| Size | Price | Stock | Qty |
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| 5mg |
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| ln Vitro |
Swertianolin was tested for its ability to suppress Hepatitis B surface antigen (HBsAg) and Hepatitis B e antigen (HBeAg) expression in cultured human hepatocellular carcinoma HepG2 cells. After 8 days of treatment, Swertianolin effectively suppressed HBeAg expression with an IC50 value of 8.0 μg/mL. The suppression was not due to cytotoxic activity, as treated cells remained viable and continued to proliferate slowly during the 8-day incubation period [2].
At the fourth day of treatment, the IC50 for suppression of HBsAg or HBeAg could not be calculated from the experimental results. By day 8, Swertianolin showed dose-dependent inhibition of HBeAg. At concentrations of 1.6, 3.1, 6.2, 12.5, and 25 μg/mL, the HBeAg inhibition rates at day 8 were 37.74%, 34.58%, 35.43%, 21.94%, and 16.48%, respectively. The cpm values (mean ± s) for HBeAg at these concentrations were 7061±1058, 7418±1029, 7322±867, 8853±1168, and 9471±1748, compared to the control group value of 11340±3474 [2]. Swertianolin showed minimal effect on HBsAg expression. At day 8, HBsAg inhibition rates ranged from -5.13% to 14.60% across the tested concentrations, with cpm values not significantly different from the control group (19805±2000) [2]. |
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| Cell Assay |
HepG2 cells were obtained from Mount Sinai School of Medicine, USA, and maintained in DMEM medium supplemented with 10% FBS, 50 U/mL streptomycin, and 3% L-glutamine. Cells were cultured in 5% CO₂ at 37°C [2].
For cytotoxicity assays, cells were seeded into 96-well plates at a density of 2.0×10⁴ cells/well and incubated for 24 hours. Various concentrations of Swertianolin were added to the culture medium, which was replaced every 4 days. After 8 days, cell viability was assessed by cytopathic effect. The median toxic concentration (TC50) was calculated according to the Reed-Muench method and found to be 50 μg/mL for Swertianolin [2]. For antigen suppression assays, HepG2 cells were seeded into 24-well plates at a density of 1.0×10⁵ cells/well and allowed to attach overnight. The medium was changed to serum-free DMEM, and cells were treated with Swertianolin at concentrations of 1.6, 3.1, 6.2, 12.5, and 25 μg/mL. The medium was replaced every 4 days with fresh compound-containing medium. Culture medium from day 4 and day 8 was collected. HBsAg and HBeAg levels were measured by radioimmunoassay kits according to manufacturer's instructions, and radioactivity was counted in a hemocytometer. All assays were performed in triplicate. The antigen inhibition percentage was calculated as: Inhibition (%) = [(cpm control - cpm experimental) / cpm control] × 100 [2]. |
| Toxicity/Toxicokinetics |
The median toxic concentration (TC50) of Swertianolin in HepG2 cells was determined to be 50 μg/mL after 8 days of treatment. The Therapeutic Index (TI), calculated as TC50/IC50, was 6.2 for Swertianolin [2].
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| References | |
| Additional Infomation |
Gentianine (Swertianolin) is a flavonoid compound with a structure similar to bellidifolin, where β-D-glucanose residues are linked at the O-8 positions via glycosidic bonds. It is primarily isolated from Gentiana campestris and Gentiana germanica. Gentianine possesses multiple functions, including as an inhibitor of EC 3.1.1.7 (acetylcholinesterase), an antioxidant, and a plant metabolite. It is a β-D-glucosinolate, belonging to the monosaccharide derivative, aromatic ether, and flavonoid glycosides. Its functions are related to bellidifolin. Gentianine has been reported to exist in Gentiana algida, Gentiana thunbergii, and other organisms with relevant data.
Swertianolin is a xanthone compound isolated from the traditional Chinese medicinal plant Swertia punicea Hemsl (family Gentianaceae). The plant has been traditionally used for the treatment of hepatitis in some rural areas of China and has been approved for pharmacological and clinical trials in Hubei and Yunnan provinces. The compound was extracted from air-dried plant material using 95% ethanol, followed by sequential partitioning with petroleum ether, ether, EtOAc, and water. Purification was achieved through silica gel column chromatography with chloroform-methanol gradients (90:10 and 75:25, v:v) and Sephadex LH-20 column chromatography. The structure was identified by comparing ¹H-NMR, ¹³C-NMR, and MS data with literature [2]. This study represents the first demonstration of anti-HBV activity of Swertianolin in vitro. The compound selectively inhibited HBeAg expression with an IC50 of 8.0 μg/mL and therapeutic index of 6.2, while showing minimal effect on HBsAg. The suppression was not due to cytotoxicity, as cells remained viable during treatment. These findings suggest that Swertianolin may have potential for development as an anti-HBV agent, particularly for suppressing HBeAg production. The study was supported by the National Natural Science Foundation of China (Grant No. 30271590) [2]. |
| Molecular Formula |
C20H20O11
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|---|---|
| Molecular Weight |
436.369
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| Exact Mass |
436.1
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| CAS # |
23445-00-3
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| PubChem CID |
5281662
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| Appearance |
White to yellow solid powder
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| Density |
1.7±0.1 g/cm3
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| Boiling Point |
806.3±65.0 °C at 760 mmHg
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| Flash Point |
287.7±27.8 °C
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| Vapour Pressure |
0.0±3.0 mmHg at 25°C
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| Index of Refraction |
1.705
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| LogP |
-1.13
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| Hydrogen Bond Donor Count |
6
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| Hydrogen Bond Acceptor Count |
11
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| Rotatable Bond Count |
4
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| Heavy Atom Count |
31
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| Complexity |
647
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| Defined Atom Stereocenter Count |
5
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| Synonyms |
Swertianolin; CCRIS-5474 CCRIS5474; CCRIS 5474;
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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 : ~25 mg/mL (~57.29 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (5.73 mM) (saturation unknown) in 10% DMSO + 40% PEG300 +5% Tween-80 + 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. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.2916 mL | 11.4582 mL | 22.9163 mL | |
| 5 mM | 0.4583 mL | 2.2916 mL | 4.5833 mL | |
| 10 mM | 0.2292 mL | 1.1458 mL | 2.2916 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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