Bufalin
(Synonyms: 蟾毒灵) 目录号 : GN10365
Bufalin是一种Na+/K+-ATPase抑制剂（α1：Kd = 42.5nM；α2：Kd = 45nM；α3：Kd = 40nM）。
Cas No.:465-21-4
Sample solution is provided at 25 µL, 10mM.
Bufalin is a Na+/K+-ATPase inhibitor (α1: Kd = 42.5nM; α2: Kd = 45nM; α3: Kd = 40nM) [1]. Bufalin primarily inhibits the activity of Na⁺/K⁺-ATPase on cell membranes, leading to elevated intracellular calcium concentrations [2]. Bufalin induction of apoptosis and inhibition of tumor cell proliferation can also have multiple anti-tumor mechanisms, including triggering autophagy and inhibiting tumor angiogenesis [3]. Bufalin is used to treat various tumors, including liver cancer, lung cancer, breast cancer, and leukemia [4].
In NCI-H640 cells, after treatment with Bufalin (1μM, 2μM, 4μM; 24h), the activity of cells decreased significantly [5]. In Ishikawa, SK-OV-3 and OMC-3 ovarian cancer cells, Bufalin (0.1-10ng/mL; 48h) can inhibit the proliferation of endometrial and ovarian cancer cells [6]. In human RCC ACHN cells, Bufalin (0-80nM; 12-72h) suppresses the proliferation and metastasis of renal cell carcinoma by inhibiting the PI3K/Akt/mTOR signaling pathway [7].
In carrageenan-induced paw edema rat model, after Bufalin (0.15mg/kg, 0.3mg/kg, 0.6mg/kg; ip; single injection) treatmentthe, volume of paw edema in rats was significantly reduced [8]. In HCCLM3 cell metastatic orthotopic tumor mouse model, orthotopic transplanted tumor tissues undergo necrosis and apoptosis induced by Bufalin (1mg/kg, 1.5mg/kg; ip; 30d) treatment [9].
References:
[1]. Katz A, Lifshitz Y, Bab-Dinitz E, et al. Selectivity of digitalis glycosides for isoforms of human Na, K-ATPase[J]. Journal of Biological Chemistry, 2010, 285(25): 19582-19592.
[2]. Wu S H, Bau D T, Hsiao Y T, et al. Bufalin induces apoptosis in vitro and has Antitumor activity against human lung cancer xenografts in vivo[J]. Environmental Toxicology, 2017, 32(4): 1305-1317.
[3]. Yin P H, Liu X, Qiu Y Y, et al. Anti-tumor activity and apoptosis-regulation mechanisms of bufalin in various cancers: new hope for cancer patients[J]. Asian Pacific journal of cancer prevention, 2012, 13(11): 5339-5343.
[4]. Lan Y L, Lou J C, Jiang X W, et al. A research update on the anticancer effects of bufalin and its derivatives[J]. Oncology letters, 2019, 17(4): 3635-3640.
[5]. Wu S H, Wu T Y, Hsiao Y T, et al. Bufalin induces cell death in human lung cancer cells through disruption of DNA damage response pathways[J]. The American Journal of Chinese Medicine, 2014, 42(03): 729-742.
[6]. Takai N, Ueda T, Nishida M, et al. Bufalin induces growth inhibition, cell cycle arrest and apoptosis in human endometrial and ovarian cancer cells[J]. International journal of molecular medicine, 2008, 21(5): 637-643.
[7]. Xie J, Lin W, Huang L, et al. Bufalin suppresses the proliferation and metastasis of renal cell carcinoma by inhibiting the PI3K/Akt/mTOR signaling pathway[J]. Oncology letters, 2018, 16(3): 3867-3873.
[8]. Wen L, Huang Y, Xie X, et al. Anti‐inflammatory and antinociceptive activities of bufalin in rodents[J]. Mediators of inflammation, 2014, 2014(1): 171839.
[9]. Zhang Z J, Yang Y K, Wu W Z. Bufalin attenuates the stage and metastatic potential of hepatocellular carcinoma in nude mice[J]. Journal of translational medicine, 2014, 12(1): 57.
Bufalin是一种Na+/K+-ATPase抑制剂（α1：Kd = 42.5nM；α2：Kd = 45nM；α3：Kd = 40nM） [1]。Bufalin主要抑制细胞膜上Na⁺/K⁺-ATPase的活性，导致细胞内钙离子浓度升高 [2]。Bufalin诱导细胞凋亡、抑制肿瘤细胞增殖，并可能通过多种抗肿瘤机制发挥作用，包括触发自噬和抑制肿瘤血管生成 [3]。Bufalin用于治疗多种肿瘤，包括肝癌、肺癌、乳腺癌和白血病 [4]。
在NCI-H640细胞中，用Bufalin（1μM，2μM，4μM；24h）处理后，细胞的活性显著下降 [5]。在Ishikawa、SK-OV-3和OMC-3卵巢癌细胞中，Bufalin（0.1-10ng/mL；48h）可抑制子宫内膜癌和卵巢癌细胞的增殖 [6]。在人肾细胞癌ACHN细胞中，Bufalin（0-80nM；12-72h）通过抑制PI3K/Akt/mTOR信号通路抑制肾细胞癌的增殖和转移 [7]。
在角叉菜胶诱发的大鼠足跖水肿模型中，Bufalin（0.15mg/kg，0.3mg/kg，0.6mg/kg；ip；单次注射）治疗后，大鼠足跖水肿体积显著减少 [8]。在HCCLM3细胞转移性原位肿瘤小鼠模型中，Bufalin（1mg/kg，1.5mg/kg；ip；30d）治疗引起原位移植肿瘤组织坏死、凋亡 [9]。
| Cell experiment [1]: | |
Cell lines | NCI-H640 cells |
Preparation Method | Approximately 2 × 105 cells/well of NCI-H640 cells in 12-well plates were incubated with Bufalin at final concentrations of 0 (vehicle, 0.5% DMSO), 1, 2 and 4μM for 24 hours. Cells from each treatment were stained with PI (5 g/ml) and analyzed by flow cytometry and cell viability was calculated. |
Reaction Conditions | 1μM, 2μM, 4μM; 24h |
Applications | After treatment with Bufalin, the activity of cells decreased significantly. |
| Animal experiment [2]: | |
Animal models | Carrageenan-induced paw edema rat model |
Preparation Method | The anti-inflammatory effect was based on the inhibition of carrageenan-induced hind paw edema. Bufalin (0.15, 0.3, and 0.6mg/kg, i.p.), indomethacin (10mg/kg, i.p.), and vehicle were administered intraperitoneally 30min prior to carrageenan injection. Each rat received a subplantar injection of carrageenan (0.1mL, 1% w/v in saline) in the right hind paw. A plethysmometer measured the volume of paw edema before and at various times (1, 2, 4, and 6h) after the carrageenan injection. The paw swelling ratio was calculated as a percentage increase from the paw volume measured prior to carrageenan injection. Rat paws were collected after the final assessment. Each hind paw was cut at the level of the calcaneus bone and used for Western blot analysis. |
Dosage form | 0.15mg/kg, 0.3mg/kg, 0.6mg/kg; ip; single injection |
Applications | After Bufalin treatment, the volume of paw edema in rats was significantly reduced. |
References: | |
| Cas No. | 465-21-4 | SDF | |
| 别名 | 蟾毒灵 | ||
| 化学名 | 5-[(3S,5R,8R,9S,10S,13R,14S,17R)-3,14-dihydroxy-10,13-dimethyl-1,2,3,4,5,6,7,8,9,11,12,15,16,17-tetradecahydrocyclopenta[a]phenanthren-17-yl]pyran-2-one | ||
| Canonical SMILES | CC12CCC(CC1CCC3C2CCC4(C3(CCC4C5=COC(=O)C=C5)O)C)O | ||
| 分子式 | C24H34O4 | 分子量 | 386.52 |
| 溶解度 | ≥ 38.7mg/mL in DMSO | 储存条件 | Store at -20°C |
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| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 2.5872 mL | 12.9359 mL | 25.8719 mL |
| 5 mM | 0.5174 mL | 2.5872 mL | 5.1744 mL |
| 10 mM | 0.2587 mL | 1.2936 mL | 2.5872 mL |
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动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
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| % DMSO % % Tween 80 % saline | ||||||||||
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计算结果:
工作液浓度： mg/ml；
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2.
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