青蒿素类衍生物结构修饰研究进展

Advances in Structure Modification of Artemisinin Derivatives

青蒿素是从传统中药黄花蒿中分离出来的一种倍半萜类化合物,具有高效的抗疟活性,临床已应用多年,但是由于其溶解性差、生物利用度低及复燃率高等缺点限制了其应用。为改善其以上缺点,人们以双氢青蒿素为母环合成了大量的青蒿素类衍生物,在这些衍生物中有些已在临床上应用多年,有一些的活性还有待评价。对近年来有关青蒿素衍生物的结构修饰新进展进行分类汇总,为其进一步研究提供参考。

Artemisinin , chemically a sesquiterpene , is isolated from plant Artemisia annua .It has a highly anti-malarial effect and has been used clinically for many years .However , the low solubility , poor bioavail-ability, as well as high recrudescence rate seriously restrict its clinical application .To overcome the disadvan-tages above , many derivatives have been synthesized from dihydroartemisinin , and out of these , the derivatives are either currently in use or being evaluated for use .In this paper , we review the modification of artemisinin derivatives in recent years .This review will provide a reference for further studies .