Arenobufagin是一种从蟾蜍毒液中提取的天然bufadienolide类化合物，Arenobufagin可通过抑制PI3K/Akt/mTOR信号通路诱导细胞凋亡和自噬，并通过下调β-catenin抑制上皮-间质转化（EMT）来抑制肿瘤转移。
Cas No.:464-74-4
Sample solution is provided at 25 µL, 10mM.
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Arenobufagin is a natural bufadienolide compound extracted from toad venom. Arenobufagin can induce apoptosis and autophagy by inhibiting the PI3K/Akt/mTOR signaling pathway and suppress tumor metastasis by downregulating β-catenin to inhibit epithelial-mesenchymal transition (EMT)[1-2]. Arenobufagin can be used in studies related to various cancers, such as liver cancer, prostate cancer, and gastric cancer[3-4].
In vitro, treatment of HepG2 cells with Arenobufagin (6–50nM) for 24 hours, Arenobufagin significantly inhibited cell proliferation and induced autophagy-dependent ferroptosis, manifested as mitochondrial shrinkage, lipid ROS accumulation, decreased levels of GSH and T-SOD, and downregulation of Nrf2 and COX-2 protein expression via the p62-Keap1-Nrf2 pathway[5]. In AGS and MKN-45 gastric cancer cells treated with Arenobufagin (40nM) in combination with Cisplatin (28.37µM) for 24 hours, Arenobufagin significantly enhanced the effect of Cisplatin, inhibiting cell viability, migration, and colony formation, inducing G2/M phase arrest and apoptosis, and activating alkaliptosis by downregulating CA9 and upregulating IKBKB and NF-κB/p65, accompanied by reduced expression of MMP-2/MMP-9 and increased expression of E-cadherin[6].
In vivo, intraperitoneal injection of Arenobufagin (3.2mg/kg/day and 6.4mg/kg/day) in tumor-bearing (SW1990 cells) nude mice (administered every other day starting from day 7 after cell inoculation for 24 days), Arenobufagin significantly inhibited tumor growth, reduced tumor volume and weight, and induced changes in the expression of apoptosis- and autophagy-related proteins in tumor tissues[7]. In tumor-bearing (HCT116 cells) NOD/SCID mice, intraperitoneal injection of Arenobufagin (0.5mg/kg/day, 1mg/kg/day, and 2mg/kg/day) (administered daily starting from day 1 after tail vein cell inoculation for 32 days), Arenobufagin significantly reduced the number of lung metastatic nodules and inhibited colorectal cancer lung metastasis[8].
References:
[1] Dong Q, Turdu G, Akber Aisa H, et al. Arenobufagin, isolated from Bufo viridis toad venom, inhibits A549 cells proliferation by inducing apoptosis and G2/M cell cycle arrest. Toxicon. 2024 Mar;240:107641.
[2] Zhang DM, Liu JS, Deng LJ, et al. Arenobufagin, a natural bufadienolide from toad venom, induces apoptosis and autophagy in human hepatocellular carcinoma cells through inhibition of PI3K/Akt/mTOR pathway. Carcinogenesis. 2013 Jun;34(6):1331-42.
[3] Shang Z, Fan Y, Xi S, et al. Arenobufagin enhances T-cell anti-tumor immunity in colorectal cancer by modulating HSP90β accessibility. Phytomedicine. 2024 Jun;128:155497.
[4] Chen K, Li A, Wang J, et al. Arenobufagin causes ferroptosis in human gastric cancer cells by increasing rev-erbα expression. J Tradit Complement Med. 2022 Nov 8;13(1):72-80.
[5] Yang Y, Liu C, Wang M, et al. Arenobufagin regulates the p62-Keap1-Nrf2 pathway to induce autophagy-dependent ferroptosis in HepG2 cells. Naunyn Schmiedebergs Arch Pharmacol. 2024 Jul;397(7):4895-4909.
[6] Liu C, Li D, Wang J, et al. Arenobufagin increases the sensitivity of gastric cancer to cisplatin via alkaliptosis. Heliyon. 2023 Oct 19;9(11):e21110.
[7] Wei X, Yang J, Mao Y, et al. Arenobufagin Inhibits the Phosphatidylinositol 3-kinase/Protein Kinase B/Mammalian Target of Rapamycin Pathway and Induces Apoptosis and Autophagy in Pancreatic Cancer Cells. Pancreas. 2020 Feb;49(2):261-272.
[8] Wang M, Hu S, Yang J, et al. Arenobufagin inhibits lung metastasis of colorectal cancer by targeting c-MYC/Nrf2 axis. Phytomedicine. 2024 May;127:155391.
Arenobufagin是一种从蟾蜍毒液中提取的天然bufadienolide类化合物，Arenobufagin可通过抑制PI3K/Akt/mTOR信号通路诱导细胞凋亡和自噬，并通过下调β-catenin抑制上皮-间质转化（EMT）来抑制肿瘤转移[1-2]。Arenobufagin可用于肝癌、前列腺癌、胃癌等多种癌症的相关研究[3-4]。
在体外，Arenobufagin（6-50nM）处理HepG2细胞24小时，Arenobufagin显著抑制细胞增殖，并诱导自噬依赖的铁死亡，表现为线粒体皱缩、脂质ROS积累、GSH和T-SOD水平下降，同时通过p62-Keap1-Nrf2通路下调Nrf2和COX-2蛋白表达[5]。Arenobufagin（40nM）联合Cisplatin（28.37μM）处理AGS和MKN-45胃癌细胞24小时，Arenobufagin显著增加Cisplatin的效应，抑制细胞活力、迁移和克隆形成，并诱导G2/M期阻滞和凋亡。Arenobufagin通过下调CA9、上调IKBKB和NF-κB/p65激活碱死亡通路，伴随MMP-2/MMP-9表达降低和E-钙黏蛋白表达升高[6]。
在体内，Arenobufagin（3.2mg/kg/day和6.4mg/kg/day）腹腔注射处理荷瘤（SW1990细胞）裸鼠（从接种细胞后第7天开始，隔日一次，持续24天），Arenobufagin显著抑制肿瘤生长，降低肿瘤体积和重量，并诱导肿瘤组织中凋亡和自噬相关蛋白的表达变化[7]。Arenobufagin（0.5mg/kg/day、1mg/k/day和2mg/kg/day）腹腔注射处理荷瘤（HCT116细胞）NOD/SCID小鼠（从尾静脉接种细胞后第1天开始，每日一次，持续32天），Arenobufagin显著减少肺转移结节数量，抑制结直肠癌肺转移[8]。
| Cell experiment [1]: | |
Cell lines | HepG2 cells (human hepatocellular carcinoma cell line) |
Preparation Method | HepG2 cells were cultured in DMEM medium supplemented with 10% fetal bovine serum (FBS), 100U/mL penicillin, and 100μg/mL streptomycin at 37°C, 5% CO₂. HepG2 cells were treated with Arenobufagin at concentrations of 6nM, 12nM, 25nM, and 50nM for 24 hours. |
Reaction Conditions | 6-50μM; 24h |
Applications | Arenobufagin significantly inhibited HepG2 cell proliferation in a dose-dependent manner, with an IC₅₀ of 35.23nM. Arenobufagin induced autophagy-dependent ferroptosis, characterized by mitochondrial shrinkage, reduced mitochondrial ridges, accumulation of lipid ROS, and decreased levels of glutathione (GSH) and superoxide dismutase (T-SOD), while increasing malondialdehyde (MDA) levels. Arenobufagin downregulated ferroptosis-related proteins (Nrf2 and COX-2) and activated the p62-Keap1-Nrf2 pathway, promoting autophagosome formation and lipid peroxidation. |
| Animal experiment [2]: | |
Animal models | BALB/c nude mice |
Preparation Method | Mice were subcutaneously inoculated with SW1990 pancreatic cancer cells (1×10⁶cells/mouse) in the right flank. After tumor formation, mice were intraperitoneally administered Arenobufagin (3.2mg/kg and 6.4mg/kg) every other day for 24 days. Tumor volume and body weight were monitored periodically. |
Dosage form | 3.2mg/kg and 6.4mg/kg; i.p.; every other day for 24 days. |
Applications | Arenobufagin significantly inhibited tumor growth in a dose-dependent manner. Arenobufagin induced apoptosis and autophagy in tumor tissues, evidenced by increased cleavage of caspase-3/7/9 and PARP, elevated LC3 expression, and downregulated PI3K pathway proteins. No significant body weight changes indicated low systemic toxicity. |
References: | |
| Cas No. | 464-74-4 | SDF | |
| 别名 | 沙蟾毒精 | ||
| Canonical SMILES | C[C@]([C@@H](C(C=C1)=COC1=O)CC2)(C3=O)[C@]2([C@@](CC[C@@]4([H])[C@@]5(CC[C@H](O)C4)C)([H])[C@]5([H])[C@@H]3O)O | ||
| 分子式 | C24H32O6 | 分子量 | 416.51 |
| 溶解度 | Ethanol : 10 mg/mL (24.01 mM) | 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 | |||
 |
1 mg | 5 mg | 10 mg |
| 1 mM | 2.4009 mL | 12.0045 mL | 24.009 mL |
| 5 mM | 480.2 μL | 2.4009 mL | 4.8018 mL |
| 10 mM | 240.1 μL | 1.2005 mL | 2.4009 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。
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