Development and validation of a LC-ESI–MS/MS method for the determination of swertiamarin in rat plasma and its application in pharmacokinetics

Li, Hongliang; Peng, Xiaojin; He, Juan; Feng, En-Fu; Xu, Gelin; Rao, G. Venkata

doi:10.1016/j.jchromb.2011.04.003

Cited by 19 publications

(13 citation statements)

References 11 publications

(21 reference statements)

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“…Protein precipitation with methanol or acetonitrile gave rise to severe matrix effects for the two analytes as found in previous studies [15,16]. Therefore, liquid‐liquid extraction was evaluated using various organic solvents including ethyl acetate, chloroform, and different ratios of ethyl acetate and isopropanol (5–95%, v/v ).…”

Section: Resultsmentioning

confidence: 95%

“…To date, several methods have been reported for the determination of gentiopicroside or swertiamarin in plant extracts based on capillary electrophoresis[10,11] HPLC[12–14] and liquid chromatography tandem mass spectrometry [15,16]. However, these methods suffer from long run time, the need for large volumes of biological samples and complicated sample preparation.…”

Section: Introductionmentioning

confidence: 99%

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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

Feng

Zhu

Guan

et al. 2014

Journal of Pharmacy and Pharmacology

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Section: Resultsmentioning

confidence: 95%

Section: Introductionmentioning

confidence: 99%

A rapid and sensitive UFLC-MS/MS method for the simultaneous determination of gentiopicroside and swertiamarin in rat plasma and its application in pharmacokinetics

Feng

Zhu

Guan

et al. 2014

Journal of Pharmacy and Pharmacology

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“…Swertiamarin (SM) is the major compound found in EL Blume and its pharmacokinetic study suggest that it is rapidly distributed in most of the tissues. Among all the tissues, the highest concentrations were found to be absorbed in the liver and its elimination was through kidney [16]. …”

Section: Introductionmentioning

confidence: 99%

Swertiamarin: An Active Lead fromEnicostemma littoraleRegulates Hepatic and Adipose Tissue Gene Expression by Targeting PPAR-γand Improves Insulin Sensitivity in Experimental NIDDM Rat Model

Patel

Soni

Parikh

et al. 2013

Evidence-Based Complementary and Alternative Medicine

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Enicostemma littorale (EL) Blume is one of the herbs widely used for treating and alleviating the effects of both type I and type II diabetes. However, lack of understanding of mechanism precludes the use of the herb and its molecules. In this study, we attempt to unravel the molecular mechanism of action of swertiamarin, a compound isolated form EL, by comparing its molecular effects with those of aqueous EL extract in alleviating the insulin resistance in type II diabetes. We further investigated hypolipidemic and insulin sensitizing effect of swertiamarin in experimentally induced noninsulin dependent diabetes mellitus (NIDDM) in rats. Swertiamarin (50 mg/kg) and aqueous extract (15 grams dried plant equivalent extract/kg) were administered to rats orally for 40 days and tight regulation of serum glucose, insulin, and lipid profile was found in both groups. Their mode of action was by restoring G6Pase and HMG-CoA reductase activities to normal levels and restoring normal transcriptional levels of PEPCK, GK, Glut 2, PPAR-γ, leptin, adiponectin, LPL, SREBP-1c, and Glut 4 genes. This suggests that both treatments increased insulin sensitivity and regulated carbohydrate and fat metabolism. This is the first report on the role of SM in regulating the PPARγ-mediated regulation of candidate genes involved in metabolism in peripheral tissues in vivo.

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“…1b ). An earlier publication [ 12 ] has discussed the MS condition of the analytes extensively, so we are not presenting this data. In a previous experiment, we developed a simple solid-phase extraction (SPE) method for the extraction of swertiamarin from rat plasma.…”

Section: Results and Discussion ▼ Lc-ms/ms And Sample Preparationmentioning

confidence: 99%

“…However, this method only reported a half-life for swertiamarin in rats ( n = 1 at each time point) after intravenous administration using arbitrary units derived from the peak area ratio of swertiamarin to the internal standard. Therefore, we developed a new LC-MS/MS method for the quantification of swertiamarin and successfully applied it to a pharmacokinetic study of swertiamarin in rats after oral administration [ 12 ] . Until now, no data have been reported on its absolute bioavailability and distribution in tissues.…”

Section: Determination Of the Plasma Pharmacokinetic And Tissue Distrmentioning

confidence: 99%

Determination of the Plasma Pharmacokinetic and Tissue Distributions of Swertiamarin in Rats by Liquid Chromatography with Tandem Mass Spectrometry

Bai

et al. 2012

Arzneimittelforschung

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An LC-MS/MS method was developed for the quantification of swertiamarin (CAS 17388-39-5) in rat plasma and tissues using gentiopicroside as the internal standard (IS). Swertiamarin and an IS were extracted from plasma and tissues by a simple solid-phase extraction (SPE) procedure. Separation was achieved on a Phenomenex kinetex-C18 column (100 mm×2.1 mm, 2.6 µm) with an isocratic mobile phase consisting of methanol and water (22:78, v/v) with 0.1% acetic acid at a flow rate of 0.2 mL/min. The analyte and IS were detected by negative ion electrospray ionisation in multiple-reaction monitoring mode while monitoring the transitions of m/z 433 [M + CH3COO] - →179 and m/z 415 [M + CH3COO] - →179 for swertiamarin and the IS, respectively. The method was validated with respect to selectivity, matrix effect, linearity, accuracy, precision, recovery and stability. The method was successfully applied in a pharmacokinetic study of swertiamarin after intravenous and oral administration to rats. The pharmacokinetics of swertiamarin showed rapid absorption and elimination, and its absolute bioavailability was low at 10.3%. After oral administration to rats, swertiamarin was rapidly and widely distributed in its tissues. High concentrations were found in the liver and kidney, indicating that swertiamarin was possibly absorbed in the liver and eliminated by the kidney.

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Development and validation of a LC-ESI–MS/MS method for the determination of swertiamarin in rat plasma and its application in pharmacokinetics

Cited by 19 publications

References 11 publications

A rapid and sensitive UFLC-MS/MS method for the simultaneous determination of gentiopicroside and swertiamarin in rat plasma and its application in pharmacokinetics

A rapid and sensitive UFLC-MS/MS method for the simultaneous determination of gentiopicroside and swertiamarin in rat plasma and its application in pharmacokinetics

Swertiamarin: An Active Lead fromEnicostemma littoraleRegulates Hepatic and Adipose Tissue Gene Expression by Targeting PPAR-γand Improves Insulin Sensitivity in Experimental NIDDM Rat Model

Determination of the Plasma Pharmacokinetic and Tissue Distributions of Swertiamarin in Rats by Liquid Chromatography with Tandem Mass Spectrometry

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