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。
| 生物活性 | Gossypetin is a hexahydroxylated flavonoid and is a potentmitogen-activated protein kinasekinase (MKK)3andMKK6inhibitor with strongly attenuates theMKK3/6-p38signaling pathway, has various pharmacological activities, including antioxidant, antibacterial and anticancer activities[1]. |
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体外研究
(In Vitro) | 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[1].
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[1].
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[1].
Gossypetin (20-40 μM; 72 hours; esophageal cancer cells) treatment induces intrinsic apoptosis of esophageal cancer cells[1].
Cell Proliferation Assay[1] | 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[1] | 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[1] | 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[1] | Cell Line: | Esophageal cancer cells | | Concentration: | 20 μM, 40 μM | | Incubation Time: | 72 hours | | Result: | Induced apoptosis of esophageal cancer cells. |
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体内研究
(In Vivo) | 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[1].
| Animal Model: | Severe combined immunodeficiency (SCID) female mice (6-9 weeks old) injection with esophageal cancer tissue[1] | | 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. |
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| 来源 | - Plants
- Crassulaceae
- Rhodiola roseaLinn.
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| 运输条件 | Room temperature in continental US; may vary elsewhere. |
| 储存方式 | | Powder | -20°C | 3 years | | 4°C | 2 years | | In solvent | -80°C | 6 months | | -20°C | 1 month |
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