SWERTISIN/SWERTISIN(P)/4H-1-Benzopyran-4-one, 6-(β-D-glucopyranosyloxy)-5-hydroxy-2-(4-hydroxyphenyl)-7-methoxy-/Sorbifolin 6-O-β-glucopyranoside/apigenin-7-methylether-6-C-glucoside/6-C-glucopyranosyl-7-O-methylapigenin/7-O-methylapigenin mono-6-C-glucoside/5-Hydroxy-2-(4-hydroxyphenyl)-7-methoxy-4-oxo-4H-chromen-6-yl β-D-glucopyranoside
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provides coniferyl ferulate(CAS#:6991-10-2) MSDS, density, melting point, boiling point, structure, formula, molecular weight etc. Articles of coniferyl ferulate are included as well.>> amp version: coniferyl ferulate
A sensitive and reliable high-performance liquid chromatography with tandem mass spectrometry was developed and validated for the quantification of swertisin in rat plasma. The samples were prepared with methanol by protein precipitation. Swertisin was separated by using an Agilent Poroshell 120 EC-C18 column (4.6 mm × 50 mm, 2.7 μm) with the mobile phase consisted of acetonitrile and water containing 0.1% formic acid running at a flow rate of 0.3 mL/min for 5 min. The analytes were detected with the multiple reaction monitoring in the negative electrospray ionization source for quantitative response of swertisin [M-H]- (445.1→281.7) and puerarin (internal standard) [M-H]- (415.1→295.0). Precision (relative standard deviation, RSD%) of the inter-day and the intra-day was <9.89% and 11.34% while accuracy (relative error, RE%) ranged from -6.01% to 4.92% and -3.97% to 4.39%, respectively. Interestingly, the expression of the γ-aminobutyric acid (GABA) receptor subunits (GABAAα1, GABAAα5 and GABAAβ1) mRNAs was enhanced in the rat hippocampal neurons treated with swertisin as analyzed by real-time polymerase chain reaction. Moreover, the method was successfully applied to determine the pharmacokinetic of swertisin in rats after tail vein injection with 4.0 mg/kg of the compound. Our results provide useful pharmacokinetic information for swertisin in vivo and suggest that the sedative function of this compound may be through inducing the expression of the GABAA receptor subunits. © Crown copyright 2016.
Pharmacokinetic Study of Swertisin by HPLC-MS/MS After Intravenous Administration in Rats.
Li Y1, Zhao X1, Zhang Y1,2, Xie J3,2, Zhang K1,2, Zhou A1.
Swertisin, a plant-derived C-glucosylflavone, is known to have antidiabetic, anti-inflammatory and antioxidant effects. In the present study, we investigated in mice the effects of swertisin on glutamatergic dysfunction induced by dizocilpine (MK-801), a non-competitive N-methyl-D-aspartate receptor antagonist. In the Acoustic Startle Response test, their MK-801-induced (given 0.2 mg/kg i.p.) pre-pulse inhibition deficit was significantly attenuated by the administration of swertisin (30 mg/kg p.o.). In the Novel Object Recognition Test, the recognition memory impairments that were induced by MK-801 (0.2 mg/kg, given i.p.) were also reversed by administration of swertisin (30 mg/kg p.o.). In addition, swertisin normalized the MK-801-induced elevation of phosphorylation levels of Akt and GSK-3β signaling molecules in the prefrontal cortex. These results indicated that swertisin may be useful in managing the symptoms of schizophrenia, including sensorimotor gating disruption and cognitive impairment, and that these behavioral outcomes may be related to Akt-GSK-3β signaling in the prefrontal cortex.
Cognitive impairment; mechanism of action; mouse study; pharmacological treatment; prepulse inhibition; schizophrenia; sensorimotor gating; startle response; swertisin
Swertisin ameliorates pre-pulse inhibition deficits and cognitive impairment induced by MK-801 in mice.
Oh HK1,2, Jeon SJ3,4, Lee S3,4, Lee HE3,4, Kim E3,4, Park SJ3,4, Kim HN3,4, Jung WY1, Cheong JH5, Jang DS3,4, Ryu JH1,3,4.
Swertisin, a C-glucosylflavone isolated from Swertia japonica, has been known to have anti-inflammatory or antidiabetic activities. Until yet, however, its cognitive function is not investigated. In the present study, we endeavored to elucidate the effects of swertisin on cholinergic blockade-induced memory impairment. Swertisin (5 or 10mg/kg, p.o.) significantly ameliorated scopolamine-induced cognitive impairment in the several behavioral tasks. Also, single administration of swertisin (10mg/kg, p.o.) in normal naïve mice enhanced the latency time in the passive avoidance task. In addition, the ameliorating effect of swertisin on scopolamine-induced memory impairment was significantly antagonized by a sub-effective dose of N6-cyclopentyladenosine (CPA, 0.1mg/kg, i.p). The adenosine A1 receptor antagonistic property of swertisin was confirmed by receptor binding assay. Furthermore, the administration of swertisin significantly increased the phosphorylation levels of hippocampal or cortical protein kinase A (PKA, 5 or 10mg/kg) and CREB (10mg/kg), and co-administration of CPA (0.1mg/kg, i.p) blocked the increased phosphorylated levels of PKA and CREB in the both cortex and hippocampus. Taken together, these results indicate that the memory-ameliorating effects of swertisin may be, in part, mediated through the adenosinergic neurotransmitter system, and that swertisin may be useful for the treatment of cognitive dysfunction observed in several diseases such as Alzheimer’s disease.
Copyright © 2016 Elsevier B.V. All rights reserved.
Adenosine; Alzheimer’s disease; Memory impairment; Swertisin
Swertisin, a C-glucosylflavone, ameliorates scopolamine-induced memory impairment in mice with its adenosine A1 receptor antagonistic property.
Lee HE1, Jeon SJ1, Ryu B1, Park SJ1, Ko SY1, Lee Y1, Kim E1, Lee S1, Kim H1, Jang DS2, Ryu JH3.
2016 Jun 1
Swertisin, a C-glucosylflavone isolated from Swertia japonica, is known to have antidiabetic, anti-inflammatory and antioxidant effects. Swertisin is an adenosine A1 receptor antagonist.