【摘要】 目的　检测四个青蒿素微生物转化产物 10 β -羟基青蒿素[1] 、去氧青蒿素[2 ] 、9β -羟基青蒿素[3] 及 3β -羟基青蒿素[4 ] ,对体外培养恶性疟原虫的作用。方法　以青蒿素和氯喹为对照 ,用体外微量法测定。结果　四个转化产物的抗疟活性比青蒿素均有不同程度的降低 ,其中 10 β -羟基青蒿素活性较好。结论　 30位、9位、10位的羟基化引起的结构改变均使青蒿素体外抗疟原虫活性有一定的减弱 ,过氧桥的断裂同样使活性降低。更多还原

【Abstract】 Objective To testin vitro antimalarial activity of several biotransformed products from artemisinin including 10β-hydroxyartemisinin [1], deoxyartemisinin [2], 9β-hydroxyartemisinin [3] and 3β-hydroxyartemisinin [4]. Method Microtest was used (check in vitro antimalarial activities by testing SC50 and SC90 of the compounds). Results The in vitro antimalarial activities of the biotransformed products decreased by comparison with artemisinin. Conclusion 10β、9β and 3β-hydroxylation of artemisinin and losing oxygen atom resulted in lower in vitro antimalarial activities.更多还原