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Bufalin/蟾毒灵 {[allProObj[0].p_purity_real_show]}

货号:A206803 同义名: NSC 89595; BF

Bufalin是一种 Na⁺/K⁺-ATPase 抑制剂,Kd 值为 42.5 nM,具有显著的抗肿瘤和抗炎活性。

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Bufalin/蟾毒灵 化学结构 CAS号:465-21-4
Bufalin/蟾毒灵 化学结构
CAS号:465-21-4
Bufalin/蟾毒灵 3D分子结构
CAS号:465-21-4
Bufalin/蟾毒灵 化学结构 CAS号:465-21-4
Bufalin/蟾毒灵 3D分子结构 CAS号:465-21-4
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Bufalin/蟾毒灵 纯度/质量文件 产品仅供科研

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Bufalin/蟾毒灵 生物活性

描述 Bufalin is an active component isolated from Chan Su, acts as a potent Na+/K+-ATPase inhibitor, binds to the subunit α1, α2 and α3, with Kd of 42.5, 45 and 40 nM, respectively[3]. Bufalin caused significant cytotoxicity in NCI-H460 cells at a concentration as low as 1 μM. DNA condensation was observed in bufalin-treated cells in a dose-dependent manner. Bufalin injected intraperitoneally in a dose-dependent manner reduced tumor size in BALB/C nu/nu mice implanted with NCI-H460 cells. Bufalin injection did not produce significant drug-related toxicity in experimental animals except at a high dose (0.4 mg/kg)[4]. Bufalin-induced disruption of the SRC-1 (steroid receptor coactivator) isoform/ERβ (estrogen receptor) axis might induce apoptosis, pyroptosis and ERS (endoplasmic reticulum-stress) signaling in endometriotic lesions, causing the suppression of endometriosis[5]. Bufalin inhibits cell proliferation and migration of HCC (hepatocellular carcinoma) cells via APOBEC3F induced intestinal immune network for IgA production signaling pathway[6].

Bufalin/蟾毒灵 细胞实验

Cell Line
Concentration Treated Time Description References
SK-N-BE(2) 90 nM 72 hours Inhibits cell proliferation and migration Int J Mol Med. 2020 Dec;46(6):2137-2149.
SH-SY5Y 30 nM 72 hours Inhibits cell proliferation and migration Int J Mol Med. 2020 Dec;46(6):2137-2149.
Vero cells 0.0625 µM, 0.125 µM, 0.25 µM, 0.5 µM, 1 µM 24 hours To evaluate the inhibitory effect of Bufalin on HSV-1 replication, results showed Bufalin significantly inhibited HSV-1 replication. Int J Mol Sci. 2023 Sep 23;24(19):14479.
PK-15 cells 0.015 µM, 0.03 µM, 0.06 µM, 0.12 µM 24 hours To evaluate the inhibitory effect of Bufalin on PRV replication, results showed Bufalin significantly inhibited PRV replication. Int J Mol Sci. 2023 Sep 23;24(19):14479.
Human umbilical vein endothelial cells (HUVECs) 10 nM 24 hours To evaluate the effect of Bufalin on TME-mediated angiogenesis, results showed that Bufalin significantly inhibited HUVEC tube formation, migration, and adhesion induced by TME cells. J Transl Med. 2021 Sep 8;19(1):383.
L02 0, 20, 40, 80, 160, 320 nM 24, 48, 72 hours Bufalin had no significant inhibitory effect on normal hepatocyte L02 cells. J Transl Med. 2023 Dec 11;21(1):900.
RBE 0, 20, 40, 80, 160, 320 nM 24, 48, 72 hours Bufalin significantly inhibited the proliferation and migration of RBE cells in a dose- and time-dependent manner. J Transl Med. 2023 Dec 11;21(1):900.
QBC-939 0, 20, 40, 80, 160, 320 nM 24, 48, 72 hours Bufalin significantly inhibited the proliferation and migration of QBC-939 cells in a dose- and time-dependent manner. J Transl Med. 2023 Dec 11;21(1):900.
HCCC-9810 0, 20, 40, 80, 160, 320 nM 24, 48, 72 hours Bufalin significantly inhibited the proliferation and migration of HCCC-9810 cells in a dose- and time-dependent manner. J Transl Med. 2023 Dec 11;21(1):900.
U266R 24 nM 48 hours Bufalin alone increased p-AKT levels in U266R cells, and combination with MK2206 enhanced apoptosis induction. Cell Death Dis. 2017 May 11;8(5):e2776.
H929R 24 nM 48 hours Bufalin alone increased p-AKT levels in H929R and U266R cells, and combination with MK2206 enhanced apoptosis induction. Cell Death Dis. 2017 May 11;8(5):e2776.
U266 12 nM 48 hours Bufalin alone moderately induced apoptosis in U266 cells, accompanied by increased p-AKT levels. Cell Death Dis. 2017 May 11;8(5):e2776.
NCI-H929 12 nM 48 hours Bufalin alone moderately induced apoptosis in H929 and U266 cells, accompanied by increased p-AKT levels. Cell Death Dis. 2017 May 11;8(5):e2776.
HepG2 cells 5, 10, 20 or 50 nM 48 hours To evaluate the effects of Bufalin on proliferation and apoptosis of HepG2 cells. Bufalin at higher concentrations could inhibit proliferation and induce apoptosis of HepG2 cells. Oncoimmunology. 2018 Feb 8;7(5):e1426434.
MHCC97 H cells 5, 10, 20 or 50 nM 48 hours To evaluate the effects of Bufalin on proliferation and apoptosis of HCC cells. Bufalin (higher than 10 nM) could inhibit cell proliferation and induce apoptosis of HCC cells. Oncoimmunology. 2018 Feb 8;7(5):e1426434.
CEF cells 0.0625 µM, 0.125 µM, 0.25 µM, 0.5 µM, 1 µM 48 hours To evaluate the inhibitory effect of Bufalin on MDV replication, results showed Bufalin significantly inhibited MDV replication. Int J Mol Sci. 2023 Sep 23;24(19):14479.
Recombinant human CYP3A4 0, 0.1, 0.5, 1, 2.5, 5, 7.5, 10, 15, 20, 30 µM 5 minutes To determine the inhibitory effect of Bufalin on CYP3A4 activity, the IC50 value was 14.52 μmol/L. Acta Pharmacol Sin. 2009 May;30(5):646-52.

Bufalin/蟾毒灵 动物实验

Species
Animal Model
Administration Dosage Frequency Description References
BALB/c mice PRV infection model Intraperitoneal injection 0.5 mg/kg Every 36 hours until all mice in the PRV-infected group had died To evaluate the therapeutic effect of Bufalin on PRV infection, results showed Bufalin significantly decreased the viral load in multiple tissues and increased the survival rate of mice. Int J Mol Sci. 2023 Sep 23;24(19):14479.
Balb/c nu/nu mice HCC xenograft model Intraperitoneal injection 0.5, 1 or 2 mg/kg Once a week (poly (I:C)) or five days a week (bufalin) for six weeks To evaluate the effects of Bufalin on lung metastasis in HCC xenograft model. Bufalin (0.5 mg/kg) could inhibit poly (I:C)-enhanced lung metastasis of HCC cells. Oncoimmunology. 2018 Feb 8;7(5):e1426434.
BALB/c nu/nu mice MOPC315 xenograft model Intraperitoneal injection 1 mg/kg Once daily for 10 days Combination treatment significantly inhibited MM tumor growth without significant side effects. Cell Death Dis. 2017 May 11;8(5):e2776.
BALB/c nude mice ICC xenograft model Intraperitoneal injection 1 mg/kg Every two days for 2-3 weeks Bufalin significantly inhibited CAMKK2 overexpression-induced ICC tumor growth. J Transl Med. 2023 Dec 11;21(1):900.
BALB/c mice Subcutaneous xenograft tumor model and liver metastasis model Intraperitoneal injection 1 mg/kg Once every other day for 21 days (flank) or 14 days (spleen) To evaluate the antiangiogenic activity of Bufalin in vivo, results showed that Bufalin significantly inhibited tumor growth and liver metastasis, reducing the number of tumor blood vessels and STAT3 phosphorylation in vascular endothelial cells. J Transl Med. 2021 Sep 8;19(1):383.
SCID/NOD mice MM xenograft model Intraperitoneal injection 1 mg/kg Twice weekly AHSA1 overexpression promotes MM cell growth and BTZ resistance J Exp Clin Cancer Res. 2022 Jan 6;41(1):11
Wistar rats Healthy male Wistar rats Oral (ig) and intravenous (iv) injection 10 mg/kg Single dose To evaluate the effect of Bufalin on CYP3A4 activity, results showed that Bufalin significantly increased AUC0–t and t1/2, and decreased CL and the formation of 1-hydroxy-midazolam. Acta Pharmacol Sin. 2009 May;30(5):646-52.
C57BL/6 mice Orthotopic HCC model Intraperitoneal injection 10 μg/kg Every other day for 3 weeks To investigate the inhibitory effect of bufalin on HCC in immunocompetent mice, results showed that bufalin promoted macrophage polarization toward M1 phenotype, activated antitumor T cell immune response, and thereby suppressed HCC growth. J Immunother Cancer. 2022 May;10(5):e004297
BALB/c nude mice 4T1 breast cancer model Intravenous injection 2 mg/kg Every 2 days for 3 weeks Evaluate the in vivo antitumor efficacy of FA-MOF/Buf NPs, showing significant tumor growth inhibition and reduced side effects. Front Pharmacol. 2022 Jan 18;12:747992
Nude mice Subcutaneous xenograft model Intraperitoneal injection 5 mg/kg Three times per week for 4 weeks Inhibits tumor growth Int J Mol Med. 2020 Dec;46(6):2137-2149.

Bufalin/蟾毒灵 参考文献

[1]Jiang L, Zhao MN, et al. Bufalin induces cell cycle arrest and apoptosis in gallbladder carcinoma cells. Tumour Biol. 2014 Nov;35(11):10931-41.

[2]Wu SH, Wu TY, et al. Bufalin induces cell death in human lung cancer cells through disruption of DNA damage response pathways. Am J Chin Med. 2014;42(3):729-42.

[3]Katz A, Lifshitz Y, Bab-Dinitz E, et al. Selectivity of digitalis glycosides for isoforms of human Na,K-ATPase. J Biol Chem. 2010;285(25):19582-19592

[4]Wu SH, Bau DT, Hsiao YT, et al. Bufalin induces apoptosis in vitro and has Antitumor activity against human lung cancer xenografts in vivo. Environ Toxicol. 2017;32(4):1305-1317

[5]Cho YJ, Lee JE, Park MJ, O'Malley BW, Han SJ. Bufalin suppresses endometriosis progression by inducing pyroptosis and apoptosis. J Endocrinol.2018;237(3):255-269

[6]Yang Z, Tao Y, Xu X, Cai F, Yu Y, Ma L. Bufalin inhibits cell proliferation and migration of hepatocellular carcinoma cells via APOBEC3F induced intestinal immune network for IgA production signaling pathway. Biochem Biophys Res Commun.2018;503(3):2124-2131

Bufalin/蟾毒灵 实验方案

计算器
存储液制备 1mg 5mg 10mg

1 mM

5 mM

10 mM

2.59mL

0.52mL

0.26mL

12.94mL

2.59mL

1.29mL

25.87mL

5.17mL

2.59mL

Bufalin/蟾毒灵 技术信息

CAS号465-21-4
分子式C24H34O4
分子量 386.52
SMILES Code O=C(C=C1)OC=C1[C@H]2CC[C@]3(O)[C@]4([H])CC[C@]5([H])C[C@@H](O)CC[C@]5(C)[C@@]4([H])CC[C@@]32C
MDL No. MFCD00056525
别名 NSC 89595; BF
运输蓝冰
存储条件

In solvent -20°C: 3-6个月 -80°C: 12个月

Pure form Inert atmosphere, 2-8°C

溶解方案

DMSO: 105 mg/mL(271.65 mM),配合低频超声助溶,注意:DMSO长时间开封后,会吸水并导致溶解能力下降,请避免使用长期开封的DMSO

请根据您的动物给药指南选择适当的溶解方案。
以下溶解方案都请先按照体外实验的方式配制澄清的储备液,再依次添加助溶剂:
——为保证实验结果的可靠性,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议现用现配,当天使用; 以下溶剂前显示的百分比是指该溶剂在终溶液中的体积占比;如在配制过程中出现沉淀、析出现象,可以通过加热和/或超声的方式助溶
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