How Effective Is Artemisinin for Malaria?

Artemisinin is a colorless needle-like crystal with peroxy group sesquiterpene lactones extracted from the stems and leaves of the inflorescence plant Artemisia annua. I discovered it in 1971 ^[1] . Artemisinin is the most effective antimalarial drug after pyrimidine, chloroquine, and primary quine, especially for cerebral malaria and anti-chloroquine malaria. It has fast-acting and low-toxicity characteristics and was once called by the World Health Organization as " The only effective malaria treatment in the world. "

Artemisinin is a colorless needle-like crystal with the chemical name (3R, 5aS, 6R, 8aS, 9R, 12S, 12aR) -octahydro-3,6,9-trimethyl-3,12-bridged oxygen -12H-pyran [4,3-j] -1,2-benzobisepine-10 (3H) -one. The molecular formula is C ₁₅ H ₂₂ O ₅ , which belongs to sesquiterpene lactones. It has a peroxy bond and a 6-lactone ring. It is very rare, and the molecule includes 7 chiral centers. Its biogenic relationship belongs to the amorphane type, which is characterized by the cyclic coupling of A and B rings, and the isopropyl group has a trans relationship with the bridgehead hydrogen.

The melting point was 156-157 ° C, [a] _D17 = + 66.3 ° (C = 1.64 chloroform).

The characteristic absorption peak of artemisinin in the infrared spectrum is a six-membered ring lactone at 1740 cm-1 and a peroxy bond at 881, 995, and 1115 cm-1. No carbon-carbon double bonds. Artemisinin

Unlike previous antimalarial drugs, the main role of artemisinin's antimalarial mechanism is to interfere with the functions of the plasmodium membrane mitochondria, etc., first acting on the food bubble membrane, surface membrane, mitochondria, and secondly on the nuclear membrane, internal Plasma reticulum also has a certain effect on the chromatin in the nucleus, eventually leading to the complete disintegration of the worm body structure, instead of interfering with the folic acid metabolism of the Plasmodium. Its mechanism of action may also mainly interfere with the function of the epithelial mitochondria, act on the food bubble membrane, block the earliest stage of nutrient intake, make the Plasmodium swiftly appear amino acid starvation, thereby forming autophagic vesicles and continuously excreting them , Plasmodium eventually lost a large amount of cytoplasm and died. The specific pharmacological action is divided into two steps: the first step is activation, artemisinin is catalyzed by iron in the body of plasmodium, and the peroxy bridge in its structure is cleaved to generate free radicals; the second step is alkylation, which is produced by the first step Free radicals are complexed with the Plasmodium protein, forming a covalent bond, causing the Plasmodium protein to lose its function and die ^[44]

Artemisinin-based combination therapy has become the standard antimalarial treatment recommended by the World Health Organization. The World Health Organization believes that artemisinin combination therapy is the most effective way to treat malaria, and it is also the drug that has the best resistance to malaria resistance. China, as the discoverer and the largest producer of antimalarial drug artemisinin, Played an important role in the fight against malaria. Artemisinin has saved millions of lives, especially in Africa, the hardest hit area of malaria. According to WHO statistics, since 2000, approximately 240 million people in sub-Saharan Africa have benefited from artemisinin combination therapy, which has prevented about 1.5 million deaths from malaria. In Benin, West Africa, the local people have called this Chinese medicine, which has obvious curative effect and low price, used by the Chinese medical team as "the magic drug from the far east".

In addition, berberine has shown attractive prospects in the treatment of other diseases. Such as anti-schistosomiasis, regulating or inhibiting the humoral immune function, increasing the lymphocyte conversion rate, choleretic, expectorant, antitussive, antiasthmatic and so on. Has developed second-generation replacement products and new drugs derived from berberine for the treatment of tumors, melanoma, lupus erythematosus and other diseases. At the same time, it has begun to explore berberine for the treatment of AIDS, malignant tumors, Leishmania, schistosomiasis, polyesterworm, toxoplasma And other diseases and new uses for detoxification.

Control

1. Mild nausea, vomiting, and diarrhea, etc., can quickly return to normal without treatment.

2. When the injection site is shallow, it can easily cause local pain and lumps.

3. Individual patients may have transient elevated aminotransferases and mild rashes.

1. This medicine is for the treatment of malaria and is not used as a preventive medicine.

2. If the injection site is shallow, it may cause local pain and induration.

3. When used for the treatment of systemic lupus erythematosus and discoid lupus erythematosus, the condition may be aggravated in the early stage of treatment (a ant-walking sensation occurs throughout the body), and gradually decreases after half a month, and generally improves after about one month.

4. When suppositories are used, such as defecation within 2 hours after anal plugging, it should be replenished once ^[58] .