青蒿素的发现和发展  

Discovery and development of artemisinin

作　　者：袁亚男[1] 姜廷良[1] 周兴[1] 刘盈[1] YUAN YaNan JIANG TingLiang ZHOU Xing LIU Ying(Institute of Chinese Materia Medica, China Academy of Chinese Medical Sicences, Beijing 100700, China)

机构地区：[1]中国中医科学院中药研究所,北京100700

出　　处：《科学通报》2017年第18期1914-1927,共14页Chinese Science Bulletin

摘　　要：卫生部中医研究院中药研究所(简称"中研院中药所",现为中国中医科学院中药研究所)屠呦呦及其研究组在对中药进行大量研究基础上,受中医典籍《肘后备急方》的启迪创建了青蒿提取方法,1971年10月获得青蒿抗疟活性化学部位,1972年11月从中发现青蒿素.青蒿素是一个仅由碳、氢、氧3种元素组成、具有过氧基团特殊结构的新型倍半萜内酯,是与已知抗疟药在化学结构、作用机制完全不同的新化合物.临床疗效几乎可达100%,具有速效、高效和低毒等特点.目前,青蒿素及其衍生物是世界上治疗疟疾最有效的药物,青蒿素联合疗法已被用于几乎所有国家和地区的疟区,每年治疗病例一亿以上,降低了全球疟疾的发生率和死亡率,已挽救了数百万人的生命.青蒿素来自中医药、发现启迪于中医药.它是中国传统医学和现代科技紧密结合.融合多学科和行业的系统创新工程,凝聚着一群中国科学家的艰辛和智慧,是中医药对人类健康事业作出的一项巨大贡献.我国政府先后11次给参加这一工程的相关单位授予国家发明奖、国家自然科学奖、国家科技进步奖等各类大奖,屠呦呦也因此获得了2015年度诺贝尔生理学或医学奖和2016年度国家最高科学技术奖.Malaria is an infectious disease, which is caused by plasmodium through mosquito biting or transfusing carriers＇ blood. Malaria is the main tropical parasitic disease globally, especially in the tropical and subtropical regions. At the end of the last century, nearly one hundred countries were affected each year, nearly 300 million people were infected and nearly one million people died. Tu Youyou, who is from Institute of Chinese Materia Medica（ICMM）, Academy of Traditional Chinese Medicine（current name： China Academy of Chinese Medical Sciences, CACMS）, inspired by the description of antimalarial usage of Qinghao（Artemisia annua L.） in Handbook of Prescriptions for Emergencies written by Ge Hong, she redesigned a method to extract the active ingredient from Qinghao, and obtained No. 191 sample in October, 1971 that could inhibit rodent malaria and monkey malaria with 100% inhibition. And Tu and her team obtained artemisinin in November, 1972 firstly. The absolute structure of artemisinin was determined by X-ray diffraction as a new sesquiterpene lactone of only carbon, hydrogen and oxygen elements with a specific structure of peroxide bridge. It is a new compound which is totally different from known antimalarial drugs in chemical structure and action mechanism. The clinical performance of artemisinin is fast, efficient, and with low toxicity. At present, artemisinin and its derivatives are the most effective drug for malaria treatment. ACT therapy has been used in almost all countries and regions of malaria endemic areas, and more than one hundred million cases per year are cured. Millions of lives are saved globally by reducing the incidence and mortality of malaria. Artemisinin is a gift from Traditional Chinese Medicine. The discovery of artemisinin is an output of the combination of Traditional Chinese Medicine with modern science and technology, an innovation system engineering integrated of multidisciplinary, together with a group of Chinese scientists＇ diligence and wisdom, which is a

关 键 词：青蒿素 青蒿素衍生物 青蒿素联合疗法 

分 类 号：R978.6[医药卫生—药品]