Gentianine
Gentianine has anti-diabetic, antipsychotic, anti-inflammatory, hypotensive, and diuretic actions, it could be developed as a safe antihypertensive drug. Gentianine has a protective effect on hippocampal CA1 neurons in rats subjected to recurrent febrile convulsion (FC), it can ameliorate FC-induced neuronal injury by enhancing glutamate acid decarboxylase activity, decreasing glutamate levels and increasing γ-aminobutyric acid levels.
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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: service@chemfaces.com
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.
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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.
J Pharm Sci. 1974 Aug;63(8):1341-2.
Letter: Chemical constituents of gentianaceae. XI. Antipsychotic activity of gentianine.[Pubmed:
4859384]
Letter: Chemical constituents of gentianaceae. XI. Antipsychotic activity of Gentianine.
Pharm. Pharmacol. Commun., 1998, 4(4): 229-30.
Hypotensive Effect of Gentiana olivieri and Its Alkaloid Gentianine in Rats.[Reference:
WebLink]
METHODS AND RESULTS:
Ethanolic and aqueous extracts of Gentiana olivieri and its pure alkaloid, Gentianine, were tested for cardiovascular activity in normotensive, pentothal-anaesthetized rats.
CONCLUSIONS:
All three fractions produced a decrease in heart rate and systolic, diastolic and mean arterial blood pressure, with Gentianine being the most effective.
J.Pharm. Pharm. Sci., 2015, 4(4):39-42.
Evaluation of Diuretic Activity of Extracts of Gentiana oliveri and Gentianine in Rats.[Reference:
WebLink]
Biological and pharmacological assays of the extracts of Gentiana oliveri and its alkaloid Gentianine proved to be highly efficacious.
Extracts of Gentiana oliveri and Gentianine were evaluated for diuretic activity in normotensive, rats.
METHODS AND RESULTS:
Oral administration of all the fractions enhanced ion excretion. A dose-dependent diuresis and electrolytes excretion was also observed when dose by Gentianine. There was marked increase in Na+, K+ and Cl- ion excretion in the aqueous extract as compared to control and furosemide. Significant increase in urinary excretion was produced by pure alkaloid (P<0.04), ethanolic extract (P<0.03), aqueous extract (P<0.01) and furosemide (P<0.001).
CONCLUSIONS:
Gentianine could be developed as a safe antihypertensive drug.
Neural Regeneration Research, 2011, 06(15):1130-5.
Gentianine protects hippocampal neurons in a rat model of recurrent febrile convulsion.[Reference:
WebLink]
Gentianine has been shown to have a protective effect on hippocampal CA1 neurons in rats subjected to recurrent febrile convulsion (FC).
METHODS AND RESULTS:
The present study sought to explore the possible mechanism of Gentianine by intraperitoneally injecting Gentianine into rats with warm water-induced FC. The results revealed that neuronal organelle injury was slightly ameliorated in the hippocampal CA1 region. The level of glutamate was decreased, but the level of γ-aminobutyric acid was increased, as detected by ninhydrin staining. In addition, glutamate acid decarboxylase expression in hippocampal CA1 was increased, as determined by immunohistochemistry.
CONCLUSIONS:
The results demonstrated that Gentianine can ameliorate FC-induced neuronal injury by enhancing glutamate acid decarboxylase activity, decreasing glutamate levels and increasing γ-aminobutyric acid levels.
Biol Pharm Bull. 2005 Apr;28(4):750-3.
Effects of gentianine on the production of pro-inflammatory cytokines in male Sprague-Dawley rats treated with lipopolysaccharide (LPS).[Pubmed:
15802824]
This study was undertaken to elucidate the mechanism of anti-inflammatory action of Gentianine, a constituent of Gentiana Macrophylla.
METHODS AND RESULTS:
The effects of Gentianine on lipopolysacharide (LPS)-induced production of pro-inflammatory cytokines were investigated in male Sprague-Dawley rats. For the first time, we found that oral administration of Gentianine (10-100 mg/kg) suppressed the increases in tumor necrosis factor-alpha (TNF-alpha) (ED(50), 37.7 mg/kg) and interleukin (IL)-6 (ED(50), 38.5 mg/kg) in the sera from the rats challenged with bacterial LPS (100 microg/kg; i.p.). However, LPS induced production of other interleukins, such as IL-alpha, was not significantly altered by Gentianine.
CONCLUSIONS:
These results suggest that the potential anti-inflammatory action of Gentianine might be at least partly based on the suppressed production of TNF-alpha and IL-6.
