Product name: (25RS)-Ruscogenin
Synonym name:
Catalogue No.: BP4726
Cas No.: 874485-32-2
Formula: C₂₇H₄₂O₄
Mol Weight: 430.629
Botanical Source:
Type of Compound: Steroids

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

(25RS)-Ruscogenin is a steroidal saponin natural product with significant biological activity, widely found in plants of the genus Ruscus (Ruscus spp.). As an important active ingredient in traditional herbal medicine, (25RS)-ruscosenoglycosin has attracted increasing attention in recent years due to its diverse pharmacological activity, especially its potential in anti-inflammatory fields. Inflammatory responses play a key role in the pathogenesis of various diseases, and the development of natural products targeting inflammation-related targets has become one of the hotspots in new drug research. This paper systematically reviews the chemical structure and physicochemical properties of (25RS)-ruscosaponin, plant origin and extraction methods, pharmacological activity and mechanism of action, druggability evaluation, and pharmacokinetic characteristics, and explores its clinical application prospects and future research directions.

Chemical structure and physicochemical properties

The molecular formula of (25RS)-ruscosaponin is C27H42O4, with a molecular weight of 430.6290, and it belongs to the steroid saponin class compounds. Its structural core is a steroid skeleton, and the 25-position carbon atom exhibits an R/S configuration isomer, hence the name (25RS). The molecule contains multiple hydroxyl and ketone groups, giving it certain polar characteristics. In terms of physicochemical properties, the LogP value of (25RS)-ruscosaponin is 4.3260, indicating strong lipophilicity, which facilitates penetration of cell membranes and the blood-brain barrier (BBB). The TPSA (topological polarity surface area) is 58.92 Ų, indicating moderate polarity and helping to maintain bioavailability. Its extremely low water solubility (0.0011 mg/mL) suggests limited solubility in the aqueous phase, which may affect oral absorption. The hERG channel inhibition test was negative, indicating a low risk of cardiotoxicity; The Ames test result was 0, indicating no significant genotoxicity risk.

Plant Origins and Extraction Methods

(25RS)-Ruscus saponins are mainly derived from plants of the genus Ruscus, especially Ruscus aculeatus and Ruscus hypoglossum. Plants of this genus are widely used in traditional medicine in parts of Europe and Asia, mainly for treating varicose veins, hemorrhoids, and chronic venous insufficiency. During extraction, alcohol solvents (such as ethanol and methanol) are typically used for reflux or ultrasonic-assisted extraction of dried plant rhizomes, followed by purification of saponins through liquid-liquid partitioning and column chromatography. In recent years, the application of supercritical CO2 extraction and high-performance liquid chromatography (HPLC) purification technologies has improved extraction efficiency and purity, providing a high-quality sample foundation for subsequent pharmacological research.

Pharmacological activity research

The pharmacological activity of (25RS)-ruscosaponin is most prominent in its anti-inflammatory effect. Multiple in vitro and in vivo experiments have shown that this compound can significantly inhibit the release of inflammatory mediators and the activation of inflammatory signaling pathways. Specifically, it inhibits the expression of pro-inflammatory cytokines such as IL-6 and TNF-α, reducing damage to inflamed tissues. Additionally, (25RS)-ruscosaponin also shows potential in regulating immune responses, providing antioxidant effects, and protecting vascular endothelial function. Some studies have pointed out its application value in alleviating chronic inflammatory diseases, neuroinflammation, and metabolic syndrome-related inflammation. In animal models, (25RS)-ruscosaponin effectively alleviates inflammation symptoms either orally or by injection, confirming its good in vivo activity.

Mechanism of action and molecular targets

The anti-inflammatory mechanism of (25RS)-ruscosaponin involves multiple molecular targets and signaling pathways. Its main targets include:

• IL-6 (interleukin-6) :(25RS)-ruscosaponin can inhibit the expression and release of IL-6, weakening its mediated inflammatory cascade.
• STAT3 (Signal Transduction and Transcription Activator 3): Blocks the transcriptional activity of its pro-inflammatory gene by inhibiting STAT3 phosphorylation and nuclear translocation.
• CASP1 (Caspase 1): Inhibits CASP1 activity, reduces activation of inflammasomes, and lowers the maturation and release of inflammatory factors such as IL-1β.
• TRPV1 and TRPA1 (transient receptor potential channels): regulate these ion channels to reduce neuroinflammation and pain responses.
• PTGS1 and PTGS2 (cyclooxygenases 1 and 2): Downregulate cyclooxygenase expression, reduce prostaglandin synthesis, and relieve inflammation and pain.
• TNF (tumor necrosis factor): inhibits the production of TNF-α and reduces inflammatory responses.
• NOS2 (induced nitric oxide synthase): Reduces NOS2 expression and reduces excessive NO production related to inflammation.
• NFKB1 (nuclear factor κB subunit): blocks activation of the NF-κB signaling pathway and inhibits the expression of inflammatory genes.

The synergistic regulation of these targets enables (25RS)-ruscosaponin to exert anti-inflammatory effects across multiple levels and pathways, demonstrating its potential as a natural anti-inflammatory drug.

Druggability evaluation and pharmacokinetics

From a druggability perspective, (25RS)-ruscosaponin has high lipid solubility (LogP=4.3260), which facilitates cell membrane penetration and blood-brain barrier permeability, supporting its application in central nervous system inflammation. TPSA is moderate, meeting the requirements for drug molecule permeability to biofilms. Low water solubility suggests that oral formulation design should consider solubility enhancement strategies, such as nanoparticle carriers and solid dispersions. Negative hERG channel inhibition and Ames test negative results indicate high safety and low risks of cardiotoxicity and genotoxicity.

Pharmacokinetic studies show that (25RS)-ruscosaponin is absorbed orally quickly, plasma concentration peaks occur at moderate times, and it is widely distributed in tissues, especially with significant accumulation in liver, kidney, and brain tissues. Metabolic pathways are mainly modified by hepatic enzyme systems for hydroxylation and glycosylation, and the activity and toxicity of these metabolites require further research. Excretion is mainly via bile and urine, with a moderate half-life, supporting reasonable clinical dosing frequency design.

Prospects and outlooks for clinical applications

Due to its remarkable anti-inflammatory activity and good safety, (25RS)-ruscosaponin has broad clinical application prospects in chronic inflammatory diseases (such as rheumatoid arthritis and inflammatory bowel disease), neuroinflammation (such as Alzheimer's disease and Parkinson's disease), and vascular-related diseases (such as varicose veins and chronic venous insufficiency). Moreover, its ability to cross the blood-brain barrier opens up the possibility of developing novel treatments for central nervous system diseases.

Future research should focus on:

1. Optimizing formulation technology to improve water solubility and bioavailability.
2. In-depth analysis of the pharmacology and safety of metabolites.
3. Conduct systematic preclinical toxicology and pharmacodynamic evaluations.
4. Explore synergistic effects and combination strategies with other anti-inflammatory drugs.
5. Validating its efficacy and safety in specific diseases through clinical trials.

Conclusion

(25RS)-Rusco saponin, as a natural steroid saponin with multi-target anti-inflammatory activity, demonstrates excellent pharmacological activity and drug potential. Its unique chemical structure endows it with excellent biofilm penetration and safety profiles, making it a strong candidate for anti-inflammatory drug development. In the future, through multidisciplinary research and technological innovation, it is expected that (25RS)-ruscosaponin will be translated into clinical application, benefiting patients with inflammation-related diseases.