| Description | Artesunate (WR-256283) is part of the artemisinin group of drugs that treat malaria. It is a semi-synthetic derivative of artemisinin that is water-soluble and may therefore be given by injection. It is on the World Health Organization's List of Essential Medicines. |
| In vitro | Artesunate 能改变胶质瘤细胞的生物力学特性，抑制细胞增殖、迁移和侵袭[2]。ART显著抑制SKM-1细胞的增殖，诱导凋亡并促进细胞周期在G0/G1阶段停滞。ART的抗MDS的机制与细胞内钙离子浓度及ROS水平的升高有关。此外，ART的促凋亡活性可能涉及BCL-2/BAX比率的调控以及P-bad 和 survivin 表达的调节[3]。ART处理通过去甲基化CDH1，进而恢复了SKM-1细胞中的E-cadherin激活[1]。 |
| In vivo | Artesunate 是一种用于治疗疟疾的化合物。在裸鼠异种移植模型中，Artesunate 能够诱导HeLa细胞的体内放射敏感性[5]。Artesunate 具有较高的免疫抑制活性和低毒性，能够抑制由有丝分裂原和异种抗原诱导的T淋巴细胞增殖[6]。 |
| Cell experiments | Growth inhibition assay: The SKM-1 cells (1×105/mL) are firstly seeded in 96-well plates. Artesunate is diluted in 0.1% dimethyl sulfoxide (DMSO) producing 0, 12.5, 25, 50µg/mL concentrations and added to the SKM-1 cells with 100 µl per well. A negative control is treated with 0.1% DMSO. At 0, 24, 48, and 72 hours, same amount of MTT solution is added into each well and cultured for extra 4 hours. MTT treated cells are fixed with 150 µL DMSO for 30 min at room temperature and then determined with Evolution 201 and 220 UV-Vis spectrophotometer system at 540 nm. (Only for Reference) |
| Synonyms | WR-256283, 青蒿琥酯 |
| molecular weight | 384.42 |
| Molecular formula | C19H28O8 |
| CAS | 88495-63-0 |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year |
| Solubility | Ethanol: 9 mg/mL(23.4 mM) H2O: < 1 mg/mL (insoluble or slightly soluble) DMSO: 55 mg/mL (143.07 mM) |
| References | 1. Xu N, et al. Int J Med Sci. 2015, 12(6):524-529. 2. Lian S, et al. Oncol Rep. 2016, 36(2):984-1990. 3. Qiao SK, et al. Zhongguo Shi Yan Xue Ye Xue Za Zhi. 2016, 24(1):131-137. 4. Lisewski AM, et al. Cell. 2014, 158(4):916-928. 5. Luo J, et al.Radiat Oncol. 2014, 9:84. 6. Wang B, et al. Artesunate sensitizes ovarian cancer cells to cisplatin by downregulating RAD51. Cancer Biol Ther. 2015;16(10):1548-56. 7. Ilamathi M, et al. Artesunate as an Anti-Cancer Agent Targets Stat-3 and Favorably Suppresses Hepatocellular Carcinoma. Curr Top Med Chem. 2016;16(22):2453-63. 8. Bowden G D, Land K M, O'Connor R M, et al. High-throughput screen of drug repurposing library identifies inhibitors of Sarcocystis neurona growth[J]. International Journal for Parasitology: Drugs and Drug Resistance. 2018 Apr；8(1): 137-144. |