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编 号:F367457
分子式:C21H20O10
分子量:432.38
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1mg
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5mg
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10mg
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生物活性:
Afzelin (Kaempferol-3-O-rhamnoside)It is a flavonol glycoside that has anti-inflammatory, anti-oxidative stress response, anti-apoptotic, and anti-cardiac cytotoxic effects. AfzelinIt can reduce mitochondrial damage, enhance mitochondrial biosynthesis, and reduce mitochondria-related proteins. Parkinand PTENinduced putative kinase 1 (putative kinase 1)s level. AfzelinCan be improved D-galactosamine(GalN)/LPSSurvival rate of mice treated with doxorubicin prophylaxis (HY-15142A)Induced cardiotoxicity and scopolamine (HY-N0296)-induced neurological injury. AfzelinAlso inhibits asthma and allergies caused by ovalbumin.

体内研究:
Afzelin (5, 10 mg/kg/day; 口服; 共 20 天) 可以浓度依赖的方式减轻 DOX 毒性导致的心脏损伤。其通过上调 p-AMP 激活蛋白激酶 α (AMPKα) 和 Sirtuin1 (SIRT1) 水平而发挥心脏保护作用。Afzelin (0.1-10 mg/kg/day; 口服; 共 5 天) 可下调哮喘小鼠模型中的 GATA 结合蛋白 3 转录因子 (GATA3) 来减轻哮喘表型。Afzelin 抑制 GATA3 而减少 Th2 细胞因子,GATA3 是 Th2 细胞因子分化和产生的主要调节因子。Afzelin(100 ng/μL; 脑室注射; 每周 3 次, 共 1 个月)可改善服用东莨菪碱 (HY-N0296) 的小鼠的突触可塑性和认知/记忆行为。Animal Model:C57BL/6 Mouse
Dosage: 5 mg/kg/day, 10 mg/kg/day
Administration:Oral gavage for 20 days, while C57BL/6 mouse were treated with 4 mg/kg/d (ip, injected at day 1, 7, 14) DXO for 3 doses.
Result:Attenuated DOX-induced cardiac damage and reduced serum levels of alanine aminotransferase and pro-inflammatory cytokines.Also upregulated the expression of p-AMP-activated protein kinase α (AMPKα) and Sirtuin1 (SIRT1).
Animal Model:Asthma murine model sensitized by ovalbumin (OVA)
Dosage:0.1, 1 and 10 mg/kg
Administration:PO; once daily from day 19 to day 23
Result:Suppressed eosinophil infiltration, allergic airway inflammation, airway hyperresponsiveness, OVA-specific IgE and Th2 cytokine secretion.
Animal Model:Scopolamine induced mouse model
Dosage:100 ng/μL
Administration:ICV, administered into the third ventricle of the hypothalamus; 3 time per week for 1 month
Result:Resulted the restoration of the cholinergic systems and molecular signal transduction via CREB-BDNF pathways.Led to improved neurocognitive and neuroprotective effects on synaptic plasticity and behaviors partly through the increase in CREB-BDNF signaling.

体外研究:
Afzelin (20-80 μM; 12 h) 可保护心肌细胞 H9C2 细胞的活力,抵抗 DOX(1 μM;12 小时)诱导的毒性。Afzelin 的抗心脏毒性作用会被 AMPKα 抑制剂 Dorsomorphin 消除。
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