产品
编 号:F757079
分子式:C21H18N4O3
分子量:374.39
产品类型
结构图
CAS No: 2944456-41-9
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生物活性:
Antimalarial agent 25 is an orally active 1,4-naphthoquinones derivative with antimalarial activity. Antimalarial agent 25 shows cytotoxicity against P. falciparum. Antimalarial agent 25 inhibits P. burghei induced parasitemia in vivo.
体内研究:
Antimalarial agent 25 (30 mg/kg; PO; QID) 可增强伯氏疟原虫小鼠的抗疟活性。Antimalarial agent 25 (300 mg/kg; 口服; 单次剂量) 在雌性小鼠中无明显的病理改变以及组织病理学损伤。Animal Model:Mice infected with Plasmodium berghei ANKA
Dosage:30 mg/kg
Administration:Oral administration; for 4 consecutive days
Result:Partly reduced P. berghei infection.Parasitemia decreased by 33% on the seventh day (post-treatment).
体外研究:
Antimalarial agent 25 (compound 8) 抑制 P. falciparum 的 IC50 为 4.2 μM,而对哺乳动物细胞的CC50 分别为 289.2 μM (HepG2) 和 400.6 μM (Vero)。Antimalarial agent 25 (compound 8) (15.62-1000 μM; 2 小时) 在未受感染的人类红细胞中,15.6 至250 μM 的浓度显示出低于 40% 的溶血活性。Antimalarial agent 25 (compound 8) (30-0.411 μg/mL; 48 h) 导致 W2 strain of P. falciparum 的细胞质完全退化,膜的完整性丧失等形态的变化。