紫铆因
中文名称:
紫铆因
中文同义词:
紫铆因;紫铆查尔酮;紫铆花素;紫铆因标准品;蛋白质酪氨酸激酶抑制剂(BUTEIN);紫铆查耳酮;2-[2-(2-氨基苯基)乙烯基]-5-甲基-8-羟基喹啉;2-[2-(2-氨基苯基)乙烯基]-5-甲基-喹啉-8-醇
英文名称:
BUTEIN
英文同义词:
(E)-1-(2,4-Dihydroxyphenyl)-3-(3,4-dihydroxyphenyl)-2-propen-1-one 2,3,4,4-Tetrahydroxychalcone;BUTEIN(P);2-Propen-1-one, 1-(2,4-dihydroxyphenyl)-3-(3,4-dihydroxyphenyl)-, (2E)-;Butein 2,3,4,4-Tetrahydroxychalcone;2-[(E)-2-(2-aminophenyl)ethenyl]-5-methyl-quinolin-8-ol;2-[(E)-2-(2-aminophenyl)ethenyl]-5-methylquinolin-8-ol;2-[(E)-2-(2-aminophenyl)vinyl]-5-methyl-8-quinolinol;2-[(E)-2-(2-aminophenyl)vinyl]-5-methyl-quinolin-8-ol
CAS号:
487-52-5
分子式:
C15H12O5
分子量:
272.25
EINECS号:
207-659-5
相关类别:
对照品;细胞生物学试剂;小分子抑制剂，天然产物;合成;植物提取物;标准品;Aromatics;Inhibitors;Intermediates Fine Chemicals;Pharmaceuticals;标准品-对照品;新品;标准品 -对照药材;查尔酮;标准品，对照品
Mol文件:
487-52-5.mol
熔点
216°C
沸点
560.9±50.0 °C(Predicted)
密度
1.483±0.06 g/cm3(Predicted)
储存条件
-20°C
溶解度
DMSO: >50 mg/mL
酸度系数(pKa)
7.44±0.35(Predicted)
形态
solid
颜色
yellow
CAS 数据库
487-52-5(CAS DataBase Reference)
生物活性
Butein，可从 Dalbergia odorifera T. Chen 分离，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)。
靶点
EGFR
16 μM (IC 50 , in HepG2 cells)
PDE4
10.4 μM (IC 50 )
EGFR
16 μM (IC 50 , in HepG2 cells)
PDE4
10.4 μM (IC 50 )
体外研究
Butein potently inhibits cAMP-specific phosphodiesterase (type IV) activity with an IC 50 of 10.4±0.4 μM. In contrast, phosphodiesterase I, III and V activities were inhibited by Butein above 100 μM.
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 (IC 50 =16 μM) and p60 c-src (IC 50 =65 μM) in vitro.
Butein (10, 20, and 40 μM; 24, 48, and 72 hours) inhibits cell growth in a dose- and time-dependent manner.
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).
Cell Viability Assay
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
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).
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.
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).
体内研究
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.
Animal Model: Nude mice (12 female 6- or 7-week old) with subcutaneous tumor xenografts
Dosage: 2 mg/kg
Administration: Intraperitoneally; every 2 days; for 3 weeks
Result: Enhanced the antitumor effects of Cisplatin in vivo.
Animal Model:
Nude mice (12 female 6- or 7-week old) with subcutaneous tumor xenografts
Dosage:
2 mg/kg
Administration:
Intraperitoneally; every 2 days; for 3 weeks
Result:
Enhanced the antitumor effects of Cisplatin in vivo.
用途
Butrin, isobutrin, and butein from medicinal plant Butea monosperma selectively inhibit nuclear factor-魏B in activated human mast cells: suppression of tumor necrosis factor-α, interleukin (IL)-6, and IL-8. Anti-inflammatory agent
安全说明
22-24/25
WGK Germany
3
海关编码
29145090
