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Artemisinin is a herbaceous plant of Artemisia genus in Compositae. Its growth height is within 50-150 cm. When the whole plant grows up, it will produce strong volatile odor. Artemisinin grows in many areas, especially in the wilderness, hillside and roadside of southern areas such as Yunnan and Guangxi. It is a very cheap and effective plant for anti-malaria drugs. Artemisia annua has a common appearance, but contains very peculiar ingredients. Artemisinin is the most effective antimalarial drug after ethylpyrimidine, chloroquine and primaquine, especially for cerebral malaria and chloroquine-resistant malaria, which has the characteristics of quick-acting and low-toxicity. It is called "the only effective malaria treatment drug in the world" by the World Health Organization.
Pharmacological effects of artemisinin
Unlike other antimalarial drugs, the main function of artemisinin in antimalarial mechanism is to interfere with the function of surface membrane mitochondria of Plasmodium. First, artemisinin acts on food vesicle, surface membrane and mitochondria, and secondly on nuclear membrane and endoplasmic reticulum. It also affects the chromatin in the nucleus to a certain extent, and ultimately leads to the whole tile of the structure of the parasite.
Specific pharmacological action is divided into two steps: the first step is activation, artemisinin is catalyzed by iron in the body of Plasmodium, the peroxide bridge in its structure is cracked to produce free radicals; the second step is alkylation, the free radicals produced in the first step are complexed with the Plasmodium protein, forming covalent bonds, so that the Plasmodium protein loses its function and dies.
Extracting method of artemisinin:
Artemisinin is extracted from Artemisia plants. When extracting, it is mainly based on the principle of extraction. There are two methods to be used frequently. The first method is ether extraction, and the second method is solvent gasoline extraction. Volatile oil is extracted by steam distillation and separated by vacuum distillation； while non-volatile components are extracted by organic solvent.
There are three main anti-malaria mechanisms of artemisinin:
Antimalarial effects of free radicals: Artemisinin produces free radicals after activation in vivo, and then oxidative free radicals interact with Plasmodium protein to form covalent bonds, which make the protein lose its function and lead to the death of plasmodium.
Direct killing effect of artemisinin on erythrocyte stage malaria: Artemisinin selectively kills erythrocyte stage malaria by affecting the function of surface mitochondria and blocking the nutrition provided by host red blood cells, so as to achieve the purpose of anti-malaria. At the same time, artemisinin has a killing effect on the gametophyte of Plasmodium.
Antimalarial effect of inhibiting PfATP6: It has been speculated that artemisinin and its derivatives have strong and specific inhibitory effect on PfATP6. Artemisinin inhibits PfATP6, increases the concentration of calcium ions in Plasmodium cytoplasm and induces apoptosis, thus playing an anti-malaria role.
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