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| 100mg |
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Purity: ≥98%
Dihydroartemisinin (DHA) is a semi-synthetic derivative and active metabolite of artemisinin that is isolated from the traditional Chinese herb Artemisia annua. Dihydro Artemisinin is an active antimalarial metabolite. It is also the main metabolite of the following substances such as Artemisinin, Arteether, Artemether, Artesunate.
| Targets |
RelA;Plasmodium;Autophagy
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|---|---|
| ln Vitro |
DHA, or dihydroartemisinin, is an antimalarial drug. Treatment with dihydroartemisinin successfully raises the level of the RelA/p65 protein in the cytosol and lowers the level of the protein in the nucleus. Rather than inhibiting the synthesis of RelA/p65 proteins, dihydroartemisinin prevents RelA/p65 from being translocated from the cytosol to the nucleus. In RPMI 8226 cells, dihydroartemisinin induces autophagy. In RPMI 8226 cells, dihydroartemisinin inhibits NF-κB activation. Using the EMSA assay, the NF-κB Dihydroartemisinin-binding activity is investigated. Following a 12-hour exposure to varying Dihydroartemisinin (10, 20, and 40 μM) concentrations, TNF-α is added as a positive control for NF-κB activation. Unlike TNF-α, dihydroartemisinin suppresses NF-κB activation in a dose-dependent manner[1].
Cell viability is examined using the MTT assay, and dihydroartemisinin (DHA) can amplify the anti-tumor effect of photodynamic therapy (PDT) on esophageal cancer cells. Dihydroartemisinin (80 μM), PDT (25 and 20 J/cm2, respectively), or both are used to treat Eca109 and Ec9706 cells. In Eca109 cells, a single treatment with Dihydroartemisinin or PDT reduces viability by 37±5% or 34±6%, and in Ec9706 cells, it reduces viability by 33±7% or 34±6%. On the other hand, PDT plus Dihydroartemisinin reduces cell viability in the cell lines by 59±6% or 61±7%, respectively[2]. |
| ln Vivo |
Given once on days 6-8 post-infection, single oral doses of Dihydroartemisinin (at 200, 300, 400, or 600 mg/kg) reduce total worm burdens by 69.2%-90.6% and female worm burdens by 62.2%-92.2%, depending on dosage in the first experiment. Similar therapies administered between days 34 and 36 after infection decrease the overall worm burden by 73.9% to 85.5% and the female worm burden by 83.8% to 95.3%[3].
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| Enzyme Assay |
The NF-κB Dihydroartemisinin-binding activity is measured using an electrophoretic mobility shift assay (EMSA). Prepared nuclear extracts are incubated for 30 minutes at 37 °C with a 45-mer double-stranded oligonucleotide, labeled with 32P ends and containing 15 μg protein and 16 fmol DNA, derived from the HIV long terminal repeat, 5′-TTGTTACAAGGGACTTTCCGCTG GGGACTTTCCAGGGAGGCGTGG-3′ (boldface designating NF-κB binding sites). On 6.6% native polyacrylamide gels, the Dihydroartemisinin-protein complex is separated from free oligonucleotide. To investigate the binding specificity of NF-κB to DNA, a double-stranded mutated oligonucleotide known as 5′-TTGTTACAA CTCACTTTCCGCTGCTCACTTTCCAGGGAGGCGTGG-3′ is employed. In addition, competition with the unlabeled oligonucleotide is used to assess the binding specificity. There is also preimmune serum (PIS) as a negative control. A Storm 820 is used to visualize the dried gels, and Imagequant software is used to quantify radioactive bands[1].
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| Cell Assay |
Cell attachment is facilitated by cultivating Eca109 (4×103 cells/well) and Ec9706 (5×103 cells/well) in 96-well plates for an entire night. Dihydroartemisinin (80 μM), PDT (25 and 20 J/cm2, respectively), or both are used to treat Eca109 and Ec9706 cells. MTT (20 μL) is added to each well and incubated for 4 hours at 37°C after the initial 24 hours of incubation. For ten minutes, while shaking, formazan crystals are dissolved in 150 μL of DMSO. The experiment is conducted three times, with the absorbance being measured at 490 nm on a plate reader[2].
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| Animal Protocol |
Mice
The mice used are Kunming strain mice, weighing 20–24 g each. In the first experiment, mice are given three daily doses of 200, 300, 400, or 600 mg of dihydroartemisinin/kg (in dose volumes of 25 mL/kg) on days 6–8, or 34–36 post-infection, respectively, in order to examine the effects of multiple doses of the drug on the schistosomula and adult worms of S. japonicum. As a control, another set of mice is also infected but does not receive the medication. |
| References |
| Molecular Formula |
C15H24O5
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|---|---|
| Molecular Weight |
284.35
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| Exact Mass |
284.16
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| Elemental Analysis |
C, 63.36; H, 8.51; O, 28.13
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| CAS # |
71939-50-9
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| Related CAS # |
Dihydroartemisinin-d3;176774-98-4
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| Appearance |
Solid powder
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| SMILES |
O[C@@H]1[C@H](C)[C@]2([H])CC[C@@H](C)[C@]3([H])CC[C@@](O4)(C)OO[C@]32[C@]4([H])O1
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| InChi Key |
BJDCWCLMFKKGEE-ISOSDAIHSA-N
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| InChi Code |
InChI=1S/C15H24O5/c1-8-4-5-11-9(2)12(16)17-13-15(11)10(8)6-7-14(3,18-13)19-20-15/h8-13,16H,4-7H2,1-3H3/t8-,9-,10+,11+,12+,13-,14-,15-/m1/s1
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| Chemical Name |
(3R,5aS,6R,8aS,9R,10S,12R,12aR)-3,6,9-trimethyldecahydro-12H-3,12-epoxy[1,2]dioxepino[4,3-i]isochromen-10-ol
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| Synonyms |
Dihydroartemisinin; Artenimol; DHQHS 2; Alaxin; JAV-110; VM-3352; AC-2067; JAV110; VM3352; AC 2067;JAV-110; VM 3352; AC 2067;
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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) |
DMSO : 25 ~50 mg/mL ( 87.92 ~175.83 mM )
Ethanol : 7~10 mg/mL(35.17 mM) |
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| Solubility (In Vivo) |
Solubility in Formulation 1: 2.08 mg/mL (7.31 mM) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), suspension solution; with heating and sonication.
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 (7.31 mM) 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; with heating and sonication. 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 (7.31 mM) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. Solubility in Formulation 4: ≥ 1 mg/mL (3.52 mM) (saturation unknown) in 10% EtOH + 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 10.0 mg/mL clear EtOH stock solution to 400 μL of PEG300 and mix evenly; then add 50 μL of Tween-80 to the above solution and mix evenly; then add 450 μL of 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 5: ≥ 1 mg/mL (3.52 mM) (saturation unknown) in 10% EtOH + 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 10.0 mg/mL clear EtOH 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. Solubility in Formulation 6: ≥ 1 mg/mL (3.52 mM) (saturation unknown) in 10% EtOH + 90% Corn Oil (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 10.0 mg/mL clear EtOH stock solution to 900 μL of corn oil and mix well. Solubility in Formulation 7: 6%DMSO + 94%Corn oil: 3mg/ml (10.55mM) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 3.5168 mL | 17.5840 mL | 35.1679 mL | |
| 5 mM | 0.7034 mL | 3.5168 mL | 7.0336 mL | |
| 10 mM | 0.3517 mL | 1.7584 mL | 3.5168 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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