- Combination therapy strategy Explore the synergistic effect of Ziliuting with existing drugs to improve treatment efficacy and reduce the risk of drug resistance.
- Expansion of applications for other diseases Based on its anti-inflammatory and antioxidant properties, explore its applications in fields such as cardiovascular disease and neurodegenerative diseases.
In summary, as a natural flavonoid compound with multiple biological activities, Ziliuting has good development prospects and is expected to become an important candidate molecule for future natural medicine development.
Conclusion
As the main active flavonoid in the heartwood of Dalbergia rosea, Ziliuting occupies an important position in the field of natural product pharmacology due to its excellent antioxidant, antiplatelet aggregation, and anti-inflammatory activities. Its multi-target mechanism of action and good pharmacological properties provide a solid foundation for the development of new anti-tumor and anti-inflammatory drugs. In the future, through systematic pharmacological mechanism research and clinical translation, Ziliuting is expected to become an effective drug for treating prostate cancer and related diseases, injecting new vitality into the development of natural product drugs.