Fisetin 是有效的Sirtuin活化化合物(STAC),可以调节Sirtuin。Fisetin 抑制 p90RSK/YB-1 信号通道并且在A375黑素瘤细胞中下调药物抗性相关的 P-糖蛋白。
Fisetin (Fustel) is a potent sirtuin activating compound (STAC) and an agent that modulates sirtuins. Plasmon Surface Resonance studies showed that fisetin binds to YB-1 with an affinity of approximately 35 µM, with both slow association and dissociation. Fisetin also inhibited EGF induced YB-1 phosphorylation and markers of EMT both in vitro and in vivo.
动物 A (mg/kg) = 动物 B (mg/kg)×动物 B的Km系数/动物 A的Km系数 | |
例如,已知某工具药用于小鼠的剂量为88 mg/kg , 则用于大鼠的剂量换算方法:将88 mg/kg 乘以小鼠的Km系数(3),再除以大鼠的Km系数(6),得到该药物用于大鼠的等效剂量44 mg/kg。
[1] Haddad et al (2010) Antiproliferative mechanisms of the flavonoids 2,2'-dihydroxychalcone and fisetin in human prostate cancer cells. Nutr.Cancer 62 668.
[2] Lee et al (2005) Mechanisms for the inhibition of DNA methyltransferases by tea catechins and bioflavonoids. Mol.Pharmacol. 68 1018.
[3] Adhami et al (2012) Dietary flavonoid fisetin: a novel dual inhibitor of PI3K/Akt and mTOR for prostate cancer management. Biochem.Pharmacol. 84 1277.
[4] Maher et al (2011) ERK activation by the polyphenols fisetin and resveratrol provides neuroprotection in multiple models of Huntington's disease. Hum.Mol.Genet. 20 261.
分子式 C15H10O6 |
分子量 286.24 |
CAS号 528-48-3 |
储存方式 ﹣20 ℃冷藏长期储存。冰袋运输 |
溶剂(常温) |
DMSO 57 mg/mL |
Water <1 mg/mL |
Ethanol 3 mg/mL |
体内溶解度
NCT Number | Conditions | Interventions | Sponsor/Collaborators | Phases | Start Date | Last Updated |
NCT02741804 | Mild Cognitive Impairment | Dietary Supplement: BBH-1001 Brain Health Supplement|Other: Lifestyle Intervention|Dietary Supplement: Brain Health Placebo | Cedars-Sinai Medical Center | 2016-05-01 | 2016-06-23 | |
NCT02909686 | Gulf War Illness | Dietary Supplement: Boswellia Serrata|Dietary Supplement: Curcumin|Dietary Supplement: Epimedium|Dietary Supplement: Fisetin|Dietary Supplement: Luteolin|Dietary Supplement: Nettle|Dietary Supplement: Pycnogenol|Dietary Supplement: Reishi Mushroom|Dietary Supplement: Resveratrol|Dietary Supplement: Placebo | University of Alabama at Birmingham|Congressionally Directed Medical Research Programs | Phase 2 | 2016-07-01 | 2016-09-16 |
注:以上所有数据均来自公开文献,并不保证对所有实验均有效,数据仅供参考。
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