紫铆因
中文名称 | 紫铆因 |
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中文同义词 | 紫铆因;紫铆查尔酮;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;2-[2-(2-氨基苯基)乙烯基]-5-甲基喹啉-8-醇;2-[(E)-2-(2-氨基苯基)乙烯基]-5-甲基-8-羟基喹啉;2-[(E)-2-(2-氨基苯基)乙烯基]-5-甲基-喹啉-8-醇;2-[(E)-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 | 小分子抑制剂,天然产物;合成;植物提取物;标准品;对照品;细胞生物学试剂;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 |
结构式 |
紫铆因 性质
熔点 | 216°C |
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沸点 | 560.9±50.0 °C(Predicted) |
密度 | 1.483±0.06 g/cm3(Predicted) |
储存条件 | 2-8°C |
溶解度 | 二甲基亚砜:>50 mg/mL |
形态 | 固体 |
酸度系数(pKa) | 7.44±0.35(Predicted) |
颜色 | 粘黄色 |
LogP | 2.405 (est) |
CAS 数据库 | 487-52-5(CAS DataBase Reference) |
EGFR 16 μM (IC 50 , in HepG2 cells) |
PDE4 10.4 μM (IC 50 ) |
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). |
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. |
Butrin, isobutrin, and butein from medicinal plant Butea monosperma selectively inhibit nuclear factor-κB in activated human mast cells: suppression of tumor necrosis factor-α, interleukin (IL)-6, and IL-8. Anti-inflammatory agent
安全信息
安全说明 | 22-24/25 |
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WGK Germany | 3 |
海关编码 | 29145090 |
提供商 | 语言 |
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英文
|