[CAS NO. 21187-73-5] Gardenin A
PRODUCTS SPECIFICATIONS [21187-73-5]
DESCRIPTION [21187-73-5]
Overview
| MDL | MFCD00017419 |
|---|---|
| Molecular Weight | 418.39 |
| Molecular Formula | C21H22O9 |
| SMILES | O=C1C=C(C2=CC(OC)=C(OC)C(OC)=C2)OC3=C(OC)C(OC)=C(OC)C(O)=C13 |
Summary
Gardenin A is an orally active and synthetic PMF analogue with the neurotrophic effect for neurite outgrowth and neuronal differentiation. Gardenin A promotes neuritogenesis via activating MAPK/ERK , PKC , and PKA , but not TrkA , CREB signaling pathways. Gardenin A also has sedative, anxiolytic, antidepressant, and anticonvulsant effects [1] [2] .
In Vitro
Gardenin A (10-20 μM; 48 h) potently induces neurite outgrowth in PC12 cells, and (10 μM; 24 h and 48 h) increases expression of neuronal differentiation and synapse formation marker proteins, growth-associated protein-43 (GAP-43), and synaptophysin
[1]
.
Gardenin A (10 μM; 30-120 min) markedly induces the phosphorylation of both cyclic AMP response element-binding protein (CREB) and CRE-mediated transcription, which was suppressed through the administration of the inhibitor 2-naphthol AS-E phosphate (KG-501) or using CREB siRNA
[1]
.
Gardenin A (10 μM; 15-120 min) increases ERK phosphorylation and PKA and PKC activities
[1]
.
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Cell Viability Assay [1]
| Cell Line: | PC12 cells |
| Concentration: | 2, 5, 10, 20 μM |
| Incubation Time: | 48 hours |
| Result: | showed cell growth supporting effect at higher concentrations (10-20 µM) and did not exert detectable 237 cytotoxicity on PC12 cells after 48 h incubation in low serum medium. |
Western Blot Analysis [1]
| Cell Line: | PC12 cells |
| Concentration: | 10 μM |
| Incubation Time: | 0, 15, 30, 60, and 120 min |
| Result: |
Significantly increased the phosphorylation of ERK1/2 (Thr202/Tyr204) at 15 min, subsequently reduced after 30 min.
Increased PKC and PKA activity peaked at 15 min. Increased CREB phosphorylation. |
In Vivo
Gardenin A (0.1-25 mg/kg; p.o.; single dose) has neuropharmacological, including sedative, anxiolytic, antidepressant, and anticonvulsant actions in mice
[2]
.
Gardenin A (1-10 mg/kg; p.o.; single dose) does not affect locomotor coordination in mice and delayed the onset of convulsions
[2]
.
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
| Animal Model: | Male Balb/c mice (24-32 g) [2] |
| Dosage: | 1 mg/kg, 10 mg/kg, 25 mg/kg |
| Administration: | Oral gavage; single dose |
| Result: | Showed sedative effects at a dose of 25 mg/kg, which increased the duration of sleep but did not alter sleep onset. |
Shipping
Room temperature in continental US; may vary elsewhere.
Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
References
- [1] Chiu SP, et al. Neurotrophic action of 5-hydroxylated polymethoxyflavones: 5-demethylnobiletin and gardenin A stimulate neuritogenesis in PC12 cells. J Agric Food Chem. 2013 Oct 2;61(39):9453-63.
- [2] Alonso-Castro AJ, et al. Evaluation of the neuropharmacological effects of Gardenin A in mice. Drug Dev Res. 2020 Aug;81(5):600-608.
