Dihydroartemisinin
(Synonyms: 双氢青蒿素; Dihydroqinghaosu; β-Dihydroartemisinin; Artenimol) 目录号 : GN10056
Dihydroartemisinin（双氢青蒿素；DHA）是青蒿素及其衍生物（ARTs）的活性代谢物，是临床广泛用于治疗疟疾的有效药物。
Cas No.:71939-50-9
Sample solution is provided at 25 µL, 10mM.
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Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
| Cell experiment [1]: | |
Cell lines | Eca109 and Ec9706 cells |
Preparation Method | Eca109 (4×103 cells/well) and Ec9706 (5×103 cells/well) cells were seeded in 96-well plates and cultured overnight. Cells were treated with 2.5-120μM Dihydroartemisinin. Cells treated with DMSO served as untreated controls. After incubation for 48 and 72h, cell viability was measured using the MTT assay. |
Reaction Conditions | 2.5-120μM; 48 and 72h |
Applications | Dihydroartemisinin reduced the viability of Eca109 and Ec9706 cells in a dose-dependent manner, with IC50 values of 76.86μM and 93.81μM, respectively. |
| Animal experiment [2]: | |
Animal models | Nude mice |
Preparation Method | HepG2 cells were suspended in sterile PBS and injected subcutaneously into the right flank of the mice. Mice were checked daily for tumor development. Mice were randomized into three groups of 6 mice/group. The Dihydroartemisinin group was given 20mg/kg Dihydroartemisinin, once daily for five consecutive days per week for 4 weeks. The control group was given normal saline, and the DMSO group received an equal volume of solvent control. After treatment at various time intervals, mouse body weight and tumor size were measured. Finally, tumors were excised, weighed and fixed in 4% of PFA. Paraffin-embedded tissues were then sectioned at 4nm and ready for immunohistochemitry and TUNEL assay. |
Dosage form | 20mg/kg; i.p. |
Applications | Dihydroartemisinin significantly inhibited the growth of HepG2 xenograft tumors and induced apoptosis in tumor tissues. |
References: | |
Dihydroartemisinin (DHA) is an active metabolite of artemisinin and its derivatives (ARTs) and is an effective drug widely used in the clinic to treat malaria[1]. Dihydroartemisinin exerts its anticancer effects through multiple molecular mechanisms, including inhibiting proliferation, inducing apoptosis, inhibiting tumor metastasis and angiogenesis, promoting immune function, inducing autophagy and endoplasmic reticulum stress[2]. Dihydroartemisinin can exert its cytotoxic effects through Fe(II)-mediated endoperoxide cleavage[3].
In vitro, Dihydroartemisinin (2.5-120μM) treated esophageal cancer cells (Eca109 and Ec9706 cells) for 48 and 72h, reducing cell viability in a dose-dependent manner, with IC50 values of 76.86μM and 93.81μM, respectively, and inducing cell apoptosis and cell cycle arrest[4]. Dihydroartemisinin (0-80µM) treatment of gastric cancer cells (SGC-7901, BGC823, and MGC803 cells) for 48 and 72h reduced cell viability in a dose-dependent manner and induced cell G1 arrest, apoptosis, and senescence[5].
In vivo, Dihydroartemisinin (20mg/kg) was intraperitoneally injected into mice inoculated with human hepatoma cells (HepG2) for 4 weeks, which significantly inhibited tumor growth and induced apoptosis of tumor tissue cells[6]. Dihydroartemisinin (20mg/kg) was intraperitoneally injected into colon cancer mice for 30 days, which significantly inhibited colon tumor formation, induced apoptosis of tumor tissue cells, and increased the expression of peroxisome proliferator-activated receptor γ (PPARγ)[7].
References:
[1] Zhang X G, Li G X, Zhao S S, et al. A review of dihydroartemisinin as another gift from traditional Chinese medicine not only for malaria control but also for schistosomiasis control[J]. Parasitology research, 2014, 113: 1769-1773.
[2] Dai X, Zhang X, Chen W, et al. Dihydroartemisinin: a potential natural anticancer drug[J]. International journal of biological sciences, 2021, 17(2): 603.
[3] Antoine T, Fisher N, Amewu R, et al. Rapid kill of malaria parasites by artemisinin and semi-synthetic endoperoxides involves ROS-dependent depolarization of the membrane potential[J]. Journal of antimicrobial chemotherapy, 2014, 69(4): 1005-1016.
[4] Du X X, Li Y J, Wu C L, et al. Initiation of apoptosis, cell cycle arrest and autophagy of esophageal cancer cells by dihydroartemisinin[J]. Biomedicine & Pharmacotherapy, 2013, 67(5): 417-424.
[5] Sun H, Meng X, Han J, et al. Anti-cancer activity of DHA on gastric cancer—an in vitro and in vivo study[J]. Tumor Biology, 2013, 34: 3791-3800.
[6] Zhang C Z, Zhang H, Yun J, et al. Dihydroartemisinin exhibits antitumor activity toward hepatocellular carcinoma in vitro and in vivo[J]. Biochemical pharmacology, 2012, 83(9): 1278-1289.
[7] Lu Z, Peng J H, Zhang R, et al. Dihydroartemisinin inhibits colon cancer cell viability by inducing apoptosis through up-regulation of PPARγ expression[J]. Saudi journal of biological sciences, 2018, 25(2): 372-376.
Dihydroartemisinin（双氢青蒿素；DHA）是青蒿素及其衍生物（ARTs）的活性代谢物，是临床广泛用于治疗疟疾的有效药物[1]。Dihydroartemisinin通过抑制增殖、诱导细胞凋亡、抑制肿瘤转移和血管生成、促进免疫功能、诱导自噬和内质网应激等多种分子机制发挥抗癌作用[2]。Dihydroartemisinin可以通过Fe(II)介导的内过氧化物裂解发挥细胞毒性作用[3]。
在体外，Dihydroartemisinin（2.5-120μM）处理食管癌细胞（Eca109和Ec9706细胞）48和72h，以剂量依赖性方式降低了细胞活力，IC50值分别为76.86μM和93.81μM，诱导了细胞凋亡和细胞周期阻滞[4]。Dihydroartemisinin（0-80µM）处理胃癌细胞（SGC-7901，BGC823，和MGC803细胞）48和72h，以剂量依赖性方式降低了细胞活力，诱导了细胞G1期停滞、细胞凋亡和衰老[5]。
在体内，Dihydroartemisinin（20mg/kg）通过腹腔注射治疗接种了人肝癌细胞（HepG2）的小鼠4周，显著抑制了肿瘤的生长，诱导了肿瘤组织细胞凋亡[6]。Dihydroartemisinin（20mg/kg）通过腹腔注射治疗结肠癌小鼠30天，显著抑制了结肠肿瘤形成，诱导了肿瘤组织细胞凋亡，增加了过氧化物酶体增殖物活化受体γ（PPARγ）的表达[7]。
| Cas No. | 71939-50-9 | SDF | |
| 别名 | 双氢青蒿素; Dihydroqinghaosu; β-Dihydroartemisinin; Artenimol | ||
| 化学名 | (3R,5aS,6R,8aS,9R,10R,12R,12aR)-3,6,9-trimethyldecahydro-3H-3,12-epoxy[1,2]dioxepino[4,3-i]isochromen-10-ol | ||
| Canonical SMILES | [H][C@@]1(C([H])([H])C2([H])[H])[C@]3([C@@]([C@@]4([H])C([H])([H])[H])([H])C([H])([H])C([H])([H])[C@@]1([H])C([H])([H])[H])OO[C@@]2(C([H])([H])[H])O[C@@]3([H])O[C@@]4([H])O[H] | ||
| 分子式 | C15H24O5 | 分子量 | 284.35 |
| 溶解度 | ≥ 14.05mg/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。 |
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| 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 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 3.5168 mL | 17.584 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 |
| 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。