| Description: |
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. |
| Targets: |
PPAR | GLUT | TNF-α | IL Receptor | Sodium Channel | Potassium Channel |
| In vitro: |
| 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. |
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| In vivo: |
| 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. |
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