Artesunate (Synonyms: Artesunic Acid, NSC 712571, WR 256283) |
| Katalog-Nr.GC10889 |
Ableitung des Naturprodukts Artemisinin
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 88495-63-0
Sample solution is provided at 25 µL, 10mM.
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Artesunate is an antimalarial compound and an inhibitor of signal transducer and activator of transcription 3 (STAT-3) and membrane glutathione S-transferase (EXP1) [1, 2]. Artesunate is a sesquiterpene lactone with anti-tumor, anti-inflammatory, anti-fibrotic, and antiviral activities [3].
In vitro, treatment of gastric cancer cell line SGC-7901 cells with artesunate (0, 30, 60, 120 mM) for 24 h significantly increased the cell apoptosis rate, Bax and Caspase-3 protein expression levels, and significantly reduced the cell proliferation index, CDC25A, Bcl-2 protein expression, and mitochondrial membrane potential [4]. Treatment of human glioma cells LN-229 with artesunate (5-50 μg/mL) induced apoptosis and necrosis, DNA oxidative damage, and a continuous increase in DNA double-strand breaks, causing a dose-dependent increase in the levels of phosphorylated ATM, ATR, Chk2, and Chk1 [5].
In vivo, Artesunate (50 mg/kg) was intraperitoneally injected into mice transplanted with ovarian cancer cells (A2780 and HO8910 cells) for 16 days. Treatment alone had no significant effect on the growth of both transplanted tumors, while the tumor growth of the group treated with cisplatin was significantly slowed down[6]. Artesunate (200 mg/kg) was orally treated with mice infected with Plasmodium berghei, which significantly reduced the number of congested capillaries, endothelial cell thickness, and detachment of leukocytes from the vascular wall in brain slices, and reduced the expression of TNF-α in brain tissue [7].
References:
[1] Ilamathi M, Santhosh S, Sivaramakrishnan V. Artesunate as an anti-cancer agent targets stat-3 and favorably suppresses hepatocellular carcinoma[J]. Current topics in medicinal chemistry, 2016, 16(22): 2453-2463.
[2] Lisewski A M, Quiros J P, Ng C L, et al. Supergenomic network compression and the discovery of EXP1 as a glutathione transferase inhibited by artesunate[J]. Cell, 2014, 158(4): 916-928.
[3] Shi M, Yang X. Research Progress on Anti-tumor Mechanism of Artesunate Combined Drugs[J]. Academic Journal of Science and Technology, 2024, 10(1): 197-201.
[4] Wang L, Liu L, Wang J, et al. Inhibitory effect of artesunate on growth and apoptosis of gastric cancer cells[J]. Archives of medical research, 2017, 48(7): 623-630.
[5] Berdelle N, Nikolova T, Quiros S, et al. Artesunate induces oxidative DNA damage, sustained DNA double-strand breaks, and the ATM/ATR damage response in cancer cells[J]. Molecular cancer therapeutics, 2011, 10(12): 2224-2233.
[6] Wang B, Hou D, Liu Q, et al. Artesunate sensitizes ovarian cancer cells to cisplatin by downregulating RAD51[J]. Cancer biology & therapy, 2015, 16(10): 1548-1556.
[7] Souza M C, Paixao F H M, Ferraris F K, et al. Artesunate Exerts a Direct Effect on Endothelial Cell Activation and NF‐κB Translocation in a Mechanism Independent of Plasmodium Killing[J]. Malaria research and treatment, 2012, 2012(1): 679090.
| Cell experiment [1]: | |
Cell lines | A375 and WM115 adherent cells |
Preparation Method | After the treatment of different concentrations of artesunate (0, 30, 60, 120mM) on the gastric cancer cell line SGC-7901 cells for 24 h, the expression of CDC25A, Bcl-2, Bax, Caspase-3 protein, mitochondrial membrane potential, cell apoptosis and cell cycle were detected by flow cytometry. |
Reaction Conditions | 0, 30, 60, 120mM; 24h |
Applications | The cell apoptosis rate, Bax and Caspase-3 protein expression levels in each artesunate group were significantly increased. The cell proliferation index, CDC25A and Bcl-2 protein expression and mitochondrial membrane potential were significantly decreased. |
| Animal experiment [2]: | |
Animal models | Female nude mice |
Preparation Method | A2780 and HO8910 cells, 5×106 cells/ in 0.2 ml PBS, were injected subcutaneously into the left inguinal area of the female nude mice. Tumor-bearing mice were randomly divided into 4 groups and were administered daily via i.p. injection of artesunate (50 mg/kg), cisplatin (2 mg/kg), or in combination of the 2 for 16 days. |
Dosage form | 50mg/kg; i.p. |
Applications | Tumor growth was significantly reduced in the group receiving combined treatment of artesunate and cisplatin. In comparison, artesunate alone had no significant effect on the growth of tumor xenografts for both cell lines. |
References: [1]Wang L, Liu L, Wang J, et al. Inhibitory effect of artesunate on growth and apoptosis of gastric cancer cells[J]. Archives of medical research, 2017, 48(7): 623-630. [2]Wang B, Hou D, Liu Q, et al. Artesunate sensitizes ovarian cancer cells to cisplatin by downregulating RAD51[J]. Cancer biology & therapy, 2015, 16(10): 1548-1556. | |
| Cas No. | 88495-63-0 | SDF | |
| Überlieferungen | Artesunic Acid, NSC 712571, WR 256283 | ||
| Canonical SMILES | O=C(CCC(O)=O)O[C@H]1O[C@@H]2O[C@@]3(C)OO[C@]42[C@@H](CC3)[C@H](C)CC[C@H]4[C@H]1C | ||
| Formula | C19H28O8 | M.Wt | 384.42 |
| Löslichkeit | ≥ 16.3mg/mL in DMSO | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
|
1 mg | 5 mg | 10 mg |
| 1 mM | 2.6013 mL | 13.0066 mL | 26.0132 mL |
| 5 mM | 0.5203 mL | 2.6013 mL | 5.2026 mL |
| 10 mM | 0.2601 mL | 1.3007 mL | 2.6013 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
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Calculation results:
Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid 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 master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
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- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 34 reference(s) in Google Scholar.)
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