+86-28-82633987
Product name: Schaftoside
Synonym name:
Catalogue No.: BP1260
Cas No.: 51938-32-0
Formula: C26H28O14
Mol Weight: 564.496
Botanical Source: Desmodii styracifolii herba
Physical Description:
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
The product could be supplied from milligrams to grams
Inquire for bulk scale.
Description:
Schaftoside has antioxidant activity, it also can inhibit phospholipase, lipoxygenase and cyclooxygenase, three pro-inflammatory enzymes.
References:
J Chromatogr B Analyt Technol Biomed Life Sci. 2013 Aug 1;932:66-73.
Simultaneous determination of four flavonoids and one phenolic acid in rat plasma by LC-MS/MS and its application to a pharmacokinetic study after oral administration of the Herba Desmodii Styracifolii extract
METHODS AND RESULTS:
A sensitive and selective liquid chromatography and tandem mass spectrometry (LC-MS/MS) method was developed and validated for the simultaneous determination of four flavonoids (Schaftoside, isovitexin, luteolin, and apigenin) and one phenolic acid (ferulic acid) in rat plasma using sulfamethoxazole as the internal standard (IS). The separation was performed using a Diamonsil C18 column, which was eluted with methanol (A) and 0.1‰ acetic acid (B). The gradient condition was as follows: 0-5min, 40-60% A; 5-6min, 60-95% A; and 6-10min, maintained at 95% A. The analytes were detected using a hybrid quadrupole linear ion trap mass spectrometer that was equipped with an electrospray ionization source in the negative ion and multiple-reaction monitoring modes. A full validation of the method was performed. The linearity of the analytical response was good, with correlation coefficients greater than 0.9925 for all of the compounds within the concentration range. The lower limits of quantitation (LLOQ) of Schaftoside, isovitexin, luteolin, apigenin, and ferulic acid in rat plasma were 1.66, 0.84, 3.69, 1.70, and 3.91ng/mL, respectively. The intra-day and inter-day precisions of the investigated components exhibited an RSD within 13.20%, and the accuracy (RE%) ranged from -8.47% to 10.90%.
CONCLUSIONS:
The results indicated that the developed method is sufficiently reliable for the pharmacokinetic study of Schaftoside, isovitexin, apigenin, luteolin, and ferulic acid in rats following oral administration of the Herba Desmodii Styracifolii extract.
Zuckerindustrie Sugar Industry, 2015, 140(10):632-639.
An HPLC-DPPH method for antioxidant activity from sugarcane molasses.
Sugarcane molasses is potentially rich in health-promoting phenolic compounds. Present study was designed to optimize experimental conditions for ultrasonic-assisted extraction of antioxidant compounds from sugarcane molasses using response surface methodology.
METHODS AND RESULTS:
An HPLCDPPH method for simultaneous determination of antioxidant activity was also developed. Ethanol concentration 80-84% (v/v), temperature 58-59 degrees C, and 47-50 min time duration were the most favorable conditions. In these conditions, the optimal experimental results were total phenolic content 18 mg gallic acid equivalents/g, with DPPH free radical scavenging ability of 92%, which was same as the predicted values by RSM model. Catechin, vanillic acid, isorhamnetin-3-O-glucoside, eugenol, Schaftoside, diosmetin-7-O-beta-D-glucopyranoside, ferulic acid, and caffeoylquinic acid were identified using HPLC-MS/MS. Among the antioxidant compounds, Schaftoside was the most abundant antioxidant (92.081 mu g/g dry substance), while ferulic acid exhibited the highest antioxidant activity.
CONCLUSIONS:
These results suggest that HPLC-DPPH method is more specific, accurate and less time consuming and can sever as a quality control tool.
HPLC of Schaftoside
Storage conditions：Short-term storage at 2~8℃, long-term storage at -20 ~ -80℃
250.9700
-.7354
-.8227
1.8667
.5349
.1989
Low
75.6829
4.7667
Yes
No
No
No
Yes
No
0.6
Yes
No
Yes
No
Schaftoside (CAS No.: 51938-32-0) is a natural flavonoid compound widely found in various Chinese medicinal herbs, especially abundant in the grass plant Eleusine indica. As a bioactive flavonoid glycoside, xiafotaside has attracted widespread attention in pharmacology and natural product chemistry in recent years due to its diverse pharmacological activities. Its main manifestations include antioxidant, anti-inflammatory, and mitochondrial function regulation, with significant potential in inhibiting the TLR4/MyD88 signaling pathway and modulating mitochondrial dynamics. This paper aims to systematically review the chemical structure, plant origin, extraction methods, pharmacological activity, mechanism of action, druggability evaluation, and clinical application prospects of xiafotaside, aiming to provide a theoretical basis and research direction for its subsequent drug development and clinical translation.
Xiafotaside belongs to the flanon-glycoside class of compounds with a molecular formula of C27H30O14 and a molecular weight of 564.4960. Its structural feature is that the flavonoid nucleus is connected to multiple glycoside groups via glycosidic bonds, specifically the C-6 and C-8 positions of the flavonoid are attached to glucose and arabinose residues, forming a disaccharide structure. This structure gives xiafotaside good water solubility (1.8667, unit unknown), but its lipid solubility is relatively low, with a LogP value of -0.7354, indicating some hydrophilicity. The topological polar surface area (TPSA) was 250.97 Ų, indicating high molecular polarity, which may affect membrane permeability and bioavailability.
Xiafotaside has good chemical stability, is not easily oxidized and degraded, and does not significantly inhibit hERG channels. The Ames mutagenic test result was 0.6, indicating a low genotoxicity risk. Multiple hydroxyl and sugar groups in its molecular structure provide the basis for its antioxidant activity, while also limiting its ability to cross the blood-brain barrier (which has low permeability).
Xiafotoside is mainly found in various traditional Chinese medicinal materials, especially in the gramine plant Eleusine indica (foxtail grass), which is found in higher concentrations. In addition, some other plants containing flavonoid glycosides, such as licorice and scutellaria baicalensis, have also been reported to contain this compound. As a common weed plant, Eleusine indica is used in traditional Chinese medicine for purposes such as clearing heat, detoxifying, and stopping bleeding. Research on its active ingredients provides scientific evidence for its pharmacological effects.
The extraction of xiafotaside typically uses ethanol or methanol as solvents, and crude extracts are obtained through reflux extraction or ultrasound-assisted extraction techniques. Subsequently, high-purity xiafota glycoside is obtained through liquid-liquid separation, column chromatography (such as silica gel columns, reversed-phase C18 columns), and high-performance liquid chromatography (HPLC). In recent years, supercritical CO2 extraction and membrane separation technologies have also been attempted to extract xiafotaside to improve yield and purity.
Optimization of extraction processes mainly focuses on regulating parameters such as solvent polarity, extraction time, temperature, and pH to maximize retention of the active components of xiafotaside and reduce impurity interference. At the same time, identification methods often use mass spectrometry (MS), nuclear magnetic resonance imaging (NMR), and UV-visible spectroscopy (UV-Vis) to ensure the accuracy of compound structures.
Xiafotaside demonstrates remarkable antioxidant capacity, effectively scavenging free radicals and reducing cellular damage caused by oxidative stress. Its mechanism of action mainly involves activating the intracellular antioxidant enzyme system, including superoxide dismutase (SOD1, SOD2), catalase peroxide (CAT), glutathione peroxidase (GPX1), and heme oxygenase 1 (HMOX1), which enhance the expression and activity of key enzymes. Additionally, xiafotaside promotes the nuclear translocation of nuclear factor E2-related factor 2 (NFE2L2/NRF2), activates antioxidant response elements (ARE), and enhances cellular defenses against oxidative damage.
Shafotaside demonstrates activity in suppressing inflammatory responses across various inflammation models. It primarily targets Toll-like receptor 4 (TLR4) and its downstream aperture protein MyD88, blocking the transmission of inflammatory signals and reducing the release of pro-inflammatory cytokines such as TNF-α, IL-6, and IL-1β, thereby alleviating inflammatory responses. This action has potential therapeutic value for chronic inflammatory diseases such as rheumatoid arthritis and inflammatory bowel disease.
Mitochondrial dynamic imbalance is an important mechanism for the occurrence and development of various diseases. Xiafotaside can reduce the expression and phosphorylation levels of mitochondrial cleavage protein Drp1, inhibit excessive mitochondrial division, and maintain the integrity and functional stability of the mitochondrial network. By regulating mitochondrial morphology, xiafotaside helps reduce mitochondria-mediated apoptosis and oxidative damage, protecting cell vitality.
Some studies have also found that xiafotaside has potential activities such as antitumor, antibacterial, and neuroprotective effects, but the related mechanisms have not been fully elucidated and require further in-depth study.
The multiple pharmacological effects of xiafotaside are attributed to its regulation of key molecular targets, mainly involving the following aspects:
TLR4/MyD88 signal pathway suppression
TLR4, as an important receptor in the innate immune system, mediates the initiation of inflammatory responses. Savota glycoside inhibits TLR4 expression and its downstream apter protein MyD88, blocking activation of inflammatory signaling pathways such as NF-κB, reducing the production of pro-inflammatory factors, and exerting anti-inflammatory effects.
NFE2L2/NRF2 pathway activation
Savoltaside promotes NFE2L2 nuclear translocation, activates ARE-driven antioxidant gene expression, enhances cellular antioxidant defense, and protects cells from oxidative stress damage.
Mitochondrial dynamics regulation
By reducing Drp1 expression and phosphorylation levels, xiafotaside inhibits excessive mitochondrial division, maintains the stability of the mitochondrial network, and prevents mitochondrial dysfunction and apoptosis.
Regulation of the antioxidant enzyme system
It enhances the expression and activity of antioxidant enzymes such as SOD1, SOD2, CAT, GPX1, and HMOX1, enhancing the cell's ability to clear reactive oxygen species (ROS).
The synergistic effect of these mechanisms enables xiafotaside to demonstrate good pharmacological activity in antioxidant, anti-inflammatory, and cell protection, providing a theoretical basis for its role as a natural drug candidate.
The druggability evaluation of xiavoltaside shows certain advantages and challenges:
Molecular weight and polarity
The molecular weight is 564.5, which is relatively large, and the TPSA value reaches as high as 250.97 Ų, indicating strong polarity, which may limit oral absorption and cell membrane permeability.
Lipophilic and water-soluble
LogP was -0.7354, indicating strong hydrophilicity and good water solubility (1.8667), which is beneficial for solubility issues in formulation development, but may affect the bioavailability related to lipid solubility.
Blood-brain barrier penetration
The prediction is low, indicating that xiafotaside struggles to cross the blood-brain barrier, limiting its use in central nervous system diseases.
Security
hERG channel inhibition test was negative, reducing the risk of cardiotoxicity; The Ames test result was 0.6, indicating a low genotoxicity risk and good safety.
Pharmacokinetics
Currently, data on the absorption, distribution, metabolism, and excretion (ADME) of xiafotaside in vivo are limited. Due to its high polarity, oral bioavailability may be limited, resulting in lower intestinal absorption. Metabolic pathways may involve hepatic glycoside hydrolysis and corresponding flavonoid metabolism; the activity and safety of these metabolites require further research.
In summary, xiafotaside has certain drug development potential, but its pharmacokinetic properties need to be optimized through structural modification or drug delivery systems to improve bioavailability and targeting.
Based on the antioxidant, anti-inflammatory, and mitochondrial protective effects of xiafota, its potential applications in various diseases have broad prospects:
Chronic inflammatory diseases
For conditions such as rheumatoid arthritis and inflammatory bowel disease, xiafotaside can reduce inflammatory responses by inhibiting the TLR4/MyD88 signaling pathway, making it a potential candidate for natural anti-inflammatory drugs.
Oxidative stress-related diseases
Including cardiovascular diseases, diabetes, and neurodegenerative diseases, xiafotaside activates the NRF2 pathway, enhancing cellular antioxidant capacity and potentially slowing disease progression.
Mitochondrial dysfunction diseases
For neurological diseases like Parkinson's and Alzheimer's, xiafotaside has potential neuroprotective effects by regulating mitochondrial dynamics and protecting nerve cells.
Anti-tumor adjuvant therapy
Preliminary studies suggest that xiafotaside may participate in tumor suppression by regulating apoptosis and oxidative stress, but the specific mechanism and clinical value still require further validation.
Future research should focus on pharmacokinetic optimization, formulation development, and preclinical safety evaluation of xiafotaside. At the same time, combining modern molecular biology techniques, the mechanism of action is deeply analyzed to expand its range of indications. The implementation of multicenter clinical trials will be a key step in verifying their clinical application value.
As a natural flavonoid glycoside with multiple biological activities, xiafotaside demonstrates broad drug development potential due to its remarkable antioxidant, anti-inflammatory, and mitochondrial protective effects. Its unique molecular structure and mechanism of action provide an important example for pharmacological research of natural products. Although there are still certain challenges in pharmacokinetics and clinical translation, through structural optimization and the assistance of modern drug delivery technologies, xiafotaside is expected to become an important candidate for future natural drug development. Systematic and in-depth basic research and clinical validation will lay a solid foundation for its clinical application, promoting the widespread use of natural products in modern medicine.
Shenshuai
Wenjing
Hedandan
