青蒿素及其衍生物是临床上用于治疗疟疾的一线药物，在疟疾的治疗中发挥着重要的作用，挽救了千万人的生命。2015年屠呦呦因发现青蒿素而获得诺贝尔医学或生理学奖，致使青蒿素在多年之后又重新 获得了人们的关注。虽然自青蒿素发现之后，人们对于青蒿素抗疟机制的研究一直没有停止，但是直到现在， 青蒿素作用于恶性疟原虫的分子机理仍然存在争议，主要体现在青蒿素的激活剂来源以及青蒿素在疟原虫中 的蛋白靶点。另外，2008年以来，陆续有报导表明出现了具有青蒿素耐药性的疟原虫株，基于临床上对于青蒿 素的依赖性，青蒿素耐药疟原虫株的传播将会造成严重的后果。因此，加快青蒿素作用机制研究以及进一步研 究疟原虫青蒿素耐药因素变得迫在眉睫。在本篇综述中，我们总结了青蒿素机制研究中具有代表性的成果，主 要包括青蒿素激活剂来源的研究、青蒿素作用靶点的研究以及青蒿素耐药机制的研究。

Artemisinin and its derivatives play a key role in malarial therapy, and have saved millions of lives as firstline drugs in the effort against malarial. In 2015, artemisinin draw renewed attention because Tu Youyou won the Novel Prize for her discovery of artemisinin in the early 1970s. Although many scientists have tried to explain the mechanism of action of artemisinin’s anti-malarial activity for decades, the underlying mechanism remains elusive. Till now, two questions remain controversial: the origin of iron sources required for artemisinin activation. The protein targets of artemisinin in malaria parasite. Since 2008, the phenomenon of artemisinin resistance has nonetheless already been reported and extensively studied. Considering the reliance on artemisinin in clinic malarial treatment, the spread of artemisinin resistance could bring unfortunate consequences. Therefore, understanding the mechanism of action and resistance of artemisinin become emergency. In the present review, we will summarize the remarkable studies on the origin of iron sources, the protein targets and the resistance mechanism of artemisinin in its research history.

国家自然科学基金委应急管理项目（81641002）：青蒿素类化合物抗疟机理研究，负责人：屠呦呦；国家科技部重大新药创制项目（2017ZX09101002-001-001-05）：青蒿素及其衍生物创新药物研究，负责人：王继刚；国家自然科学基金委青年基金项目（81803456）：载药外泌体诱 导生成多能干细胞用于治疗AD的研究，负责人：王宇彤。