产品描述

Artesunate 是一种抗疟类药，作用于小细胞肺癌细胞系H69，IC50为< 5 μM。它是一种潜在的STAT3抑制剂，在体外对癌细胞有选择性细胞毒性作用；是有效的EXP1抑制剂。

靶点（IC50 & Targe）

STAT

体外研究

ART could alter the biomechanical properties of the glioma cells to inhibit cell proliferation, migration and invasion [2]. The ART significantly suppresses the cell proliferation, induces the apoptosis and promoted cell cycle arrest at G0/G1 phase in SKM-1 cells. The mechanisms of ART anti-MDS is associated with the increase of intracellular calciumion concentration and ROS levels. In addition, the pro-apoptotic activity of ART may be involved in the regulation of BCL-2 /BAX ratio and the expressions of P-bad and survivin[3]. ART treatment demethylates CDH1, which, in turn recovers the E-cadherin activation in SKM-1 cells[1].

体内研究

Artesunate is a medication used to treat malaria. Artesunate can induce radiosensitivity of HeLa cells in vivo using Xenograft model of nude mice[5]. Artesunate had a relatively high immunosuppressive activity with low toxicity, and could inhibit T lymphocyte proliferation induced by mitogen and alloantigen[6].

细胞实验

Cell lines: SKM-1 cells

Concentrations: 0, 12.5, 25, 50 µg/mL

Incubation Time: 0, 24, 48, and 72 h

Method: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)

动物实验

Animal Models: BALB/c mice

Formulation: Dissolved in DMSO and diluted with sterile PBS

Dosages: 100 mg/kg/day

Administration: i.p.

(Only for Reference)

参考文献

[1] Xu N, et al. Int J Med Sci. 2015, 12(6):524-529.

[2] Lian S, et al. Oncol Rep. 2016, 36(2):984-990.

[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] Li T, et al. Int Immunopharmacol. 2013, 16(2):306-312.

[7] Ilamathi M, et al. Curr Top Med Chem. 2016, 16(22):2453-63.