Klayman D L
Science. 1985 May 31;228(4703):1049-55. doi: 10.1126/science.3887571.
The herb Artemisia annua has been used for many centuries in Chinese traditional medicine as a treatment for fever and malaria. In 1971, Chinese chemists isolated from the leafy portions of the plant the substance responsible for its reputed medicinal action. This compound, called qinghaosu (QHS, artemisinin), is a sesquiterpene lactone that bears a peroxide grouping and, unlike most other antimalarials, lacks a nitrogen-containing heterocyclic ring system. The compound has been used successfully in several thousand malaria patients in China, including those with both chloroquine-sensitive and chloroquine-resistant strains of Plasmodium falciparum. Derivatives of QHS, such as dihydroqinghaosu, artemether, and the water-soluble sodium artesunate, appear to be more potent than QHS itself. Sodium artesunate acts rapidly in restoring to consciousness comatose patients with cerebral malaria. Thus QHS and its derivatives offer promise as a totally new class of antimalarials.
青蒿在中国传统医学中用于治疗发热和疟疾已有数百年历史。1971年,中国化学家从该植物的叶部分离出了具有其所谓药用作用的物质。这种化合物名为青蒿素(QHS),是一种倍半萜内酯,带有过氧化物基团,与大多数其他抗疟药不同,它缺乏含氮杂环系统。该化合物已在中国数千名疟疾患者中成功使用,包括对氯喹敏感和耐氯喹的恶性疟原虫菌株患者。青蒿素的衍生物,如双氢青蒿素、蒿甲醚和水溶性青蒿琥酯钠,似乎比青蒿素本身更有效。青蒿琥酯钠能迅速使脑型疟昏迷患者苏醒。因此,青蒿素及其衍生物有望成为一类全新的抗疟药。