What is artemisinin?

Artemisinin is extracted from traditional Chinese medicine artemisinin peroxide groups have sesquiterpene lactone drugs. Its murine plasmodia of ultrastructure, mainly Plasmodium membrane system changes, the drug acts on the first food vacuole membrane, surface membrane, mitochondria, endoplasmic reticulum, in addition to the nuclear chromatin has some effects. Tip artemisinin main mode of action is an interference surface membrane - mitochondrial function. Artemisinin may act on the food vacuole membrane, thereby blocking the nutritional intake of the earliest stages of the parasite occurs faster amino acid starvation, the rapid formation of autophagic vacuoles, and continue to discharge the parasite, but the parasite cytoplasm and a significant loss of deaths. Plasmodium falciparum in vitro tritiated intake isoleucine also shows its mode of action may be inhibition of the initial parasite protein synthesis.


Introduction:

Artemisinin Common name: Artemisinin
Name: Artemisinin
Chinese alias: Artemisia annua vegetarian, yellow pigment, yellow Artemisinin
English Synonyms: Arteannuin, Artemisinine, Qinghaosu
MF: C15H22O5
Molecular Weight: 282.33
Colorless needle crystal, bitter taste.
In acetone, ethyl acetate, chloroform, benzene, and acetic acid soluble in ethanol and methanol, ether and petroleum
Soluble in ether, almost insoluble in water.
Melting point :156-157 ℃ (decoction decomposition)
MDL number: MFCD00081057

Pharmacokinetics:
Artemisinin rapidly absorbed from the gut after oral administration of 0.5 to 1 hour after the peak plasma concentration, decreased by half after 4 hours, 72 hours only a trace of blood. It is within the red blood cell concentration is less than plasma concentrations. After absorption of the tissue to the intestine, liver, kidney more content. The product is a fat-soluble substance, it can be through the blood-brain barrier into the brain tissue. Rapidly metabolized in the body, the structure and properties of metabolites is unclear. Mainly from the kidney and intestinal tract, 24 hours can be discharged 84%, only a small amount of residual 72 hours. Since metabolism and excretion are fast, effective blood concentration to maintain a short time, is not conducive to completely kill the parasite, so the high recurrence rate. Artemisinin derivative artesunate, T1 / 2 was 0.5 hours, it should be repeated administration.

Indications:
Mainly for vivax malaria, falciparum malaria symptom control, as well as chloroquine-resistant strains of insects of treatment, can also be used to treat dangerous type of falciparum malaria, such as cerebral, jaundice type. Also for the treatment of systemic lupus erythematosus and discoid lupus erythematosus.
Chemical structure
Artemisinin formula C15H22O5, molecular weight 282.33, component content: C 63.81%, H 7.85%, O 28.33%.

Properties:
Colorless needle crystal, bitter taste. In acetone, ethyl acetate, chloroform, benzene, and acetic acid soluble in ethanol and methanol, ether and petroleum ether soluble, almost insoluble in water. Melting point :156-157 ℃

Study of history:

Chinese antimalarial drug research from 1967 established five hundred twenty-three project, its wholly-known Chinese malaria research collaboration project, founded in 1967, May 23, due to top-secret military project, then set code 523.
After 380 times murine malaria screening, in October 1971 to obtain the medicine artemisinin screening success. 1972 was isolated from Artemisia annua effective antimalarial monomer named artemisinin malaria rat, monkey malaria parasite inhibition rate reached 100%.
1973 made by clinical and laboratory research consistent results, antimalarial drug artemisinin was born.
October 1981, held in Beijing organized by the World Health Organization, "artemisinin" international conference, China "artemisinin chemical research," the statement, causing great interest representatives, and that "this new found to be more important is that the design and synthesis of new drugs will be further pointed out the direction. "
In 1986, a new class of drug artemisinin obtain certificates Dihydroartemisinin also received a new drug certificate. These results were obtained the National Invention Award and the National Top Ten Technology Achievement Award.
September 2011, China Tu Yo Yo female pharmacists create new antimalarial --- due to artemisinin and dihydroartemisinin award of the Nobel Prize known as the "wind vane" of the Lasker Award. This is China's biomedical community so far received the most advanced world-class awards.

Main sources:

Is the main source of artemisinin from Artemisia annua directly extracted; or extract of Artemisia annua with higher levels of acid, and then semi-synthesized.
 
At present, except outside Artemisia annua, artemisinin has not been found to contain other natural plant resources. While speaking world annua widespread species, but artemisinin content vary greatly with different origin. According to the findings so far, except for China Eastern Chongqing, Fujian, Guangxi, Hainan, parts, but most areas of the world in the production of Artemisia annua artemisinin content is very low, no value in use. According to the national authorities investigate, on a global scale, only China Youyang Wu Mu Mountains region that has the industrial growth of artemisinin extract value. Youyang Artemisia annua is the world's most important production base, its production of Artemisia annua cultivation technology has passed the national GAP certification, enjoy the "World annua town" reputation, with 80 percent of global raw material produced from Artemisia annua youyang. Drugs of this unique resource, the relevant state ministries and commissions since the 1980s the explicit provision of artemisinin original plant (Artemisia annua), seeds, fresh and dried whole herb and artemisinin prohibited export bulk drugs.

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From:Advanced Chemicals