棉花素 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（轻微）、甲醇（轻微、加热、超声处理）） |
| 酸度系数(pKa) | 6.47±0.40(Predicted) |
| 形态 | 固体 |
| 颜色 | 深黄色 |
| LogP | 1.160 (est) |
棉花素 用途与合成方法
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p38 MAP kinase
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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. |
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. |
