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Ramesh K. Goyal - One of the best experts on this subject based on the ideXlab platform.
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Role of 5-HT2 receptors in diabetes: Swertiamarin seco-iridoid glycoside might be a possible 5-HT2 receptor modulator
Physiology & Behavior, 2015Co-Authors: Rakesh Deelip Sonawane, Vijaykumar B. Deore, Savita D Patil, Sanjay J Surana, Chandragouda R Patil, Ramesh K. GoyalAbstract: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. 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. In the light of present investigation, the mechanism of these drugs can correlate the role of central and peripheral 5-HT2 receptors in diabetes.
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anti diabetic activity of Swertiamarin is due to an active metabolite gentianine that upregulates ppar γ gene expression in 3t3 l1 cells
Phytotherapy Research, 2013Co-Authors: Hitesh Vaidya, Ramesh K. Goyal, Sukhinder K CheemaAbstract: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. 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. 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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beneficial effects of Swertiamarin on dyslipidaemia in streptozotocin induced type 2 diabetic rats
Phytotherapy Research, 2012Co-Authors: Hitesh Vaidya, M. Rajani, V. Sudarsanam, Harish Padh, Alpesh Prajapati, Ramesh K. GoyalAbstract:Dyslipidaemia is one of the major risk factors for cardiovascular disease in diabetes mellitus. Lipid changes associated with diabetes mellitus are attributed to increases in free fatty acid flux, secondary to insulin resistance. In the present study, we have investigated the beneficial effects of Swertiamarin on dyslipidaemic conditions associated with type 2 diabetes in streptozotocin-induced type 2 diabetic rats. Swertiamarin (50 mg/kg, i.p.) administered once a day for 6 weeks resulted in significant (p < 0.001) reductions in serum triglycerides, cholesterol and low-density lipoprotein levels in diabetic animals as compared with diabetic control animals. Serum fasting glucose was significantly (p < 0.05) decreased, moreover, the insulin sensitivity index was significantly (p < 0.05) increased in Swertiamarin treated animals. Overall the data suggest that Swertiamarin has beneficial effects on diabetic associated complications such as dyslipidaemia. Copyright © 2012 John Wiley & Sons, Ltd.
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Beneficial effects of Swertiamarin on dyslipidaemia in streptozotocin-induced type 2 diabetic rats.
Phytotherapy research : PTR, 2012Co-Authors: Hitesh Vaidya, M. Rajani, V. Sudarsanam, Harish Padh, Alpesh Prajapati, Ramesh K. GoyalAbstract:Dyslipidaemia is one of the major risk factors for cardiovascular disease in diabetes mellitus. Lipid changes associated with diabetes mellitus are attributed to increases in free fatty acid flux, secondary to insulin resistance. In the present study, we have investigated the beneficial effects of Swertiamarin on dyslipidaemic conditions associated with type 2 diabetes in streptozotocin-induced type 2 diabetic rats. Swertiamarin (50 mg/kg, i.p.) administered once a day for 6 weeks resulted in significant (p
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Amelioration of STZ-induced type 1 diabetic nephropathy by aqueous extract of Enicostemma littorale Blume and Swertiamarin in rats
Molecular and Cellular Biochemistry, 2010Co-Authors: Rakesh D. Sonawane, Harish Padh, Santosh L. Vishwakarma, S. Lakshmi, Mandapati Rajani, Ramesh K. GoyalAbstract:Diabetic nephropathy (DN) is one of the foremost causes of renal failure and a primary cause of diabetes mellitus related death. Previously, we have reported that aqueous extract of Enicostemma littorale has potential antidiabetic activity. In the present study, we have investigated the effect of aqueous extract of E. littorale 1 g/kg, p.o. and Swertiamarin 50 mg/kg, p.o. daily for 3 weeks in type 1 DN complications in SD rats. DN was assessed by serum urea, creatinine, lipid profile and water intake levels. Treatment with aqueous extract of E. littorale and Swertiamarin significantly decreased serum urea and creatinine and other parameters associated with the development of DN in type 1 diabetic rats. We have also found considerable improvement in histology of glomerular function of aqueous extract of E. littorale and Swertiamarin-treated animals.
Hitesh Vaidya - One of the best experts on this subject based on the ideXlab platform.
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anti diabetic activity of Swertiamarin is due to an active metabolite gentianine that upregulates ppar γ gene expression in 3t3 l1 cells
Phytotherapy Research, 2013Co-Authors: Hitesh Vaidya, Ramesh K. Goyal, Sukhinder K CheemaAbstract: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. 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. 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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beneficial effects of Swertiamarin on dyslipidaemia in streptozotocin induced type 2 diabetic rats
Phytotherapy Research, 2012Co-Authors: Hitesh Vaidya, M. Rajani, V. Sudarsanam, Harish Padh, Alpesh Prajapati, Ramesh K. GoyalAbstract:Dyslipidaemia is one of the major risk factors for cardiovascular disease in diabetes mellitus. Lipid changes associated with diabetes mellitus are attributed to increases in free fatty acid flux, secondary to insulin resistance. In the present study, we have investigated the beneficial effects of Swertiamarin on dyslipidaemic conditions associated with type 2 diabetes in streptozotocin-induced type 2 diabetic rats. Swertiamarin (50 mg/kg, i.p.) administered once a day for 6 weeks resulted in significant (p < 0.001) reductions in serum triglycerides, cholesterol and low-density lipoprotein levels in diabetic animals as compared with diabetic control animals. Serum fasting glucose was significantly (p < 0.05) decreased, moreover, the insulin sensitivity index was significantly (p < 0.05) increased in Swertiamarin treated animals. Overall the data suggest that Swertiamarin has beneficial effects on diabetic associated complications such as dyslipidaemia. Copyright © 2012 John Wiley & Sons, Ltd.
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Beneficial effects of Swertiamarin on dyslipidaemia in streptozotocin-induced type 2 diabetic rats.
Phytotherapy research : PTR, 2012Co-Authors: Hitesh Vaidya, M. Rajani, V. Sudarsanam, Harish Padh, Alpesh Prajapati, Ramesh K. GoyalAbstract:Dyslipidaemia is one of the major risk factors for cardiovascular disease in diabetes mellitus. Lipid changes associated with diabetes mellitus are attributed to increases in free fatty acid flux, secondary to insulin resistance. In the present study, we have investigated the beneficial effects of Swertiamarin on dyslipidaemic conditions associated with type 2 diabetes in streptozotocin-induced type 2 diabetic rats. Swertiamarin (50 mg/kg, i.p.) administered once a day for 6 weeks resulted in significant (p
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decrease in serum matrix metalloproteinase 9 and matrix metalloproteinase 3 levels in zucker fa fa obese rats after treatment with Swertiamarin
Experimental & Clinical Cardiology, 2012Co-Authors: Hitesh Vaidya, S Giri, M Jain, R K GoyalAbstract:Diabetes mellitus encompasses a group of chronic metabolic conditions associated with cardiovascular complications such as atherosclerosis, cardiomyopathy and nephropathy. In the present study, the authors investigated the beneficial effects of Swertiamarin in diabetes and its associated cardiovascular complications in Zucker fa/fa rats. Six male Zucker fa/fa rats in each group were treated for 28 days with Swertiamarin (75 mg/kg/day, intraperitoneally) or pioglitazone (30 mg/kg orally). Blood samples were collected and evaluated for several parameters. Elevated serum glucose, triglyceride, nonesterified free-fatty acid and cholesterol levels were found in untreated Zucker fa/fa rats. Serum matrix metalloproteinase (MMP)-9 and MMP-3 levels were also found to be significantly higher in untreated Zucker fa/fa rats. Treatment with Swertiamarin significantly (P<0.05) reduced serum glucose, triglyceride, nonesterified free-fatty acid and cholesterol levels, and also reduced serum MMP-9 and MMP-3 levels compared with untreated rats. Swertiamarin also significantly (P<0.05) decreased serum levels of urea compared with untreated Zucker fa/fa rats. Overall, the data suggest that Swertiamarin produced beneficial effects with respect to diabetes-induced cardiovascular complications such as atherosclerosis and nephropathy. A Swertiamarin-induced decrease in serum MMP-9 and MMP-3 levels is one of the possible mechanisms responsible for improvement of these complications.
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Decrease in serum matrix metalloproteinase-9 and matrix metalloproteinase-3 levels in Zucker fa/fa obese rats after treatment with Swertiamarin.
Experimental and clinical cardiology, 2012Co-Authors: Hitesh Vaidya, S Giri, M Jain, R K GoyalAbstract:Diabetes mellitus encompasses a group of chronic metabolic conditions associated with cardiovascular complications such as atherosclerosis, cardiomyopathy and nephropathy. In the present study, the authors investigated the beneficial effects of Swertiamarin in diabetes and its associated cardiovascular complications in Zucker fa/fa rats. Six male Zucker fa/fa rats in each group were treated for 28 days with Swertiamarin (75 mg/kg/day, intraperitoneally) or pioglitazone (30 mg/kg orally). Blood samples were collected and evaluated for several parameters. Elevated serum glucose, triglyceride, nonesterified free-fatty acid and cholesterol levels were found in untreated Zucker fa/fa rats. Serum matrix metalloproteinase (MMP)-9 and MMP-3 levels were also found to be significantly higher in untreated Zucker fa/fa rats. Treatment with Swertiamarin significantly (P
Savarimuthu Ignacimuthu - One of the best experts on this subject based on the ideXlab platform.
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Swertiamarin a natural steroid prevent bone erosion by modulating rankl rank opg signaling
International Immunopharmacology, 2017Co-Authors: M I Hairulislam, Krishnaraj Thirugnanasambantham, S. Saravanan, Muthiah Chellappandian, Simon Durai C Raj, Gabriel M Paulraj, Kulandaivelu Karikalan, Savarimuthu IgnacimuthuAbstract:Bone erosion is a central feature of rheumatoid arthritis (RA) that is characterized by the infiltration of the synovial lining by osteoclasts and lymphocytes. In the present study, Swertiamarin a major secoiridoid glycoside was evaluated for anti-osteoclastogenic property to prevent bone erosion in Freund's complete adjuvant (FCA) induced in-vivo model, in-vitro osteoblast and osteoclasts as well as in co-culture system and in-silico molecular docking analysis. The Swertiamarin treatment decreased the expression of TRAP, RANKL, and RANK levels and increased the levels of OPG levels significantly in both in vitro and in vivo models. In in vitro, the compound treatment significantly increased the cell proliferation and ALP levels in osteoblast cells; the high proliferation (153.8600±5.23%) and ALP release (165.6033±4.13%) were observed at 50μg/ml concentration of Swertiamarin treatment. At the same time the treatment decreased the TRAP positive cells in osteoclast cells; the high reductions of TRAP positive cells (39.32±3.19%) were observed at 50μg/ml of Swertiamarin treatment. The treatment modulated the levels of pro-inflammatory cytokines, MMPs and NF-κB levels in osteoblast and osteoclast co-culture system. In in silico analysis Swertiamarin had affinity towards the proteins RANK, RANKL and OPG residues with low binding energy -4.5, -3.92 and -5.77kcal/mol respectively. Thus, the results of this study revealed the anti-osteoclastogenic activity of Swertiamarin on the prevention of bone destruction.
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Swertiamarin, a natural steroid, prevent bone erosion by modulating RANKL/RANK/OPG signaling
International immunopharmacology, 2017Co-Authors: M.i. Hairul-islam, M. Gabriel Paulraj, Krishnaraj Thirugnanasambantham, S. Saravanan, Muthiah Chellappandian, C. Simon Durai Raj, Kulandaivelu Karikalan, Savarimuthu IgnacimuthuAbstract:Bone erosion is a central feature of rheumatoid arthritis (RA) that is characterized by the infiltration of the synovial lining by osteoclasts and lymphocytes. In the present study, Swertiamarin a major secoiridoid glycoside was evaluated for anti-osteoclastogenic property to prevent bone erosion in Freund's complete adjuvant (FCA) induced in-vivo model, in-vitro osteoblast and osteoclasts as well as in co-culture system and in-silico molecular docking analysis. The Swertiamarin treatment decreased the expression of TRAP, RANKL, and RANK levels and increased the levels of OPG levels significantly in both in vitro and in vivo models. In in vitro, the compound treatment significantly increased the cell proliferation and ALP levels in osteoblast cells; the high proliferation (153.8600±5.23%) and ALP release (165.6033±4.13%) were observed at 50μg/ml concentration of Swertiamarin treatment. At the same time the treatment decreased the TRAP positive cells in osteoclast cells; the high reductions of TRAP positive cells (39.32±3.19%) were observed at 50μg/ml of Swertiamarin treatment. The treatment modulated the levels of pro-inflammatory cytokines, MMPs and NF-κB levels in osteoblast and osteoclast co-culture system. In in silico analysis Swertiamarin had affinity towards the proteins RANK, RANKL and OPG residues with low binding energy -4.5, -3.92 and -5.77kcal/mol respectively. Thus, the results of this study revealed the anti-osteoclastogenic activity of Swertiamarin on the prevention of bone destruction.
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In Vivo and In Vitro Immunomodulatory Potential of Swertiamarin Isolated from Enicostema axillare (Lam.) A. Raynal That Acts as an Anti-inflammatory Agent
Inflammation, 2014Co-Authors: S. Saravanan, V. I. Hairul Islam, M. Gabriel Paulraj, Keshava Balakrishna, Krishnaraj Thirugnanasambantham, Perumal Pandikumar, N. Prakash Babu, Savarimuthu IgnacimuthuAbstract:Swertiamarin is a secoiridoid glycoside found in Enicostema axillare (Lam) A. Raynal, a medicinal plant used as a depurative in the Indian system of traditional medicine. The present study evaluated the immunomodulatory activity of isolated Swertiamarin. In vivo immunomodulatory activity of Swertiamarin (2, 5, and 10 mg/kg b.w.) was evaluated in a model of sheep red blood cells (SRBC) by assessing its effect on organ weight, hemagglutinating antibody titer (HA), plaque-forming cells (PFC), quantitative hemolysis of SRBC, and delayed type hypersensitivity (DTH). In vitro immunomodulatory potential was studied on isolated splenocytes, neutrophils, and peritoneal macrophages. In silico immunomodulatory effects were evaluated by docking of Swertiamarin on proinflammatory cytokines to confirm its potential. In in vivo studies, the animals treated with Swertiamarin showed a significant ( P ≤ 0.05) increase in antibody titer, plaque-forming cells, and also in weight of the thymus and spleen. A decreased response to DTH reaction was recorded with the treatment of Swertiamarin. In in vitro studies, treatment with Swertiamarin modulated the messenger RNA (mRNA) and protein expression of IFN-γ, IL-10, and IL-4 significantly ( P ≤ 0.05) and also favored Th2-mediated response on concanavalin A (Con A)-induced splenocytes. The compound inhibited the release of free radicals significantly ( P ≤ 0.05) in phytohemagglutinin (PHA)-induced neutrophils and also ameliorated the mRNA and protein expression of proinflammatory cytokines (TNF-α, IL-1β, and IL-6) in lipopolysaccharide (LPS)-induced macrophages. In in silico , the best docked pose of Swertiamarin with the target proteins (TNF-α, IL-1β, and IL-6) was confirmed that Swertiamarin acted as an anti-inflammatory mediator.
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Swertiamarin attenuates inflammation mediators via modulating nf κb i κb and jak2 stat3 transcription factors in adjuvant induced arthritis
European Journal of Pharmaceutical Sciences, 2014Co-Authors: S. Saravanan, Krishnaraj Thirugnanasambantham, Perumal Pandikumar, Savarimuthu Ignacimuthu, V Hairul I Islam, Prakash N Babu, Muthiah Chellappandian, Simon Durai C Raj, Gabriel M PaulrajAbstract: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. 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. 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.
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Swertiamarin ameliorates inflammation and osteoclastogenesis intermediates in IL-1β induced rat fibroblast-like synoviocytes
Inflammation Research, 2014Co-Authors: S. Saravanan, Krishnaraj Thirugnanasambantham, V. I. Hairul Islam, N. Pazhanivel, N. Raghuraman, M. Gabriel Paulraj, Savarimuthu IgnacimuthuAbstract:Objective and design Rheumatoid arthritis is a chronic inflammatory and autoimmune disease that leads to aggressive joint cartilage and bone destruction. Swertiamarin is a secoiridoid glycoside found in Enicostema axillare (Lam) A. Raynal, a medicinal plant used in the Indian system of traditional medicine. In the present study, the potential of Swertiamarin was evaluated in IL-1β induced fibroblast-like synoviocytes (FLS). Methods The FLS were isolated from Freund’s Complete Adjuvant induced arthritic (AA) rats and cultured with IL-1β. The normal FLS and AA-FLS were cultured and used for subsequent experiment in fibroblastic morphology form. The efficacy of Swertiamarin (10–50 μg/ml) was evaluated on mRNA and protein expression levels of inflammatory and osteoclastogenesis mediators. The efficacy was also evaluated on p38 MAPKα levels with time course studies (2, 4, 6, 8 and 12 h). Results IL-1β induced cell proliferation (149.46 ± 13.73 %) and NO production (162.03 ± 11.03 %) in AA-FLS; treatment with Swertiamarin controlled proliferation (82.77 ± 4.22 %) and NO production (82.06 ± 3.91 % at 50 μg/ml) in a dose-dependent manner. It also significantly ( P
Wenshu Liu - One of the best experts on this subject based on the ideXlab platform.
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a rapid and sensitive uflc ms ms method for the simultaneous determination of gentiopicroside and Swertiamarin in rat plasma and its application in pharmacokinetics
Journal of Pharmacy and Pharmacology, 2014Co-Authors: Bo Feng, Heyun Zhu, Jiao Guan, Longshan Zhao, Lei Yin, Paul J Fawcett, Wenshu LiuAbstract:Objectives Radix Gentianae is a traditional Chinese medicine derived from medicinal plants of the family Gentianaceae. Its pharmacological effects have been primarily attributed to the presence of a number of secoiridoid glycosides, in particular gentiopicroside and Swertiamarin. In this study, a rapid and sensitive method based on ultrafast liquid chromatography-tandem mass spectrometry has been developed for the simultaneous determination of gentiopicroside and Swertiamarin in rat plasma using paeoniflorin as internal standard (IS). Methods After liquid-liquid extraction with ethyl acetate-isopropanol (95 : 5, v/v), separation was achieved on a Shim-pack XR-ODS C18 column (75 mm × 3.0 mm, 2.2 μm) with a mobile phase consisting of methanol : 0.1% formic acid (30 : 70, v/v) at a flow rate of 0.4 ml/min. Detection on an API 3200 QTRAP mass spectrometer equipped with an electrospray ionization source operated in the negative ionization mode was performed by multiple reaction monitoring of the precursor-to-product ion transitions of gentiopicroside, Swertiamarin and IS at m/z 401.0 → 179.0, 419.0 → 179.1 and 525.1 → 121.0 respectively. The calibration curves were linear over the concentration range of 20–10 000 and 2–1000 ng/ml for gentiopicroside and Swertiamarin with corresponding lower limits of quantification of 20 and 2 ng/ml. The limits of detection were 4 and 0.5 ng/ml for gentiopicroside and Swertiamarin, respectively. The intraday and interday precisions were below 11.9% for gentiopicroside and below 9.5% for Swertiamarin in terms of relative standard deviation, and the accuracy was within ±8.3% for gentiopicroside and within ±10.2% for Swertiamarin in terms of relative error. Extraction recovery, matrix effect and stability were satisfactory in rat plasma. The method was fully validated and applied to a pharmacokinetic study involving oral administration of a Radix Gentianae extract to groups of male and female rats. Key findings Results showed that in female rats, both compounds were absorbed to a greater extent and eliminated more slowly than in male rats, although the rate of absorption was similar in the two groups. Conclusions There were remarkable differences in pharmacokinetic properties of gentiopicroside and Swertiamarin between male and female rats. The results will provide helpful information for the development of suitable dosage forms and clinical references on rational administration.
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A rapid and sensitive UFLC‐MS/MS method for the simultaneous determination of gentiopicroside and Swertiamarin in rat plasma and its application in pharmacokinetics
The Journal of pharmacy and pharmacology, 2014Co-Authors: Bo Feng, Heyun Zhu, Jiao Guan, Longshan Zhao, Lei Yin, J. Paul Fawcett, Wenshu LiuAbstract:Objectives Radix Gentianae is a traditional Chinese medicine derived from medicinal plants of the family Gentianaceae. Its pharmacological effects have been primarily attributed to the presence of a number of secoiridoid glycosides, in particular gentiopicroside and Swertiamarin. In this study, a rapid and sensitive method based on ultrafast liquid chromatography-tandem mass spectrometry has been developed for the simultaneous determination of gentiopicroside and Swertiamarin in rat plasma using paeoniflorin as internal standard (IS). Methods After liquid-liquid extraction with ethyl acetate-isopropanol (95 : 5, v/v), separation was achieved on a Shim-pack XR-ODS C18 column (75 mm × 3.0 mm, 2.2 μm) with a mobile phase consisting of methanol : 0.1% formic acid (30 : 70, v/v) at a flow rate of 0.4 ml/min. Detection on an API 3200 QTRAP mass spectrometer equipped with an electrospray ionization source operated in the negative ionization mode was performed by multiple reaction monitoring of the precursor-to-product ion transitions of gentiopicroside, Swertiamarin and IS at m/z 401.0 → 179.0, 419.0 → 179.1 and 525.1 → 121.0 respectively. The calibration curves were linear over the concentration range of 20–10 000 and 2–1000 ng/ml for gentiopicroside and Swertiamarin with corresponding lower limits of quantification of 20 and 2 ng/ml. The limits of detection were 4 and 0.5 ng/ml for gentiopicroside and Swertiamarin, respectively. The intraday and interday precisions were below 11.9% for gentiopicroside and below 9.5% for Swertiamarin in terms of relative standard deviation, and the accuracy was within ±8.3% for gentiopicroside and within ±10.2% for Swertiamarin in terms of relative error. Extraction recovery, matrix effect and stability were satisfactory in rat plasma. The method was fully validated and applied to a pharmacokinetic study involving oral administration of a Radix Gentianae extract to groups of male and female rats. Key findings Results showed that in female rats, both compounds were absorbed to a greater extent and eliminated more slowly than in male rats, although the rate of absorption was similar in the two groups. Conclusions There were remarkable differences in pharmacokinetic properties of gentiopicroside and Swertiamarin between male and female rats. The results will provide helpful information for the development of suitable dosage forms and clinical references on rational administration.
M. Rajani - One of the best experts on this subject based on the ideXlab platform.
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beneficial effects of Swertiamarin on dyslipidaemia in streptozotocin induced type 2 diabetic rats
Phytotherapy Research, 2012Co-Authors: Hitesh Vaidya, M. Rajani, V. Sudarsanam, Harish Padh, Alpesh Prajapati, Ramesh K. GoyalAbstract:Dyslipidaemia is one of the major risk factors for cardiovascular disease in diabetes mellitus. Lipid changes associated with diabetes mellitus are attributed to increases in free fatty acid flux, secondary to insulin resistance. In the present study, we have investigated the beneficial effects of Swertiamarin on dyslipidaemic conditions associated with type 2 diabetes in streptozotocin-induced type 2 diabetic rats. Swertiamarin (50 mg/kg, i.p.) administered once a day for 6 weeks resulted in significant (p < 0.001) reductions in serum triglycerides, cholesterol and low-density lipoprotein levels in diabetic animals as compared with diabetic control animals. Serum fasting glucose was significantly (p < 0.05) decreased, moreover, the insulin sensitivity index was significantly (p < 0.05) increased in Swertiamarin treated animals. Overall the data suggest that Swertiamarin has beneficial effects on diabetic associated complications such as dyslipidaemia. Copyright © 2012 John Wiley & Sons, Ltd.
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Beneficial effects of Swertiamarin on dyslipidaemia in streptozotocin-induced type 2 diabetic rats.
Phytotherapy research : PTR, 2012Co-Authors: Hitesh Vaidya, M. Rajani, V. Sudarsanam, Harish Padh, Alpesh Prajapati, Ramesh K. GoyalAbstract:Dyslipidaemia is one of the major risk factors for cardiovascular disease in diabetes mellitus. Lipid changes associated with diabetes mellitus are attributed to increases in free fatty acid flux, secondary to insulin resistance. In the present study, we have investigated the beneficial effects of Swertiamarin on dyslipidaemic conditions associated with type 2 diabetes in streptozotocin-induced type 2 diabetic rats. Swertiamarin (50 mg/kg, i.p.) administered once a day for 6 weeks resulted in significant (p
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antihyperlipidaemic activity of Swertiamarin a secoiridoid glycoside in poloxamer 407 induced hyperlipidaemic rats
Journal of Natural Medicines, 2009Co-Authors: Hitesh Vaidya, M. Rajani, V. Sudarsanam, Harish Padh, Ramesh K. GoyalAbstract: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. Overall Swertiamarin is an effective lipid-lowering lead compound and can be useful for preventing atherosclerosis.
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Swertiamarin: A lead from Enicostemma littorale Blume. for anti-hyperlipidaemic effect
European Journal of Pharmacology, 2009Co-Authors: Hitesh Vaidya, M. Rajani, V. Sudarsanam, Harish Padh, Ramesh K. GoyalAbstract:We have investigated the hypolipidemic effects of Swertiamarin an active lead isolated from a perennial herb Enicostemma littorale Blume. in high cholesterol fed rats. Swertiamarin (50 and 75 mg/kg) and atorvastatin (50 mg/kg) was given orally daily for seven consecutive day to the high cholesterol feed rats. Serum total cholesterol, triglycerides, low density lipoprotein and very low density lipoprotein were found to be markedly elevated in the high cholesterol fed control rats and these changes were significantly prevented in Swertiamarin treated animals. However, there was no significant effect on serum high density lipoprotein level. The 3-hydroxy 3-methyl glutaryl Co A (HMG-Co A) reductase activity was significantly inhibited in Swertiamarin and atorvastatin treated groups compared to high cholesterol fed control group. Swertiamarin was also found to increased excretion of fecal bile acid and total sterols compared to control animals. In conclusion our data suggest that Swertiamarin possess high antiatherogenic potential and an effective cholesterol lowering agent and inhibition of HMG-Co A reductase may be one of the main mechanisms of hypolipidemic effect of Swertiamarin.
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A Sensitive HPTLC method for Estimation of Swertiamarin in Enicostemma littorale Blume, Swertia chirata (Wall) Clarke, and in formulations containing E. littorale
JPC – Journal of Planar Chromatography – Modern TLC, 2004Co-Authors: Santosh L. Vishwakarma, M. Rajani, Milind S. Bagul, Ramesh K. GoyalAbstract:Swertiamarin is a secoiridoid glucoside present in members of the Gentianaceae family, including Swertia chirata (Wall) Clarke, S. japonica Makino, S. angustifolia Buch.-Ham.ex D. Don, and Enicostemma littorale Blume. It has antidepressant and anticholinergic activity and can thus be used as a biomarker. We have developed a simple HPTLC method for quantification of Swertiamarin which can be used for analysis of plant materials and formulations to determine Swertiamarin content. The method was validated for precision, repeatability, and accuracy and found to be precise; intraand inter-day relative standard deviations ( RSD ) were in the ranges 0.68 to 0.85 and 0.71 to 1.03, respectively, for two different concentrations. Instrumental precision and repeatability of the method were 0.95 and 0.69 (% CV ), respectively. The accuracy of the method was checked by determination of recovery at two different levels and the average recovery was found to be 100.13%. The method was used for estimation of the Swertiamarin content of whole plants of E. littorale and S. chirata and of herbal formulations containing E. littorale as an ingredient. The method requires no clean-up of sample extracts before TLC and Swertiamarin was well resolved from other components of the extracts. The method is simple, precise, specific, sensitive, and accurate and can be used for routine quality control of raw materials and herbal formulations. The method is suitable for quantification of Swertiamarin in samples containing amounts ranging from 0.15 to 7.7% (w/w). E. littorale whole plant was found to be a rich source of Swertiamarin (7.7% w/w ).
