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Storage conditions：Short-term storage at 2~8℃, long-term storage at -20 ~ -80℃
Diphyllin O-glucoside (CAS No.: 30021-77-3) is a natural compound with significant biological activity and belongs to the lignan class of compounds. In recent years, with the growing demand for bone metabolic diseases and antiviral drug development, scopin O-glucoside has gradually attracted widespread attention from the scientific community due to its unique pharmacological activity. This compound not only exhibits potent V-ATPase inhibitory effects (IC50=17 nM), but also effectively suppresses HIV-1 viral replication (IC50=0.38 μM), demonstrating its dual potential in antiviral and bone metabolism regulation. Especially in bone metabolism-related diseases, sanyloin O-glucoside effectively inhibits bone resorption by inhibiting osteoclast lysosomal acidification and bone resorption pit acidification (inhibiting acid inflow into IC50=0.6 nM), without significantly affecting osteoblast bone formation, indicating good application prospects in treating osteoporosis and other conditions.
This paper will systematically review the chemical structure and physicochemical properties of Gynophyllin O-glucoside, plant origin and extraction methods, pharmacological activity and mechanism of action, druggability evaluation, and clinical application prospects, aiming to provide comprehensive and in-depth reference materials for researchers in related fields.
Gynophyllin O-glucoside is a typical lignan glycoside compound with a molecular formula of C27H30O12 and a molecular weight of 542.4930. Its structural features include a core structure of gynophyllin connected to a glucose unit via an O-glycosidic bond. This structure gives it good water solubility and biological activity.
In terms of physicochemical properties, the LogP value of Gyosin O-glucoside is 1.0331, indicating moderate lipophilicity and beneficial oral absorption. Its topological polar surface area (TPSA) is 162.6 Ų, and its higher polarity helps bind molecules to biological macromolecule targets. The water solubility is 0.1709 mg/mL, indicating a certain solubility in water and facilitating formulation development. The blood-brain barrier has a relatively low penetration capacity, suggesting a lower risk of side effects in the central nervous system. The hERG channel inhibition test was negative, indicating a low risk of cardiotoxicity. The Ames test result was 0.9, indicating that this compound does not show significant mutagenicity.
In summary, the physicochemical properties of Yama Hehein O-glucoside are suitable for oral administration and have a solid safety foundation.
Phylleia O-glucoside is mainly found in various plants rich in lignans, especially in Diphylleia sinensis and its related species, with higher concentrations. In traditional Chinese medicinal materials, hibiscoid compounds are widely used in anti-inflammatory, analgesic, and bone metabolism regulation.
The extraction method typically uses ethanol or methanol as solvents for extraction and combines ultrasonic-assisted extraction technology to improve extraction efficiency. The extract undergoes concentration, liquid-liquid distribution, and multiple column chromatography purifications, and is finally separated and purified by high-performance liquid chromatography (HPLC) to obtain high-purity mountain leaf extract O-glucosides. In recent years, the application of supercritical CO2 extraction technology and membrane separation technology has also provided new ideas for the industrial extraction of this compound.
Optimization of the extraction process not only increases yield but also ensures the stability of the active ingredients of the compound, laying a foundation for subsequent pharmacological research and clinical applications.
Phyllin O-glucoside, as a highly effective V-ATPase inhibitor, plays a key role in regulating osteoclast function. V-ATPase is a key enzyme for osteoclast lysosomes and bone resorption pit acidification, regulating bone matrix dissolution and bone resorption processes. Gynophyllin O-glucoside effectively blocks acidification of osteoclasts and acid inflow into bone resorption depressions by inhibiting V-ATPase activity (IC50=17 nM), thereby suppressing bone resorption.
In vitro cell experiments showed that Gyan Ligin O-glucoside can significantly inhibit osteoclast-mediated bone resorption without affecting osteoblast bone formation, indicating its potential for selective regulation of bone metabolism. Animal model studies have also confirmed that this compound can slow the progression of osteoporosis and reduce levels of bone resorption markers.
Phyloside O-glucoside exhibited significant inhibitory effects against HIV-1 virus, with an IC50 of 0.38 μM. Its antiviral mechanism involves multiple targets, including various enzymes and receptors required for viral replication, such as HIV1-protease (HIV1-PR), integrase (INT), viral envelope glycoprotein gD, as well as CCR5 and CXCR4 receptors associated with viral entry. Through multi-target synergistic inhibition, Gyolein O-glucoside effectively blocks several key steps in the viral lifecycle.
In addition, Gynophyllin O-glucoside exhibits certain inhibitory activity against various viral proteins (such as UL42, UL54, ICP27, TK), indicating broad-spectrum antiviral potential. Its low cytotoxicity and good oral activity make it a promising candidate drug against HIV and other viral infections.
Gynosin O-glucoside directly binds to and inhibits the enzyme activity of V-ATPase, blocking proton pump function and causing acidification of osteoclast lysosomes and bone resorption depressions. This process inhibits the dissolution of bone matrix and the bone resorption function of osteoclasts, reducing bone loss. The specificity of this mechanism gives it a clear advantage in treating bone metabolic diseases, avoiding negative impacts on osteoblast bone formation.
Phyllin O-glucoside inhibits HIV-1 viral replication through multi-target action. Its targets include:
Through the synergistic action of multiple targets, Phyllin O-glucoside effectively reduces viral load and delays disease progression.
The druggability parameters of Gynophyllin O-glucoside indicate that it has promising potential for drug development. A molecular weight of 542.4930 is within a reasonable range, and a LogP value of 1.0331 indicates moderate lipid solubility, which is beneficial for oral absorption. A higher TPSA (162.6 Ų) suggests strong polarity, which may affect membrane permeability, but its water solubility (0.1709 mg/mL) aids formulation design.
The blood-brain barrier has low penetration capacity, reducing the risk of central nervous system side effects. The hERG channel was inhibited negatively and the Ames test showed no mutagenicity, further confirming its good safety.
Pharmacokinetics: Although current data are limited, studies have shown that oral saliphyllin O-glucoside has high bioavailability, stable metabolism in the body, and is mainly metabolized through the hepatic enzyme system, with excretion primarily via the kidneys. Further systematic pharmacokinetic and toxicological studies are needed in the future to support clinical development.
Phyllosin O-glucoside shows broad application prospects in both bone metabolic diseases and antiviral fields. In osteoporosis and diseases related to bone overabsorption (such as rheumatoid arthritis and bone metastases), it selectively inhibits osteoclast function without affecting osteoblasts, offering a new therapeutic strategy that is expected to overcome the side effects and resistance issues of existing anti-osteoresorption drugs such as bisphosphonates.
In the field of antiviral therapy, the multi-target ability of shanzifolin O-glucoside to inhibit HIV-1 viral replication provides a potential new drug candidate for antiretroviral therapy. Its oral efficacy and low toxicity make it suitable for long-term treatment. Moreover, its inhibitory effect on other viral proteins suggests potential value in broad-spectrum antiviral drug development.
In the future, it is necessary to strengthen preclinical pharmacokinetics, toxicology, and pharmacodynamic research on Phyllin O-glucoside, exploring its potential for combination use and formulation optimization. At the same time, based on its structural characteristics, structural modification and drug design are expected to yield more efficient and safer derivatives, driving their clinical translation.
Phyllin O-glucoside is a natural product with significant V-ATPase inhibitory activity and anti-HIV-1 viral activity, combining functions of bone metabolism regulation and antiviral activity. Its unique mechanism of action, good druggability, and safety provide new ideas and directions for the development of bone metabolic diseases and antiviral drugs. With further research, Gynophyllin O-glucoside is expected to become an important candidate for treating diseases such as osteoporosis and HIV infection. Future systematic research and clinical validation will further reveal its potential and drive it toward clinical application.
