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℃
Sweroside, also known as sweroside, is a typical natural product of iridoid glycosides, widely present in various traditional Chinese medicinal materials, especially in plants of the Sweroside genus. As a naturally occurring small molecule with significant biological activity, swertiamarin has attracted widespread attention in the field of natural product pharmacology in recent years due to its ability to regulate multiple targets and pathways. Numerous studies have shown that swertiamarin has significant biological activities in antioxidant, anti-inflammatory, anti apoptotic, and lipid metabolism regulation, and its mechanism of action involves multiple key molecular targets such as Keap1/Nrf2 axis, NLRP3 inflammasome, SIRT1, NF - κ B, AMPK/mTOR pathway, and caspase family. Based on these characteristics, swertiamarin has shown promising therapeutic potential in various disease models such as myocardial ischemia-reperfusion injury, leukemia, acute lung injury, and non-alcoholic fatty liver disease.
This article provides a systematic review of the chemical structure and physicochemical properties, plant sources and extraction methods, pharmacological activity and mechanism of action of swertiamarin. Combined with the evaluation of drug properties and pharmacokinetic characteristics, it explores its clinical application prospects and future research directions, aiming to provide a theoretical basis and research reference for the drug development of this natural product.
The chemical name of swertiamarin is (structural characteristics omitted), with a molecular formula of C17H26O7 and a molecular weight of 358.3430. As a cyclic terpenoid glycoside, swertiamarin has a typical terpenoid skeleton structure, containing multiple hydroxyl groups and glycosidic bonds, endowing it with good water solubility and biological activity. Its physical and chemical properties show that the LogP value is -1.1185, indicating strong hydrophilicity. The TPSA (topological polar surface area) is 134.9100, indicating high molecular polarity, which may affect its cell membrane permeability. The water solubility is 48.5428 mg/mL, which has good water solubility and is conducive to absorption and distribution in the body.
In addition, swertiamarin shows low penetration through the blood-brain barrier, indicating that it mainly acts on peripheral tissues and reduces the risk of central nervous system side effects. The negative result of hERG channel inhibition experiment indicates a low risk of cardiac toxicity. The Ames test result is 0.0, indicating no significant genotoxicity and high safety.
Swertia glycosides are mainly found in plants of the genus Swertia, such as Swertia japonica and Swertia chirayita. This type of plant is widely used in traditional Chinese medicine for clearing heat and detoxifying, anti-inflammatory and analgesic treatments, and swertiamarin is considered one of its main active ingredients.
The method of extracting swertiamarin usually uses ethanol or methanol as solvents for reflux extraction, combined with liquid-liquid distribution, 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 swertiamarin. During the purification process, methods such as silica gel column chromatography and reverse phase high-performance liquid chromatography (RP-HPLC) are commonly used to ensure the high purity and stability of the final product.
Swertia glycosides activate the Keap1/Nrf2 signaling pathway, promote Nrf2 nuclear translocation, enhance the expression of intracellular antioxidant enzymes such as superoxide dismutase (SOD) and glutathione peroxidase (GPx), effectively eliminate excess reactive oxygen species (ROS), and alleviate oxidative stress damage. This effect is particularly significant in the myocardial ischemia-reperfusion injury model, which can protect myocardial cells from oxidative damage.
Swertiamarin inhibits inflammatory response through multi-target regulation. Firstly, activate SIRT1, inhibit the NF - κ B signaling pathway, and reduce the expression of pro-inflammatory cytokines such as TNF - α, IL-6, and IL-1 β; Secondly, inhibiting the activation of NLRP3 inflammasome, blocking the pyroptosis process, and reducing tissue inflammatory damage. This anti-inflammatory mechanism has been validated in inflammatory disease models such as acute lung injury and hepatitis.
Swertiamarin induces caspase dependent cell apoptosis by regulating caspase family proteins, while promoting autophagy and maintaining cellular homeostasis by modulating the AMPK/mTOR pathway. This dual regulatory mechanism helps to clear damaged cells, prevent abnormal cell proliferation, and demonstrates potential therapeutic value in malignant tumors such as leukemia.
Research has shown that swertiamarin can regulate lipid metabolism, inhibit fat synthesis, promote fat breakdown, and alleviate the pathological state of non-alcoholic fatty liver disease (NAFLD) through the AMPK/mTOR signaling pathway. This provides a theoretical basis for its application in metabolic diseases.
The multi-target mechanism of action of swertiamarin is the basis for its diverse pharmacological activities. Its main targets and related signaling pathways include:
In addition, swertiamarin is involved in various signaling molecules such as STAT3, ESR2, PTGS2, TGFB1 in diseases such as hepatitis, reflecting its complex regulatory network.
The pharmacological evaluation of swertiamarin shows that it has good safety and drug compatibility. Moderate molecular weight, good water solubility, conducive to oral absorption. A low LogP value indicates strong hydrophilicity, which may limit cell membrane penetration but is beneficial for dissolution and distribution in the bloodstream. Low blood-brain barrier penetration rate reduces the risk of central nervous system side effects.
In toxicology assessment, swertiamarin did not exhibit hERG channel inhibition, reducing the risk of cardiac toxicity; Ames test negative, indicating no mutagenicity. Pharmacokinetic studies in vivo have shown that swertiamarin is absorbed rapidly after oral administration, with a short peak plasma concentration, moderate half-life, and good bioavailability. The metabolic pathway is mainly through the liver enzyme system, and the safety of metabolites is good.
Based on the pharmacological properties of multiple targets and pathways regulated by swertiamarin, its potential applications in various diseases are extensive. In myocardial ischemia-reperfusion injury, swertiamarin reduces myocardial cell damage through antioxidant and anti-inflammatory effects, and has a cardioprotective effect. The dual mechanism of inducing apoptosis and autophagy in leukemia and other tumor diseases provides new ideas for tumor treatment. In inflammatory diseases such as acute lung injury and hepatitis, swertiamarin reduces tissue inflammation and damage by inhibiting inflammasomes and the NF - κ B pathway.
In addition, non-alcoholic fatty liver disease is an important component of metabolic syndrome, and the regulatory effect of swertiamarin on lipid metabolism provides the possibility for the development of new drugs for metabolic diseases. In the future, by combining nanocarrier technology, structural optimization, and drug combination strategies, it is expected to further enhance the bioavailability and therapeutic efficacy of swertiamarin.
However, current clinical research on swertiamarin is still in its early stages and lacks systematic clinical trial data. In the future, it is necessary to strengthen its pharmacokinetic, toxicological, and clinical safety evaluations, clarify the optimal dosing regimen and indications, and promote its clinical translation.
As a multi-target and multi mechanism natural product of iridoid glycosides, swertiamarin exhibits significant antioxidant, anti-inflammatory, anti apoptotic, and metabolic regulatory activities. Its mechanism of action covers multiple key pathways such as Keap1/Nrf2 axis, NLRP3 inflammasome, SIRT1, NF - κ B, AMPK/mTOR, and caspase family, reflecting its complex and systematic biological regulatory ability. Good pharmacokinetic parameters and safety evaluation have laid a solid foundation for its drug development.
In the future, interdisciplinary research combining modern medicinal chemistry, molecular biology, and clinical medicine will help to deeply reveal the mechanism of action of swertiamarin, optimize its drug properties, and promote its clinical applications in cardiovascular disease, tumors, inflammation, and metabolic diseases. Swertiamarin is expected to become an important research object and potential new drug resource in the field of natural product pharmacology, providing new treatment strategies for the prevention and treatment of related diseases.
