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青蒿琥酯是新抗疟药青蒿素的水溶性衍生物。本实验通过大鼠骨髓微核试验对其遗传学毒性进行了研究。结果表明,青蒿琥酯 100~300mg/kg单次尾静脉注射后6 h均诱发早期微核,并与剂量呈正相关。青蒿琥酯 48和 96 mg/ kg(分别相当于临床剂量的20和40倍)给药后6、12、24 h引起骨髓多染红细胞(PCE)微核频率增高,PCE/NCE(正成红细胞)比率下降, 24mg/kg(临床剂量的 10倍)对微核率及PCE/ NCE比率均未见明显改变。结果提示,高剂量青蒿琥酯不仅可引起大鼠骨髓红系造血抑制,而且可能引起遗传学毒性。
Artesunate is a water-soluble derivative of the new antimalarial drug artemisinin. In this experiment, the genetic toxicity of rat bone marrow micronucleus test was studied. The results showed that early micronuclei were induced at 6 h after a single tail vein injection of artesunate at doses of 100-300 mg / kg and were positively correlated with the dose. The frequency of micronuclei in bone marrow polychromatic erythrocytes (PCE) was increased at 6, 12 and 24 h after artesunate treatment at doses of 48 and 96 mg / kg (20 and 40 times the clinical dose, respectively) ) Ratio, 24mg / kg (10 times the clinical dose) on the micronucleus rate and PCE / NCE ratio were not significantly changed. The results suggest that high doses of artesunate can not only cause hematopoietic inhibition of bone marrow erythroblasts, but may also cause genetic toxicity.