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℃
Macranthoside A is a natural triterpenoid glycoside derived from plants of the genus Macranthoside. In recent years, with the increasing importance of natural products in drug development, Lonicera japonica saponins A have received widespread attention due to their significant antibacterial and anti-inflammatory activities. Its unique chemical structure and multi-target mechanism of action demonstrate potential application value in the treatment research of inflammation related diseases. This article aims to provide a systematic review of the chemical structure and physicochemical properties, plant sources and extraction methods, pharmacological activity, mechanism of action, pharmacological evaluation, and clinical application prospects of Lonicera japonica saponins A. It is expected to provide theoretical basis and reference for the in-depth research and drug development of this compound.
Gray felt honeysuckle saponin A (CAS number: 128730-82-5) belongs to the triterpenoid glycoside class, with a molecular weight of 913.1080 and high molecular weight characteristics. Its structural core is a triterpenoid skeleton, which connects polysaccharide groups through glycosidic bonds to form a typical saponin structure. The LogP value of this molecule is 2.2565, indicating that it has moderate lipid solubility, which is beneficial for cell membrane penetration but not excessively hydrophobic. The polar surface area (TPSA) is 274.75 Å ², indicating that the molecule has strong polarity and hydrogen bonding ability, which may affect its bioavailability and pharmacokinetic properties. The water solubility is 0.1303, which belongs to low water solubility compounds, indicating that solubility improvement strategies need to 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 experiment showed a negative result, indicating a low risk of cardiac toxicity. The Ames mutagenicity test result is 0.0, indicating that its genetic toxicity risk is relatively low and has a good safety basis.
The saponin A of Lonicera macranthoeides is mainly distributed in plants of the Lonicera genus, which is widely used in traditional Chinese medicine and has the effects of clearing heat, detoxifying, anti-inflammatory, and relieving pain. As a secondary metabolite of this plant, saponins A from Lonicera japonica often exist in its roots, stems, and leaves.
In terms of extraction methods, organic solvent extraction combined with column chromatography separation technology is usually used. The specific process includes: first, reflux extraction is carried out using ethanol or methanol as the extraction agent. After concentration, the extraction solution is subjected to preliminary separation using silica gel column chromatography with water ethanol gradient elution. Subsequently, further purification was carried out by high-performance liquid chromatography (HPLC) to obtain high-purity Lonicera japonica saponins A. In recent years, the application of ultrasound assisted extraction and supercritical fluid extraction technology has also improved extraction efficiency and purity, reduced the use of organic solvents, and is in line with the concept of green chemistry.
The pharmacological activity research of Lonicera japonica saponins A mainly focuses on its antibacterial and anti-inflammatory effects. In vitro experiments have shown that the compound has significant inhibitory effects on various Gram positive and Gram negative bacteria, especially exhibiting low minimum inhibitory concentrations (MIC) against Staphylococcus aureus and Escherichia coli, indicating its potential as a natural antibacterial agent.
In terms of anti-inflammatory activity, Lonicera japonica saponins A can significantly inhibit the release of inflammatory mediators and the activation of inflammatory signaling pathways. Both in vivo and in vitro models have shown that it can alleviate inflammatory reactions, reduce tissue edema, and decrease inflammatory cell infiltration. Its anti-inflammatory effect is closely related to the regulation of multiple inflammation related targets, exhibiting the characteristics of multi-target and multi pathway synergistic effects.
In addition, saponin A from Lonicera japonica Thunb. also exhibits certain activities in oxidative stress and immune regulation, indicating its potential therapeutic value in various chronic inflammatory and immune related diseases.
The anti-inflammatory mechanism of Lonicera japonica saponins A involves multiple molecular targets and signaling pathways, mainly including:
IL-6/STAT3 signaling pathway
IL-6, as an important pro-inflammatory cytokine, promotes inflammatory response by activating the STAT3 signaling pathway. Gray felt honeysuckle saponin A can inhibit the expression of IL-6 and the phosphorylation of downstream STAT3, block the transmission of inflammatory signals, and alleviate inflammatory reactions.
NF - κ B signaling pathway
NFKB1 is a key member of the NF - κ B family, regulating the expression of various inflammatory genes. This compound exerts anti-inflammatory effects by inhibiting the activation of NFKB1 and reducing the expression of pro-inflammatory factors such as TNF - α, IL-6, and PTGS2 (COX-2).
Regulation of inflammation related enzymes
PTGS1 and PTGS2 encode COX-1 and COX-2, respectively, and are involved in the synthesis of prostaglandins, regulating inflammation and pain. Gray felt honeysuckle saponin A has inhibitory effects on these two enzymes, reducing the production of inflammatory mediators. In addition, inhibition of NOS2 (inducible nitric oxide synthase) reduces the production of nitric oxide at the site of inflammation, alleviating oxidative damage.
Inflammatory bodies and apoptosis related proteins
CASP1 (caspase-1) is involved in the activation of inflammasomes, promoting the maturation and release of pro-inflammatory cytokines. Gray felt honeysuckle saponin A can inhibit the activity of CASP1 and block the inflammatory response mediated by inflammasomes.
Adjustment of TRP channel
TRPV1 and TRPA1 are important ion channels for sensing pain and inflammatory stimuli. This compound regulates the activity of these two channels, reducing pain and neural sensitivity caused by inflammation.
In summary, the saponin A from Lonicera japonica var. mongolica exhibits excellent anti-inflammatory potential by synergistically regulating inflammatory responses through multiple targets and pathways.
The development of medicinal properties is a crucial step in the development of natural product drugs. The physicochemical properties of Lonicera japonica Hook. f. Hook. f. Hook. f. f. Hook. f. Hook. f. Hook. f. Hook. f. Hook. f. Hook. f. Hook. f. Hook. f. Hook. f. Hook. f. Hook. f. Hook. f. Hook. f. Hook. f. Hook. f. Hook. f. Hook. f. Hook. f. Hook. f. Hook. f. Hook. f. Hook. f. Hook. f. Its LogP value is moderate, which is beneficial for cell membrane penetration, but a high TPSA value indicates limited ability to penetrate the cell membrane. The blood-brain barrier has low permeability and is suitable for the treatment of peripheral inflammatory diseases, 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 cardiac toxicity. The Ames test has no mutagenicity and good safety. Combined with its anti-inflammatory activity, Lonicera japonica saponin A has a good safety basis.
Pharmacokinetic data is currently limited, but based on its structural characteristics, it is expected that its in vivo metabolism will mainly be through glycoside hydrolysis and triterpenoid skeleton modification by the liver enzyme system. Further in vivo pharmacokinetic studies are needed in the future to clarify its absorption, distribution, metabolism, and excretion (ADME) characteristics, providing a basis for dosage form optimization and clinical application.
Gray felt honeysuckle saponin A has broad clinical application prospects due to its significant antibacterial and anti-inflammatory activities. Its multi-target mechanism of action gives it potential advantages in treating various inflammatory related diseases such as rheumatoid arthritis, inflammatory bowel disease, and skin inflammation. In addition, its antibacterial activity provides a new natural drug candidate for anti infective therapy.
Future research should focus on the following aspects:
In depth mechanism research
By using multiple omics methods such as genomics, proteomics, and metabolomics, the molecular network of Lonicera japonica saponins A and its interaction with inflammation related signaling pathways were further revealed.
Pharmacokinetic and Toxicological Evaluation
Conduct in vivo pharmacokinetic studies to clarify its bioavailability, metabolic pathways, and excretion characteristics. Simultaneously conduct long-term toxicological evaluation to ensure its safety.
Formulation development and optimization of administration routes
To address the issues of low water solubility and oral bioavailability, new dosage forms such as nanoparticles, liposomes, or solid dispersions are developed to improve their in vivo stability and absorption efficiency.
Preclinical and clinical research
Design reasonable animal models and clinical trial protocols to verify their efficacy and safety, and promote their translation into clinical applications.
Combination therapy research
Explore the synergistic effect of Lonicera japonica saponins A and existing anti-inflammatory or antibacterial drugs to enhance therapeutic efficacy and reduce drug tolerance.
As a natural triterpenoid glycoside product with multi-target anti-inflammatory and antibacterial activities, Lonicera japonica saponins A from Lonicera japonica exhibit good pharmacological activity and safety characteristics. Its unique chemical structure and multiple mechanisms of action provide new ideas and drug candidates for the treatment of inflammation related diseases. Although its pharmacokinetics and clinical research are still in the preliminary stage, with the deepening of research, Lonicera japonica saponins A is expected to become an important breakthrough in the development of natural product drugs. In the future, the comprehensive application of modern medicinal chemistry, molecular biology, and pharmaceutical technology will promote its clinical translation and benefit more patients.
