| 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. |
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| 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. |
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