Chinese Inventions Codexery

Artemisinin

Artemisinin is a key antimalarial drug discovered in 1972.

Artemisinin

Wikipedia / Wikimedia Commons

Artemisinin and its semisynthetic derivatives are drugs used to treat malaria caused by *Plasmodium falciparum*. The compound was discovered in 1972 by Tu Youyou, who received the 2015 Nobel Prize in Physiology or Medicine for this work, sharing the prize with William C. Campbell and Satoshi Ōmura—one half was awarded jointly to Campbell and Ōmura, the other half to Tu Youyou. Artemisinin-based combination therapies (ACTs) are now the global standard for treating malaria from *P. falciparum* and other *Plasmodium* species.

The drug comes from the herb *Artemisia annua* (sweet wormwood), a plant used in traditional Chinese medicine. It can also be made semisynthetically from a precursor produced by genetically engineered yeast, a method far more efficient than plant extraction. Artemisinin and its derivatives are sesquiterpene lactones with an unusual peroxide bridge—a 1,2,4-trioxane ring—that gives them antimalarial activity. Few other natural compounds contain this structure.

These drugs treat malaria. Compared to other antiparasitics, they clear parasites faster and work across more stages of the parasite’s life cycle. However, they have low bioavailability, poor pharmacokinetics, and high cost. The World Health Organization (WHO) strongly discourages using artemisinin alone (monotherapy) because malaria parasites show signs of developing resistance. Combination therapies, pairing artemisinin or its derivatives with another antimalarial, are the current standard of care.

For medical use, the WHO recommends artemisinin or one of its derivatives—usually with a longer-acting partner drug—as frontline treatment for all malaria cases. For uncomplicated malaria, the WHO advises three days of oral treatment with any of five ACTs: artemether/lumefantrine, artesunate/amodiaquine (ASAQ), artesunate/mefloquine, dihydroartemisinin/piperaquine, or artesunate/sulfadoxine/pyrimethamine. In these combinations, the artemisinin derivative kills parasites quickly but leaves the body rapidly, while the partner drug lasts longer to kill remaining parasites and offer some protection against reinfection.

For severe malaria, the WHO recommends intravenous or intramuscular artesunate for at least 24 hours, continuing until the patient can take oral medication, then switching to a three-day ACT course. If artesunate is unavailable, intramuscular artemether (a less potent deriva

used_for
Treatment of malaria

Lore & Background

Artemisinin was discovered in 1972 by Tu Youyou, who received the 2015 Nobel Prize in Physiology or Medicine for her discovery, sharing the prize with William C. Campbell and Satoshi Ōmura—one half was awarded jointly to Campbell and Ōmura, the other half to Tu Youyou. It can be extracted from the herb Artemisia annua (sweet wormwood), which is used in traditional Chinese medicine, or prepared by a semi-synthetic method from a precursor compound produced using a genetically engineered yeast, which is much more efficient than extraction from the plant. Artemisinin and its derivatives are all sesquiterpene lactones containing an unusual peroxide bridge, the endoperoxide 1,2,4-trioxane ring, which is responsible for their antimalarial properties. Few other natural compounds with such a peroxide bridge are known.

Reader's Guide

Artemisinin and its derivatives have been used for the treatment of malarial and parasitic worm infections. Advantages over other anti-parasitics include faster parasite elimination and broader efficacy across the parasite life-cycle; disadvantages include low bioavailability, poor pharmacokinetic properties, and high cost. Use of the drug by itself as a monotherapy is explicitly discouraged by the World Health Organization, as there have been signs that malarial parasites are developing resistance to the drug. Combination therapies, featuring artemisinin or its derivatives alongside some other antimalarial drug, constitute the contemporary standard-of-care treatment regimen for malaria. The WHO recommends artemisinin or one of its derivatives as frontline therapy for all cases of malaria, with specific regimens for uncomplicated and severe malaria. Artemisinins are not used for malaria prevention because of the extremely short activity (half-life) of the drug. Clinical evidence for artemisinin drug resistance in southeast Asia was first reported in 2008, and the parasite's kelch gene on chromosome 13 appears to be a reliable molecular marker for clinical resistance in Southeast Asia.

Did You Know?

Frequently Asked Questions

Who is credited with discovering Artemisinin?

Tu Youyou identified the compound in 1972 while investigating traditional Chinese herbal remedies for antimalarial activity. Her work was later recognized with the 2015 Nobel Prize in Physiology or Medicine.

What plant is Artemisinin originally derived from?

The compound is extracted from Artemisia annua, commonly called sweet wormwood, a species long used in traditional Chinese medicine. In modern production it can also be synthesized semi-synthetically from a precursor made by genetically modified yeast.

What medical condition is Artemisinin primarily used to treat?

It serves as the core agent in the standard global therapy for malaria caused by Plasmodium falciparum and other Plasmodium species. It is typically delivered as part of combination regimens rather than as a standalone drug.

Why is Artemisinin considered a landmark Chinese contribution to medicine?

It gave the world an effective treatment against drug-resistant malaria parasites and fundamentally reshaped global antimalarial strategy. The discovery also demonstrated how centuries-old herbal knowledge could be translated into modern pharmacology.

Can Artemisinin be produced without harvesting the sweet wormwood plant?

Yes, it can be made semi-synthetically from a precursor compound generated by genetically engineered yeast. This biotechnological route provides a scalable alternative to relying exclusively on agricultural harvests of the herb.

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