咯萘啶、阿莫地喹、甲氟喹及青蒿素对伯氏疟原虫的疗效

THE BLOOD SCHIZONTOCIDAL EFFECTS OF PYRONARIDINE,AMODIAQUINE,MEFLOQUINE AND QINGHAOSU ON MICE INFECTED WITH PLASMODIUM BERGHBI

用4天抑制试验法给感染伯氏疟原虫ANKA株小鼠灌胃咯萘啶12.5mg/kg·d或阿莫地喹25mg/kg·d均能完全杀灭原虫;甲氟喹25mg/kg·d或青蒿素100mg/kg·d虽有抑制作用但治愈率仅为50％及0％。咯萘啶12.5mg/kg·d对中度抗氯喹的NS系原虫亦有明显作用,洽愈率70％,而阿莫地喹100mg/kg·d、甲氟喹100mg/kg·d及青蒿素200mg/kg·d均无治愈鼠,示后3种药与氯喹有不同程度的交叉抗性。上述剂量的阿莫地喹、甲氟喹和青蒿素对高度抗咯萘啶的伯氏疟原虫无明显抑制作用,示它们与咯萘啶有交叉抗性。

The asexual stages of P.berghei ANKA were completely eliminated as revealed in a '4-day suppressive test' with the daily dose of pyronaridine 12.5mg base/kg or amodiaquine 25 mg base/kg.Mefloquine 25 mg base/kg and qinghaosu 100mg/kg though exerted obvious suppressive effect,the cure rates were only 50% and 0%,respectively.In treating chloroquine-sensitive P.berghei ANKA strain pyronaridine exhibited the best therapeutic activity,which was followed by amodiaquine,mefloquine and qinghaosu.In treating moderately chloroquine-resistant P.berghei NS line the cure rate of pyronaridine 12.5mg/ kg·d×4 was 70% ,but none of the 10 infected mice from any group was cured by amodiaquine 100 mg/kg2d,mefloquine 100 mg/kg·d or qinghaosu 200 mg/kg·d.Though the latter 3 drugs showed prominent suppressive effects,parasitemia remained positive or recrudesced after dosing.We demonstrate that parasites resistant to chloroquine had cross resistance to amodiaquine,mefloquine and qinghaosu at various degrees.Amodiaquine 100 mg/kg·d,mefloquine 100mg/kg·d and qinghaosu 200 mg/kg·d exhibited no obvious suppressive activity on highly pyronaridine-resistant line of P.berghei,indicating the existence of cross resistance to pyronaridine.