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Storage conditions：Short-term storage at 2~8℃, long-term storage at -20 ~ -80℃
197.7400
.0266
.0268
.5457
.5090
.4024
Low
79.5616
4.4560
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1.5
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Glycyroside (CAS No.: 125310-04-5) is a natural isoflavone disaccharide product isolated from the plant Glycyrrhiza eurycarpa P. C. Li in the genus Glycyrrhiza. As one of the components in the licorice family with a unique structure and bioactivity, licorice flavin has attracted widespread attention in recent years due to its remarkable pharmacological activity, especially its potential applications in the anti-ulcer field. Ulcerative diseases, as common digestive system disorders in clinical practice, have complex causes involving multiple mechanisms such as damage to the gastric mucosal barrier, abnormal gastric acid secretion, and inflammatory responses. Although traditional therapeutic drugs are effective, they often come with certain side effects. Natural products, due to their structural diversity and biological activity, have become important resources for new drug development. This paper will systematically review the chemical structure and physicochemical properties of licorice glucoside, plant origin and extraction methods, pharmacological activity and mechanism of action, druggability evaluation, and pharmacokinetic characteristics, and explore its clinical application prospects and future research directions.
Alicolitizin glycyrrhizin is an isoflavone disaccharide glycoside with a molecular formula of C27H30O13 and a molecular weight of 562.5240. Its structural features include a core isoflavone structure connected to two glycosidic groups via glycosidic bonds, giving it high polarity and water solubility. The LogP value is 0.0266, indicating strong hydrophilicity, and water solubility is 0.5457, suitable for dissolution and absorption in aqueous media. The total polar surface area (TPSA) is 197.7400 Ų, with a larger polar surface area typically associated with lower membrane permeability. Low blood-brain barrier permeability suggests limited distribution in the central nervous system, which may reduce the risk of central nervous system side effects. The hERG inhibition test results were negative, indicating that aligcyrrhizin has a weak inhibitory effect on cardiac potassium channels and carries a lower risk of cardiotoxicity. The Ames test value was 1.5, indicating a low genotoxicity risk and meeting safety requirements.
Licorice glycyrrhizin mainly comes from the licorice genus Glycyrrhiza eurycarpa P. C. LI, which is widely used in traditional Chinese medicine and has effects of harmonizing various herbs and relieving gastrointestinal discomfort. The rhizome part of plants is the main accumulation site for alagrithizizi glycyprizin. The extraction method typically uses a mixed solvent of alcohols (such as ethanol, methanol) and water for extraction extraction, combined with ultrasound-assisted extraction or reflux extraction techniques to improve extraction efficiency. The extract undergoes concentration, liquid-liquid separation, and column chromatography purification to obtain high-purity alicolityrin. Modern separation technologies such as high-performance liquid chromatography (HPLC) and mass spectrometry (LC-MS) are widely used for qualitative and quantitative analysis to ensure the quality and purity of extracts.
Pharmacological activity studies of licorice mainly focus on its anti-ulcer effect. Experimental models include alcohol-induced gastric mucosal injury, rat stress ulcers, and nonsteroidal anti-inflammatory drug (NSAID) induced gastric ulcer models. Research shows that glycyrrhizin can significantly reduce gastric mucosal injury, promote ulcer healing, and demonstrate good protective effects on the gastric mucosa. In addition, aliconicidin has anti-inflammatory, antioxidant, and gastrointestinal hormone secretion functions, which synergistically promote mucosal repair and functional recovery. Its anti-inflammatory effect mainly works by inhibiting prostaglandin synthasetypes PTGS1 and PTGS2, thereby reducing the generation of inflammatory mediators. Licorice regulates the gastric mucus-related protein MUC5AC, helping to strengthen the gastric mucosal barrier function. Relevant in vitro cell experiments and animal models have confirmed its good safety and efficacy.
The anti-ulcer effect of licocyrrhizin involves multi-target and multi-pathway regulation. The main targets include:
Overall, licocyrrhizin in fantraginate exerts its anti-ulcer effect through multiple mechanisms: anti-inflammation, protecting the gastric mucosal barrier, regulating gastric acid secretion, and promoting tissue repair.
Druggability evaluation of licorice showed good safety and drug properties. The molecular weight is 562.5240, slightly above the ideal range for traditional small molecule drugs, but its low LogP and high TPSA indicate good water solubility, making it suitable for oral formulation development. Low blood-brain barrier permeability, reducing central toxic risk. hERG channel inhibits negative effects, reducing the risk of cardiotoxicity. Ames test results show low genotoxicity and high safety.
Pharmacokinetics, due to glycocyrrhizin containing glycosyls in its structure, it may release active isoflavones in the gastrointestinal tract through enzymatic hydrolysis, affecting its bioavailability. It has good water solubility, which is beneficial for gastrointestinal absorption, but its large polar surface area may limit its cell membrane permeability, affecting its distribution in the body. The metabolic pathway of the liver is not yet fully understood, but it is presumed to be mainly metabolized through corresponding glycosidases and oxidases. Key pharmacokinetic parameters such as in vivo half-life and clearance rate still require further systematic research.
Given the significant activity of aliconithizizi glycosides in anti-ulcer and gastrointestinal protection, it holds great potential as a candidate molecule for novel anti-ulcer drugs. Currently, clinical treatment of gastric ulcers mainly relies on proton pump inhibitors (PPIs) and H2 receptor antagonists, but long-term use raises issues of drug tolerance and side effects. With its advantages in multiple targets and mechanisms, alatin glycyrrhizin is expected to become a safe and effective alternative or adjunctive therapy.
Future research should focus on its pharmacokinetic characteristics, formulation optimization, and clinical safety evaluation. At the same time, by integrating modern drug design technologies and using structural modifications to enhance bioavailability and targetability, oral sustained-release or gastric mucosa-targeted formulations are being developed. In addition, the potential role of licocyrrhizin in other gastrointestinal diseases such as gastritis and enteritis is also worth further exploration. The implementation of multicenter clinical trials will be key to driving their clinical translation.
Licocyrrhizin glycyrrhiz, a type of isoflavone disaccharide derived from Glycyrrhiza eurycarpa, demonstrates significant pharmacological activity and multi-target mechanism in the anti-ulcer field due to its unique chemical structure and excellent physicochemical properties. Its excellent safety and druggability provide a solid foundation for new drug development. In the future, through in-depth pharmacokinetic research and clinical validation, alatin glycyrrhizin is expected to become an important natural drug resource in the treatment of gastrointestinal diseases. Ongoing basic and clinical research will drive it from the laboratory to clinical applications, benefiting a wide range of patients.
Shenshuai
Wenjing
Hedandan
