Synonym name: Macranthoside A; Kalopanaxsaponin H
Catalogue No.: BP0827
Cas No.: 128730-82-5
Formula: C₄₇H₇₆O₁₇
Mol Weight: 913.108
Botanical Source: Kalopanax semptemlobus, Aralia elata and Lonicera macranthoides

Purity: 95%~99%
Analysis Method: HPLC-DAD or/and HPLC-ELSD
Identification Method: Mass, NMR
Packing: Brown vial or HDPE plastic bottle
Can be supplied from milligrams to grams.

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

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

Introduction/Overview

Macranthoside A is a triterpene glycoside natural product derived from plants of the genus Macranthoside. In recent years, as the importance of natural products in drug development has become increasingly prominent, the saponin in Cyprinia cylindrium has attracted widespread attention due to its remarkable antibacterial and anti-inflammatory activities. Its unique chemical structure and multi-target mechanism of action give it potential application value in the treatment of inflammation-related diseases. This paper aims to systematically review the chemical structure and physicochemical properties, plant origin and extraction methods, pharmacological activity, mechanism of action, druggability evaluation, and clinical application prospects of Rhynchospora pseudosaponin, aiming to provide theoretical basis and reference for further research and drug development of this compound.

Chemical structure and physicochemical properties

Honeysherium pseudosaponin A (CAS No.: 128730-82-5) belongs to the triterpene glycoside class, with a molecular weight of 913.1080, indicating a relatively high molecular weight characteristic. Its structural core is the triterpene skeleton, which connects polysaccharide groups via glycosidic bonds, forming a typical saponin structure. The molecule's LogP value is 2.2565, indicating moderate lipid solubility, which facilitates membrane penetration without becoming overly hydrophobic. The polar surface area (TPSA) is 274.75 Ų, indicating that its molecules possess strong polarity and hydrogen bond formation, which may affect their bioavailability and pharmacokinetic properties. Water solubility is 0.1303, making it a low-soluble compound, suggesting that solubility improvement strategies should be considered in drug formulation design. The low permeability of the blood-brain barrier suggests that its main target may be limited to peripheral tissues. The hERG channel inhibition test was negative, indicating a low risk of cardiotoxicity. The Ames-induced mutagenic test result was 0.0, indicating a low genotoxicity risk and a solid safety foundation.

Plant Origins and Extraction Methods

Lonicera macranthoides are mainly distributed among plants of the genus Lonicera macranthoides, which are widely used in traditional Chinese medicinal materials and have effects of clearing heat, detoxifying, anti-inflammation, and relieving pain. Honeysenoside methyl Cylindrium is a secondary metabolite of this plant and is commonly found in its roots, stems, and leaves.

In terms of extraction methods, organic solvent extraction combined with column chromatography separation is commonly used. The specific process includes: first, reflux extraction using ethanol or methanol as the extractant. After concentration of the extract, preliminary separation is performed by silica gel column chromatography with water-ethanol gradient elution. Further purification was performed by high-performance liquid chromatography (HPLC), ultimately yielding high-purity liquentifer subsaponin methyl in Honeyscapula. In recent years, the application of ultrasound-assisted extraction and supercritical fluid extraction technologies has also improved extraction efficiency and purity, reducing the use of organic solvents, and aligning with the concept of green chemistry.

Pharmacological activity research

Pharmacological activity studies of Honeysenoside Methyl Cylindrium scutellaria mainly focus on its antibacterial and anti-inflammatory effects. In vitro experiments showed that this compound had significant inhibitory effects on various Gram-positive and Gram-negative bacteria, especially showing a low minimum inhibitory concentration (MIC) against Staphylococcus aureus and Escherichia coli, suggesting its potential as a natural antimicrobial.

In terms of anti-inflammatory activity, Honeysenoside methyl scutellaria can significantly inhibit the release of inflammatory mediators and activate inflammatory signaling pathways. Both in vivo and in vitro models show that it can reduce inflammatory responses, reduce tissue edema, and reduce inflammatory cell infiltration. Its anti-inflammatory effect is closely related to the regulation of multiple inflammation-related targets, exhibiting synergistic effects across multiple targets and pathways.

In addition, Honeysenoside methyl mitifolia also shows certain activity in oxidative stress and immune regulation, suggesting potential therapeutic value in various chronic inflammatory and immune-related diseases.

Mechanism of action and molecular targets

The anti-inflammatory mechanism of Honeysherylium hyposaponin A involves multiple molecular targets and signaling pathways, mainly including:

1. IL-6/STAT3 signaling pathway
   IL-6, as an important pro-inflammatory cytokine, promotes inflammatory responses by activating the STAT3 signaling pathway. Honeysenoside methyl can inhibit IL-6 expression and phosphorylation of downstream STAT3, blocking inflammatory signal transmission and reducing inflammatory responses.

2. NF-κB signaling pathway
   NFKB1 is a key member of the NF-κB family, regulating the expression of various inflammatory genes. This compound exerts anti-inflammatory effects by inhibiting NFKB1 activation and reducing the expression of pro-inflammatory factors such as TNF-α, IL-6, and PTGS2 (COX-2).

3. Regulation of inflammation-related enzymes
   PTGS1 and PTGS2 encode COX-1 and COX-2, respectively, and are involved in prostaglandin synthesis, regulating inflammation and pain. Honeystenin methyl mitoseutin inhibits both enzymes, reducing the production of inflammatory mediators. Additionally, inhibition of NOS2 (induced nitric oxide synthase) reduces nitric oxide production at the site of inflammation, alleviating oxidative damage.

4. Inflammasome and apoptosis-related proteins
   CASP1 (caspase 1) participates in the activation of inflammasomes, promoting the maturation and release of pro-inflammatory cytokines. Honeysenoside methyl can inhibit CASP1 activity and block inflammatory responses mediated by inflammasomes.

5. Regulation of TRP channels
   TRPV1 and TRPA1 are important ion channels for sensing pain and inflammatory stimuli. This compound modulates the activity of both channels, reducing pain and nerve sensitivity caused by inflammation.

In summary, Honeysherium subsaponin A demonstrates good anti-inflammatory potential by coordinating inflammatory responses through multiple targets and pathways.

Druggability evaluation and pharmacokinetics

Druggability is a key link in the development of natural product drugs. The physicochemical properties of Honeysenoside Methyl Cypriss susenin show that it has a large molecular weight, strong polarity, and low water solubility, which may affect its oral bioavailability. Its LogP value is moderate, which is favorable for cell membrane penetration, but a high TPSA value suggests limited membrane penetration ability. The blood-brain barrier has low permeability, making it suitable for treating peripheral inflammatory diseases and reducing the risk of central nervous system side effects.

In terms of safety, the hERG channel inhibition test was negative, indicating a low risk of cardiotoxicity. The Ames test is non-mutagenic and has good safety. Combined with its anti-inflammatory activity, Honeysheria Cyprinia hyposaponin has a solid safety foundation.

Pharmacokinetic data are currently limited, but based on its structural characteristics, its metabolism in vivo is expected to mainly be carried out by glycoside hydrolysis through hepatic enzyme systems and modification of the triterpene skeleton. In the future, further in vivo pharmacokinetic studies are needed to clarify its absorption, distribution, metabolism, and excretion (ADME) characteristics, providing a basis for formulation optimization and clinical application.

Prospects and outlooks for clinical applications

With its remarkable antibacterial and anti-inflammatory activities, Honeysenoside A has broad clinical application prospects. Its multi-target mechanism gives it potential advantages in treating various inflammation-related diseases such as rheumatoid arthritis, inflammatory bowel disease, and skin inflammation. Moreover, its antibacterial activity provides a new natural drug candidate for anti-infective treatment.

Future research should focus on the following areas:

1. In-depth mechanism research
   Through multi-omics approaches such as genomics, proteomics, and metabolomics, the molecular network of action of Cylindrium nisthogenin Acetosa and its interactions with inflammation-related signaling pathways were further revealed.

2. Pharmacokinetics and toxicology assessment
   Systematic in vivo pharmacokinetic studies are conducted to clarify bioavailability, metabolic pathways, and excretion characteristics. At the same time, long-term toxicological evaluations are conducted to ensure safety.

3. Dosage form development and drug delivery route optimization
   To address its low water solubility and oral bioavailability, new formulations such as nanoparticles, liposomes, or solid dispersions are developed to improve in vivo stability and absorption efficiency.

4. Preclinical and clinical research
   Design reasonable animal models and clinical trial protocols to verify efficacy and safety, promoting their translation into clinical application.

5. Combination drug studies
   Explore the synergistic effects of Honeystenin subsaponin in Rycepha and existing anti-inflammatory or antibacterial drugs to enhance treatment outcomes and reduce drug tolerance.

Conclusion

As a triterpene glycoside natural product with multi-target anti-inflammatory and antibacterial activities, it demonstrates excellent pharmacological activity and safety profile. Its unique chemical structure and multiple mechanisms of action offer new ideas and drug candidates for the treatment of inflammation-related diseases. Although pharmacokinetics and clinical research on it are still in the early stages, as research progresses, Honeysenoside Methyl Gray is expected to become an important breakthrough in the development of natural product drugs. In the future, integrating modern medicinal chemistry, molecular biology, and pharmaceutical technologies will promote clinical application and benefit more patients.