Butein 是一种 cAMP 特异性的PDE抑制剂，对PDE4的IC50为 10.4 μM。Butein 是蛋白酪氨酸激酶抑制剂，对EGFR和p60c-src的IC50分别为 16 和 65 μM。Butein 通过 AKT 和 ERK/p38 MAPK 通路，靶向 FoxO3a 使 HeLa 细胞对 Cisplatin 敏感。Butein 还是一种SIRT1激活剂 (STAC)。
| 生物活性 | Butein is a cAMP-specificPDEinhibitor with anIC50of 10.4 μM forPDE4[1]. Butein is a specific protein tyrosine kinase inhibitor withIC50s of 16 and 65 μM forEGFRandp60c-srcin HepG2 cells[2]. Butein sensitizes HeLa cells to Cisplatin throughAKTand ERK/p38 MAPK pathways by targeting FoxO3a[3]. Butein is aSIRT1activator (STAC). |
| IC50& Target[1] | EGFR 16 μM (IC50, in HepG2 cells) | PDE4 10.4 μM (IC50) |
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体外研究
(In Vitro) | Butein potently inhibits cAMP-specific phosphodiesterase (type IV) activity with an IC50of 10.4±0.4 μM. In contrast, phosphodiesterase I, III and V activities were inhibited by Butein above 100 μM[1].
Butein, a plant polyphenol, is a specific protein tyrosine kinase inhibitor. Butein inhibits not only the EGF-stimulated auto-phosphotyrosine level of EGFR in HepG2 cells but also tyrosine-specific protein kinase activities of EGFR (IC50=16 μM) and p60c-src(IC50=65 μM) in vitro[2].
Butein (10, 20, and 40 μM; 24, 48, and 72 hours) inhibits cell growth in a dose- and time-dependent manner[3].
Butein exhibits anticancer activity through the inhibition of the activation of PKB/AKT and MAPK pathways, which are two pathways known to be involved in resistance to cisplatin. Butein (20 μM) decreases phosphorylation of AKT, ERK and p38 following 24 h of co-treatment with Cisplatin (20 μM)[3].
Cell Viability Assay[3] | Cell Line: | HeLa cells | | Concentration: | 10, 20, and 40 μM | | Incubation Time: | 24, 48, and 72 hours | | Result: | Inhibited cell growth in a dose- and time-dependent manner. |
Western Blot Analysis[3] | Cell Line: | HeLa cells | | Concentration: | 20 μM | | Incubation Time: | 24 hours | | Result: | Decreased phosphorylation of AKT, ERK and p38 co-treatment with Cisplatin (20 μM). |
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体内研究
(In Vivo) | Butein (2 mg/kg every 2 days) in combination with Cisplatin (2 mg/kg every 2 days) for 3 weeks suppresses tumor growth in vivo[3].
| Animal Model: | Nude mice (12 female 6- or 7-week old) with subcutaneous tumor xenografts[3] | | Dosage: | 2 mg/kg | | Administration: | Intraperitoneally; every 2 days; for 3 weeks | | Result: | Enhanced the antitumor effects of Cisplatin in vivo. |
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| 运输条件 | Room temperature in continental US; may vary elsewhere. |
| 储存方式 | | Powder | -20°C | 3 years | | 4°C | 2 years | | In solvent | -80°C | 6 months | | -20°C | 1 month |
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| 溶解性数据 | In Vitro: DMSO : 50 mg/mL(183.65 mM;Need ultrasonic) 配制储备液 | 1 mM | 3.6731 mL | 18.3655 mL | 36.7309 mL | | 5 mM | 0.7346 mL | 3.6731 mL | 7.3462 mL | | 10 mM | 0.3673 mL | 1.8365 mL | 3.6731 mL |
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储备液的保存方式和期限：-80℃, 6 months; -20℃, 1 month。-80℃ 储存时，请在 6 个月内使用，-20℃ 储存时，请在 1 个月内使用。 In Vivo: 请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照In Vitro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，建议您现用现配，当天使用；
以下溶剂前显示的百
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此方案可获得 ≥ 2.5 mg/mL (9.18 mM，饱和度未知) 的澄清溶液。 以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。 2. 请依序添加每种溶剂： 10% DMSO 40%PEG300 5%Tween-80 45% saline Solubility: 1.67 mg/mL (6.13 mM); Suspended solution; Need ultrasonic
此方案可获得 1.67 mg/mL (6.13 mM) 的均匀悬浊液，悬浊液可用于口服和腹腔注射。 以 1 mL 工作液为例，取 100 μL 16.7 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。 *以上所有助溶剂都可在本网站选购。
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