Product name: Vaccarin E
Synonym name:
Catalogue No.: BP5104
Cas No.: 2252345-81-4
Formula: C₄₂H₄₈O₂₂
Mol Weight: 904.824
Botanical Source:
Type of Compound: Flavonoids

Purity: 95%~99%
Analysis Method: HPLC-DAD or/and HPLC-ELSD
Identification Method: Mass, NMR
Packing: Brown vial or HDPE plastic bottle

Storage: Store in a well closed container, protected from air and light. Put into refrigerate or freeze for long term storage.
Whenever possible, you should prepare and use solutions on the same day. However, if you need to make up stock solutions in advance, we recommend that you store the solution as aliquots in tightly sealed vials at -20℃. Generally, these will be useable for up to two weeks.

The product could be supplied from milligrams to grams
Inquire for bulk scale.

For Reference Standard and R&D, Not for Human Use Directly.

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

Introduction/Overview

Vaccarin E is a natural C-flavonoid carboside isolated from the plant Vincetoxicum hispanica, and has attracted widespread attention in recent years due to its remarkable biological activity and potential medicinal value. As a natural product, Wang Bu Liu Xing Flavonoid Glycoside E exhibits good pharmacological activity in cardiovascular protection, involving multiple key targets and signaling pathways, demonstrating its potential in the prevention and treatment of cardiovascular diseases. This paper systematically reviews the chemical structure and physicochemical properties of Wang Bu Liuxing Flavonoid E, plant origin and extraction methods, pharmacological activity, mechanism of action, druggability evaluation, and clinical application prospects, aiming to provide theoretical basis and reference for subsequent research and drug development.

Chemical structure and physicochemical properties

Wang Buliuxing Flavonoid Glycoside E belongs to the C-flavonoid carboside class of natural products, with a complex molecular formula and a molecular weight of 904.8240. Its structural feature is that the flavonoid nucleus is connected to glycosides via carbon bonds, distinguishing it from the common O-glycosides. The carbon-glycosidic bonds of C-glycosides provide it with high chemical and metabolic stability. The LogP value of Wang Buliuxing flavonoid glycoside E was -0.1574, indicating strong hydrophilicity. Combined with its high polar surface area (TPSA of 354.6500), it exhibited good water solubility (1.5801), which is beneficial for absorption and distribution in the body. The low permeability of the blood-brain barrier suggests limited impact on the central nervous system and may reduce the risk of central nervous system toxicity. The hERG channel inhibition test was negative, indicating a low risk of cardiotoxicity, while the Ames mutagenicity test was 0.0, indicating no significant mutagenicity and a solid safety foundation.

Plant Origins and Extraction Methods

Vincetoxicum hispanica is mainly derived from Vincetoxicum hispanica, a plant widely distributed along the Mediterranean coast and commonly used in traditional Chinese medicine to promote blood circulation, remove blood stasis, reduce swelling, and relieve pain. Common methods for extracting Wang Buliuxing Flavonoid Glycoside E include solvent extraction, ultrasound-assisted extraction, and high-performance liquid chromatography (HPLC) separation and purification. Ethanol or methanol is usually used as extraction solvents, combined with ultrasonic assistance to improve extraction efficiency. After concentration, separation, and chromatographic separation, the extract was used for structural identification and purity confirmation using mass spectrometry and nuclear magnetic resonance (NMR) technology. In recent years, green extraction technologies such as supercritical fluid extraction and microwave-assisted extraction have also been attempted to efficiently extract Wang Bu Liuxing flavonoid E to improve yield and purity and reduce environmental impact.

Pharmacological activity research

The pharmacological activity of Wang Buliuxing Flavonoid Glycoside E mainly focuses on its cardiovascular protective effects. Multiple in vitro and in vivo experiments have shown that this compound has anti-inflammatory, antioxidant, vascular endothelial function, and lipid regulation. Its significant anti-inflammatory activity is reflected in inhibiting the expression of inflammatory factors such as ICAM1 and VCAM1, reducing adhesion and inflammatory responses of vascular endothelial cells. In terms of antioxidant properties, Wang Buliuxing Flavonoid Glycoside E can enhance the activity of nitric oxide synthase (NOS3) in endothelial cells, increase nitric oxide (NO) production, and reduce oxidative stress damage. Additionally, this compound inhibits angiotensin-converting enzyme (ACE), helping to regulate blood pressure and improve vascular function. Animal model studies have shown that Wang Buliuxing flavonoid glycoside E can significantly improve hypertension, atherosclerosis, and myocardial ischemia-reperfusion injury, demonstrating good cardiovascular protective effects.

Mechanism of action and molecular targets

Wang Buliuxing Flavonoid Glycoside E exerts its cardiovascular protective effect through multiple targets and multiple pathways in synergistic action. Its main targets include:

• SELP (Selectin P): Regulates the adhesion of platelets and white blood cells, and participates in inflammatory responses. Wang Buliu administered flavonoid glycoside E by inhibiting SELP expression, reducing vascular inflammation and thrombosis.
• PPARG (Peroxisome Proliferator-Activated Receptor γ): Regulates lipid metabolism and inflammatory responses. Wang Buliu activates the PPARG pathway with flavonoid glycosides, improving lipid metabolism disorders and inhibiting inflammation.
• ACE (angiotensin-converting enzyme): a key blood pressure regulator, Wang Buliu uses flavonoid glycoside E to inhibit ACE activity, reducing vasoconstriction and alleviating hypertension.
• AKT1 (protein kinase B): involved in cell survival and metabolic regulation, Wang Buliu activates AKT1 signaling by using flavonoid E, promoting endothelial cell survival and functional recovery.
• ADRB2 (β2 adrenergic receptor): Regulates vasodilation and myocardial function. Wang Buliuxing flavonoid glycoside E helps improve cardiovascular responses by modulating ADRB2.
• KCNH2 (hERG potassium channel): regulates cardiac action potentials; Wang Buliu's flavonoid glycoside E does not inhibit hERG channels, reducing arrhythmia risk.
• NOS3 (endothelial nitric oxide synthase): promotes NO production, dilates blood vessels, and Wang Bu Liu uses flavonoid glycoside E to enhance NOS3 activity and improve vasodilatory ability.
• ICAM1 and VCAM1 (intercellular adhesion molecules): mediate the adhesion of inflammatory cells; Wang Bu Liu administered flavonoid E to inhibit their expression and reduce vascular inflammation.
• SLC8A1 (sodium-calcium exchanger): Regulates cellular calcium homeostasis. Wang Buliu uses flavonoid glycoside E to regulate SLC8A1, which helps protect myocardial cell function.

Overall, Wang Buliuxing Flavonoid Glycoside E demonstrates a complex and multidimensional pharmacological mechanism by modulating the above targets to synergistically inhibit inflammatory responses, improve vascular endothelial function, regulate blood pressure, and protect myocardium.

Druggability evaluation and pharmacokinetics

From the perspective of druggability, Wang Bu Liu Xing Flavonoid Glycoside E has high water solubility and moderate molecular weight, which is beneficial for absorption and distribution in the body. Its LogP value is close to neutral, indicating that it has certain solubility in both aqueous and lipid phases, facilitating transmembrane transport. High polar surface area (TPSA) may limit its oral bioavailability, but its stable C-glycosidic bond structure helps resist gastrointestinal enzymatic digestion and improves in vivo stability. The blood-brain barrier has low permeability, reducing the risk of central nervous system side effects. hERG channels have no inhibitory effect and reduce potential cardiotoxicity; a negative Ames test indicates a low genotoxicity risk.

Pharmacokinetics, current research is limited. Preliminary in vitro metabolic experiments show that Wang Buliuxing Flavonoid Glycoside E is stably metabolized in hepatic microsomes and is mainly excreted by the kidneys. In the future, further studies on in vivo absorption, distribution, metabolism, and excretion (ADME) are needed to clarify bioavailability, half-life, and metabolites, and optimize dosing regimens.

Prospects and outlooks for clinical applications

As one of the leading causes of death worldwide, cardiovascular disease urgently requires safe and effective new treatments. Wang Bu Liu Xing Flavonoid Glycoside E, with its multi-target cardiovascular protection and good safety, demonstrates broad clinical application potential. Its anti-inflammatory, antioxidant, blood pressure-regulating, and vascular function effects provide new ideas for adjunctive treatment of hypertension, atherosclerosis, coronary heart disease, and myocardial ischemia.

Future research should focus on:

1. In-depth pharmacological mechanisms: Using genomics, proteomics, and metabolomics technologies, a comprehensive analysis of the molecular action network of Wang Bu Liu Xingflavonoid E is conducted.
2. Pharmacokinetics and safety evaluation: Systematic in vivo pharmacokinetic studies and long-term toxicological evaluations are conducted to ensure clinical safety.
3. Dosage form development and route optimization: Based on their physicochemical properties, develop formulations suitable for oral or other administration routes to improve bioavailability.
4. Clinical trial design: Conduct early clinical trials to verify efficacy and safety in patients with cardiovascular diseases.

In addition, by combining the advantages of modern medicinal chemistry and natural product chemistry, and optimizing the pharmacodynamic and pharmacokinetic properties of Wang Bu Liuxing Flavonoid Glycoside E through structural modification and drug design, it is expected that new highly effective, low-toxicity cardiovascular protective drugs will be developed.

Conclusion

Wang Bu Liu Xing Flavonoid Glycoside E, derived from Wang Bu Liu Xing, is a natural C-flavonoid carboside derived from Wang Bu Liu Xing. Due to its unique chemical structure and significant cardiovascular protective activity, it has become a hot topic in natural product pharmacological research. Its multi-target mechanism of action and good safety profile provide new drug candidates for the prevention and treatment of cardiovascular diseases. Although research on its pharmacokinetics and clinical applications is still in its early stages, as research deepens, Wang Bu Liuxing Flavonoid Glycoside E is expected to become an important natural drug resource in the treatment of cardiovascular diseases. In the future, through multidisciplinary collaboration, promoting the transformation from basic research to clinical practice will greatly advance the application and development of natural products in modern medicine.