Bufotalin
(Synonyms: 蟾蜍他灵) 目录号 : GC33134
Bufotalin是一种天然的强心类固醇，来源于蟾蜍分泌物。
Cas No.:471-95-4
Sample solution is provided at 25 µL, 10mM.
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Bufotalin is a natural cardiotonic steroid derived from toad secretions [1]. Bufotalin inhibits Na⁺/K⁺-ATPase and induces apoptosis of cancer cells [2]. Bufotalin has potent anti-tumor and cardiotonic effects [3-4].
In R-HepG2 cells, treatment with a relatively low concentrations of Bufotalin (0.05μM, 0.125μM; 24h, 48h) induced a remarkable G2/M arrest [5]. In A375 cells, Bufotalin (10-80ng/mL; 24h) significantly inhibited cell proliferation [6]. In MDA-MB-231 cells, Bufotalin (1-10μM; 72h) inhibits the proliferation of cells in a dose-dependent manner [7].
In bleomycin-induced lung fibrosis mice model, Bufotalin (1mg/kg, 2mg/kg; ip; 7d) reduces lung injury, inflammation, and fibrosis, and protects lung function [8]. In Sjögren’s syndrome (ESS) murine model, Bufotalin (10μg/kg; iv; twice a week for 7 weeks) inhibits Th17 polarization and secretion of cytokines IL-17 and IFN-γ [9]. In mice bearing U251 cell xenografts, Bufotalin (1mg/kg, 2mg/kg, 5mg/kg; ip; 14d) treatment resulted in a significant dose-dependent decrease in tumor volume and weight [10].
References:
[1]. El-Seedi HR, Yosri N, El-Aarag B, et al. Chemistry and the potential antiviral, anticancer, and anti-inflammatory activities of cardiotonic steroids derived from toads. Molecules. 2022 Oct 5; 27(19): 6586.
[2]. Mijatovic T, Dufrasne F, Kiss R. Cardiotonic steroids-mediated targeting of the Na+/K+-ATPase to combat chemoresistant cancers. Current medicinal chemistry. 2012 Feb 1; 19(5): 627-646.
[3]. Tian H, Zhao F, Yue BS, et al. Combinational Antitumor Strategies Based on the Active Ingredients of Toad Skin and Toad Venom. Drug Design, Development and Therapy. 2024 Dec 31:3549-3594.
[4]. Jia J, Li J, Zheng Q, et al. A research update on the antitumor effects of active components of Chinese medicine ChanSu. Frontiers in Oncology. 2022 Sep 27; 12: 1014637.
[5]. Zhang DM, Liu JS, Tang MK, et al. Bufotalin from Venenum Bufonis inhibits growth of multidrug resistant HepG2 cells through G2/M cell cycle arrest and apoptosis. European journal of pharmacology. 2012 Oct 5; 692(1-3): 19-28.
[6]. Pan Z, Qu C, Chen Y, et al. Bufotalin induces cell cycle arrest and cell apoptosis in human malignant melanoma A375 cells. Oncology reports. 2019 Apr; 41(4): 2409-2417.
[7]. Park SJ, Jung HJ. Bufotalin suppresses proliferation and metastasis of triple-negative breast cancer cells by promoting apoptosis and inhibiting the STAT3/EMT axis. Molecules. 2023 Sep 23; 28(19): 6783.
[8]. Yin JZ, Li ZQ, Zhang XD, et al. Bufotalin attenuates pulmonary fibrosis via inhibiting Akt/GSK-3β/β-catenin signaling pathway. European Journal of Pharmacology. 2024 Feb 5; 964: 176293.
[9]. Huang Y, Yang G, Fei J, et al. Bufotalin ameliorates experimental Sjögren’s syndrome development by inhibiting Th17 generation. Naunyn-Schmiedeberg's Archives of Pharmacology. 2020 Oct; 393: 1977-1985.
[10]. Tan J, Lin G, Zhang R, et al. Bufotalin induces oxidative stress-mediated apoptosis by blocking the ITGB4/FAK/ERK pathway in glioblastoma. Antioxidants. 2024 Sep 27; 13(10): 1179.
Bufotalin是一种天然的强心类固醇，来源于蟾蜍分泌物 [1]。Bufotalin可抑制Na⁺/K⁺-ATPase并诱导癌细胞凋亡 [2]。Bufotalin具有强效的抗肿瘤和强心作用 [3-4]。
在R-HepG2细胞中，较低浓度的Bufotalin（0.05μM、0.125μM；24h、48h）处理可诱导显著的G2/M期阻滞 [5]。在A375细胞中，Bufotalin（10-80ng/mL；24h）显著抑制细胞增殖 [6]。在MDA-MB-231细胞中，Bufotalin（1-10μM；72h）以剂量依赖性方式抑制细胞增殖 [7]。
在博来霉素诱导的肺纤维化小鼠模型中，Bufotalin（1mg/kg、2mg/kg；ip；7d）可减轻肺损伤、炎症和纤维化，并保护肺功能 [8]。在干燥综合征（ESS）小鼠模型中，Bufotalin（10μg/kg；iv；每周两次，持续7周）可抑制Th17极化以及细胞因子IL-17和IFN-γ的分泌 [9]。在携带U251细胞异种移植的小鼠中，Bufotalin（1mg/kg、2mg/kg、5mg/kg；ip；14d）治疗导致肿瘤体积和重量显著剂量依赖性下降 [10]。
| Cell experiment [1]: | |
Cell lines | R-HepG2 cells |
Preparation Method | Cell cycle distribution of R-HepG2 cells after Bufotalin treat ment was detected by flow cytometry. Briefly, R-HepG2 cells (about 6 × 105/well) were collected and fixed in 70% ethanol at 4℃ overnight. Before analysis, cells were centrifuged at 2500rpm for 3min to remove the ethanol. Then, cells were suspended in 500mL phosphate-buffered saline (PBS) containing 0.02mg/mL propidium iodide (PI) and 0.1mg/mL Ribonuclease A (RNase A) in darkness at 37℃ for 30min. Fluorescence emitted from PI-DNA complexes was measured by Epics XL flow cytometry. |
Reaction Conditions | 0.05μM, 0.125μM; 24h, 48h |
Applications | Cell cycle analysis showed that treatment with a relatively low concentrations of Bufotalin induced a remarkable G2/M arrest in R-HepG2 cells. |
| Animal experiment [2]: | |
Animal models | Bleomycin (BLM)-induced lung fibrosis mice model |
Preparation Method | Male C57BL/6 mice (6 weeks old, average weight approximately 22g) were housed in a standard environment which was characterized by 12h light/dark cycle, 22-25℃, and 40–60% humidity with free access to water and chow. A BLM-induced lung fibrosis model was performed. Firstly, a total of thirty-five mice were randomly divided into five groups: (i) sham control group; (ii) vehicle group; (iii) Bufotalin (1mg/kg) group; (iv) Bufotalin (2mg/kg) group; (v) positive control [pirfenidone (PFD, 30mg/kg)] group. Then, mice were anesthetized with 1% pentobarbital sodium (50mg/kg) by intraperitoneal injection and intratracheally administered 3mg/kg BLM in 50μL of sterile saline. Mice administered the same volume of sterile saline served as sham controls. From day 7 after BLM administration, mice were treated with Bufotalin, PFD, or their vehicle (15% PEG400 and 15% tween 80 saline solution) by intraperitoneal injection every day for 14 consecutive days. Finally, the mice were sacrificed 21 days post-BLM challenge. |
Dosage form | 1mg/kg, 2mg/kg; ip; 7d |
Applications | Bufotalin reduces lung injury, inflammation, and fibrosis, and protects lung function. |
References: | |
| Cas No. | 471-95-4 | SDF | |
| 别名 | 蟾蜍他灵 | ||
| Canonical SMILES | C[C@@]1(CC[C@@]2([H])[C@@]3([H])CC[C@@]4([H])[C@@]2(CC[C@H](O)C4)C)[C@@H](C(C=C5)=COC5=O)[C@@H](OC(C)=O)C[C@@]13O | ||
| 分子式 | C26H36O6 | 分子量 | 444.56 |
| 溶解度 | DMSO : ≥ 4.6 mg/mL (10.35 mM) | 储存条件 | Store at -20°C,protect from light |
| 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 | 2.2494 mL | 11.2471 mL | 22.4942 mL |
| 5 mM | 0.4499 mL | 2.2494 mL | 4.4988 mL |
| 10 mM | 0.2249 mL | 1.1247 mL | 2.2494 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。
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Quality Control & SDS
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- Purity: 98.46%
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