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目的:分析胍丁胺对伯氏疟原虫K173株及伯氏疟原虫抗氯喹株的杀虫作用。方法:用Peters四天抑制实验分析了胍丁胺对伯氏疟原虫K173株及其抗氯喹株的杀虫作用。结果:每日口服胍丁胺(12.5-200 mg/kg)能显著抑制伯氏疟原虫K173株及其抗氯喹株的生长,IC_(50)分别为139mg/kg和126mg/kg,每日三次皮下注射胍丁胺(5-40mg/kg)比口服显示了更强的抗疟作用,IC_(50)约为30mg/kg,亚精胺拮抗胍丁胺对这两种疟原虫株的抗疟作用,胍丁胺不能逆转抗氯喹株伯氏疟原虫对氯喹的抗药性,皮下注射二氟甲基鸟氨酸(10-50mg/kg,daily)也能抑制疟原虫的生长,且此作用被亚精胺拮抗。结论:胍丁胺有抗疟作用,机制与抑制多胺尤其是亚精胺合成有关。
OBJECTIVE: To analyze the insecticidal effect of agmatine on Plasmodium berghei K173 and Plasmodium berghei against chloroquine. Methods: Four-day inhibition of Peters was used to analyze the insecticidal effect of agmatine on Plasmodium berghei K173 and its resistance to chloroquine. RESULTS: Daily oral administration of agmatine (12.5-200 mg / kg) significantly inhibited the growth of P. berghei K173 and its chloroquine resistant strains with IC 50 values of 139 mg / kg and 126 mg / kg, respectively, three times daily Subcutaneous injections of agmatine (5-40 mg / kg) showed a stronger antimalarial effect than orally, with an IC50 of about 30 mg / kg, with spermidine antagonizing agmatine against malaria strains of both Agmatine failed to reverse the resistance of chloroquine resistant Plasmodium berghei to chloroquine. Subcutaneous injection of difluoromethylornithine (10-50 mg / kg, daily) also inhibited the growth of Plasmodium, and this effect was inhibited by Spermidine antagonism. Conclusion: Agmatine has anti-malarial effect and its mechanism is related to the inhibition of polyamine, especially spermidine synthesis.