Product name: Acanthoside B
Synonym name: Eleutheroside E1;(+)-Syringaresinol 4-O-β-D-glucoside,(+)-Syringaresinol 4'-O-β-D-glucoside
Catalogue No.: SBP00183
Cas No.: 7374-79-0
Formula: C₂₈H₃₆O₁₃
Mol Weight: 580.583
Botanical Source:
Physical Description: Powder
Type of Compound: Lignans

Purity: 95%~99%
Analysis Method: HPLC-DAD or/and HPLC-ELSD
Identification Method: Mass, NMR
Packing: Brown vial or HDPE plastic bottle
The product could be supplied from milligrams to grams. Inquire for bulk scale.
We provide solution to improve the water-solubility of compounds, thereby facilitating the variety of activity tests and clinic uses.

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

HPLC of Eleutheroside E1

NMR of Eleutheroside E1

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

Introduction/Overview

Eleutheroside E1 is a natural compound isolated from eleutherococcus senticosus and belongs to the glycoside class. As a traditional Chinese medicinal material, Siberian ginseng has been widely studied for its remarkable immunomodulatory and anti-fatigue effects. In recent years, with the deepening of natural drug research, eleutherococcin E1 has gradually become a research hotspot in the field of immune regulation due to its unique chemical structure and multi-target pharmacological activity. This compound not only shows potential in regulating immune system function but also demonstrates regulatory effects on various signaling pathways, especially closely related to key immune-related molecules such as TLR4, STAT3, and NFKB1. This paper aims to systematically review the chemical structure, origin, pharmacological activity, mechanism of action, and druggability evaluation of eleutherococcin E1, exploring its potential clinical value in immunoregulation-related diseases.

Chemical structure and physicochemical properties

The molecular formula of eleutherococcin E1 is C28H44O12, with a molecular weight of 580.5830 and CAS number 7374-79-0. Its chemical structure belongs to the glycoside class, containing multiple hydroxyl and glycosyl groups, giving it good water solubility (2.0719) and low lipid solubility (LogP 0.6293). The compound has a polar surface area (TPSA) as high as 174.99 Ų, indicating a rich concentration of polar groups, which may affect its biofilm permeability and distribution in vivo. Eleutherococcin E1 has low blood-brain barrier permeability, suggesting its role in the central nervous system is limited. Additionally, the hERG channel inhibition test results were negative, indicating a low risk of cardiotoxicity; The Ames test result was 0.0, indicating no significant mutagenicity and meeting safety requirements.

Chemically, eleutherococcin E1 contains a steroid backbone and glycoside components, is structurally stable, and is suitable for obtaining through various extraction and purification techniques. The presence of its polyhydroxyl groups provides a possible basis for binding to various protein targets and is one of the molecular foundations for its immunomodulatory effects.

Plant Origins and Extraction Methods

Eleutherococcus senticoccus (eleutherococcus senticosus), a plant of the Araliaceae family, is widely distributed in East Asia, especially in Northeast China, the Korean Peninsula, and the Russian Far East. As a traditional medicinal plant, Eleutherococcus senticosus contains various active ingredients in its roots, stems, and leaves, with glycoside compounds being among its main bioactive components.

Common methods for extracting eleutherococcin E1 include solvent extraction, ultrasound-assisted extraction, and high-performance liquid chromatography (HPLC) purification. Ethanol or methanol is generally used as extraction solvents, combined with aqueous phase extraction to improve the recovery rate of polar glycosides. After concentration, separation, and purification, the extract is identified and content determined using HPLC or liquid-mass spectrometry (LC-MS). In recent years, the application of supercritical fluid extraction and membrane separation technologies has improved extraction efficiency and purity, providing technical support for the large-scale preparation of eleutherococcin E1.

Pharmacological activity research

Acantherococcin E1 has demonstrated significant immunomodulatory activity in multiple in vivo and in vitro studies. Its main pharmacological effects focus on regulating immune cell function, suppressing inflammatory responses, and modulating immune signaling pathways.

1. Immune cell regulation
   Acantheroside E1 can promote T cell proliferation and activation, enhancing the phagocytic ability of natural killer cells (NK cells) and macrophages. Studies have shown that this compound can upregulate the expression of IL-2 and IFN-γ, promote cellular immune responses, and maintain immune homeostasis by modulating the balance of FOXP3-positive regulatory T cells (Tregs).

2. Anti-inflammatory effects
   Eleutherococcin E1 reduces the release of pro-inflammatory factors such as TNF-α and IL-6 by inhibiting the NFKB1 signaling pathway, thereby alleviating inflammatory responses. It has a significant inhibitory effect on TLR4-mediated inflammatory signals, indicating its potential application value in infectious and autoimmune diseases.

3. Antioxidant and cell protection
   This compound exhibits antioxidant activity, scavenging free radicals and reducing cellular damage caused by oxidative stress, thereby protecting immune cell function and tissue integrity.

4. Regulates cytokine networks
   Acantherococcin E1 regulates the expression of various cytokines such as TGFB1, IL10, and members of the STAT family, participating in the balance of immune tolerance and inflammatory responses.

Mechanism of action and molecular targets

The immunomodulatory effects of eleutherococcin E1 involve multiple signaling pathways and key molecular targets, with the specific mechanisms as follows:

1. TLR4 signaling pathway
   As an important receptor for innate immunity, TLR4 recognizes pathogen-related molecular patterns (PAMPs) and initiates downstream inflammatory signals. Eleutherococcin E1 inhibits TLR4 activation, blocks MyD88-dependent signaling, reduces NFKB1 nuclear translocation, and lowers pro-inflammatory cytokine expression, achieving anti-inflammatory effects.

2. STAT signaling pathway
   Eleutherococcin E1 regulates the activities of STAT3 and STAT4, affecting cytokine signaling. The regulation of STAT3 helps suppress inflammatory responses and promote immune tolerance, while STAT4 is involved in enhancing cellular immune responses. By regulating these two, eleutherococcin E1 achieves bidirectional regulation of the immune system.

3. Cytokine regulation
   Eleutherococcin E1 promotes the expression of IL2 and IFNG, enhancing T cell proliferation and effector functions. At the same time, upregulation of IL10 and TGFB1 helps with immunosuppression and tissue repair. Regulation of CTLA4 affects immune checkpoints and modulates immune activity.

4. Regulatory T cell (Treg) function
   By influencing FOXP3 expression, eleutherococcin E1 promotes the development and function of Treg cells, maintains immune tolerance, and prevents excessive activation of autoimmune responses.

In summary, Eleutherococcin E1 achieves fine regulation of the immune system through the synergistic action of multiple targets and pathways, demonstrating excellent immunomodulatory potential.

Druggability evaluation and pharmacokinetics

The druggability evaluation of eleutherococcin E1 indicates good safety and drug compatibility. Although the molecular weight of 580.5830 is slightly higher, its reasonable polarity and water solubility (2.0719) are beneficial for absorption in the body. A LogP value of 0.6293 indicates strong hydrophilicity, which may limit its ability to cross lipid membranes but aids in dissolution and distribution in the blood.

The low permeability of the blood-brain barrier suggests limited efficacy in the central nervous system, but this also reduces the risk of potential CNS toxicity. The hERG channel was inhibited negatively and the Ames test showed no mutagenicity, further confirming its safety.

Pharmacokinetics, existing research is limited, but it is speculated that its oral bioavailability is limited and may require improved formulations or combination administration to increase effective concentrations in vivo. Its metabolic pathway has not yet been systematically elucidated; it is expected to be mainly processed by hepatic metabolic enzyme systems, and the activity and safety of these metabolites require further research.

Prospects and outlooks for clinical applications

As a natural immunomodulator, eleutheroide E1 has broad clinical application potential. It regulates the immune system through multiple targets and is suitable for adjunctive treatment of various immune-related diseases, including autoimmune diseases, chronic inflammatory diseases, and states of immunodeficiency.

1. Autoimmune diseases
   By regulating Treg cells and suppressing inflammatory signals, eleutherococcin E1 holds promise for the treatment of autoimmune diseases such as rheumatoid arthritis and systemic lupus erythematosus, reducing immune-mediated tissue damage.

2. Infectious diseases
   Its inhibitory effect on TLR4 and NFKB1 helps control excessive inflammatory responses triggered by infections and reduces pathological progression of sepsis and inflammatory diseases.

3. Immune function regulation
   In immunocompromised patients, eleutherococcin E1 can enhance immune cell activity, improve resistance, and assist immune recovery in cancer patients and the elderly.

4. Potential for combination therapy
   Combined with modern immunotherapy strategies, eleutherococcin E1 can serve as an immunomodulatory adjuvant, enhancing the efficacy of immune checkpoint inhibitors and reducing side effects.

Future research should focus on optimizing its pharmacokinetics, developing dosage forms, and validating clinical trials to clarify its safe, effective dosage and indication ranges. In addition, in-depth analysis of its molecular mechanisms and metabolic product bioactivity will lay a solid foundation for its clinical translation.

Conclusion

As an important active ingredient in eleutherococcus, eleutherococcus E1 demonstrates broad medicinal value and development potential thanks to its unique chemical structure and multi-target immunomodulatory mechanism. Its good safety profile and remarkable immunomodulatory activity have made it a research hotspot in the field of natural product pharmacology. Although systematic research on its pharmacokinetics and clinical applications is still insufficient, with technological advances and deeper research, eleutheroide E1 is expected to become a new generation of natural immunomodulatory drugs, providing new ideas and means for the treatment of immune-related diseases. Future research should strengthen mechanistic analysis, dosage form optimization, and clinical validation to promote its transition from laboratory to clinical application, maximizing the medicinal value of natural products.