GLPBio

Bufotalin

Catalog No.: GC33134Purity:98.46%Synonyms: NSC 89596
COASDSData Sheet
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.

Bufotalin
Cas No.: 471-95-4
10mM (in 1mL DMSO)In Stock
$91.00
1
5mgIn Stock
$82.00
1
10mgIn Stock
$138.00
1
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Description

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.

Protocol

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:
[1]. 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.
[2]. Yin JZ, Li ZQ, Zhang XD, et al. Bufotalin attenuates pulmonary fibrosis via inhibiting Akt/GSK-3?/?-catenin signaling pathway. European Journal of Pharmacology. 2024 Feb 5; 964: 176293.

Product Documents

Purity:98.46%Appearance:A solid
COASDSData Sheet

Chemical Properties

CAS No.
471-95-4
Synonyms
NSC 89596
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
Molecular Formula
C26H36O6
Molecular Weight
444.56
Solubility
DMSO : ≥ 4.6 mg/mL (10.35 mM)
Storage
Store at -20°C,protect from light
General tips
Select a suitable solvent according to the product solubility data. Once prepared, aliquot the stock solution to avoid repeated freeze-thaw cycles.
Use stock solutions within 6 months when stored at -80°C or within 1 month when stored at -20°C.
To improve solubility, warm the tube to 37°C and sonicate it for an appropriate period.
Shipping Condition
Evaluation samples are shipped with blue ice. Other available sizes are shipped at room temperature or with blue ice upon request.

CalculatorsMolarity / Dilution / Molecular Weight / Unit Conversion / In Vivo Formulation / Solubility

g/mol

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