生物活性

• 靶点	PI3Kγ Kd:0.17μM

• 描述PI3Kγ signalling through Akt and mTor inhibits NFκB activation while stimulating C/EBPβ (CCAAT/enhancer binding protein) activation, thereby inducing a transcriptional program that promotes immune suppression during inflammation and tumour growth. Myricetin has a K_d of 0.17 μM for PI3Kγ. As one of the major flavonols in red wine, myricetin is also a novel inhibitor of MEK1 (mitogen-activated protein kinase) activity and transformation of JB6 P+ mouse epidermal cells. Myricetin (10 mM) inhibited 12-O-tetradecanoylphorbol-13-acetate (TPA) or epidermal growth factor (EGF)-induced cell transformation by 76 or 72%, respectively. It strongly inhibited MEK1 kinase activity and suppressed TPA- or EGF-induced phosphorylation of extracellular signal-regulated kinase (ERK) or p90 ribosomal S6 kinase, downstream targets of MEK. Moreover, myricetin inhibited H-Ras-induced cell transformation. Myricetin inhibits viability of SKOV3 ovarian cancer cells in a dose-dependent manner. It induces DNA DSBs and ER stress, which leads to apoptosis in SKOV3 cells. Exposure to 150 μM myricetin causes 14%, 26%, 5% and 49% inhibition of rabbit platelet aggregation, induced by ADP, arachidonic acid, collagen and PAF (platelet-activating factor), respectively.

• 动物研究
  剂量	Rat: 5 mg/kg, 10 mg/kg[3] (i.p.); 0.05 mg/kg - 5 mg/kg[4] (i.v.) Mice: 10 mg/kg - 100 mg/kg[5] (p.o.)
  给药途径	i.p., i.v., p.o.