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Storage conditions：Short-term storage at 2~8℃, long-term storage at -20 ~ -80℃
370.9700
1.5847
-1.0143
.2549
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75.8429
6.7207
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Stipuleanoside R2 (CAS No.: 96627-72-4) is a natural product derived from traditional Chinese medicinal materials, and has attracted widespread attention in recent years due to its remarkable pharmacological activity and potential clinical value. As a natural compound with a complex glycoside structure, Pingbian Sanqi glycoside R2 demonstrates unique advantages in regulating inflammatory responses and myocardial protection, especially during the inhibition α of TNFα-induced activation of nuclear factor κB (NF-κB), showing dose-dependent inhibitory effects. Its IC50 value is 4.1 μM, indicating high biological activity. The NF-κB signaling pathway plays a key role in the pathogenesis of various cardiovascular diseases, making the research of Trichinosin R2 in the field of myocardial protection of significant theoretical significance and promising applications.
This review aims to systematically summarize the chemical structure and physicochemical properties of Pingbian Trinotane Glycoside R2, plant origin and extraction methods, pharmacological activity and mechanism of action, druggability evaluation, and pharmacokinetic characteristics. Combined with its relevant targets and disease context, it explores its clinical application potential in myocardial protection, aiming to provide scientific basis and theoretical support for subsequent basic research and clinical translation.
Pingbian Trichiphenogin R2 is a naturally occurring triterpene saponin compound with a relatively high molecular weight, with a molecular weight of 1089.2320, exhibiting a relatively complex molecular structure. The compound has a LogP value of 1.5847, indicating moderate lipid solubility, which facilitates membrane penetration but is not overly hydrophobic, which would affect bioavailability. Its polar surface area (TPSA) reaches as high as 370.9700, reflecting the presence of many polar groups in the molecule, especially the glycoside part, which gives it good water solubility (0.2549), which positively affects the solubility and distribution of oral administration.
Structurally, Trichinoside R2 contains a triterpene backbone with multiple glycosyl-linked groups. The presence of glycosides not only increases molecular polarity but may also affect its binding ability to biological targets and metabolic stability. Its lower blood-brain barrier permeability indicates that the compound has limited penetration ability in the central nervous system, reducing the risk of central nervous system side effects. The hERG channel inhibition test results were negative, indicating a low risk of cardiotoxicity. The Ames mutagenic test result was 0.0, indicating that Pingbian Trinotane Glycoside R2 has no significant genotoxicity and has a good safety foundation.
Pingbian Sanqi glycoside R2 is mainly found in certain specific Chinese medicinal plants, with Panax notoginseng and its closely related species as the primary sources. As a traditional Chinese medicinal herb, Sanqi has long been used to promote blood circulation, remove blood stasis, stop bleeding, and relieve pain. Modern research has found it contains abundant triterpene saponin compounds, among which Pingbian Sanqi glycoside R2 is one of the important active components.
The extraction of Trinocygin R2 from the screen edge typically uses multi-step solvent extraction combined with chromatography separation technology. First, ethanol or methanol is used for reflux extraction of dried plant powders. After concentration, the extract is preliminarily separated using a water-ethanol gradient elution method. Subsequently, further purification was performed using high-performance liquid chromatography (HPLC) or reversed-phase column chromatography, combined with mass spectrometry (MS) and nuclear magnetic resonance (NMR) techniques for structural identification. In recent years, the application of ultrasound-assisted extraction and microwave-assisted extraction technologies has improved extraction efficiency and purity, while reducing solvent usage and extraction time, aligning with the concept of green chemistry.
Pharmacological activity studies of Pingbian Trinotane Glycoside R2 mainly focus on its anti-inflammatory and myocardial protective effects. Numerous in vitro cell experiments have shown that Pingbian Trinotane Glycoside R2 can significantly inhibit TNFα-induced activation of the NF-κB signaling pathway, exhibiting dose-dependence, with an IC50 value of 4.1 μM, indicating strong inflammatory regulatory ability. NF-κB, as a transcription factor, regulates the expression of various inflammatory factors and apoptosis-related genes. Its abnormal activation is closely related to myocardial ischemia-reperfusion injury, heart failure, and other cardiovascular diseases.
Additionally, animal model studies further confirmed the potential value of screen-edged tritycoside R2 in myocardial protection. By regulating key targets such as angiotensin-converting enzyme (ACE), endothelial nitric oxide synthase (NOS3), calcichannel protein (CACNA1C), sodium-calcium exchange protein (SLC8A1), potassium channel (KCNJ2), myocardial plasma reticulum calcium release channel (RYR2), and angiotensin II receptor type 1 (AGTR1), Pingbian trichizagin R2 can improve ionic homeostasis in myocardial cells, reduce oxidative stress and inflammatory responses, thereby alleviating myocardial injury and enhancing cardiac function.
Pingbian Trinotane Glycoside R2 achieves its myocardial protective effects through multi-target and multi-pathway synergistic effects. Its main mechanisms include:
Inhibits the NF-κB signaling pathway
Pingbian Tricotylin R2 can block TNFα-induced degradation of IκBα, inhibit the translocation of NF-κB from the cytoplasm to the nucleus, reduce the expression of inflammatory factors such as IL-6, IL-1β, and TNFα, and alleviate myocardial inflammatory responses.
Regulates the angiotensin system
By inhibiting ACE activity and downregulating AGTR1 expression, Pingbian Trinotoginseng R2 reduces the production of angiotensin II and receptor-mediated systolic signaling, lowering myocardial load and preventing myocardial remodeling.
Promotes nitric oxide synthesis
Upregulate NOS3 expression and activity, enhance NO release by endothelial cells, dilate blood vessels, improve myocardial ischemia, inhibit platelet aggregation, and protect myocardial cells.
Regulates ion channels in myocardial cells
By modulating key ion channel proteins such as CACNA1C, SLC8A1, KCNJ2, and RYR2, it maintains the electrophysiological stability of myocardial cells and prevents arrhythmias and apoptosis.
The synergistic effect of these mechanisms enables Pingbian Sanqi Glycoside R2 to exhibit multidimensional pharmacological effects in myocardial protection, showing strong potential for clinical translation.
Druggability evaluation of Pingbian Trinocypine R2 shows good safety and drug compatibility. Although its molecular weight is relatively large, its moderate LogP value and good water solubility help its absorption and distribution in the body. Its low blood-brain barrier permeability reduces the risk of central nervous system side effects. A negative hERG channel inhibition test indicates a low cardiotoxicity risk, while the Ames test shows no mutagenicity and good safety.
In terms of pharmacokinetics, although systematic studies on Pingbian Trinotane Glycoside R2 are currently limited, based on its structural characteristics, its oral bioavailability may be limited by its high polarity and molecular weight. In the future, drug delivery system optimization is needed, such as nanocarriers and liposome encapsulation strategies, to enhance in vivo stability and targeting. In addition, metabolic pathways may mainly be carried out through hepatic glycosyllase enzymes and corresponding phase I and II metabolases, and the activity and safety of these metabolites also require further research.
Pingbian Tritynocylin R2 shows broad clinical application prospects in the field of myocardial protection. By regulating inflammation, oxidative stress, and ionic homeostasis in myocardial cells through multiple targets, it has potential to treat myocardial ischemia, heart failure, arrhythmias, and other diseases. Combined with its excellent safety and low toxicity, Pingbian Sanqi Glycoside R2 is expected to become an important candidate for the development of novel cardiovascular drugs.
Future research should focus on the following aspects:
Systematic pharmacokinetics and pharmacodynamics research
Clarify the absorption, distribution, metabolism, and excretion characteristics in the body to optimize the administration regimen.
In-depth mechanism analysis and target validation
Using modern technologies such as gene editing and proteomics, further clarify its network of action and key targets.
Preclinical safety and efficacy evaluation
Ensure the safety of clinical applications through animal models and toxicological research.
Dosage form development and drug delivery route optimization
Exploring multiple approaches such as oral, injectable, and local administration to improve bioavailability and patient compliance.
Research on combination medication strategies
Combine with existing cardiovascular drugs to assess synergies and potential drug interactions.
Pingbian Trinocylin R2, a natural product with significant NF-κB inhibitory activity and multi-target myocardial protection, demonstrates excellent pharmacological activity and druggability. Its potential in cardiovascular disease prevention and treatment is continuously being revealed, providing new ideas and directions for natural product pharmacology and cardiovascular drug development. In the future, through in-depth mechanistic research and preclinical evaluation, it is expected that Pingbian trichigan R2 will be translated into clinical application, benefiting a wide range of cardiovascular disease patients.
Shenshuai
Wenjing
Hedandan
