Artemisinin

Artemisinin, also known as qinghaosu, is an organic compound with the molecular formula C15H22O5 and a relative molecular weight of 282.34.
Qinghaosu is one of the best drugs for treating malaria resistance. A combination therapy based on qinghaosu-class drugs is currently the most effective and important means of treating malaria. In recent years, as research has continued, other actions of qinghaosu have also been discovered, such as anti-tumor, treatment of pulmonary hypertension, anti-diabetes, teratogenicity, anti-fungal, immune regulation, anti-viral, anti-inflammatory, anti-pulmonary fibrosis, anti-bacterial, cardiovascular effects, and other pharmacological actions.

Artemisinin is a colorless acicular crystal, soluble in chloroform, acetone, ethyl acetate and benzene, soluble in ethanol, ether, slightly soluble in cold petroleum ether, almost insoluble in water. Because of its special peroxy groups, it is thermally unstable and susceptible to decomposition by humidity, heat and reducing substances.

When it comes to artemisinin, people will first think of its anti-malaria function, WHO believes that artemisinin is the best drug to treat malaria resistance, and the combination therapy based on artemisinin-based drugs is also the most effective and important means to treat malaria at present. However, with the deepening of research in recent years, more and more other effects of artemisinin have been discovered and applied, such as anti-tumor, treatment of pulmonary hypertension, anti-diabetes, embryonic toxicity, antifungal, immune regulation and so on.

​antimalarial
Malaria is an insect-borne infectious disease, an infectious disease caused by the bite of the parasite infected by the parasite, which can cause liver and spleen enlargement after multiple attacks for a long time, and accompanied by anemia and other symptoms. Artemisinin has been instrumental in achieving a certain level of treatment for malaria. The peroxy bond in artemisinin structure is oxidizing and is an essential antimalarial group. The mechanism of action is that the free groups produced by artemisinin in vivo bind to plasmodium protein and change the membrane structure of plasmodium. After the free group binds to the malarial protein, the double membrane of the mitochondria will burst and eventually fall off, resulting in the destruction of the cell structure and function of the malaria parasite, and the chromatin in the nucleus will also be affected to a certain extent. Amino acids, on the other hand, are the building blocks of proteins after artemisinin action. The absorption of isoleucine by Plasmodium parasites is reduced, which leads to the obstruction of the synthesis of parasite proteins. Artemisia flavescens can not only kill pathogens, but also have anti-schistosomiasis, treatment of toxoplasma infection, anti-pneumocystis carinii, anti-coccidia and so on. Clinical trials have proved that artemisinin and its derivatives have not been found to have particularly significant side effects in the treatment of malaria.

​​antitumor
Malignant tumor is the biggest killer of human health, if not treated in time, it will endanger life safety. In vitro experiments show that a certain dose of artemisinin can induce apoptosis of liver cancer cells, breast cancer cells, cervical cancer cells and other cancer cells, and significantly inhibit the growth of cancer cells. It was found that artemisinin could regulate the expression of cyclin in tumor cells, enhance the effect of CKIs, and lead to cell cycle arrest. Or it can cause cell apoptosis and inhibit tumor angiogenesis to resist the occurrence and development of tumors. Artemisinin is used in the treatment of leukemia by acting on the cell membrane of leukemia cells, increasing the permeability of the membrane, changing osmotic pressure, resulting in an increase in the concentration of calcium ions in the cell, thus activating calpsin, causing the cell membrane to burst, and accelerating the release of apoptotic substances to increase the rate of apoptosis.

​​Treatment of pulmonary hypertension
Pulmonary hypertension (PAH) is a pathophysiological condition characterized by pulmonary artery remodeling and elevated pulmonary artery pressure to a certain limit, which can be a complication or syndrome. Artemisinin is used to treat pulmonary hypertension: it reduces pulmonary artery pressure and improves symptoms in patients with PAH by dilating blood vessels. Zaiman et al. found that artemisinin has anti-inflammatory effect, artemisinin and its kernel substances can inhibit a variety of inflammatory factors, and can inhibit the production of nitric oxide by inflammatory mediators. Artemisinin has immunomodulatory effects. Feng Yibai et al. found through experimental studies that artemisinin can inhibit the proliferation of vascular endothelial cells and vascular smooth muscle cells, and thus play an important role in the treatment of PAH. Artemisinin can inhibit the activity of matrix metalloproteinases and thus inhibit pulmonary vascular remodeling. Artemisinin can inhibit the expression of PAH related cytokines, and further enhance the anti-vascular remodeling effect of artemisinin.

​​Immunomodulation
It was found that the dose of artemisinin and its derivatives could inhibit T lymphocyte mitogen well without causing cytotoxicity, thus inducing the proliferation of mouse spleen lymphocytes. This finding has a good reference value for the treatment of autoimmune diseases mediated by T lymphocytes. Artemisinin vinegar can enhance non-specific immunity and increase the total complement activity in mouse serum. Dihydroartemisinin can directly inhibit the proliferation of B lymphocytes, thereby reducing the secretion of autoantibodies by B lymphocytes, alleviating humoral immune response, inhibiting humoral immunity to a certain extent, and reducing the formation of immune complexes.

​​Antifungal
The antifungal action of artemisinin also makes artemisinin exhibit certain antibacterial activity. The study confirmed that artemisinin residue powder and water decoction had strong antibacterial action against Bacillus anthracis, Staphylococcus epidermidis, Coccus catarrhus and Bacillus diphtheriae, and also had certain antibacterial action against Bacillus tuberculosis, Bacillus aeruginosa, Staphylococcus aureus and Bacillus dysenteriae.

​​Antidiabetic
On December 1, 2016, a study in the journal Cell suggests that artemisinin may also save people with diabetes. Scientists from the CeMM Center for Molecular Medicine at the Austrian Academy of Sciences and other institutions found that artemisinin can make glucagon-producing alpha cells "transform" into insulin-producing beta cells. Artemisinin binds to a protein called gephyrin. Gephyrin activates the GABA receptor, the main switch for cell signaling. Subsequently, numerous biochemical reactions change, leading to the production of insulin. Another study showed that in a mouse model, injection of GABA also caused alpha cells to turn into beta cells, suggesting that both substances target the same mechanism, but the long-term effects of artemisinin need to be further tested.

​​Treatment of polycystic ovary syndrome
On June 13, 2024, Professor Tang Qiqun's team of Zhongshan Hospital Affiliated to Fudan University and the team of Fudan Basic Medical College jointly published a research paper online in the journal Science, which found that artemisinin derivatives can treat polycystic ovary syndrome, and explained the relevant mechanism, providing a new idea for the clinical treatment of PCOS and androgen increase related diseases.

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Artemisinin is mainly extracted directly from artemisinin, or extracted from artemisinin with a higher content of artemisinin, and then semi-synthesized. Although artemisinin is widely distributed in different parts of the world, the content of artemisinin varies greatly with different places, and it has remarkable ecological significance. According to the study, except for parts of China, the content of artemisinin produced in most regions of the world is very low and has no use value.

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