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    Swertiamarin
    Information
    CAS No. 17388-39-5 Price $40 / 20mg
    Catalog No.CFN99818Purity>=98%
    Molecular Weight374.3 Type of CompoundIridoids
    FormulaC16H22O10Physical DescriptionPowder
    Download Manual    COA    MSDSSimilar structuralComparison (Web)
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    Biological Activity
    Description: Swertiamarin possesses anti-hyperglycemic, anti-hyperlipidemic, anti-diabetic activity and enhances β cell regeneration which causes reversal of diabetes. Swertiamarin also possesses significant wound healing, anti-inflammatory, antioxidant, hepatoprotective, peripheral and central antinociceptive properties. Swertiamarin inhibits the development of arthritis by modulating NF-κB/IκB and JAK2/STAT3 signaling, it acts as an anti-rheumatic agent.
    Targets: 5-HT Receptor | NF-kB | p65 | IkB | JAK | STAT | PPAR | GLUT | IKK
    In vitro:
    Planta Med. 2006 Mar;72(4):289-94.
    Effects of gentiopicroside, sweroside and swertiamarine, secoiridoids from gentian (Gentiana lutea ssp. symphyandra), on cultured chicken embryonic fibroblasts.[Pubmed: 16557467]
    Wound healing properties of Gentian (Gentiana lutea ssp. symphyandra) extract and its main constituents, gentiopicroside, sweroside and Swertiamarine (compounds 1-3, respectively) were evaluated by comparison with dexpanthenol on cultured chicken embryonic fibroblasts.
    METHODS AND RESULTS:
    The extract was also analyzed by HPLC to quantify its constituents. Chicken embryonic fibroblasts from fertilized eggs were incubated with the plant extract and its constituents, compounds 1-3. Using microscopy, mitotic ability, morphological changes and collagen production in the cultured fibroblasts were evaluated as parameters. Wound healing activity of Gentian seems to be mainly due to the increase in the stimulation of collagen production and the mitotic activity by compounds 2 and 3, respectively (p < 0.005 in all cases). All three compounds also exhibited cytoprotective effects, which may cause a synergism in terms of wound healing activity of Gentian.
    CONCLUSIONS:
    The findings demonstrated the wound healing activity of Gentian, which has previously been based only on ethnomedical data.
    Phytother Res. 2013 Apr;27(4):624-7.
    Anti-diabetic activity of swertiamarin is due to an active metabolite, gentianine, that upregulates PPAR-γ gene expression in 3T3-L1 cells.[Pubmed: 22718571 ]
    We have previously shown the anti-diabetic effects of Swertiamarin; however, pharmacokinetic analysis showed that Swertiamarin had a plasma half-life of 1.3 h. Gentianine is an active metabolite of Swertiamarin that possesses a pharmacophoric moiety. The aim of this study was to explore the possibility whether the anti-diabetic effect of Swertiamarin is due to gentianine.
    METHODS AND RESULTS:
    Swertiamarin treatment had no significant effect on adipogenesis, or the mRNA expression of PPAR-γ and GLUT-4; however, there was a significant increase in the mRNA expression of adiponectin. On the other hand, treatment with gentianine significantly increased adipogenesis, which was associated with a significant increase in the mRNA expression of PPAR-γ, GLUT-4 and adiponectin.
    CONCLUSIONS:
    These findings suggest, for the first time, that the anti-diabetic effect of Swertiamarin is due to gentianine, an active metabolite of Swertiamarin.
    In vivo:
    J Ethnopharmacol. 2010 Jul 6;130(1):103-6.
    Antioxidant and hepatoprotective effect of swertiamarin from Enicostemma axillare against D-galactosamine induced acute liver damage in rats.[Pubmed: 20420896 ]
    The whole plant of Enicostemma axillare Raynal (Family: Gentianaceae) is used in variety of diseases in traditional Indian system of medicine including hepatic ailments. Swertiamarin isolated from Enicostemma axillare Raynal was evaluated for antioxidant and hepatoprotective activity.
    METHODS AND RESULTS:
    Swertiamarin was isolated from successive ethyl acetate extract of the plant Enicostemma axillare belongs to the family Gentianaceae. The concentration of Swertiamarin was determined by high performance thin layer chromatography (HPTLC). The hepatoprotective and antioxidant activity of Swertiamarin (100 and 200mg/kg body weight) was carried out against d-Galactosamine (d-GalN) (200mg/kg body weight intraperitoneally i.p.) induced liver injury in rats. Swertiamarin a secoiridoid glycoside was found to contain a major constituent of the extract. d-GalN caused significant hepatotoxicity by alteration of several hepatic parameters. It also caused significant lipid peroxidation and reduced the levels of antioxidant defense mechanisms. The treatment with Swertiamarin at 100 and 200mg/kg body weight when administered orally for 8 days prior to d-GalN caused a significant restoration of all the altered biochemical parameters due to d-GalN towards the normal, indicating the potent antioxidant and hepatoprotective nature of Swertiamarin.
    CONCLUSIONS:
    Swertiamarin isolated from Enicostemma axillare possesses significant antioxidant and hepatoprotective properties against d-GalN induced hepatotoxicity given at 100 and 200mg/kg body weight orally for 8 days, which might be due to its in vitro antioxidant activity.
    J Nat Med. 2009 Oct;63(4):437-42.
    Antihyperlipidaemic activity of swertiamarin, a secoiridoid glycoside in poloxamer-407-induced hyperlipidaemic rats.[Pubmed: 19633811]

    METHODS AND RESULTS:
    We have investigated antihyperlipidaemic effect of Swertiamarin (50 mg/kg, oral once) isolated from the perennial herb Enicostemma littorale Blume in poloxamer 407 (P-407)-induced hyperlipidaemic rats. Rats were made hyperlipidaemic by intraperitoneal administration of P-407 (400 mg/kg). Serum lipid levels such as total cholesterol, triglycerides and low-density lipoprotein cholesterol increased significantly (P < 0.001) compared with normal control rats. All these changes were significantly prevented in the rats treated with Swertiamarin. Serum high-density lipoprotein (HDL) cholesterol was found to be reduced in the P-407 control rats. However, administration of Swertiamarin significantly (P < 0.01) increased HDL levels and it showed a significant lipid-lowering effect, as well as a high antiatherogenic potential.
    CONCLUSIONS:
    Overall Swertiamarin is an effective lipid-lowering lead compound and can be useful for preventing atherosclerosis.
    Fitoterapia. 2011 Sep;82(6):827-33.
    Effects of Swertia japonica extract and its main compound swertiamarin on gastric emptying and gastrointestinal motility in mice.[Pubmed: 21571047 ]
    The Swertia japonica is used clinically as a remedy for gastrointestinal symptoms in Japan.
    METHODS AND RESULTS:
    We examined the effects of a S. japonica and Swertiamarin on gastric emptying and gastrointestinal motility in atropine-, dopamine-, and 5-hydroxytryptamine (5-HT)-treated mice. All three preparations inhibited reductions in gastric emptying and gastrointestinal motility induced by dopamine (1mg/kg, intraperitoneal injection, ip). Neither the powder, Swertiamarin, nor itopride had any effect on the reductions in gastric emptying and gastrointestinal motility caused by 5-HT (4 mg/kg, ip).
    CONCLUSIONS:
    These findings suggest that the powder and Swertiamarin stimulate gastric emptying and gastrointestinal motility by inhibiting the dopamine D(2) receptor.
    Swertiamarin Description
    Source: The herbs of Swertia bimaculata.
    Solvent: DMSO, Pyridine, Methanol, Ethanol, etc.
    Storage: Providing storage is as stated on the product vial and the vial is kept tightly sealed, the product can be stored for up to 24 months(2-8C).

    Wherever 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 -20C. Generally, these will be useable for up to two weeks. Before use, and prior to opening the vial we recommend that you allow your product to equilibrate to room temperature for at least 1 hour.

    Need more advice on solubility, usage and handling? Please email to: service@chemfaces.com

    After receiving: The packaging of the product may have turned upside down during transportation, resulting in the natural compounds adhering to the neck or cap of the vial. take the vial out of its packaging and gently shake to let the compounds fall to the bottom of the vial. for liquid products, centrifuge at 200-500 RPM to gather the liquid at the bottom of the vial. try to avoid loss or contamination during handling.
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    Calculate Dilution Ratios(Only for Reference)
    1 mg 5 mg 10 mg 20 mg 25 mg
    1 mM 2.6717 mL 13.3583 mL 26.7165 mL 53.4331 mL 66.7913 mL
    5 mM 0.5343 mL 2.6717 mL 5.3433 mL 10.6866 mL 13.3583 mL
    10 mM 0.2672 mL 1.3358 mL 2.6717 mL 5.3433 mL 6.6791 mL
    50 mM 0.0534 mL 0.2672 mL 0.5343 mL 1.0687 mL 1.3358 mL
    100 mM 0.0267 mL 0.1336 mL 0.2672 mL 0.5343 mL 0.6679 mL
    * Note: If you are in the process of experiment, it's need to make the dilution ratios of the samples. The dilution data of the sheet for your reference. Normally, it's can get a better solubility within lower of Concentrations.
    Protocol
    Kinase Assay:
    Physiol Behav. 2015 May 15;144:66-72.
    Role of 5-HT2 receptors in diabetes: Swertiamarin seco-iridoid glycoside might be a possible 5-HT2 receptor modulator.[Pubmed: 25708274]
    In the present review, we are focusing on modulators of 5-HT2 receptors, Swertiamarin and their role in diabetes. These drugs possess both central and peripheral actions in various animal models of depression, diabetes and obesity.
    METHODS AND RESULTS:
    Swertiamarin and 5-HT2 antagonist are reported antidepressant, hypolipidemic and beneficial in peripheral vasculopathy. In contrast to this, 5-HT2C selective agonist decreases hyperglycemia, hyperlipidemia and insulin secretogogue by action. Selective serotonin reuptake inhibitors (SSRIs) are known antidepressant having weight gain as an adverse effect. Swertiamarin has similar pharmacological actions as 5-HT2 antagonist and 5-HT2C selective agonist. This warrants that Swertiamarin might modulate 5-HT2 receptors rather than affecting the uptake of serotonin.
    CONCLUSIONS:
    In the light of present investigation, the mechanism of these drugs can correlate the role of central and peripheral 5-HT2 receptors in diabetes.
    Eur J Pharm Sci. 2014 Jun 2;56:70-86.
    Swertiamarin attenuates inflammation mediators via modulating NF-κB/I κB and JAK2/STAT3 transcription factors in adjuvant induced arthritis.[Pubmed: 24582615]
    Rheumatoid arthritis (RA) is an autoimmune and chronic inflammatory disease that leads to pannus formation followed by severe joint destruction, characterized by synovial hyperplasia, inflammation and angiogenesis. Swertiamarin is a secoiridoid glycoside that is used as an anti-inflammatory compound, mainly found in Enicostema axillare (Lam) A. Raynal, a medicinal plant used in Indian system of traditional medicine.
    METHODS AND RESULTS:
    In the present study, the effect of Swertiamarin was evlauated in experimental adjuvant arthritis animal model by the estimation of biochemical (paw thickness, lysosomal enzymes, and urinary degradative products) parameters, proinflammatory cytokines and enzymes along with histopathological and radiographic observations. The proteins of phosphorylated NF-κB/IκB and JAK2/STAT3 transcription factors were also quantified from experimental animals as well as LPS induced RAW 264.7 macrophage cells. In in silico analysis, Swertiamarin was docked with proinflammatory enzymes to confirm its potential. The administration of Swertiamarin (2, 5, 10mg/kg bw) significantly (P⩽0.05) inhibited the levels of paw thickness, lysosomal enzymes and increased the body weight of experimental animals in a dose dependent manner. In molecular analysis, the treatment decreased the release of proinflammatory cytokines (IL1, TNF, IL-6) and proangiogenic enzymes (MMPs, iNOS, PGE2, PPARγ and COX-2); and also significantly (P⩽0.05) increased the levels of antiinflammatory proteins (IL-10, IL-4) when compared to the disease groups. The Swertiamarin treatment significantly (P⩽0.05) inhibited the release of NF-κB p65, p-IκBα, p-JAK2 and p-STAT3 signaling proteins levels on both experimental animals and LPS induced cells. Histopathological and radiological analysis evidenced the curative effect of Swertiamarin on bone destruction. The docking studies of Swertiamarin on proinflammatory enzymes supported the results from the in vivo experiments.
    CONCLUSIONS:
    Thus the Swertiamarin inhibited the development of arthritis by modulating NF-κB/IκB and JAK2/STAT3 signaling. These findings suggested that Swertiamarin acted as an anti-rheumatic agent.
    Animal Research:
    J Endocrinol Invest. 2015 Jun;38(6):669-84.
    Immunohistochemistry, histopathology, and biomarker studies of swertiamarin, a secoiridoid glycoside, prevents and protects streptozotocin-induced β-cell damage in Wistar rat pancreas.[Pubmed: 25770453]
    Diabetes mellitus is globally the major cause for metabolic syndrome in STZ-induced diabetic rats, leading to mortality. Treatment of diabetes by oral hypoglycemic agents causes adverse side effects and thus treatment with natural herbal drugs like Swertiamarin is promising. Swertiamarin, an active compound isolated from Enicostemma littorale possesses antidiabetic activity and enhances β cell regeneration which causes reversal of diabetes. The present study aims at the following: (1) to evaluate antidiabetic, anti-hyperlipidaemic, activity of Swertiamarin in Streptozotocin- induced diabetic rats using biomarkers. (2) To assess histopathological alterations in Pancreas, Liver, Kidney, and Heart of Swertiamarin-treated STZ-induced diabetic rats and confirm cytoprotective activity of Swertiamarin by Immunohistochemistry and morphometric investigations.
    METHODS AND RESULTS:
    Diabetes was induced intraperitoneally in male Wistar rats by Streptozotocin (STZ 50 mg/kg). After STZ-induction, hyperglycemic rats were treated with doses of Swertiamarin orally (15, 25, 50 mg/kg) each for 28 days. Glibenclamide (2.5 mg/kg), a sulphonyl urea, was used as a standard drug. The glycemic control was measured by the biochemical parameter assays. Histopathology analysis of organs and immunohistochemistry of islets were carried out. Our study results showed that oral administration of Swertiamarin at a dosage of 15, 25, 50 mg/kg bw for 28 days resulted in a significant (p < 0.01) decrease in fasting blood glucose, HbA1c, TC, TG, LDL, and increased the levels of hemoglobin, plasma insulin, TP, body weight, and HDL levels significantly (p < 0.01) when compared to STZ-induced diabetic rats, as confirmed by immunohistochemical studies. The effect of Swertiamarin on Carbohydrate-metabolizing enzymes was investigated and found to have normal therapeutic activity. Histopathological studies of Pancreas of Swertiamarin-treated diabetic rats showed regeneration of islets when compared to STZ-induced diabetic rats, as confirmed by immunohistochemical studies.
    CONCLUSIONS:
    Our research results clearly substantiate that Swertiamarin possesses antihyperglycemic, antihyperlipidemic, cytoprotective, and immune reactivity and also a broad spectrum potential of treating diabetes and other complications related to diabetes and hence can be developed into a potent oral antidiabetic drug.
    Phytomedicine. 2009 Mar;16(2-3):227-32.
    Antinociceptive activity of swertiamarin isolated from Enicostemma axillare.[Pubmed: 19019644 ]
    Many traditional Indian medicinal plants which contain large quantity of a secoiridoid, Swertiamarin are being used to relieve pain. Iridoids present in a wide variety of medicinal plants possess a large number of medicinal properties.
    METHODS AND RESULTS:
    In the present study in vivo antinociceptive activity of Swertiamarin isolated from E. axillare was carried out using three different methods in mice. In the hot plate method, a significant increase in the latency period was observed for the treatment with Swertiamarin at 100 and 200 mg/kg bw after 30 and 45 min. The percent protection observed after 45 min was 109.42, 147.42 and 157.14, respectively, for the standard paracetamol and Swertiamarin at 100 and 200 mg/kg bw treatments. A significant increase in the tail withdrawal reflex was observed for the Swertiamarin treatment at both the doses with percent protections of 150 and 200, respectively. In both these methods, Swertiamarin produced potent activity than that of standard paracetamol. In the acetic acid induced writhing, Swertiamarin at 100 and 200 mg/kg bw reduced the number of writhes significantly. Dose dependent results were observed in all the three methods and among the two doses, Swertiamarin at 200 mg/kg bw showed potent activity.
    CONCLUSIONS:
    These results prove that Swertiamarin possess both peripheral and central antinociceptive activity.