|Source:||The seeds of Ziziphus jujuba|
|Biological Activity or Inhibitors:||1. Spinosin ameliorated memory impairment induced through AβO, the serotonergic neurotransmitter system, and these effects were regulated, in part, through neuroprotective activity via the anti-inflammatory effects of Spinosin.
2. Spinosin exerts anxiolytic-like effects, and its mechanism of action appears to be modulated by GABAA and 5-HT1A receptors.
3. There was a wide brain regional tissue distribution of Spinosin. The concentrations of Spinosin in corpus striatum and hippocampus were higher than that in other areas.
4. Spinosin can potentiate pentobarbital-induced sleep via the serotonergic system.
5. Spinosin has inhibitory effect on 8-OH-DPAT-induced hypothermia and has potentiating effect on pentobarbital-induced loss of righting reflex (LORR) in mice,presynaptic 5-HT(1A) autoreceptor mechanisms may be involved in the effects.
|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: firstname.lastname@example.org
|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.|
|1 mg||5 mg||10 mg||20 mg||25 mg|
|1 mM||1.6433 mL||8.2163 mL||16.4325 mL||32.865 mL||41.0813 mL|
|5 mM||0.3287 mL||1.6433 mL||3.2865 mL||6.573 mL||8.2163 mL|
|10 mM||0.1643 mL||0.8216 mL||1.6433 mL||3.2865 mL||4.1081 mL|
|50 mM||0.0329 mL||0.1643 mL||0.3287 mL||0.6573 mL||0.8216 mL|
|100 mM||0.0164 mL||0.0822 mL||0.1643 mL||0.3287 mL||0.4108 mL|
Biomol Ther (Seoul). 2015 Mar;23(2):156-64.
|Spinosin, a C-Glucosylflavone, from Zizyphus jujuba var. spinosa Ameliorates Aβ1-42 Oligomer-Induced Memory Impairment in Mice.[Pubmed: 25767684]|
|Alzheimer's disease (AD) is a neurodegenerative disorder associated with progressive memory loss and neuronal cell death. Although numerous previous studies have been focused on disease progression or reverse pathological symptoms, therapeutic strategies for AD are limited. Alternatively, the identification of traditional herbal medicines or their active compounds has received much attention. The aims of the present study were to characterize the ameliorating effects of Spinosin, a C-glucosylflavone isolated from Zizyphus jujuba var. spinosa, on memory impairment or the pathological changes induced through amyloid-β1-42 oligomer (AβO) in mice. Memory impairment was induced by intracerebroventricular injection of AβO (50 μM) and Spinosin (5, 10, and 20 mg/kg) was administered for 7 days. In the behavioral tasks, the subchronic administration of Spinosin (20 mg/kg, p.o.) significantly ameliorated AβO-induced cognitive impairment in the passive avoidance task or the Y-maze task. To identify the effects of Spinosin on the pathological changes induced through AβO, immunohistochemistry and Western blot analyses were performed. Spinosin treatment also reduced the number of activated microglia and astrocytes observed after AβO injection. In addition, Spinosin rescued the AβO-induced decrease in choline acetyltransferase expression levels. These results suggest that Spinosin ameliorated memory impairment induced through AβO, and these effects were regulated, in part, through neuroprotective activity via the anti-inflammatory effects of Spinosin. Therefore, Spinosin might be a useful agent against the amyloid b protein-induced cognitive dysfunction observed in AD patients.|
Pharmacol Biochem Behav. 2015 Jan;128:41-9.
|GABA and 5-HT systems are implicated in the anxiolytic-like effect of spinosin in mice.[Pubmed: 25449359]|
|The present study investigated the anxiolytic-like effects of Spinosin, one of the major flavonoids in Ziziphi Spinosae Semen (ZSS), in experimental models of anxiety compared with a known anxiolytic, diazepam. Repeated treatment with Spinosin (2.5 and 5mg/kg/day, p.o.) significantly increased the percentage of entries into and time spent on the open arms of the elevated plus maze compared with the control group. In the light/dark box test, Spinosin exerted an anxiolytic-like effect at 5mg/kg. In the open-field test, 5mg/kg Spinosin increased the number of central entries. Spinosin did not affect spontaneous activity. The anxiolytic-like effects of Spinosin in the elevated plus maze, light/dark box test, and open field test were blocked by the γ-aminobutyric acid-A (GABAA) receptor antagonist flumazenil (3mg/kg, i.p.) and 5-hydroxytryptamine-1A (5-HT1A) receptor antagonist WAY-100635 (1mg/kg, i.p.). These results suggest that Spinosin exerts anxiolytic-like effects, and its mechanism of action appears to be modulated by GABAA and 5-HT1A receptors.|
Pharmacol Biochem Behav. 2014 May;120:88-94.
|Ameliorating effect of spinosin, a C-glycoside flavonoid, on scopolamine-induced memory impairment in mice.[Pubmed: 24582850]|
|Spinosin is a C-glycoside flavonoid isolated from the seeds of Zizyphus jujuba var. spinosa. This study investigated the effect of Spinosin on cholinergic blockade-induced memory impairment in mice. Behavioral tests were conducted using the passive avoidance, Y-maze, and Morris water maze tasks to evaluate the memory-ameliorating effect of Spinosin. Spinosin (10 or 20mg/kg, p.o.) significantly ameliorated scopolamine-induced cognitive impairment in these behavioral tasks with a prolonged latency time in the passive avoidance task, an increased percentage of spontaneous alternation in the Y-maze task and a lengthened swimming time in target quadrant in the Morris water maze task. In addition, a single administration of Spinosin in normal naïve mice also enhanced the latency time in the passive avoidance task. To identify the mechanism of the memory-ameliorating effect of Spinosin, receptor antagonism analysis and Western blotting were performed. The ameliorating effect of Spinosin on scopolamine-induced memory impairment was significantly antagonized by a sub-effective dose (0.5mg/kg, i.p.) of 8-hydroxy-2-(di-N-propylamino)tetralin, a 5-HT1A receptor agonist. In addition, Spinosin significantly increased the expression levels of phosphorylated extracellular signal-regulated kinases and cAMP response element-binding proteins in the hippocampus. Taken together, these results indicate that the memory-ameliorating effect of Spinosin may be, in part, due to the serotonergic neurotransmitter system, and that Spinosin may be useful for the treatment of cognitive dysfunction in diseases such as Alzheimer's disease.|
J Chromatogr Sci. 2015 Jan;53(1):97-103.
|Brain tissue distribution of spinosin in rats determined by a new high-performance liquid chromatography-electrospray ionization-mass/mass spectrometry method.[Pubmed: 24771055]|
|Spinosin, a ﬂavone-C-glycoside, is a bioactive ingredient isolated from a traditional Chinese herb Zizyphi Spinosi Semen. In this study, a new high-performance liquid chromatography-electrospray ionization-mass/mass spectrometry method was developed and validated to determine Spinosin in brain tissues including olfactory region, hippocampus, corpus striatum, cerebrum (cerebral cortex) and cerebellum, after intravenous administration with the dose of 5 mg/kg. The tissue homogenate samples were pretreated and extracted with acetonitrile by a simple protein precipitation method. The separation was performed on a YMC ODS-AQ(TM) column (250 × 2.0 mm, 3.5 μm) with the mobile phase of acetonitrile-aqueous phase (0.1% formic acid) (25 : 75, v/v) at a ﬂow rate of 0.3 mL/min. The retention times of Spinosin and naringin (internal standard) were 3.3 and 5.1 min, respectively. Multiple reaction monitoring mode was used to monitor precursor/product ion transitions of m/z 607.2 → 427.0 for Spinosin and m/z 579.2 → 271.0 for naringin. The proposed method was successfully applied to the preclinical brain tissue distribution of Spinosin in rats. The results showed that there was a wide brain regional tissue distribution of Spinosin. The concentrations of Spinosin in corpus striatum and hippocampus were higher than that in other areas.|
Pharmacol Biochem Behav. 2008 Sep;90(3):399-403.
|Spinosin, a C-glycoside flavonoid from semen Zizhiphi Spinozae, potentiated pentobarbital-induced sleep via the serotonergic system.[Pubmed: 18466960 ]|
|Semen Zizhiphi Spinozae has been used extensively for the treatment of insomnia. This study investigated the effect and possible mechanism of action of Spinosin (also known as 2''-beta-o-glucopyranosyl swertisin), a major constituent of semen Zizhiphi Spinozae, on sleep in mice. The present results showed that Spinosin significantly and dose-dependently augmented pentobarbital (45 mg/kg, i.p.)-induced sleep, reflected by increased sleep time and reduced sleep latency assessed with the loss-of-righting reflex, and these effects were potentiated by the 5-hydroxytryptamine (serotonin) precursor 5-hydroxytryptophan (5-HTP, 2.5 mg/kg,i.p.). With a subhypnotic dose of pentobarbital (28 mg/kg, i.p.), Spinosin significantly increased the rate of sleep onset and exhibited a synergistic effect with 5-HTP (2.5 mg/kg, i.p.). Pretreatment with p-chlorophenylalanine (PCPA, 300 mg/kg, s.c.), an inhibitor of tryptophan hydroxylase, significantly decreased pentobarbital-induced sleep time, and Spinosin significantly reversed this effect. The dopamine precursor L-3-(3, 4-dihydroxyphenylalanine (L-DOPA) reduced pentobarbital-induced sleep, an effect not significantly affected by Spinosin. These results suggest that Spinosin potentiated pentobarbital-induced sleep via a serotonergic mechanism.|
J Pharm Pharmacol. 2012 Feb;64(2):277-82.
|Augmentative effect of spinosin on pentobarbital-induced loss of righting reflex in mice associated with presynaptic 5-HT1A receptor.[Pubmed: 22221104 ]|
|The results demonstrated that the 5-HT(1A) agonist 8-OH-DPAT (s.c.) induced reductions in duration of LORR at 0.1, 0.5 and 1.0 mg/kg (P < 0.01), and prolongation of LORR latency at 0.5 and 1.0 mg/kg (s.c., P < 0.01) in pentobarbital (45 mg/kg, i.p.)-treated mice. This effect of 8-OH-DPAT was antagonized either by 5-HT(1A) antagonist p-MPPI (5 mg/kg, i.p.) or by Spinosin (15 mg/kg, i.g.) with significance, respectively. Co-administration of Spinosin and p-MPPI both at ineffective doses (Spinosin at 5.0 mg/kg, i.g. and p-MPPI at 1.0 mg/kg, i.p.) showed significant augmentative effects in reducing latency to LORR, and increasing LORR duration (P < 0.01) in pentobarbital-treated mice. On the other hand, Spinosin inhibited 8-OH-DPAT-induced hypothermia, which has been generally attributed to the activation of somatodendritic 5-HT(1A) autoreceptors in mice. CONCLUSIONS: Based on our previous results and the present data, it should be presumed that presynaptic 5-HT(1A) autoreceptor mechanisms may be involved in the inhibitory effect of Spinosin on 8-OH-DPAT-induced hypothermia and also in the potentiating effect of Spinosin on pentobarbital-induced LORR in mice.|