Bufotalin (Synonyms: NSC 89596) |
Catalog No.GC33134
One-Click Copy Product Info
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Bufotalin is a natural cardiotonic steroid derived from toad secretions.
Products are for research use only. Not for human use. We do not sell to patients.
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.
| 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 | |
| Synonyms | NSC 89596 | ||
| 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 | ||
| Formula | C26H36O6 | M.Wt | 444.56 |
| Solubility | DMSO : ≥ 4.6 mg/mL (10.35 mM) | Storage | Store at -20°C,protect from light |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
|
1 mg | 5 mg | 10 mg |
| 1 mM | 2.2494 mL | 11.2471 mL | 22.4942 mL |
| 5 mM | 449.9 μL | 2.2494 mL | 4.4988 mL |
| 10 mM | 224.9 μL | 1.1247 mL | 2.2494 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
g
μL
Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)
Calculation results:
Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )
Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL saline, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
- View current batch:
- Purity: 98.46% Appearance: A solid
- COA (Certificate of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 26 reference(s) in Google Scholar.)