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| Targets |
Gardenin A targets multiple signaling pathways involved in neurogenesis and neuroprotection. It activates MAPK/ERK, PKC, and PKA signaling pathways in PC12 cells. Unlike neurotrophins, Gardenin A does not activate TrkA or CREB signaling pathways. The compound also modulates the GABAergic system and noradrenergic pathways, contributing to its sedative, anxiolytic, antidepressant, and anticonvulsant effects. Its primary applications are in neuroscience research for studying neuronal differentiation and neuroprotection.
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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].
In vitro, Gardenin A (10-20 μM; 48 hours) potently induces neurite outgrowth in PC12 cells. At 10 μM for 24 and 48 hours, it increases expression of neuronal differentiation and synapse formation marker proteins, including growth-associated protein-43 (GAP-43) and synaptophysin. Gardenin A (10 μM; 15-120 minutes) increases ERK phosphorylation, PKC activity, and PKA activity. It also markedly induces CREB phosphorylation and CRE-mediated transcription at 10 μM for 30-120 minutes. The compound shows cell growth-supporting effects at higher concentrations (10-20 µM) without detectable cytotoxicity in PC12 cells. |
| 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].
In vivo, Gardenin A demonstrates a range of neuropharmacological effects in mice at oral doses of 0.1-25 mg/kg, including sedative, anxiolytic, antidepressant, and anticonvulsant activities. At 25 mg/kg, it increases the duration of sleep without altering sleep onset. Treatment with 100 mg/kg Gardenin A improves associative memory and decreases abnormalities in mobility and gait in A53T-α-synuclein overexpressing mice. It also attenuates increases in phosphorylated alpha-synuclein and reductions in tyrosine hydroxylase expression. In male Wistar rats, doses of 50 and 100 mg/kg demonstrate neuroprotective potential. |
| Enzyme Assay |
The in vitro enzyme activity assay for Gardenin A typically involves measuring kinase activity in PC12 cell lysates. Cells are treated with Gardenin A (10 μM) for varying time points (0-120 minutes), and ERK1/2 phosphorylation at Thr202/Tyr204 is measured by Western blotting. PKC and PKA activity are assessed using specific kinase activity assay kits. CREB phosphorylation and CRE-mediated transcription are measured using phospho-specific antibodies and reporter gene assays, respectively. Neurite outgrowth is quantified by microscopic imaging of PC12 cells treated for 48 hours.
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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. Cellular assays for Gardenin A are conducted in PC12 cells, a rat pheochromocytoma cell line commonly used for neuronal differentiation studies. Cells are treated with Gardenin A at concentrations of 2, 5, 10, and 20 μM for 48 hours. Cell viability is assessed using standard assays such as MTT. Neurite outgrowth is quantified by microscopy, and the percentage of cells with neurites is calculated. Western blot analysis is performed for GAP-43, synaptophysin, phosphorylated ERK, PKC, PKA, and CREB. CRE-mediated transcription is measured using luciferase reporter assays. |
| 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. In vivo studies are conducted in male BALB/c mice (24-32 g) and A53T-α-synuclein overexpressing mice. Gardenin A is administered orally (po; oral gavage) at doses ranging from 0.1 to 100 mg/kg as a single dose or in repeated dosing regimens. Neuropharmacological effects are assessed using behavioral tests including sleep duration measurement, elevated plus maze, forced swim test, and pentylenetetrazole-induced seizure models. In A53T-α-syn mice, cognitive and motor function are evaluated using associative memory tests and gait analysis. Brain tissue is collected for biochemical analysis of synuclein pathology and tyrosine hydroxylase expression. |
| ADME/Pharmacokinetics |
Gardenin A is orally bioavailable with favorable pharmacokinetic properties. It has a molecular weight of 418.39 g/mol and a molecular formula of C₂₁H₂₂O₉. The compound is soluble in DMSO and is typically administered orally in vivo. Detailed pharmacokinetic parameters such as half-life, bioavailability, and tissue distribution are not extensively reported in the available literature, but the compound's oral activity in multiple in vivo studies confirms adequate systemic exposure.
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| Toxicity/Toxicokinetics |
Toxicity data for Gardenin A is derived from in vivo studies in mice and rats. In PC12 cell assays, Gardenin A did not exert detectable cytotoxicity after 48 hours of incubation at concentrations up to 20 μM. In mouse studies, the compound was well-tolerated at doses up to 100 mg/kg without reported significant adverse effects. Motor coordination was not impaired in treated mice. As with all research compounds, Gardenin A is intended for research use only and not for human therapeutic applications. Comprehensive toxicology studies would be required for clinical development.
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| References | |
| Additional Infomation |
Reports indicate that gardenia (Gardenia resinifera), tamarisk (Tamarix dioica), and Murraya paniculata contain geniposide A, and relevant data is available for reference.
Gardenin A is an orally bioavailable synthetic polymethoxyflavone analog with neurotrophic effects on neurite outgrowth and neuronal differentiation. It promotes neurogenesis by activating MAPK/ERK, PKC, and PKA signaling pathways, but does not activate TrkA or CREB. The compound exhibits sedative, anxiolytic, antidepressant, and anticonvulsant effects, likely involving the GABAergic and noradrenergic systems. Gardenin A has been studied in A53T-α-synuclein mouse models of Parkinson's disease, where it improves cognitive and motor function. It is a valuable research tool for studying neurogenesis, neuroprotection, and neurodegenerative diseases. |
| Molecular Formula |
C21H22O9
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|---|---|
| Molecular Weight |
418.39
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| Exact Mass |
418.126
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| CAS # |
21187-73-5
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| PubChem CID |
261859
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| Appearance |
Off-white to light yellow solid powder
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| Density |
1.3g/cm3
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| Boiling Point |
624.2ºC at 760 mmHg
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| Melting Point |
162-163ºC
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| Flash Point |
218.5ºC
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| Vapour Pressure |
3.57E-16mmHg at 25°C
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| Index of Refraction |
1.573
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| LogP |
3.217
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
9
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| Rotatable Bond Count |
7
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| Heavy Atom Count |
30
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| Complexity |
610
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| Defined Atom Stereocenter Count |
0
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| InChi Key |
MQBFFYQCZCKSBX-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C21H22O9/c1-24-13-7-10(8-14(25-2)17(13)26-3)12-9-11(22)15-16(23)19(27-4)21(29-6)20(28-5)18(15)30-12/h7-9,23H,1-6H3
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| Chemical Name |
5-hydroxy-6,7,8-trimethoxy-2-(3,4,5-trimethoxyphenyl)chromen-4-one
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| HS Tariff Code |
2934.99.9001
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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 Vitro) |
May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples
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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.) |
| 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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