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| Targets |
Ponicidin inhibits the phosphorylation of Janus kinase 2 (JAK2) and signal transducer and activator of transcription 3 (STAT3) in MKN28 gastric carcinoma cells. It also downregulates vascular endothelial growth factor (VEGF) and VEGF receptor 2 (VEGFR2) protein expression. [1]
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| ln Vitro |
In MKN28 gastric carcinoma cells, Ponicidin (10, 25, and 50 μmol/L) significantly inhibited cell viability in a time- and dose-dependent manner as measured by CCK8 assay. At 50 μmol/L for 48 h, cell viability was markedly decreased. [1]
Ponicidin (10–50 μmol/L for 48 h) induced apoptosis in a dose-dependent manner. The percentage of early apoptotic cells increased from 2.13% ± 0.15% in controls to 59.03% ± 1.84% at 50 μmol/L (P < 0.01). [1] Cell cycle analysis showed that ponicidin (25–50 μmol/L for 48 h) increased the percentage of cells in G0–G1 phase from 46.40% ± 2.26% (control) to 60.68% ± 0.78% (50 μmol/L) (P < 0.01), and increased the sub-G1 population in a dose-dependent manner. The S and G2–M phase populations decreased. [1] Ponicidin (10–50 μmol/L) increased reactive oxygen species (ROS) generation in MKN28 cells in a time- and dose-dependent manner. At 50 μmol/L for 48 h, fluorescence intensity increased from 2826.07% ± 195.51% (control) to 2,102,040% ± 62,200.04% (P < 0.01). [1] Western blot analysis showed that ponicidin (10–50 μmol/L for 6 h) decreased the phosphorylation of JAK2 and STAT3 in a dose-dependent manner without affecting total JAK2 and STAT3 protein levels. [1] Ponicidin (25–50 μmol/L for 48 h) decreased the protein expression of VEGF, VEGFR2, and Bcl-2, and increased the expression of Bax and the active form of caspase-3 in a dose-dependent manner. [1] Caspase-3 activity was increased by ponicidin (10–50 μmol/L) in a time- and dose-dependent manner. At 50 μmol/L for 48 h, caspase-3 activity increased from 15.57% ± 0.47% (control) to 28.76% ± 0.38% (P < 0.01). [1] |
| Cell Assay |
Cell viability was assessed using the Cell Counting Kit-8 (CCK8). MKN28 cells (5×10³ cells/well) were seeded in 96-well plates and treated with ponicidin (10, 25, 50 μmol/L) for 0, 12, 24, 48, and 72 h. Absorbance was measured at 450 nm. [1]
Apoptosis was detected by annexin V-FITC/propidium iodide (PI) double staining and flow cytometry. Cells were treated with ponicidin (10, 25, 50 μmol/L) for 48 h, then resuspended in binding buffer with annexin V-FITC and PI, incubated in the dark for 10 min, and analyzed by flow cytometry. [1] Cell cycle analysis was performed by PI staining. Cells were treated with ponicidin (10, 25, 50 μmol/L) for 48 h, fixed in 70% cold ethanol overnight, washed, incubated with RNase (1 mg/mL) for 10 min, stained with PI (1 mg/mL) for 30 min at 4°C, and analyzed by flow cytometry. [1] Intracellular ROS generation was measured using dihydroethidium (DHE). After treatment with ponicidin (10, 25, 50 μmol/L) for 1, 6, 24, and 48 h, cells were resuspended with 50 μmol/L DHE, and fluorescence intensity was measured by flow cytometry. [1] Western blot analysis was performed using standard protocols. Cells were lysed, proteins were separated by SDS-PAGE, transferred to membranes, and probed with antibodies against JAK2, p-JAK2, STAT3, p-STAT3, VEGF, VEGFR2, Bcl-2, Bax, caspase-3, and GAPDH (loading control). [1] Caspase-3 activity was measured using a colorimetric assay kit. After treatment, cells were lysed, and 100 μg of protein was incubated with substrate. Absorbance was read at 405 nm. [1] |
| References | |
| Additional Infomation |
Ponicidin is a diterpenoid compound extracted from the traditional Chinese herbs Rabdosia rubescens or Isodon japonicas. It has been reported to have immunoregulatory, anti-inflammatory, and anti-viral effects, particularly in upper respiratory tract infections. This study demonstrates that ponicidin inhibits proliferation and induces apoptosis in MKN28 gastric carcinoma cells via suppression of the JAK2/STAT3 signaling pathway, downregulation of Bcl-2, upregulation of Bax, and activation of caspase-3. Ponicidin may serve as a potential therapeutic agent for gastric carcinoma. [1]
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| Molecular Formula |
C20H26O6
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|---|---|
| Molecular Weight |
362.41684
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| Exact Mass |
362.172
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| CAS # |
52617-37-5
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| PubChem CID |
14564539
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| Appearance |
White to off-white solid powder
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| Density |
1.5±0.1 g/cm3
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| Boiling Point |
580.9±50.0 °C at 760 mmHg
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| Flash Point |
210.0±23.6 °C
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| Vapour Pressure |
0.0±3.7 mmHg at 25°C
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| Index of Refraction |
1.649
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| LogP |
3.11
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| Hydrogen Bond Donor Count |
3
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| Hydrogen Bond Acceptor Count |
6
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| Rotatable Bond Count |
0
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| Heavy Atom Count |
26
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| Complexity |
761
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| Defined Atom Stereocenter Count |
0
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| InChi Key |
WHRDRHNMTIXZNY-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C20H26O6/c1-8-9-4-5-10-18-11(21)6-7-17(2,3)12(18)14(23)20(24)19(10,13(8)22)15(9)25-16(18)26-20/h9-12,14-16,21,23-24H,1,4-7H2,2-3H3
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| Chemical Name |
13,14,19-trihydroxy-16,16-dimethyl-6-methylidene-10,12-dioxahexacyclo[9.8.0.01,15.02,8.05,9.08,13]nonadecan-7-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 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 : ~125 mg/mL (~344.90 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (5.74 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 20.8 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: ≥ 2.08 mg/mL (5.74 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 20.8 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: ≥ 2.08 mg/mL (5.74 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 | 2.7592 mL | 13.7961 mL | 27.5923 mL | |
| 5 mM | 0.5518 mL | 2.7592 mL | 5.5185 mL | |
| 10 mM | 0.2759 mL | 1.3796 mL | 2.7592 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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