产品
编 号:F750952
分子式:C20H22N4O3
分子量:366.41
产品类型
结构图
CAS No: 2299199-56-5
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生物活性:
Antimalarial agent 26 is an orally active 1,4-naphthoquinones derivative with antimalarial activities. Antimalarial agent 26 shows cytotoxicity against P. falciparum and selectivity over mammalian cell lines. Antimalarial agent 26 inhibits P. burghei induced parasitemia in vivo.
体内研究:
Antimalarial agent 26 (compound 11) (30 mg/kg;口服;每天一次,连续 4 天) 在雌性白化病瑞士小鼠中显示出抗疟活性。Antimalarial agent 26 (300 mg/kg;口服;单次剂量) 在雌性小鼠导致肝细胞损伤的病理损伤。Animal Model:Female albino swiss mice
Dosage:300 mg/kg
Administration:PO; single dose
Result:Presented necrosis of hepatocytes in moderate to severe degrees, acidophilic cytoplasm with macro vacuoles and micro steatosis, granular degeneration and congestion of the lobular center vein and hepatic portal vein. In the kidney, Resulted an atrophic glomerulus was observed with congested capillaries, reduction of mesangial cells and podocytes with discrete thickening of the basal membrane.
体外研究:
Antimalarial agent 26 (compound 11) 抑制 P. falciparum 的 IC50 为 2.7 μM,而对哺乳动物细胞的 CC50 分别为 440.9 μM (HepG2) 和 1336 μM (Vero)。Antimalarial agent 26 (1000-15.62 μM;2 小时) 在浓度为 250 至 15.6 μM 时显示溶血活性低于 40%。