青蒿化学成份及其与青蒿素伍用对鼠疟的药效学研究

实验采用鼠疟模型及Peters4天抑制试验法,对从青蒿中分离得到的主要化学成份及其与青蒿素伍用进行了药效学评价。结果显示,青蒿素（QHS）的ED50和ED90分别为（10.2±1.3）mg/kg/d和（29.0±2.7）mg/kg/d。将青蒿素、青蒿酸、青蒿乙素、东莨菪内酯按1∶1∶1∶1混合得到QHH,其ED50和ED90分别为（12.6±1.1）mg/kg/d和（47.0±5.7）mg/kg/d。青蒿酸（QHA）、青蒿乙素（QHB）、东莨菪内酯（QHC）、青蒿黄酮1（QHD）、青蒿黄酮2（QHE）5种成份对鼠疟均有不同程度的抑制作用,但剂量高达500mg/kg/d时,抑制率最高也仅达到59%,远低于QHS的疗效。将分离的5种成份分别与QHS的半数有效剂量配伍进行药效测定,仅QHC的高剂量组显示一定的协同作用,其他各个组均未显示增效。QHH中QHS仅占1/4,但对鼠疟药效测定的结果ED50和ED90的值与QHS相近,提示QHA、QHB、QHC混合成份对QHS有一定的协同作用。因此,传统中药青蒿对疟疾的疗效是由以青蒿素为主的多组份共同作用的结果。

STUDIES ON THE ANTIMALARIAL ACTIVITIES OF DIFFERENT INGREDIENTS OF ARTEMISIA ANNUA L.AND THE COMBINATIONS WITH QHS ON PLASMODIUM BERGHEI

Peters 4d inhibition test were used to determine the antimalarial activity of different ingredients of Artemisia annua L. and their combinations with Qinghaosu （QHS） on P. berghei. The ED50 and ED90 of QHS are （10.2 ± 1.3） and （29.0 ± 2.7） mg/kg/d respectively ; and those of QHH （ Qinghaosu ： Qinghao acid ： Qinghao B ： Scopoletin = 1 ： 1 ： 1 ： 1 ） are （ 12.6 ± 1.1 ） and （47.0 ± 5.7） mg/kg/d respectively. Qinghao acid （ QHA）, Qinghao B （ QHB）, Scopoletin （QHC）, Casticin （QHD） and Chrysosplenol D （QHE） had some antimalarial activities on P. berghei. Even when the dosage was up to 500 mg/kg/d, the maximal inhibition rate was only 59%, which is less active than QHS. Therapeutic effect of different ingredients of A. auuna and QHS combinations on P. berghei appeared synergistic effects only with high dosage of QHC. Although QHS only accounts for 1/4 in QHH, QHH and QHS have similar antimalarial activity. The results revealed that the mixture of QHA, QHB and QHC enhanced the antimalarial activity of QHS on P. berghei. It was proved that the antimalarial activity of QHS primarily together with other ingredients of A. annua is the result of the antimalarial activity on P. berghei of A. annua in the study.