Artemisinin's success is Chinese medicine is a major contribution to the world. Parses the artemisinin from Artemisia annua, Tu Yo Yo completed the most critical step. It is like the Tu Yo Yo said: "Artemisinin is a true gift of ancient Chinese medicine." Developed gradually caught in the face of Western medicine can not find the plight of Chinese medicine and Chinese medicine prescription specifies a valid research, but also to find new drugs a wealth of medicinal resources, can shorten the development cycle, but also can reduce the development costs.
Artemisinin development process, confirming the traditional Chinese medicine is indispensable. Antimalarial originally not from Artemisia annua, but from another plant - the cinchona tree. 19th century, the French chemist from cinchona bark ingredient isolated antimalarial quinine. Subsequently found a quinine substitute - chloroquine. Chloroquine drugs to fight malaria cure once. The subsequent emergence of drug resistance, the epidemic is difficult to control. Drug artemisinin and related derivatives birth to the world suffering from malaria-afflicted patients to bring the gospel.
Artemisinin Introduction:
CAS; 63968-64-9
Plant Origin:Artemisia annua
Appearance: white or colorless crystal
Spec.: 99%;
Plant used: leaves
Extraction Type: Solvent Extraction
Molecular Formulas:C15H22O5
Molecular Weight:282.33
Melting point:156-157°C
Pharmacology of artemisinin:
Artemisinin is extracted from Artemisia annua with peroxide groups sesquiterpene lactone drugs. Is efficient, quick, low toxicity antimalarials. On plasmodia of a strong role in the killing and fast, rapid control of clinical seizures and symptoms. The mechanism of action of artemisinin is not very clear, interference is mainly a parasite surface membrane mitochondrial function. Artemisinin by affecting the ultrastructure of plasmodia to membrane system change. Because of the role of food vacuole membrane, blocking the parasite's nutritional intake, when the parasite cytoplasm and a significant loss of nutrients, and the lack of supplement, which soon died. Its role is through its endoperoxide (dioxygen) bridge, produced by the decomposition of hemoglobin mediated by free iron, resulting in unstable organic free radicals and / or other pro-electron mediator, and then with the parasite proteins form covalent adducts, leaving the parasite death. Artemether artemisinin antimalarial activity than six times larger.
Toxicology of artemisinin
The drug has certain embryo toxicity, manifested as embryonic absorption.
Artemisinin test:
Objective:To establish HPLC-ECD chromatograpH determined Artemisinin method. Using this method measure the solubility of Artemisinin in different solvents, its oil-water distribution coefficients and low concentration biological samples. Through this data preliminary speculate the influence factors of Artemisinin bioavailability.This study may offer helpful reference for study of the preparations of Artemisinin. Method: Using the uniform experimental design method to determine a good derivative method
Extraction of artemisinin
With artemisinin raw material, the use of industrial alcohol maceration extraction of artemisinin through experiments to determine the optimum process conditions: Alcohol by volume (mL) and Artemisia annua mass (g) ratio of 10:1, 3 times extracted liquor volume (mL) of Artemisia annua mass (g) of 2.5 times the volume of extraction solvent of ethyl acetate and the mother liquor ratio of 1:1, was extracted 4 times with active carbon, crystallization and recrystallization, and dried to give white needles of the Green artemisinin crystals obtained product yield of artemisinin 2.73 ‰, a purity of 99%, this process has the safe operation, extraction rate, low production costs, product content is high.
Studies on the synthesis of artemisinin; (+) Artemisinin is a sesquiterpene endoperoxide lactone with an unprecedented structure is a natural medicine for the treatment of malaria in particular drug against drug resistant malaria and cerebral malaria. The total synthesis of this novel sesquiterpene is described using an inter-molecular radical reaction on important intermediate iodolactone starting from terpene (+) isolimonene.
Progress in other artemisinin drugs;
Dihydroartemisinin, artesunate, artemether, arteether.
Chinese artemisinin rats proved by the research group [1], rat after oral artemisinin 150mg, rapidly absorbed completely, but the plasma concentration is low, maintain a short time, showing first-pass effect. Artemisinin 150mg intravenous blood aqueous suspension schedule two compartment model, t1 / 2 was 30min, Vd is 4.1L, indicates that artemisinin is widely distributed in the body and eliminate quickly. Intramuscular injection in humans artemether oil 3.2mg, 6.0mg, 10.0mg and after the peak plasma concentration time is 4h ~ 6h, the average retention time was 10.2h, 15.6h and 19.0h, show by intramuscular artemether injection may persist longer in the body, in the body of sodium intravenous artesunate 2.0mg and 3.8mg after the blood is in accord with two-compartment model, t1 / 2 was 30min and 36min ~ 48min. to drug accumulation in urine within 7h after discharge dose of unchanged drug accounted for only 0.1% to 6.8%, indicating that the drug in the body mainly through the elimination of metabolic transformation. Artesunate reported soon after entering the body into DHA. Determination users free drug concentration in body fluids, it is difficult to dihydro-artemisinin and artesunate make a difference, the measured concentration is likely to be the sum of two kinds of substance concentration.
artemisinin drugs other pharmacological research
1, the anti-tumor effects
2, the immunomodulatory effects
3, the role of anti-schistosome
4, the anti-inflammatory effects
5, the hepatoprotective effect
6, antiarrhythmic
7, antiviral
8, the treatment effect of Toxoplasma gondii infection
9, the role of anti-dog Eperythrozoon
10. anticoccidial
11, anti-asthmatic effect
12, anti-progesterone effect
This article addresses：http://www.hnkeyuan.com/news/Industry News/Pharmacology-and-Toxicology-of-Artem.html
Next：Will Semi-Synthetic Artemisinin replace natural artemisinin for Malaria control?
Previous： Overview of Cardiovascular disease (heart disease)