| CAS |
63968-64-9 |
| Chinese Name |
青蒿素 |
| English Name |
Artemisinin |
| Synonyms |
NSC 369397 |
| Molecular Formula |
C15H22O5 |
| Molecular Weight |
282.33 |
| Solubility |
Soluble in DMSO ≥10mg/mL |
| Purity |
HPLC≥98% |
| Appearance |
White to off-white Solid |
| Storage |
Powder:2-8℃，2 years;Insolvent(Mother Liquid):-20℃，6 months;-80℃，1 year |
| EC |
EINECS 1806241-263-5 |
| MDL |
MFCD00081057 |
| SMILES |
O=C1[C@H](C)[C@]2([H])CC[C@@H](C)[C@]3([H])CC[C@@](O4)(C)OO[C@]32[C@]4([H])O1 |
| InChIKey |
BLUAFEHZUWYNDE-NNWCWBAJSA-N |
| InChI |
InChI=1S/C15H22O5/c1-8-4-5-11-9(2)12(16)17-13-15(11)10(8)6-7-14(3,18-13)19-20-15/h8-11,13H,4-7H2,1-3H3/t8-,9-,10+,11+,13-,14-,15-/m1/s1 |
| PubChem CID |
68827 |
| Target Point |
Others |
| Passage |
Others |
| Background |
Artemisin is a sesquiterpene lactone with anti malaria activity. Artemisin can reduce the proliferation, migration, invasion, tumorigenesis and metastasis of cancer cells, and also has neuroprotective activities. |
| Biological Activity |
Artemisinin (also known as qinghaosu in Chinese), discovered by Tu Youyou (2015 Nobel Prize winner in Medicine), is an anti-malarial drug isolated from the aerial parts of Artemisia annua L. plants. Artemisinin and its semi-synthetic derivatives are a group of drugs that possess the most rapid action of all current drugs against Plasmodium falciparum malaria.[6] |
| In Vitro |
青蒿素(3.125-100μM)浓度依赖性地抑制Aβ25-35在PC12细胞中诱导的细胞毒性。青蒿素(25μM)抑制Aβ25-35诱导的LDH释放，细胞凋亡和ROS产生，减弱Aβ诱导的线粒体膜电位损失和caspase 3/7活性增加，并在时间和浓度下刺激ERK1/2的磷酸化。依赖于PC12细胞的方式。 ERK 1/2途径介导青蒿素对PC12细胞的保护作用[1]。青蒿素在MCF-7/Dox细胞系中显示细胞毒活性，处理24小时后IC50为3.7±0.4μg/ mL。此外，青蒿素处理MCF-7细胞，对Dox和DDP敏感和抗性，导致蛋白质如LF，FTH1和HEP的表达降低。由于抑制VEGF表达和细胞迁移，青蒿素激活p38 MAPK激酶级联，而不管氧化应激[2]。青蒿素(50，100或200 mg)显著抑制异氟醚诱导的海马神经元丢失，降低caspase-3阳性细胞计数，并切割caspase-3表达，并调节凋亡途径蛋白的表达。青蒿素调节JNK/ERK 1/2信号传导和组蛋白乙酰化[3]。青蒿素以剂量依赖性方式抑制HCV复制，EC50值为167±38μM。青蒿素及其最有效的类似物通过诱导活性氧(ROS)部分抑制HCV的体外复制[4]。青蒿素以剂量依赖的方式显著抑制VSMC增殖。青蒿素(1 mM)72 h显著降低增殖细胞核抗原信使RNA的表达[5]。 |
| In Vivo |
青蒿素(50，100或200mg/kg b.wt /天，po)防止异氟醚诱导的工作记忆损伤，如在T迷宫测试中观察到的。青蒿素增强暴露于异氟醚的大鼠的空间导航和记忆。与单独使用异氟醚的大鼠相比，青蒿素处理的大鼠表现出明显更好的表现[3]。 |
| Cell Experiment |
为此目的，将细胞在补充有胰岛素的DMEM中的96孔板中培养。将青蒿素，Dox和DDP以不同浓度添加到培养基中，并将细胞培养24或48小时。为此目的，青蒿素在培养基中的0.01％DMSO中稀释。此后，向细胞中加入10μLMTT染料溶液(在磷酸盐缓冲盐水中5mg/mL);将细胞在相同条件下孵育3小时。离心(1500rpm，5分钟)后，除去上清液。向每个孔中加入100μL二甲基亚砜，以溶解甲..使用多孔分光光度计在540nm的波长下测量吸收。 |
| Animal Experiment |
通过口服强饲法每天从P2到P21给予单独的一组大鼠幼仔(总大鼠幼崽80;每组n = 16)青蒿素(50，100或200mg/kg体重)。在P7上，幼崽在温度控制室中暴露于异氟烷(0.75％在30％氧气或空气中)6小时。未暴露于麻醉但未给予青蒿素的动物作为对照组，而单独接受异氟醚的大鼠被归类为麻醉对照。 |
| Kinase Experiment |
简言之，将PC12细胞在裂解缓冲液中裂解并以12，500×g离心5分钟。将15mL细胞裂解物与50mL 2X底物工作溶液在室温下在96孔板中孵育30分钟。然后通过Infinite M200 PRO多模微孔板在490nm的激发波长和520nm的发射下测定荧光强度。将每个样品的荧光强度标准化为样品的蛋白质浓度。将％caspase 3/7活性的所有值标准化为对照组。 |
| Data Literature Source |
[1]. Zeng Z，et al. Artemisinin protects PC12 cells against β-amyloid-induced apoptosis through activation of the ERK1/2 signaling pathway. Redox Biol. 2017 Apr 4;12:625-633.
[2]. Chekhun VF，et al. Artemisinin modulating effect on human breast cancer cell lines with different sensitivity to cytostatics. Exp Oncol. 2017 Mar;39(1):25-29.
[3]. Xu G，et al. Neuroprotective effects of artemisinin against isoflurane-induced cognitive impairments and neuronal cell death involve JNK/ERK1/2 signalling and improved hippocampal histone acetylation in neonatal rats. J Pharm Pharmacol. 2017 Mar 12.
[4]. Obeid S，et al. Artemisinin analogues as potent inhibitors of in vitro hepatitis C virus replication. PLoS One. 2013 Dec 11;8(12):e81783.
[5]. Wang HY，et al. The effects of artemisinin on the proliferation and apoptosis of vascular smooth muscle cells of rats. Cell Biochem Funct. 2013 Sep 17.
[6]. Redox Biol. 2017 Apr 4;12:625-633. |
| Unit |
Bottle |
| Specification |
50mg 10mM*1mL in DMSO 200mg |
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