Swertiamarin
(Synonyms: 獐牙菜苦苷) 目录号 : GC38426A secoiridoid glycoside with diverse biological activities
Cas No.:17388-39-5
Sample solution is provided at 25 µL, 10mM.
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Swertiamarin is an orally bioavailable secoiridoid glycoside that has been found in E. axillare and has diverse biological activities, including antioxidant, anti-inflammatory, antidiabetic, and hepatoprotective properties.1,2,3,4,5 It scavenges ABTS radicals and hydrogen peroxide (IC50s = 2.83 and 5.7 μM, respectively).1 Swertiamarin (50 μg/ml) inhibits nitric oxide (NO) production in IL-1β-stimulated fibroblast-like synoviocytes (FLSs) isolated from rat hindpaw.2 Swertiamarin (25 μg/ml) inhibits oleate-induced lipid droplet and triglyceride accumulation in HepG2 cells.4 It decreases liver lipid accumulation, ballooning degeneration, and TNF-α and IL-6 levels in a mouse model of fructose-induced nonalcoholic fatty liver disease (NAFLD) when administered at a dose of 50 mg/kg per day.5 Swertiamarin (50 mg/kg per day) also decreases fasting blood glucose and serum cholesterol levels in a rat model of diabetes induced by streptozotocin .3
1.Vaijanathappa, J., and Badami, S.Antiedematogenic and free radical scavenging activity of swertiamarin isolated from Enicostemma axillarePlanta Med.75(1)12-17(2009) 2.Saravanan, S., Islam, V.I., Thirugnanasambantham, K., et al.Swertiamarin ameliorates inflammation and osteoclastogenesis intermediates in IL-1β induced rat fibroblast-like synoviocytesInflamm. Res.63(6)451-462(2014) 3.Sonawane, R.D., Vishwakarma, S.L., Lakshmi, S., et al.Amelioration of STZ-induced type 1 diabetic nephropathy by aqueous extract of Enicostemma littorale Blume and swertiamarin in ratsMol. Cell Biochem.340(1-2)1-6(2010) 4.Patel, T.P., Rawal, K., Soni, S., et al.Swertiamarin ameliorates oleic acid induced lipid accumulation and oxidative stress by attenuating gluconeogenesis and lipogenesis in hepatic steatosisBiomed. Pharmacother.83785-791(2016) 5.Yang, Y., Li, J., Wei, C., et al.Amelioration of nonalcoholic fatty liver disease by swertiamarin in fructose-fed micePhytomedicine59152782(2019)
Cas No. | 17388-39-5 | SDF | |
别名 | 獐牙菜苦苷 | ||
Canonical SMILES | C=C[C@@H]([C@@H]1O[C@]([C@@H]([C@@H](O)[C@@H]2O)O)([H])O[C@@H]2CO)[C@@](C3=CO1)(CCOC3=O)O | ||
分子式 | C16H22O10 | 分子量 | 374.34 |
溶解度 | 250 mg/mL in DMSO | 储存条件 | 4°C, protect from light |
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1 mg | 5 mg | 10 mg | |
1 mM | 2.6714 mL | 13.3568 mL | 26.7137 mL |
5 mM | 0.5343 mL | 2.6714 mL | 5.3427 mL |
10 mM | 0.2671 mL | 1.3357 mL | 2.6714 mL |
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Swertiamarin-mediated immune modulation/adaptation confers protection against Plasmodium berghei
Future Microbiol 2022 Aug;17:931-941.PMID:35704297DOI:10.2217/fmb-2021-0298.
Aims: Development of resistance by the malaria parasite, a systemic inflammatory and infectious pathogen, has raised the need for novel efficacious antimalarials. Plant-derived natural compounds are known to modulate the immune response and eradicate the infectious pathogens. Therefore we carried out experiments with Swertiamarin to dissect its anti-inflammatory and immunomodulatory potential. Materials & methods: We carried out studies in Swiss albino mice that received infectious challenge with Plasmodium berghei and Swertiamarin treatment in a prophylactic manner. Results & conclusion: Oral administration of Swertiamarin prior to infectious challenge with P. berghei in experimental mice showed delayed parasite development as compared with untreated control. IFN-γ and IL-10 appeared to be adapted/modulated by regular Swertiamarin treatment. Further, withdrawal of Swertiamarin pressure did not affect parasite replication. However, the short half-life of Swertiamarin limited its long-lasting therapeutic effect, requiring higher and frequent dosing schedules.
Proteomic Analysis of Swertiamarin-treated BV-2 Cells and Possible Implications in Neuroinflammation
J Oleo Sci 2022 Mar 2;71(3):395-400.PMID:35153246DOI:10.5650/jos.ess21333.
The purpose of this study was to explore the neuroprotective role of Swertiamarin on neuro-inflammation, and analyzed its potential mechanism by proteomics. We used LPS to induce a inflammatory model on BV-2 cells, then 10, 25, 50 μg/mL Swertiamarin was used to treat the LPS pretreated BV-2 cells. We used ELISA to detect the effect of Swertiamarin on the expression of inflammation related indicators such as IL-1β, il-6, IL-18 and TNF-α. The proteomics based on TMT-LC-MS/MS analysis was performed to explore the anti-inflammatory effects of Swertiamarin by bioinformatics analysis. We found swertiamain was able to inhibit pro-inflammatory cytokines secretion in a does dependent manner, including IL-1β, IL-6, IL-18 and TNF-α. These results were further verified by western blot. The proteomics analysis results suggested that the potential bioprocessings which regulated by Swertiamarin mainly involved in cellular response to carbon monoxide, strand displacement, palmitoleoyltransferase activity, D2 dopamine receptor binding, RNA polymerase II transcription cofactor activity. The present study may provide a promising approach to treat and prevent neuro-inflammation diseases. It is preliminarily indicated that Swertiamarin will play an important role in clinical anti-neuroinflammation process in the future.
A systematic review of the protective role of Swertiamarin in cardiac and metabolic diseases
Biomed Pharmacother 2016 Dec;84:1051-1060.PMID:27780133DOI:10.1016/j.biopha.2016.10.044.
Background: Swertiamarin, is a secoiridoid glycoside found in genera of Enicostemma Species (Enicostemma littorale and Enicostemma axillare) belonging to the family of gentianaceae, which has been reported to cure many diseases such as diabetes, hypertension, atherosclerosis, arthritis, malaria and abdominal ulcers. However, to the best of our knowledge, till date systematic studies to understand the molecular basis of cardiac and metabolic disease preventing properties of Swertiamarin has not been reported. Aim of the review: The present review aims to compile an up-to-date information on the progress made in the protective role of Swertiamarin in cardiac and metabolic diseases with the objective of providing a guide for future research on this bioactive molecule. Materials and methods: Information on the Swertiamarin was collected from major scientific databases (Pubmed, Springer, google scholar, and Web of Science) for publication between1974-2016. In this review, the protective role of Swertiamarin on cardiac and metabolic diseases was discussed. Results: Swertiamarin reported to exhibit a wide range of biological activities such as anti-atherosclerotic, antidiabetic, anti-inflammatory and antioxidant effects. These activities were mainly due to its effect on various signaling pathways associated with cardiac remodeling events such as inhibition of NF-kB expression, LDL oxidation, apoptosis, inflammatory and lipid peroxidation markers and stimulation of antioxidant enzymes. Conclusion: Sweriamarin exhibit a wide range of biological activities. This review presents evidence supporting the point of view that Swertiamarin should be considered a potential therapeutic agent against cardiac and metabolic diseases, giving rise to novel applications in their prevention and treatment.
Swertiamarin supplementation prevents obesity-related chronic inflammation and insulin resistance in mice fed a high-fat diet
Adipocyte 2021 Dec;10(1):160-173.PMID:33794740DOI:10.1080/21623945.2021.1906510.
Obesity is characterized by low-grade chronic inflammation, which underlies insulin resistance and non-alcoholic fatty liver disease (NAFLD). Swertiamarin is a secoiridoid glycoside that has been reported to ameliorate diabetes and NAFLD in animal models. However, the effects of Swertiamarin on obesity-related inflammation and insulin resistance have not been fully elucidated. Thus, this study investigated the effects of Swertiamarin on inflammation and insulin resistance in high-fat diet (HFD)-induced obese mice. C57BL/6 mice were fed a HFD or HFD containing Swertiamarin for 8 weeks. Obesity-induced insulin resistance and inflammation were assessed in the epididymal white adipose tissue (eWAT) and livers of the mice. Swertiamarin attenuated HFD-induced weight gain, glucose intolerance, oxidative stress, and insulin resistance, and enhanced insulin signalling in mice. Compared to HFD-fed mice, the swertiamarin-treated mice exhibited increased lipolysis and reduced adipocyte hypertrophy and macrophage infiltration in eWAT. Moreover, Swertiamarin alleviated HFD-mediated hepatic steatosis and inflammation by suppressing activation of the p38 MAPK and NF-κB pathways within the eWAT and liver of obese mice. In conclusion, supplementation with Swertiamarin attenuated weight gain and hepatic steatosis, and alleviated obesity-associated inflammation and insulin resistance, in obese mice.
The Molecular Targets of Swertiamarin and its Derivatives Confer Anti- Diabetic and Anti-Hyperlipidemic Effects
Curr Drug Targets 2018;19(16):1958-1967.PMID:29623834DOI:10.2174/1389450119666180406113428.
The herbal plant extract of Enicostemma littorale is widely used to medicate and treat type II Diabetes. This extract in medicine has shown its value in reducing blood glucose & lipid levels, and improving the kidney functioning, lipid profile, controlling blood pressure and heart rate. The well characterized chemical components such as iridoid and secoiridoid glycosides are present in aqueous and ethanolic extracts of the plant. Swertiamarin, a secoiridoid glycoside, is identified as the lead compound that confers anti-hyperglycemic & anti-hyperlipidemic effects. The Swertiamarin binds with one or more molecular targets to alter their expression and/or activity. The in silico, in vivo and in vitro studies have been carried out to uncover the underlying molecular mechanism of action of Swertiamarin and its derivatives for showing the better anti-diabetic & anti-hyperlipidemic activities. In brief, the present review focuses on unraveling the information about molecular targets of Swertiamarin. Our review will open new avenues to develop therapeutic approaches and drugs to treat diabetes and other inflammatory diseases.