紫铆因

生物活性靶点体外研究体内研究紫铆因试剂级价格

紫铆因

CAS号:487-52-5
英文名:BUTEIN
中文名:紫铆因
CBNumber:CB8136455
分子式:C15H12O5
分子量:272.25
MOL File:487-52-5.mol

紫铆因化学性质

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 :DMSO: >50 mg/mL
形态 :solid
酸度系数(pKa) :7.44±0.35(Predicted)
颜色 :yellow
LogP :2.405 (est)
CAS 数据库 :487-52-5(CAS DataBase Reference)

安全信息

安全说明 :22-24/25
WGK Germany :3
海关编码 :29145090

紫铆因性质、用途与生产工艺

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 )

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).

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.

用途
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