Product name: Sweroside
Synonym name:
Catalogue No.: BP1348
Cas No.: 14215-86-2
Formula: C₁₆H₂₂O₉
Mol Weight: 358.343
Botanical Source: Swertia japonica, Tabernaemontana psorocarpa, Centaurium spicatum and Gentiana rhodentha
Physical Description: Powder
Type of Compound: Iridoids

Purity: 95%~99%
Analysis Method: HPLC-DAD or/and HPLC-ELSD
Identification Method: Mass, NMR
Packing: Brown vial or HDPE plastic bottle

Storage: Store in a well closed container, protected from air and light. Put into refrigerate or freeze for long term storage.
Whenever possible, you should prepare and use solutions on the same day. However, if you need to make up stock solutions in advance, we recommend that you store the solution as aliquots in tightly sealed vials at -20℃. Generally, these will be useable for up to two weeks.

The product could be supplied from milligrams to grams, up to kilograms
Inquire for bulk scale.

Descriptions:
Sweroside and swertiamarine are main constituents in Gentian (Gentiana lutea ssp. symphyandra), Gentian has wound healing activity, seems to be mainly due to the increase in the stimulation of collagen production and the mitotic activity by sweroside and swertiamarine , respectively; they also have cytoprotective effects, which may cause a synergism in terms of wound healing activity of Gentian. [1]
Sweroside has the anti-osteoporotic effect on the MG-63 cells and osteoblasts, it has a direct osteogenic effect on the proliferation and differentiation of cultured MG-63 cells and osteoblasts in vitro. [2]
Sweroside can inhibit potent melanogenesis in melan-a cells at 300uM without cytotoxicity, also decreases tyrosinase, tyrosinase-related protein-1 (TRP-1) and TRP-2 protein production in melan a cells, it may be an effective skin-whitening agent through the regulates the expression of MAP kinase and melanogenic enzymes. [3]
Sweroside and gentiopicroside suppress Pck1 expression and induce phosphorylation of components in the insulin signalling cascade, demonstrates that sweroside and gentiopicroside show insulin-mimicking effects on the regulation of Pck1 expression. [4]

References:
[1] Oztürk N, Korkmaz S, Oztürk Y, et al. Planta Med, 2006, 72(4):289-94.
[2] Sun H, Li L, Zhang A, et al. Fitoterapia, 2013, 84(1):174-9.
[3] Yong T J, Sang C J, Hwang J S, et al. Chem-biol interact, 2015, 238:33-9.
[4] Dr. Xianju Huang, Li J, Mr. ZhiYi Mei, et al. Biochem Cell Biol, 2016, 94(3): 270-8.
[5] Xin-Yu J I, Wang C, Liu B. Chinese J Exp Trad Med Formulae, 2014, 20(17):102-5.

HPLC of  Sweroside

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

Introduction/Overview

Sweroside (also known as Dangyaodin) is a typical cycloether terpene glycoside natural product, widely found in various Chinese medicinal materials, especially abundant in plants of the Dangyao genus. As a natural small molecule with significant biological activity, Cycycypine has attracted widespread attention in the field of natural product pharmacology in recent years due to its multi-target and multi-pathway regulatory capabilities. Extensive studies have shown that genocyanin exhibits significant biological activity in antioxidant, anti-inflammatory, anti-apoptotic, and lipid metabolism regulation, with its mechanism involving key molecular targets such as the Keap1/Nrf2 axis, NLRP3 inflammasome, SIRT1, NF-κB, AMPK/mTOR pathways, and the caspase family. Based on these characteristics, genocyanidin demonstrates good therapeutic potential in various disease models, including myocardial ischemia-reperfusion injury, leukemia, acute lung injury, and non-alcoholic fatty liver disease.

This paper systematically reviews the chemical structure and physicochemical properties of Cycyphedrin deer, plant origin and extraction methods, pharmacological activity and mechanism of action, combined with druggability evaluation and pharmacokinetic characteristics, to explore its clinical application prospects and future research directions, aiming to provide a theoretical foundation and research reference for drug development of this natural product.

Chemical structure and physicochemical properties

The chemical name of Cycytin (structural features omitted) has a molecular formula of C_17H_26O_7 and a molecular weight of 358.3430. As a cycloalene ether terpene glycoside, Denthedrin has a typical terpenoid backbone structure, containing multiple hydroxyl and glycosidic bonds, which imparts excellent water solubility and biological activity. Its physicochemical properties show a LogP value of -1.1185, indicating strong hydrophilicity, and TPSA (Topological Polar Surface Area) of 134.9100, suggesting high molecular polarity that may affect cell membrane permeability. Water solubility is 48.5428 mg/mL, with good water solubility, which is beneficial for absorption and distribution in the body.

Additionally, roodontocypine has relatively low blood-brain barrier penetration, suggesting it mainly acts on peripheral tissues to reduce the risk of central nervous system side effects. The hERG channel inhibition test was negative, indicating a low risk of cardiotoxicity. The Ames test result was 0.0, indicating no significant genotoxicity and relatively high safety.

Plant Origins and Extraction Methods

Cycypine is mainly found in plants of the genus Swertia, such as Swertia japonica and Swertia chirayita. These plants are widely used in traditional Chinese medicine for clearing heat and detoxifying, reducing inflammation and pain, and is considered one of the main active ingredients.

The extraction method for genitinoside usually uses ethanol or methanol as solvent for reflux extraction, combined with liquid-liquid separation and column chromatography and other separation and purification techniques. In recent years, the application of new green extraction technologies such as ultrasound-assisted extraction and microwave-assisted extraction has significantly improved the extraction efficiency and purity of genitocyanide. During purification, silica gel column chromatography and reversed-phase high-performance liquid chromatography (RP-HPLC) are commonly used to ensure high purity and stability of the final product.

Pharmacological activity research

Antioxidant activity

Cycypine activates the Keap1/Nrf2 signaling pathway, promotes Nrf2 nuclear translocation, enhances the expression of intracellular antioxidant enzymes such as superoxide dismutase (SOD) and glutathione peroxidase (GPx), effectively scavenging excess reactive oxygen species (ROS) and reducing oxidative stress damage. This effect is particularly evident in models of myocardial ischemia-reperfusion injury, protecting myocardial cells from oxidative damage.

Anti-inflammatory activity

Cycypine inhibits inflammatory responses by regulating multiple targets. First, it activates SIRT1 to inhibit the NF-κB signaling pathway, reducing the expression of pro-inflammatory cytokines such as TNF-α, IL-6, and IL-1β; Second, it inhibits the activation of NLRP3 inflammasomes, blocks pyroptosis, and reduces tissue inflammatory damage. This anti-inflammatory mechanism has been validated in models of acute lung injury, hepatitis, and other inflammatory diseases.

Anti-apoptotic effects

Cycypine regulates caspase family proteins to induce caspase-dependent apoptosis, while also promoting autophagy by modulating the AMPK/mTOR pathway to maintain cellular homeostasis. This dual regulatory mechanism helps clear damaged cells and prevent abnormal cell proliferation, demonstrating potential therapeutic value in malignant tumors such as leukemia.

Regulates lipid metabolism

Research shows that genocyanine can regulate lipid metabolism through the AMPK/mTOR signaling pathway, inhibit fat synthesis, promote lipolysis, and alleviate the pathological state of non-alcoholic fatty liver disease (NAFLD). This provides a theoretical basis for its application in metabolic diseases.

Mechanism of action and molecular targets

The multi-target mechanism of deer genocidin is the basis for its pharmacological diversity. Its main targets and related signaling pathways include:

• Keap1/Nrf2 axis: Cycypine competitively binds to Keap1, releasing Nrf2, promoting its nuclear translocation, activating antioxidant gene expression, and resisting oxidative stress.
• NLRP3 inflammasomes: Inhibit NLRP3 assembly and activation, block pyroptosis pathways, and reduce inflammatory responses.
• SIRT1: Activates SIRT1 deacetylation activity, inhibits the NF-κB signaling pathway, and reduces pro-inflammatory factor expression.
• NF-κB pathway: Through SIRT1-mediated negative regulation, it inhibits NF-κB nuclear translocation and alleviates inflammatory responses.
• AMPK/mTOR pathway: activates AMPK, inhibits mTOR signaling, promotes autophagy, and regulates cellular metabolism and survival.
• Caspase family: Induces activation of caspase-3, caspase-9, and promotes cell apoptosis.

In addition, in diseases like hepatitis, Dentinogenin is involved in various signaling molecules such as STAT3, ESR2, PTGS2, and TGFB1, reflecting its complex regulatory network.

Druggability evaluation and pharmacokinetics

Druggability evaluation of genocyanin shows good safety and drug compatibility. It has a moderate molecular weight and good water solubility, making it easy for oral absorption. Low LogP values suggest strong hydrophilicity, which may limit cell membrane penetration but facilitate dissolution and distribution in the bloodstream. Low blood-brain barrier penetration reduces the risk of central nervous system side effects.

In toxicological evaluation, deercycytriin did not show hERG channel inhibition, reducing the risk of cardiotoxicity; Ames test was negative, indicating no mutagenicity. In vivo pharmacokinetic studies show that genocyanidin is rapidly absorbed orally, with a short peak plasma concentration duration and a moderate half-life, exhibiting good bioavailability. The metabolic pathway mainly passes through the liver enzyme system, and the metabolites are safe.

Prospects and outlooks for clinical applications

Based on the pharmacological properties of genitin with multiple targets and multiple pathways, it has broad application potential in various diseases. In myocardial ischemia-reperfusion injury, deercanin reduces myocardial cell damage through antioxidant and anti-inflammatory effects, providing a cardioprotective effect. In neoplastic diseases such as leukemia, the dual mechanisms of inducing apoptosis and autophagy provide new approaches for tumor treatment. In inflammatory diseases such as acute lung injury and hepatitis, genitinoside reduces tissue inflammation and injury by inhibiting inflammasome and NF-κB pathways.

Additionally, as an important component of metabolic syndrome, non-alcoholic fatty liver disease has the role of odontocyin in regulating lipid metabolism, providing possibilities for developing new drugs for metabolic diseases. In the future, combining nanocarrier technology, structural optimization, and drug combination strategies is expected to further enhance the bioavailability and therapeutic efficacy of odontoside.

However, current clinical research on genocyanin is still in its early stages and lacks systematic clinical trial data. In the future, it is necessary to strengthen pharmacokinetics, toxicology, and clinical safety assessments, clarify the optimal dosing regimen and indications, and promote clinical translation.

Conclusion

As a natural cycloetherterpenoid glycoside with multiple targets and mechanisms, Cycycydine exhibits significant antioxidant, anti-inflammatory, anti-apoptotic, and metabolic regulatory activities. Its mechanism of action covers several key pathways including the Keap1/Nrf2 axis, NLRP3 inflammasomes, SIRT1, NF-κB, AMPK/MTOR, and the caspase family, demonstrating its complex and systematic bioregulatory capabilities. Excellent druggability parameters and safety evaluation have laid a solid foundation for its drug development.

In the future, combining multidisciplinary research combining modern medicinal chemistry, molecular biology, and clinical medicine will help deeply reveal the mechanism of action of Denthatin, optimize its drug properties, and promote its clinical application in cardiovascular diseases, oncology, inflammation, and metabolic diseases. Dental cythogonine is expected to become an important research subject and potential new drug resource in the field of natural product pharmacology, providing new therapeutic strategies for the prevention and treatment of related diseases.