紫铆因
| 中文名称 | 紫铆因 |
|---|---|
| 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;标准品-对照品;Aromatics;Inhibitors;Intermediates & Fine Chemicals;Pharmaceuticals;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 |
|---|---|
| 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 |
| InChI | 1S/C15H12O5/c16-10-3-4-11(14(19)8-10)12(17)5-1-9-2-6-13(18)15(20)7-9/h1-8,16,18-20H/b5-1+ |
| InChIKey | AYMYWHCQALZEGT-ORCRQEGFSA-N |
| 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 |
|---|---|
| WGK Germany | 3 |
| 海关编码 | 29145090 |
| 存储类别 | 11 - 可燃固体 |
| 提供商 | 语言 |
|---|---|
|
英文
|