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Artemisinin powder is an organic compound with molecular formula of C15H22O5,CAS 63968-64-9. It is a colorless needle crystal. It is easily soluble in chloroform, acetone, ethyl acetate and benzene, soluble in ethanol and ether, slightly soluble in cold petroleum ether and almost insoluble in water. Because of its special peroxy group, it is unstable to heat and is easy to decompose under the influence of moisture, heat and reducing substances. In October 2015, Tu youyou and her team created new antimalarial drugs artemisinin and dihydroartemisinin.

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Chemical Formula |
C15H22O5 |
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Exact Mass |
282 |
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Molecular Weight |
282 |
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m/z |
282 (100.0%), 283 (16.2%), 284 (1.2%), 284 (1.0%) |
|
Elemental Analysis |
C, 63.81; H, 7.85; O, 28.33 |
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When it comes to artemisinin, people first think of its anti malaria function. Who believes that artemisinin is the best drug for the treatment of malaria resistance. The combination therapy based on artemisinin drugs is also the most effective and important means for the treatment of malaria. But in recent years, with the development of research, more and more artemisinin's other functions have been discovered and applied, such as anti-tumor, treatment of pulmonary hypertension, anti diabetes, embryotoxicity, antifungal, immunomodulation and so on.
Take a certain amount of dry powder of Artemisia annua branches and leaves, add ethanol, stir and extract to obtain ethanol extract, dry under reduced pressure, and dissolve it in ether water two-phase solution to obtain artemisinin and artemisinic acid respectively. The yield of artemisinic acid was 90% and the extraction rate of artemisinin was 57%. This separation method is simple to operate, which can effectively realize the preliminary separation of the two components and provide reference for the subsequent purification of active substances in Artemisia annua.
Ethanol method:

Take a certain amount of dry powder of Artemisia annua branches and leaves, soak it in dilute ethanol for 24 hours to obtain ethanol extract, inject it into the continuous extraction device, and then extract it with solvent gasoline containing benzene and ethyl acetate to obtain alcohol phase and extraction phase. The alcohol phase can be recycled. The extraction phase is decolorized with activated carbon, filtered, the solvent is recovered, and then a concentrated solution is obtained, The crude artemisinin crystal is obtained by cooling and crystallization, and the finished artemisinin is obtained by recrystallization with ethanol. This method has the advantages of high yield, low cost, less steps, simple operation and safety.
Take a certain amount of dry powder of Artemisia annua branches and leaves, soak it with 8 ~ 10 times of No. 120 solvent gasoline for 3 times, obtain the solvent gasoline extract, concentrate it under reduced pressure and place it for crystallization to obtain the crude artemisinin, wash it with a small amount of No. 120 solvent gasoline for many times, and crystallize it with 50% ethanol alcohol for 2 ~ 3 times, and finally obtain the white needle crystal of artemisinin. This method has simple process steps and is easy to be used in mass artemisinin powder.

Artemisinin synthesis method:

Solvent extraction and recrystallization method generally adopts solvent gasoline method, ethanol method and alkali water extraction and acid precipitation method for production. This method significantly increases the effective utilization rate of artemisinin plants.Solvent extraction and recrystallization method generally adopts solvent gasoline method, ethanol method and alkali water extraction and acid precipitation method for production. This method significantly increases the effective utilization rate of artemisinin plants.
Different extraction processes have obvious differences in raw material consumption, operation cost and product purity. The gasoline process features high artemisinin extraction efficiency but has potential safety risks due to flammable solvent. The ethanol method is safer and environmentally friendly, yet accompanied by more impurities. The alkali water extraction and acid precipitation technique reduces organic solvent dosage, while the product needs further refining. Comprehensive comparison indicates that combining ethanol extraction with ether two-phase separation can balance safety, extraction yield and production economy, suitable for scaled preliminary separation of artemisinin and artemisinic acid.



When it comes to artemisinin, people first think of its anti malaria function. Who believes that artemisinin is the best drug for the treatment of malaria resistance, and the combination therapy based on artemisinin is also the most effective and important means for the treatment of malaria. But in recent years, with the deepening of research, more and more other effects of artemisinin have been discovered and applied, such as the treatment of pulmonary hypertension, anti diabetes, embryotoxicity, antifungal, immune regulation and so on.

Immune regulation:
It has been found that the dosage of artemisinin and its derivatives can better inhibit T lymphocyte mitogen and induce the proliferation of spleen lymphocytes in mice without causing cytotoxicity. This finding has a good reference value for the treatment of autoimmune diseases mediated by T lymphocytes. Artemisia glass vinegar has the effect of enhancing non-specific immunity, and can improve the total complement activity of mouse serum.
Dihydroartemisinin can directly inhibit the proliferation of B lymphocytes, thus reducing the secretion of autoantibodies by B lymphocytes, reducing humoral immune response, having a certain inhibitory effect on humoral immunity and reducing the formation of immune complexes. It alleviates immune-mediated tissue injury and provides theoretical basis for treating autoimmune inflammatory disorders.


Antifungal:
The antifungal effect of artemisinin also makes artemisinin show certain antibacterial activity. The research confirmed that the residue powder and water decoction of artemisinin have strong bacteriostatic effects on anthrax bacillus, Staphylococcus epidermidis, Catacoccus and Diphtheria Bacillus, and also have certain bacteriostatic effects on tuberculosis bacillus, Pseudomonas aeruginosa, Staphylococcus aureus and dysentery bacillus.
Pseudomonas aeruginosa, Staphylococcus aureus and dysentery bacillus. Its bacteriostatic mechanism is associated with interfering with bacterial membrane lipid homeostasis and blocking energy metabolism pathways, which differs from conventional quinolone antibiotics, offering potential for developing novel anti-infective agents against multidrug-resistant strains.Further exploration is required for its in vivo pharmacodynamic characteristics.

When it comes to artemisinin powder, people first think of its anti malaria function. WHO believes that artemisinin is the most effective drug for treating drug-resistant malaria, and combination therapy with artemisinin based drugs is currently the most effective and important means of treating malaria. But in recent years, with the deepening of research, other effects of artemisinin have been more and more discovered and applied, such as anti-tumor, treatment of pulmonary hypertension, anti diabetes, embryotoxicity, antifungal, immune regulation, etc.

Anti malaria
Malaria (commonly known as pendulum cold fever) is a vector borne infectious disease, which is caused by the bite of malaria parasites on the human body. After multiple episodes over a long period of time, it can lead to liver and spleen enlargement, accompanied by symptoms such as anemia. Malaria can be treated to a certain extent, and artemisinin plays an indispensable role. The peroxide bond in the structure of artemisinin is oxidative and is an essential functional group for antimalarial treatment.
The mechanism of action is that artemisinin produces free radicals in the body that bind to malaria parasite proteins, altering the cell membrane structure of the malaria parasite. After binding with malaria parasite protein, free radicals will cause the double layered membrane of mitochondria to swell and eventually detach, leading to the destruction of the cell structure and function of malaria parasites. At the same time, the chromatin in the nucleus will also be affected to some extent.


On the other hand, amino acids are the basic substances that make up proteins, and after the action of artemisinin. The absorption of isoleucine by malaria parasites is reduced, leading to obstruction of protein synthesis in the parasite. Artemisia annua not only kills pathogenic protozoa, but also has anti schistosomiasis, anti Toxoplasma infection, anti Pneumocystis carinii, and anti coccidiosis effects. Clinical trials have shown that artemisinin and its derivatives have not been found to have particularly significant side effects in the treatment of malaria.
Anti tumor
Malignant tumors are the number one killer of human health, and if left untreated, they can endanger life safety. In vitro experiments showed that artemisinin at a certain dose could induce apoptosis of many cancer cells, such as liver cancer cells, breast cancer cells, cervical cancer cells, and significantly inhibit the growth of cancer cells. Research has found that artemisinin can regulate the expression of cyclins in tumor cells, enhance the action of CKIs, and lead to tumor cell cycle arrest.


Or it can lead to cell apoptosis, inhibit tumor angiogenesis, etc. to resist the occurrence and development of tumors. Artemisinin is used to treat leukemia by acting on the cell membrane of leukemia cells, increasing membrane permeability, altering osmotic pressure, and causing an increase in intracellular calcium ion concentration. This activates calpain, causing the cell membrane to swell and rupture, while accelerating the release of apoptotic substances and increasing the rate of cell apoptosis.
Treatment of pulmonary arterial hypertension
Pulmonary arterial hypertension (PAH) is a pathological and physiological state characterized by pulmonary artery remodeling and elevated pulmonary artery pressure to a certain threshold, which can be a complication or syndrome. Artemisinin is used to treat pulmonary arterial hypertension: by dilating blood vessels, it reduces pulmonary arterial pressure in PAH patients and improves symptoms. Zaiman et al. found that artemisinin has anti-inflammatory effects.


Artemisinin and its core substances have inhibitory effects on various inflammatory factors and can also inhibit the production of nitric oxide by inflammatory mediators; Artemisinin has immunomodulatory effects; Feng Yibai et al. found through experimental research that artemisinin can inhibit the proliferation of vascular endothelial cells and vascular smooth muscle cells, thereby playing an important role in the treatment of PAH.
Artemisinin powder can inhibit the activity of matrix metalloproteinases, thereby suppressing pulmonary vascular remodeling; Artemisinin can inhibit the expression of PAH related cytokines, further enhancing its anti vascular remodeling effect, ameliorating pulmonary microcirculation disorders and restraining abnormal proliferation of pulmonary artery smooth muscle cells in pathological conditions.


Immune regulation
Research has found that the dosage of artemisinin and its derivatives can effectively inhibit T lymphocyte mitogens without causing cytotoxicity, thereby inducing the proliferation of mouse spleen lymphocytes. This discovery has great reference value for the treatment of autoimmune diseases mediated by T lymphocytes. Artemisinin has the effect of enhancing non-specific immunity and can increase the total complement activity in mouse serum.
Dihydroartemisinin can directly inhibit the proliferation of B lymphocytes, thereby reducing their secretion of autoantibodies and alleviating humoral immune responses. It exerts obvious inhibitory effects on humoral immunity and hinders the formation of immune complexes, which helps relieve inflammatory damage mediated by autoimmune reactions and provides new ideas for the intervention of autoimmune diseases.


Antifungal activity
The antifungal effect of artemisinin also makes artemisinin exhibit certain antibacterial activity. Research has confirmed that artemisinin residue powder and water decoction have strong antibacterial effects on Bacillus anthracis, Staphylococcus epidermidis, Staphylococcus aureus, and Corynebacterium diphtheriae, as well as on Mycobacterium tuberculosis, Pseudomonas aeruginosa, Staphylococcus aureus, Shigella, and other bacteria.
Its endoperoxide bridge structure serves as the core functional group to disrupt bacterial redox equilibrium, triggering oxidative damage to cytoplasmic components. Unlike common bactericides targeting cell wall synthesis, it presents unique action characteristics. Such properties lay a foundation for exploiting crude Artemisia annua byproducts to develop low-cost natural anti-microbial preparations against drug-resistant pathogens.


Treatment of polycystic ovary syndrome
On June 13, 2024, Professor Tang Qiqun's team from Zhongshan Hospital affiliated with Fudan University, in collaboration with the team from Fudan School of Basic Medicine, published a research paper online in the journal Science. They found that artemisinin derivatives can treat polycystic ovary syndrome and elucidate the relevant mechanisms, providing new ideas for the clinical treatment of PCOS and androgen related diseases.
Anti diabetes
On December 1, 2016, a study in Cell magazine showed that artemisinin may also save diabetes patients. Scientists from institutions such as the CeMM Molecular Medicine Research Center of the Austrian Academy of Sciences have discovered that artemisinin can transform alpha cells that produce glucagon into beta cells that produce insulin. Artemisinin binds to a protein called gephyrin.


Gephyrin can activate the main switch of cellular signaling - GABA receptors. Subsequently, countless biochemical reactions underwent changes, leading to the production of insulin. Another study showed that injecting GABA in a mouse model can also lead to the transformation of alpha cells into beta cells, indicating that both substances target the same mechanism, but the long-term effects of artemisinin need further testing.
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