双氢青蒿素衍生物研究进展

Advances in Research of Dihydroartemisinin Derivative

青蒿素是从中国传统药用草本植物青蒿中提取得到的倍半萜类化合物。青蒿素具有优异的抗疟活性,对耐氯喹恶性疟效果更加显著。双氢青蒿素(dihydroartemisinin, DHA)是青蒿素的最重要衍生物,不仅是比青蒿素更好的抗疟药物,而且以此出发获得了蒿甲醚、青蒿琥酯等第一代上市药物。迄今为止,全球研究人员不仅发现了抗疟活性更好的DHA衍生物,而且发现某些衍生物具有抗肿瘤、抗利什曼虫病、抗吸血虫病、抗病毒、抗菌、抗炎、降脂等生物活性。本研究室也开展了DHA衍生物的研究,发现了很多高活性分子及新的生物活性。本文收集整理了国内外关于DHA衍生物合成及生物活性的研究情况,试图为DHA的后续研究提供线索。

Artemisinin is a sesquiterpene compound extracted from the Chinese traditional medicinal herb Artemisia annua. Artemisinin has excellent antimalarial activity, especially potent for chloro-quine-resistant falciparum malaria. Dihydroartemisinin (DHA) is the most important derivative of artemisinin, which is not only a better antimalarial drug than artemisinin, but also developed suc-cessfully the first generation drugs such as artemether and artesunate originated from it. Until now, global researchers have not only found DHA derivatives with better antimalarial activity, but also found that some derivatives have anti-tumor, anti-leishmaniasis, anti-blood schistosomiasis, an-ti-virus, antibacterial, anti-inflammatory, and lipid-lowering and so on. Our laboratory has also car-ried out researches on DHA derivatives and found many highly active molecules with new biological activities. This article collected and summarized the research advances with respect of the synthe-sis and biological activity of DHA derivatives at home and abroad, trying to provide clues for the fu-ture research of DHA.