Summary

This book presents Tu Youyou's systematic chemical investigation of *Artemisia annua* L., the sweet wormwood plant, which led to the discovery of artemisinin as a potent antimalarial compound. The central thesis is that a low-temperature extraction method, guided by a classical Chinese medical text from the 4th century, could isolate a previously overlooked active principle with superior efficacy against drug-resistant malaria parasites. Tu details her team's isolation of artemisinin (qinghaosu) using ether at low temperatures, its structural elucidation as a sesquiterpene lactone with an endoperoxide bridge, and the development of derivatives like dihydroartemisinin. The book also covers the chemical characterization of other constituents in *A. annua*, including volatile oils and flavonoids, and the optimization of extraction protocols. A reader takes away a concrete understanding of how ethnopharmacology and careful chemical methodology can yield a life-saving drug, and the importance of preserving traditional knowledge in modern drug discovery.

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Key concepts

Artemisinin (qinghaosu) — A sesquiterpene lactone with an endoperoxide bridge, isolated from *Artemisia annua*, that is highly effective against chloroquine-resistant *Plasmodium falciparum* malaria.
Low-temperature ether extraction — The key methodological innovation, inspired by a 4th-century text (Ge Hong's *Handbook of Prescriptions for Emergencies*), that prevented thermal degradation of the active compound during isolation.
Endoperoxide bridge — The unique chemical structure (C-O-O-C) within artemisinin responsible for its antimalarial activity through iron-mediated cleavage and free radical generation.
Dihydroartemisinin — A semisynthetic derivative of artemisinin with improved solubility and potency, used as a precursor for other artemisinin-based combination therapies (ACTs).
Sesquiterpene lactone — A class of terpenoid compounds characterized by a 15-carbon skeleton and a lactone ring, to which artemisinin belongs.
Ethnopharmacological screening — The process of testing traditional herbal remedies for modern pharmacological activity, which guided Tu's selection of *Artemisia annua* from over 2,000 candidate Chinese herbs.