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| ln Vitro |
Neurite outgrowth is induced in PC12 cells by gardenin A (10–20 μM; 48 hours), and neuronal differentiation and synapse formation marker protein, growth-associated protein–43 (GAP–43), and synaptophysin expression are similarly increased (10 μM; 24 and 48 hours) [1]. Using the inhibitor 2-naphthol AS-E phosphate (KG-501) or CREB siRNA, gardenin A (10 μM; 30-120 min) dramatically increases the phosphorylation of the cyclic AMP response element binding protein (CREB) and CRE-mediated transcription [1]. PKA and PKC activity as well as ERK phosphorylation levels are increased by gardenin A (10 μM; 15-120 minutes) [1].
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| ln Vivo |
For mice, gardenin A (0.1–25 mg/kg; oral; single dosage) exhibits a range of neuropharmacological effects, such as sedative, anxiolytic, antidepressant, and anticonvulsant [2]. Mice treated with geniposide A (1–10 mg/kg; oral; single dose) do not have a reduction in motor coordination, and convulsions occur later [2].
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| Cell Assay |
Cell Viability Assay[1]
Cell Types: PC12 cells Tested Concentrations: 2, 5, 10, 20 μM Incubation Duration: 48 hrs (hours) Experimental Results: demonstrated 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 Types: PC12 cells Tested Concentrations: 10 μM Incubation Duration: 0, 15, 30, 60, and 120 min Experimental Results: Dramatically increased the phosphorylation of ERK1/2 (Thr202/Tyr204) at 15 min, subsequently decreased after 30 min. Increased PKC and PKA activity peaked at 15 min. Increased CREB phosphorylation. |
| Animal Protocol |
Animal/Disease Models: Male balb/c (Bagg ALBino) mouse: (24-32 g)[2]
Doses: 1 mg/kg, 10 mg/kg, 25 mg/kg Route of Administration: po (oral gavage); single dose Experimental Results: demonstrated sedative effects at a dose of 25 mg/kg, which increased the duration of sleep but did not alter sleep onset. |
| 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. |
| Molecular Formula |
C21H22O9
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|---|---|
| Molecular Weight |
418.39
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| CAS # |
21187-73-5
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| SMILES |
COC1=C(OC)C=C(C2=CC(=O)C3=C(C(=C(C(OC)=C3O2)OC)OC)O)C=C1OC
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
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| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.3901 mL | 11.9506 mL | 23.9011 mL | |
| 5 mM | 0.4780 mL | 2.3901 mL | 4.7802 mL | |
| 10 mM | 0.2390 mL | 1.1951 mL | 2.3901 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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