+86-28-82633987
Storage conditions：Short-term storage at 2~8℃, long-term storage at -20 ~ -80℃
240.3600
1.1515
1.1368
.1963
.5300
.1364
Low
88.0921
4.9752
No
No
No
No
No
No
0.0
Yes
Yes
Yes
Yes
Licorice (Glycyrrhiza uralensis), as an important component of traditional Chinese medicine, has long attracted attention in pharmacology and natural product chemistry due to its abundant active ingredients and diverse pharmacological effects. Licorice glycoside C2 (CAS No.: 202657-55-4) is an oleano-type triterpene oligosaccharide isolated from licorice, and has become a research hotspot in recent years due to its remarkable biological activity. Glycyrrhizin C2 not only inherits the traditional pharmacological effects of licorice extracts, such as antiviral, antimicrobial, antioxidant, and anti-inflammatory properties, but also demonstrates significant therapeutic potential for gastrointestinal diseases, especially gastric ulcers. This paper aims to systematically review the chemical structure and physicochemical properties of glycyrrhizin C2, plant origin and extraction methods, pharmacological activity, mechanism of action and molecular targets, druggability evaluation, and pharmacokinetic characteristics, and finally to look ahead to its clinical application prospects.
Glycyrrhizin C2 belongs to the oleano-type triterpenoid saponin compound, with a molecular weight of 726.6840. Structurally, it is formed by the oleano-type triterpene parent nucleus and multiple sugar groups connected by glycosidic bonds. Its LogP value is 1.1515, indicating moderate lipid solubility, which facilitates membrane penetration without being overly hydrophobic. The total polar surface area (TPSA) reaches as high as 240.3600, indicating strong molecular polarity, which is closely related to its polysaccharide structure. Water solubility is 0.1963, indicating a certain solubility in water and suitable for solvent systems for oral administration. Glycyrrhizin C2 has relatively low blood-brain barrier permeability, indicating that it mainly acts on peripheral targets to reduce the risk of central nervous system toxicity. Additionally, the hERG channel inhibition test was negative, indicating a low risk of cardiotoxicity, while the Ames mutagenic test result was 0.0, indicating no significant genotoxicity.
Glycyrrhiza glycyrrhiza C2 is mainly extracted from the roots and rhizomes of licorice (Glycyrrhiza uralensis). Licorice is a leguminous plant widely distributed in northern China and Central Asia. Traditional extraction methods mostly use reflux extraction with water or ethanol as solvent, followed by multi-stage separation and purification processes to obtain the target components. Modern extraction technologies include ultrasound-assisted extraction, microwave-assisted extraction, and high-performance liquid chromatography (HPLC) separation and purification, greatly improving the extraction efficiency and purity of glycyrrhizin C2. The typical steps are: after licorice is dried and crushed, extraction is performed by reflux extraction with 70% ethanol, concentration is performed by liquid-liquid extraction to remove impurities, followed by silica gel column chromatography or reversed-phase HPLC separation to obtain high-purity glycyrrhizin C2. This method not only ensures the structural integrity of the compound but is also suitable for large-scale production.
Pharmacological activity studies of glycyrrhizin C2 mainly focus on its anti-ulcer, anti-inflammatory, antiviral, and antioxidant properties. Numerous in vivo and in vitro experiments have shown that glycyrrhizin C2 can significantly relieve gastric mucosal damage and promote ulcer healing. Its anti-ulcer effect is not only reflected in reducing gastric acid secretion and protecting the gastric mucosal barrier, but also in regulating the expression of gastrointestinal hormones and inflammatory factors.
In terms of anti-inflammation, glycyrrhizin C2 demonstrates good anti-inflammatory effects by inhibiting the release of inflammatory mediators and regulating immune cell function. Antioxidant activity is mainly achieved by scavenging free radicals, inhibiting lipid peroxidation, and enhancing endogenous antioxidant enzyme activity. Additionally, some studies report that glycyrrhizin C2 has inhibitory effects on certain viruses such as HIV, suggesting its potential application value in the antiviral field.
The anti-ulcer effect of glycyrrhizin C2 involves multiple molecular targets and signaling pathways. Its main targets include:
Additionally, glycyrrhizin C2 inhibits inflammatory signaling pathways such as NF-κB through antioxidant and anti-inflammatory mechanisms, reduces the expression of inflammatory factors like TNF-α and IL-1β, and alleviates gastric mucosal inflammation.
The druggability parameters of glycyrrhizin C2 indicate that it has good potential for drug development. A moderate LogP value and high water solubility ensure good absorption and distribution in the body. Although the higher polar surface area limits its blood-brain barrier penetration, it helps reduce central nervous system side effects. hERG is inhibited negative and non-mutagenic, indicating a relatively high safety.
Currently, pharmacokinetic research on glycyrrhizin C2 is relatively limited. Preliminary data indicate that after oral administration, glycyrrhizin C2 can be absorbed by the gastrointestinal tract, the plasma concentration reaches a moderate peak, and the internal half-life is suitable for routine administration. Its metabolism mainly passes through hepatic enzyme systems, and its metabolites may include deglycosyl compounds, some of which remain bioactive. The main excretion routes are bile and urine. In the future, further systematic pharmacokinetic and toxicological studies are needed to improve the foundation for clinical development.
Given the significant activity of glycyrrhizin C2 in anti-ulcer and gastrointestinal protection, its development as a novel gastric ulcer treatment has broad prospects. Compared with traditional drugs, glycyrrhizin C2's multi-target mechanism of action and good safety provide advantages for its clinical application. In addition, its anti-inflammatory, antioxidant, and antiviral effects also offer potential for treating related gastrointestinal diseases and viral infections.
Future research should focus on preclinical safety evaluation, dosage form optimization, and clinical trial design of glycyrrhizin C2, exploring its application in adjuvant therapy for gastric ulcers, gastritis, and even gastric cancer. At the same time, combining modern molecular biology techniques to further elucidate its mechanisms of action and target networks, it helps guide precise drug use and combination treatment strategies.
Glycyrrhizin C2, as an important class of oledane-type triterpenoid oligosaccharide in licorice, demonstrates great potential in treating ulcers and gastrointestinal diseases due to its diverse pharmacological activity and good druggability. Systematic chemical, pharmacological, and mechanistic research has laid a solid foundation for its clinical translation. In the future, as research deepens and technology advances, glycyrrhizin C2 is expected to become an important candidate molecule in the development of natural product drugs, offering new treatment options for patients with gastrointestinal diseases.
Shenshuai
Wenjing
Hedandan
