Artemisinin in the context of "Tu Youyou"

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⭐ Core Definition: Artemisinin

Artemisinin (/ˌɑːrtɪˈmsɪnɪn/) and its semisynthetic derivatives are a group of drugs used in the treatment of malaria due to Plasmodium falciparum. It was discovered in 1972 by Tu Youyou, who shared the 2015 Nobel Prize in Physiology or Medicine for her discovery. Artemisinin-based combination therapies (ACTs) have become standard treatment worldwide for P. falciparum malaria as well as malaria due to other species of Plasmodium. Artemisinin can be extracted from the herb Artemisia annua (sweet wormwood), which is used in traditional Chinese medicine. Alternatively, it can be prepared by a semi-synthetic method from a precursor compound that can be 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. This endoperoxide 1,2,4-trioxane ring is responsible for their antimalarial properties. Few other natural compounds with such a peroxide bridge are known.

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👉 Artemisinin in the context of Tu Youyou

Tu Youyou (Chinese: 屠呦呦; pinyin: Tú Yōuyōu; born on December 30, 1930, in Ningbo, Zhejiang province) is a Nobel Prize-winning malariologist and pharmaceutical chemist and member of the China Academy of Chinese Medical Sciences. She received the Nobel Prize for Physiology or Medicine in 2015 for her discovery and development of artemisinin and related compounds. Tu pursued her education in pharmaceutical sciences at the Peking University School of Medicine (Beijing Medical College) and later focused on traditional Chinese medicine at the Institute of Materia Medica. Her achievements and experience have inspired other researchers and emphasized the development of traditional Chinese medicine.

Malaria is caused by a single-cell parasite that causes severe fever. During the Vietnam War in 1967, China and Vietnam were significantly affected by malaria, with approximately 30 million cases and 300,000 deaths just from China. Scientists worldwide had screened over 240,000 compounds without success for finding a cure. She then investigated the history of Chinese medical classics, visiting practitioners of traditional Chinese medicine across the country on her own. She gathered her findings in a notebook titled "A Collection of Single Practical Prescriptions for Anti-Malaria." By 1971, her team had screened over 2,000 traditional Chinese recipes and made 380 herbal extracts, from some 200 herbs, which were tested on mice. Finally, she discovered breakthrough medicines, artemisinin and dihydroartemisinin, used to treat malaria. In the 1970s, after studies of traditional herbal medicines, Tu Youyou focused on sweet wormwood and extracted a substance, artemisinin, that inhibits the malaria parasite. Artesunate is special among artemisinin-based drugs because it dissolves in water, allowing rapid absorption into the body. The fast absorption enables the doctor to inject the medicine into a vein, muscle, or rectum; moreover, severe malaria can cause symptoms that deteriorate quickly, and patients cannot take medicine orally. Artemisinin-based medication has led to the survival and improved health of millions of people. This treatment saved millions of lives in South China, Southeast Asia, Africa, and South America.

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Artemisinin in the context of Semisynthesis

Semisynthesis, or partial chemical synthesis, is a type of chemical synthesis that uses chemical compounds isolated from natural sources (such as microbial cell cultures or plant material) as the starting materials to produce novel compounds with distinct chemical and medicinal properties. The novel compounds generally have a high molecular weight or a complex molecular structure, more so than those produced by total synthesis from simple starting materials. Semisynthesis is a means of preparing many medicines more cheaply than by total synthesis since fewer chemical steps are necessary.

Drugs derived from natural sources are commonly produced either by isolation from their natural source or, as described here, through semisynthesis of an isolated agent. From the perspective of chemical synthesis, living organisms act as highly efficient chemical factories, capable of producing structurally complex compounds through biosynthesis. In contrast, engineered chemical synthesis, although powerful, tends to be simpler and less chemically diverse than the complex biosynthetic pathways essential to life.

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Artemisinin in the context of Antimalarial medication

Antimalarial medications or simply antimalarials are a type of antiparasitic chemical agent, often naturally derived, that can be used to treat or to prevent malaria, in the latter case, most often aiming at two susceptible target groups, young children and pregnant women. As of 2018, modern treatments, including for severe malaria, continued to depend on therapies deriving historically from quinine and artesunate, both parenteral (injectable) drugs, expanding from there into the many classes of available modern drugs. Incidence and distribution of the disease ("malaria burden") is expected to remain high, globally, for many years to come; moreover, known antimalarial drugs have repeatedly been observed to elicit resistance in the malaria parasite—including for combination therapies featuring artemisinin, a drug of last resort, where resistance has now been observed in Southeast Asia. As such, the needs for new antimalarial agents and new strategies of treatment (e.g., new combination therapies) remain important priorities in tropical medicine. As well, despite very positive outcomes from many modern treatments, serious side effects can affect some individuals taking standard doses (e.g., retinopathy with chloroquine, acute haemolytic anaemia with tafenoquine).

Specifically, antimalarial drugs may be used to treat malaria in three categories of individuals, (i) those with suspected or confirmed infection, (ii) those visiting a malaria-endemic regions who have no immunity, to prevent infection via malaria prophylaxis, and (iii) or in broader groups of individuals, in routine but intermittent preventative treatment in regions where malaria is endemic via intermittent preventive therapy. Practice in treating cases of malaria is most often based on the concept of combination therapy (e.g., using agents such as artemether and lumefantrine against chloroquine-resistant Plasmodium falciparum infection), since this offers advantages including reduced risk of treatment failure, reduced risk of developed resistance, as well as the possibility of reduced side-effects. Prompt parasitological confirmation by microscopy, or alternatively by rapid diagnostic tests, is recommended in all patients suspected of malaria before treatment is started. Treatment solely on the basis of clinical suspicion is considered when a parasitological diagnosis is not possible.

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Artemisinin in the context of Artemisia annua

Artemisia annua, also known as sweet wormwood, sweet annie, sweet sagewort, annual mugwort or annual wormwood, is a common type of wormwood native to temperate Asia, but naturalized in many countries including scattered parts of North America.

The chemical compound artemisinin, which is isolated from A. annua, is a medication used to treat malaria due to Plasmodium falciparum, the deadliest species of malarial parasite. Discovery of artemisinin and its antimalarial properties made the Chinese scientist Tu Youyou recipient of the 2011 Lasker Prize and 2015 Nobel Prize in Physiology or Medicine.

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Artemisinin in the context of 1,2,4-trioxane

1,2,4-Trioxane is one of the isomers of trioxane. It has the molecular formula C3H6O3 and consists of a six membered ring with three carbon atoms and three oxygen atoms. The two adjacent oxygen atoms form a peroxide functional group and the other forms an ether functional group. It is like a cyclic acetal but with one of the oxygen atoms in the acetal group being replaced by a peroxide group.

1,2,4-Trioxane itself has not been isolated or characterized, but rather only studied computationally. However, it constitutes an important structural element of some more complex organic compounds. The natural compound artemisinin, isolated from the sweet wormwood plant (Artemisia annua), and some semi-synthetic derivatives are important antimalarial drugs containing the 1,2,4-trioxane ring. Completely synthetic analogs containing the 1,2,4-trioxane ring are important potential improvements over the naturally derived artemisinins. The peroxide group in the 1,2,4-trioxane core of artemisinin is cleaved in the presence of the malaria parasite leading to reactive oxygen radicals that are damaging to the parasite.

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