Synonym name: Swertiamaroside
Catalogue No.: BP1349
Cas No.: 17388-39-5
Formula: C₁₆H₂₂O₁₀
Mol Weight: 374.342
Botanical Source: Swertia japonica, Anthocleista procera, Centaurium littorale, Swertia pseudochinensis, Swertia mileensis and Enicostema litorale

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.

HPLC of Swertiamarin

HNMR of Swertiamarin

Storage conditions：Short-term storage at 2~8℃, long-term storage at -20 ~ -80℃

Introduction/Overview

Swertiamarin is a natural monoterpene bitter glycoside widely found in the genus Swertia spp. and related plants. Due to its remarkable pharmacological activity and good oral bioavailability, it has become a hot topic in pharmacological research of natural products in recent years. As a natural compound with multiple biological activities, fenna fracin shows good therapeutic potential in lowering blood sugar, blood lipids, rheumatism, antioxidant, and anti-inflammatory properties, especially in experimental models of diabetes, arthritis, and liver diseases, showing significant protective effects. This paper aims to systematically review the chemical structure, physicochemical properties, plant origin, and extraction methods of Henan sentrachetin, focusing on its pharmacological activity and mechanism of action. Combined with the latest molecular target studies, it evaluates its druggability and pharmacokinetic characteristics, explores its clinical application prospects and future research directions, and provides theoretical basis and research reference for the development and application of this natural product.

Chemical structure and physicochemical properties

The chemical name of Malicin in roe deer cabbage is (2S,3R,4S,5S,6R)-2-(β-D-pyranglucosyloxy)-3,4,5,6-tetrahydroxycyclohexylacetate lactone, molecular formula C16H22O10, and molecular weight 374.3420. Its structural feature is a monoterpenoid backbone connected by a β-D-glucoside bond, containing multiple hydroxyl and lactone rings, which imparts high polarity and water solubility. In terms of physicochemical properties, the LogP value of Macroside in Tooth Cypritis was -1.5760, indicating strong hydrophilicity; the topological pole surface area (TPSA) was 155.14 Ų, indicating good polar group distribution, which is favorable for binding to biological macromolecules. Water solubility is about 44.73 mg/mL, indicating good water solubility and facilitating oral administration. Its blood-brain barrier permeability is relatively low, with negative results in hERG channel inhibition tests and 0 in Ames mutagenic tests, indicating high safety and low risk of toxic side effects.

Plant Origins and Extraction Methods

The bitter glycoside of Tooth Root is mainly found in plants of the gentianaceae family, such as Swertia japonica, Swertia chirayita, and Swertia mussotii. These plants are widely used in traditional Chinese medicine to treat liver and gallbladder diseases, diabetes, and rheumatic diseases. The content of picroside in Tooth jade in plants varies depending on species, collection time, geographical environment, and extraction process.

Common extraction methods include solvent extraction extraction, ultrasonic-assisted extraction, and microwave-assisted extraction. Typically, ethanol-water mixed solvents (such as 70% ethanol) are used for extraction extraction, combined with ultrasound assistance to improve extraction efficiency. After concentration and separation purification, the extract was used for qualitative and quantitative analysis using high-performance liquid chromatography (HPLC). In recent years, supercritical fluid extraction and membrane separation technologies have also been applied to the efficient extraction and purification of matroside in Venus, further improving purity and yield.

Pharmacological activity research

Blood sugar and lipid-lowering effects

Malay glycoside has significant hypoglycemic activity, mainly by improving insulin sensitivity, promoting glucose metabolism, and inhibiting gluconeogenesis. Animal experiments have shown that Malay in Tooth Chloride can lower fasting blood glucose levels in diabetic rats, improve glucose tolerance, and simultaneously decrease plasma triglycerides and total cholesterol, demonstrating good lipid-lowering effects. Its mechanism may involve activation of the AMPK signaling pathway, promoting lipid metabolism and energy homeostasis regulation.

Anti-inflammatory and anti-rheumatic effects

In the rheumatoid arthritis model, fantrine mithrin reduces joint inflammation and tissue destruction by inhibiting the release of pro-inflammatory cytokines (such as TNF-α, IL-1β, IL-6) and downregulating the expression of inflammation-related enzymes (MMPs). Its mechanism of action is closely related to the regulation of the JAK2/STAT3 signaling pathway, which can inhibit the overexpression of inflammatory mediators and slow down the course of inflammation. Preclinical studies have shown that Malayin has potential value in antirheumatic drug development.

Antioxidant and liver-protective effects

Maline glycosides in roe deer showed significant antioxidant activity in various oxidative stress models. Taking carbon tetrachloride (CCl4)-induced liver injury as an example, carcinoside can activate the Nrf2/HO-1 antioxidant defense pathway, reduce liver oxidative damage, alleviate hepatocyte necrosis and inflammatory responses, and demonstrate good liver-protective effects. In addition, it can regulate the activity of various antioxidant enzymes, enhancing the body's ability to eliminate free radicals.

Promotes bone formation

Research has found that maline glycosides can promote the proliferation and differentiation of osteoblasts, regulate the expression of bone metabolism-related genes, and have potential preventive and therapeutic effects for osteoporosis. Its mechanism of promoting bone formation involves regulating the bone morphogenetic protein (BMP) signaling pathway and inhibiting the expression of bone resorption-related MMPs, demonstrating potential application in the treatment of bone and joint diseases.

Mechanism of action and molecular targets

The multiple pharmacological effects of Masaside in Tooth Virtus are closely related to its regulation of multiple signaling pathways and molecular targets. The main mechanisms of action include:

1. Regulates pro-inflammatory cytokines and NF-κB signaling pathways
   Malay in roe deer cabbage can inhibit NF-κB activation, reduce the expression of pro-inflammatory factors such as TNF-α, IL-1β, and IL-6, and alleviate inflammatory responses. NF-κB, as a core transcription factor in inflammatory responses, helps alleviate rheumatoid arthritis and other inflammatory diseases.

2. Activates the Nrf2/HO-1 antioxidant pathway
   By promoting Nrf2 nuclear translocation and enhancing the expression of HO-1 and other antioxidant enzymes, Malicin effectively resists oxidative stress, protects liver cells from free radical damage, and exerts hepatoprotective and anti-fibrotic effects.

3. Regulating JAK2/STAT3 signaling pathways
   In adjuvant-induced arthritis models, Malayin in Venusa reduces the production of inflammatory mediators by inhibiting abnormal activation of JAK2/STAT3, alleviating joint inflammation and tissue destruction.

4. Affects targets related to liver fibrosis
   Mamarin can regulate key targets such as AMPK, BCL2, STAT3, MMP2, MMP9, SMAD3, and PPARG, inhibit hepatic stellate cell activation, block fibrotic progression, and has anti-fibrotic potential.

5. Promotes osteoblast proliferation and differentiation
   By regulating genes and signaling pathways related to bone metabolism, promoting bone formation, and inhibiting bone resorption, Zhang Tooth Bitter Glycoside is expected to become a new natural drug for treating osteoporosis and bone and joint diseases.

Druggability evaluation and pharmacokinetics

The molecular weight of Malay in Tooth Moss is 374.34, making it a medium-weight natural product. Its LogP value is -1.576, indicating strong hydrophilicity, which is beneficial for dissolution and absorption of oral formulations. High TPSA (155.14 Ų) suggests strong polarity, which may limit blood-brain barrier penetration, consistent with its characteristics of low central nervous system side effects. It has good water solubility (44.73 mg/mL), which is beneficial for formulation development.

In terms of safety, Mamarin did not show hERG channel inhibitory effects, reducing the risk of cardiotoxicity; Ames test was negative, indicating no obvious mutagenicity. Preliminary pharmacokinetic studies show that oral oral tosal amarins have good bioavailability, moderate plasma half-life, and are mainly metabolized by the liver, with excretion primarily via the kidneys. Its low blood-brain barrier permeability reduces the likelihood of central nervous system toxic side effects.

However, the oral absorption and metabolic kinetics of Maline in roe carrot still require further systematic research, especially since its in vivo metabolites and pharmacodynamic material basis are not yet fully determined. Future studies should combine in vivo and in vitro pharmacokinetics and pharmacodynamics to optimize dosage formulation design and improve clinical conversion rates.

Prospects and outlooks for clinical applications

As a natural active ingredient with multiple targets and mechanisms, Maline glycoside has attracted widespread attention for its therapeutic potential in chronic metabolic and inflammatory diseases such as diabetes, rheumatoid arthritis, and liver diseases. Its excellent safety and multiple pharmacological effects provide a solid foundation for the development of novel natural medicines.

The future clinical application prospects are mainly reflected in the following aspects:

1. Treatment of diabetes and metabolic syndrome
   Mollusk maline glycoside improves insulin resistance and regulates lipid metabolism, making it a potential adjunct treatment for diabetes and related metabolic diseases.

2. Development of antirheumatic and anti-inflammatory drugs
   Its regulatory effects on the JAK2/STAT3 and NF-κB pathways give it potential therapeutic value in rheumatoid arthritis and other inflammatory diseases.

3. Liver protection and anti-liver fibrosis
   By activating the Nrf2/HO-1 pathway and modulating multiple fibrosis-related targets, antherraside may become a candidate drug for liver fibrosis and liver injury.

4. Osteoporosis and bone and joint diseases
   It promotes osteoblast proliferation and differentiation, providing new ideas for the treatment of osteoporosis and bone and joint diseases.

However, the clinical translation of Maline in Tooth cabbage still faces many challenges, including improving pharmacokinetic characteristics, optimizing formulations, and evaluating clinical safety and efficacy. In the future, it is necessary to strengthen multicenter, large-sample clinical research, integrating modern medicinal chemistry and pharmacology techniques to promote its application from the laboratory to clinical application.

Conclusion

As a natural product with rich pharmacological activity and good safety, malcoside shows broad application prospects in diabetes, inflammatory diseases, liver diseases, and other fields. Its multi-target and multi-mechanism mode of action provides new strategies for the comprehensive treatment of complex diseases. Future research should focus on deeply elucidating its molecular mechanisms, optimizing drug formulations, improving pharmacokinetic data, and conducting systematic clinical evaluations to promote the clinical translation and industrial application of Maline in Hena canali. Through multidisciplinary collaboration, Fenagin is expected to become an important representative in the development of natural product drugs, contributing new natural drug resources to human health.