Artemisinine
(Synonyms: 青蒿素; Qinghaosu; NSC 369397) 目录号 : GN10647
Artemisinine是一种从青蒿植物（Artemisia annua）中提取的倍半萜内酯类抗疟药。
Cas No.:63968-64-9
Sample solution is provided at 25 µL, 10mM.
_1-3.$$$39978408@51.jpg');)
_1-9.$$$38538795@65.jpg');)
_1-9.$$$39112701@51.jpg');)
_1-7.$$$37316672@70.jpg');)
_366-372.$$$36198801@70.jpg');)
.$$$38565142@65.jpg');)
_1867-1883.$$$33248023@67.jpg');)
_eads6055.$$$39977546@45.jpg');)
_eadm9805.$$$40080571@45.jpg');)
_eadj3020.$$$39666821@45.jpg');)
_1-20.$$$39757301@28.jpg');)
_1-24.$$$38898113@28.jpg');)
_273-287.$$$36806353@46.jpg');)
_1-16.$$$37156877@44.jpg');)
_1-19.$$$37460805@44.jpg');)
_1291-1307.$$$34518654@46.jpg');)
Artemisinine is a sesquiterpene lactone antimalarial drug extracted from the plant Artemisia annua[1]. Artemisinine interferes with the biological membrane structure of the malaria parasite, particularly the mitochondrial and endoplasmic reticulum membranes, leading to the death of the parasite and thus is widely used in the treatment of malaria[2]. Artemisinine has also been studied for its potential applications in treating various diseases, including antiviral activity, cancer, metabolic syndrome, and fibrosis[3][4].
In vitro, pretreatment of PC12 cells with Artemisinine(3.125–100μM; 1h) concentration-dependently inhibited Aβ25–35-induced cytotoxicity, reduced the release of lactate dehydrogenase (LDH), decreased intracellular reactive oxygen species (ROS) generation, restored mitochondrial membrane potential (△ψm), and inhibited the increase in caspase 3/7 activity associated with apoptosis[5]. Pretreatment of HT-22 cells with Artemisinine(25μM; 12h) significantly reduced glutamate-induced cell death and activated Akt/Bcl-2 signaling[6].
In vivo, treatment of STZ-induced T2DM mice with Artemisinine (40mg/kg/day; i.p.; 4 weeks) significantly reversed diabetic cognitive impairments, decreased the levels of ROS, MDA, and Fe²⁺ in the hippocampus, increased the levels of Nrf2, HO-1, GPX4, and GSH, and alleviated neuronal ferroptosis and neuronal loss in the hippocampal CA1 region[7]. Artemisinine (10mg/kg/day; i.p.; 7 days) reversed ischemic stroke-induced neuronal pyroptosis in photochemically induced thrombosis (PIT) model mice, decreased the levels of IL-1β and IL-18 in serum, and downregulated the expression of key proteins NLRP3, ASC-1, Caspase-1, and TXNIP in mouse brain tissue[8].
References:
[1] Tu Y. Artemisinin-A Gift from Traditional Chinese Medicine to the World (Nobel Lecture). Angew Chem Int Ed Engl. 2016;55(35):10210-10226.
[2] Ribbiso KA, Heller LE, Taye A, Julian E, Willems AV, Roepe PD. Artemisinin-Based Drugs Target the Plasmodium falciparum Heme Detoxification Pathway. Antimicrob Agents Chemother. 2021;65(4):e02137-20.
[3] Augustin Y, Staines HM, Krishna S. Artemisinins as a novel anti-cancer therapy: Targeting a global cancer pandemic through drug repurposing. Pharmacol Ther. 2020;216:107706.
[4] Addissouky T A .Artemisinin and its derivatives throughout the therapeutic mechanisms and clinical potential.Discover Chemistry. 2025, 2(1):1-16.
[5] Zeng Z, Xu J, Zheng W. Artemisinin protects PC12 cells against β-amyloid-induced apoptosis through activation of the ERK1/2 signaling pathway. Redox Biol. 2017;12:625-633.
[6] Lin SP, Li W, Winters A, Liu R, Yang SH. Artemisinin Prevents Glutamate-Induced Neuronal Cell Death Via Akt Pathway Activation. Front Cell Neurosci. 2018;12:108.
[7] Wang B, Zhu S, Guo M, et al. Artemisinin ameliorates cognitive decline by inhibiting hippocampal neuronal ferroptosis via Nrf2 activation in T2DM mice. Mol Med. 2024;30(1):35.
[8] Wang Y, Yuan H, Shen D, et al. Artemisinin attenuated ischemic stroke induced pyroptosis by inhibiting ROS/TXNIP/NLRP3/Caspase-1 signaling pathway. Biomed Pharmacother. 2024;177:116894.
Artemisinine是一种从青蒿植物（Artemisia annua）中提取的倍半萜内酯类抗疟药[1]。Artemisinine通过干扰疟原虫的生物膜结构，特别是线粒体和内质网膜，导致疟原虫死亡，因此被广泛用于疟疾治疗[2]。Artemisinine还被研究用于抗病毒、抗癌、代谢综合征、纤维化等多种疾病的治疗[3][4]。
在体外实验中，用Artemisinine（3.125–100μM；1小时）预处理PC12细胞，浓度依赖性地抑制了Aβ25–35诱导的细胞毒性，减少了乳酸脱氢酶（LDH）的释放，降低了细胞内活性氧（ROS）的生成，恢复了线粒体膜电位（△ψm），并抑制了与凋亡相关的caspase 3/7活性的增加[5]。用Artemisinine（25μM；12小时）预处理HT-22细胞，显著减少了谷氨酸诱导的细胞死亡，并激活了Akt/Bcl-2信号通路[6]。
在体内实验中，用Artemisinine（40mg/kg/天；腹腔注射；4周）处理STZ诱导的2型糖尿病（T2DM）小鼠，显著改善了糖尿病引起的认知功能障碍，降低了海马体中ROS、丙二醛（MDA）和Fe²⁺的水平，增加了Nrf2、HO-1、GPX4和GSH的水平，并减轻了海马体CA1区的神经元铁死亡和神经元丢失[7]。Artemisinine（10mg/kg/天；腹腔注射；7天）逆转了光化学诱导血栓（PIT）模型小鼠中缺血性中风诱导的神经元焦亡，降低了血清中IL-1β和IL-18的水平，并下调了小鼠脑组织中关键蛋白NLRP3、ASC-1、Caspase-1和TXNIP的表达[8]。
| Cell experiment [1]: | |
Cell lines | PC12 cells |
Preparation Method | PC12 cells were cultured in 75cm2 flasks in DMEM supplemented with 5% fetal bovine serum (FBS), 5% horse serum, 100μg/ml streptomycin, 100U/ml penicillin and incubated at 37°C with 5% CO2 humidified atmosphere. The medium was replaced every 2–3 days, and cells were sub-cultured by trypsin treatment twice a week, at a split of 1:4. PC12 cells were seeded in 96-well plates (coated with 10μg/ml poly-D-lysine) at a density of 4–8×105 cells/well in 1% serum medium for 24h. After serum starvation, the cultures were incubated with Artemisinine(3.125–100μM) for 1h, and then treated with Aβ 25-35; 24h later MTT assay was performed. Then the cells were incubated with MTT (0.5mg/ml) for additional 3h. The medium was aspirated from each well and DMSO (200μl) was added. The absorbance of each well solution was obtained with a Multiskan Ascent Revelation Plate Reader and the data are presented as Optical Density (OD) at wavelength of 570nm. Assays were repeated at least three to six times in quadruplicate. |
Reaction Conditions | 3.125–100μM; 1h |
Applications | Artemisinine significantly inhibit cell death induced by Aβ 25-35. |
| Animal experiment [2]: | |
Animal models | C57BL/6J mice |
Preparation Method | Eighty four C57BL/6J mice (male, 5 weeks) were kept in an environment with a 12h light/dark cycle and a relative humidity of 60–65% at 25±1°C and had free access to food and water. T2DM mouse models were induced by a high fat diet (HFD) and STZ. These T2DM mice were further randomly divided into T2DM group and T2DM+Artemisinine group (n=12 per group). The mice were given Artemisinine (40mg/kg, i.p.) or an equal volume of vehicle (5% DMSO solution) once daily for 4 consecutive weeks. After the Y-maze test (YMT) Morris water maze test (MWMT), hippocampal tissues were harvested for hematoxylin and eosin (H&E) staining, transmission electron microscopy (TEM) analysis, and measurement of the iron, ROS, MDA and GSH concentrations by kits. The protein levels of p-Nrf2 and GPX4 were detected by western blotting. |
Dosage form | 40mg/kg/day; i.p.; 4 weeks |
Applications | Artemisinine(40mg/kg/day; i.p.; 4 weeks) significantly reversed diabetic cognitive impairments, decreased the levels of ROS, MDA, and Fe²⁺ in the hippocampus, increased the levels of Nrf2, HO-1, GPX4, and GSH, and alleviated neuronal ferroptosis and neuronal loss in the hippocampal CA1 region. |
References: | |
| Cas No. | 63968-64-9 | SDF | |
| 别名 | 青蒿素; Qinghaosu; NSC 369397 | ||
| 化学名 | (5aS,6R,8aS,9R,12S,12aR)-3,6,9-trimethyloctahydro-3H-3,12-epoxy[1,2]dioxepino[4,3-i]isochromen-10(12H)-one | ||
| Canonical SMILES | O=C1O[C@]2([H])OC3(C([H])([H])[H])OO[C@]42[C@](C([H])([H])C3([H])[H])([H])[C@@](C([H])([H])[H])([H])C([H])([H])C([H])([H])[C@@]4([H])[C@@]1([H])C([H])([H])[H] | ||
| 分子式 | C15H22O5 | 分子量 | 282.33 |
| 溶解度 | ≥ 13.7mg/mL in DMSO | 储存条件 | Store at 2-8°C |
| General tips | 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。 储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
||
| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
 |
1 mg | 5 mg | 10 mg |
| 1 mM | 3.542 mL | 17.7098 mL | 35.4195 mL |
| 5 mM | 0.7084 mL | 3.542 mL | 7.0839 mL |
| 10 mM | 0.3542 mL | 1.771 mL | 3.542 mL |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。
Quality Control & SDS
- View current batch:
- Purity: >99.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet