棉花素

生物活性靶点体外研究体内研究棉花素试剂级价格

棉花素

CAS号:489-35-0
英文名:GOSSYPETIN
中文名:棉花素
CBNumber:CB0373362
分子式:C15H10O8
分子量:318.24
MOL File:489-35-0.mol

棉花素化学性质

熔点 :302-304°C
沸点 :679.3±55.0 °C(Predicted)
密度 :1.912
储存条件 :Hygroscopic, Refrigerator, under inert atmosphere
溶解度 :DMSO (Slightly), Methanol (Slightly, Heated, Sonicated))
酸度系数(pKa) :6.47±0.40(Predicted)
形态 :Solid
颜色 :Dark Yellow
LogP :1.160 (est)

棉花素性质、用途与生产工艺

生物活性 Gossypetin 是六羟基化的类黄酮，是一种有效的 MKK3 和 MKK6 抑制剂，可强烈减弱 MKK3/6-p38 信号传导途径，具有多种药理活性，包括抗氧化，抗菌和抗癌活性。
靶点

p38 MAP kinase

体外研究

Gossypetin (20-60 μM; 48 hours; KYSE30, KYSE450 and KYSE510 cells) treatment significantly inhibits anchorage-dependent esophageal cancer cell growth in dose dependent manner. Gossypetin strongly suppresses anchorage-independent cell growth in esophageal cancer cells.
Gossypetin (60 μM; 3 hours; KYSE30 and KYSE410 cells) treatment strongly inhibits p38 activity in a dose-dependent manner and confirms that Gossypetin directly suppresses MKK3 or MKK6 activity.
Gossypetin (20-40 μM; 48 hours; KYSE450 and KYSE510 cells) treatment reduces S phase and induces G2 phase cell cycle arrest in a dose-dependent manner.
Gossypetin (20-40 μM; 72 hours; esophageal cancer cells) treatment induces intrinsic apoptosis of esophageal cancer cells.

Cell Proliferation Assay

Cell Line:	KYSE30, KYSE450 and KYSE510 cells
Concentration:	20 μM, 40 μM, 60 μM
Incubation Time:	48 hours
Result:	Anchorage-dependent esophageal cancer cell growth was significantly inhibited.

Western Blot Analysis

Cell Line:	KYSE30 and KYSE410 ccells
Concentration:	60 μM
Incubation Time:	3 hours
Result:	p38 activity was strongly inhibited in a dose-dependent manner.

Cell Cycle Analysis

Cell Line:	KYSE450 and KYSE510 cells
Concentration:	20 μM, 40 μM
Incubation Time:	48 hours
Result:	Reduced S phase and induces G2 phase cell cycle arrest in a dose-dependent manner.

Apoptosis Analysis

Cell Line:	Esophageal cancer cells
Concentration:	20 μM, 40 μM
Incubation Time:	72 hours
Result:	Induced apoptosis of esophageal cancer cells.

体内研究

Gossypetin (100 mg/kg; oral administration; 5 times per week; for 21 days; severe combined immunodeficiency (SCID) female mice) treatment significantly decreases the volume of esophageal tumor growth and without significant loss of body weight. The expression of Ki67 is significantly decreased by Gossypetin. There are no obvious morphological differences between tissues from treated or untreated mic. The phosphorylation of p38, the direct downstream protein of MKK3/6 strongly inhibited in the Gossypetin-treated group.

Animal Model:	Severe combined immunodeficiency (SCID) female mice (6-9 weeks old) injection with esophageal cancer tissue
Dosage:	100 mg/kg
Administration:	Oral administration; 5 times per week; for 21 days
Result:	Suppressed patient-derived esophageal xenograft tumor growth in an in vivo mouse model.