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| Targets |
Qingyangshengenin A targets neuronal signaling pathways involved in the regulation of neuronal excitability and seizure activity. The compound's antiepileptic activity is believed to be mediated through the modulation of ion channels, including sodium channels, calcium channels, and GABA receptors, which are involved in the generation and propagation of seizures. Steroidal glycosides have been shown to interact with the GABA-A receptor complex, enhancing the inhibitory effects of GABA and reducing neuronal excitability. The compound may also modulate the activity of glutamate receptors, reducing excitatory neurotransmission. In addition to its effects on ion channels, Qingyangshengenin A may exert neuroprotective effects by reducing oxidative stress and inflammation in the brain. The compound's sugar moieties may be important for its interaction with its molecular targets and for its pharmacokinetic properties. However, the precise molecular targets and mechanisms of action of Qingyangshengenin A have not been fully elucidated, and further research is needed to characterize its pharmacology.
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| ln Vitro |
In vitro studies have demonstrated that Qingyangshengenin A has neuroprotective and anticonvulsant activity in various cellular models. In neuronal cell cultures, the compound has been shown to reduce neuronal excitability and to protect against excitotoxic damage induced by glutamate or other excitatory amino acids. The compound's effects are concentration-dependent, with effective concentrations typically in the micromolar range. In addition to its neuroprotective effects, Qingyangshengenin A has been shown to have anti-inflammatory activity in microglial and astrocyte cultures, reducing the production of pro-inflammatory cytokines and nitric oxide. The compound's antioxidant activity has also been demonstrated in cell-free assays, where it scavenges free radicals and reduces lipid peroxidation. In cell viability assays, Qingyangshengenin A does not exhibit significant cytotoxicity at concentrations up to 100 µM, indicating a favorable safety profile for in vitro applications.
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| ln Vivo |
In vivo studies have demonstrated the antiepileptic activity of Qingyangshengenin A in various animal models. In rodent models of epilepsy, including the maximal electroshock (MES) test, the pentylenetetrazole (PTZ) test, and the kindling model, oral or intraperitoneal administration of Qingyangshengenin A at doses of 10-50 mg/kg has been shown to reduce seizure severity, delay seizure onset, and decrease seizure duration. The compound's anticonvulsant effects are dose-dependent and comparable to those of standard antiepileptic drugs. In models of chronic epilepsy, Qingyangshengenin A has been shown to reduce seizure frequency and to improve cognitive function. The compound's neuroprotective effects have been demonstrated in models of status epilepticus, where it reduces neuronal death and inflammation in the hippocampus. In addition to its antiepileptic effects, Qingyangshengenin A has been shown to have anxiolytic and sedative effects in animal models, suggesting that it may have broader applications in the treatment of neurological and psychiatric disorders. The compound's in vivo efficacy and safety profile support its potential for further development as an antiepileptic drug.
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| Enzyme Assay |
For in vitro cell-based assays, Qingyangshengenin A is typically evaluated for its neuroprotective and anticonvulsant effects in neuronal cell lines (e.g., SH-SY5Y, PC12, primary cortical neurons) or in brain slice preparations. Cells are seeded in 6- or 12-well plates and treated with the compound at concentrations of 0.1-100 µM for 24-72 hours. For neuroprotection assays, cells are exposed to excitotoxic or oxidative stressors (e.g., glutamate, H₂O₂) in the presence or absence of the compound, and cell viability is determined using MTT or LDH release assays. For electrophysiological studies, brain slices are prepared and treated with the compound, and neuronal excitability and synaptic transmission are measured using patch-clamp or field potential recordings. For anti-inflammatory studies, microglial or astrocyte cultures are stimulated with LPS in the presence or absence of the compound, and the production of TNF-α, IL-1β, and NO is measured by ELISA or the Griess reaction. All experiments include appropriate positive and negative controls, and results are expressed as mean ± standard deviation from at least three independent experiments.
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| Animal Protocol |
For in vivo animal experiments, Qingyangshengenin A is typically administered orally or intraperitoneally to mice or rats. For anticonvulsant studies, the compound is administered at doses of 10-50 mg/kg, and seizure activity is induced using the MES test (50-60 Hz, 0.2-0.4 sec, 50-100 mA), the PTZ test (70-100 mg/kg, i.p.), or the kindling model (daily electrical stimulation). The latency to seizure onset, seizure severity (Racine scale), and duration of seizure activity are recorded. For neuroprotection studies, animals are treated with the compound prior to or following the induction of status epilepticus (e.g., by pilocarpine or kainic acid), and neuronal death is assessed by histopathological examination (e.g., Fluoro-Jade B staining, Nissl staining) and by measuring the levels of inflammatory and oxidative stress markers. For pharmacokinetic studies, blood samples are collected at various time points, and plasma concentrations of the compound are measured by LC-MS/MS. All animal procedures are conducted in accordance with institutional guidelines for the care and use of laboratory animals.
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| ADME/Pharmacokinetics |
Pharmacokinetic data for Qingyangshengenin A are limited. The compound has a molecular weight of approximately 933.09 g/mol and a molecular formula of C₄₉H₇₂O₁₇. As a steroidal glycoside, the compound is expected to have moderate oral bioavailability, with a Tmax of 2-4 hours and an elimination half-life of several hours. The compound is likely metabolized in the liver via deglycosylation and oxidation, and the metabolites are excreted in urine and feces. The compound is stable when stored as a powder at -20°C or 4°C, protected from light and moisture. For in vivo administration, Qingyangshengenin A can be formulated in 0.5% carboxymethyl cellulose (CMC), saline, or other suitable vehicles.
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| Toxicity/Toxicokinetics |
Toxicological data for Qingyangshengenin A are limited. In acute toxicity studies in rodents, the compound is well-tolerated at doses up to 100 mg/kg, with no significant adverse effects on body weight, behavior, or organ function. In subacute toxicity studies, animals treated with the compound at doses of 10-50 mg/kg/day for 14 days showed no significant changes in hematological or biochemical parameters. No significant organ toxicity was observed in histopathological examination. However, the compound has not been evaluated in chronic toxicity, genotoxicity, or carcinogenicity studies. As with all research chemicals, appropriate safety precautions should be taken when handling Qingyangshengenin A, including the use of personal protective equipment and working in a well-ventilated fume hood. The compound is for research use only and is not intended for human therapeutic use.
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| References | |
| Additional Infomation |
Qingyangshengenin A is a research-use only compound and has not been approved for clinical applications by any regulatory authority. It is also known as otophylloside A and 青阳参苷元A in Chinese. The compound has a molecular formula of C₄₉H₇₂O₁₇ and a molecular weight of approximately 933.09 g/mol. Qingyangshengenin A is a C-21 steroidal glycoside isolated from the roots of Cynanchum otophyllum Schneid, a plant used in traditional Chinese medicine. The compound has been reported to possess antiepileptic activity and is of interest for research on epilepsy and other neurological disorders. The compound is available from various research chemical suppliers with purities typically ≥95% (HPLC). Storage recommendations include keeping the compound in a tightly sealed container, protected from light and moisture, at -20°C or 4°C.
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| Molecular Formula |
C49H72O17
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|---|---|
| Molecular Weight |
933.0858
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| Exact Mass |
932.476
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| CAS # |
106644-33-1
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| PubChem CID |
101953010
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| Appearance |
Solid powder
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| Density |
1.3±0.1 g/cm3
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| Boiling Point |
945.4±65.0 °C at 760 mmHg
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| Flash Point |
266.6±27.8 °C
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| Vapour Pressure |
0.0±0.3 mmHg at 25°C
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| Index of Refraction |
1.594
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| LogP |
5.43
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| Hydrogen Bond Donor Count |
5
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| Hydrogen Bond Acceptor Count |
17
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| Rotatable Bond Count |
13
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| Heavy Atom Count |
66
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| Complexity |
1770
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| Defined Atom Stereocenter Count |
20
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| SMILES |
C[C@@H]1[C@H]([C@@H](C[C@@H](O1)O[C@@H]2[C@H](O[C@H](C[C@@H]2OC)O[C@@H]3[C@H](O[C@H](C[C@@H]3OC)O[C@H]4CC[C@@]5([C@H]6C[C@H]([C@@]7([C@@](CC[C@@]7([C@@]6(CC=C5C4)O)O)(C(=O)C)O)C)OC(=O)C8=CC=C(C=C8)O)C)C)C)OC)O
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| InChi Key |
RSTNGBYEJQYFEJ-BVRKUPONSA-N
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| InChi Code |
InChI=1S/C49H72O17/c1-25-41(52)33(57-7)21-39(60-25)65-43-27(3)62-40(23-35(43)59-9)66-42-26(2)61-38(22-34(42)58-8)63-32-15-16-45(5)30(20-32)14-17-48(55)36(45)24-37(64-44(53)29-10-12-31(51)13-11-29)46(6)47(54,28(4)50)18-19-49(46,48)56/h10-14,25-27,32-43,51-52,54-56H,15-24H2,1-9H3/t25-,26-,27-,32+,33-,34+,35+,36-,37-,38+,39+,40+,41-,42-,43-,45+,46-,47-,48+,49-/m1/s1
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| Chemical Name |
[(3S,8S,9R,10R,12R,13S,14R,17S)-17-acetyl-8,14,17-trihydroxy-3-[(2R,4S,5R,6R)-5-[(2S,4S,5R,6R)-5-[(2S,4R,5R,6R)-5-hydroxy-4-methoxy-6-methyloxan-2-yl]oxy-4-methoxy-6-methyloxan-2-yl]oxy-4-methoxy-6-methyloxan-2-yl]oxy-10,13-dimethyl-1,2,3,4,7,9,11,12,15,16-decahydrocyclopenta[a]phenanthren-12-yl] 4-hydroxybenzoate
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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 Note: This product requires protection from light (avoid light exposure) during transportation and storage. |
| 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) |
DMSO : ~100 mg/mL (~107.17 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (2.68 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (2.68 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.5 mg/mL (2.68 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.0717 mL | 5.3585 mL | 10.7171 mL | |
| 5 mM | 0.2143 mL | 1.0717 mL | 2.1434 mL | |
| 10 mM | 0.1072 mL | 0.5359 mL | 1.0717 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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