CAS： 88495-63-0
MF： C19H28O8
Appearance： white crystalline powder
| Description | Also known as dihydroartemisinin-12-α-succinate, Artesunate is a semi-synthetic peroxide-bridged sesquiterpene lactone. ART is derived from artemisinin, the active compound in Artemisia annua. Hebei KuiSheng Trading Co., LTD ，a company specializing in the production and supply of chemicals for various industries. we take pride in our ability to carefully formulate chemicals that meet the highest standards of quality, efficiency, and safety. Through advanced technology and strict quality control measures, we ensure that our products consistently deliver exceptional performance and reliability. Whether you are in need of chemicals for pharmaceutical, agricultural, or industrial applications, we offer a wide range of solutions to meet your specific requirements. Our team is dedicated to providing excellent customer service and we strongly believe in establishing long-lasting business relationships built on trust and mutual success. |
| Mechanism of Action | Artesunate acts by targeting Plasmodium schizonts in the erythrocytic stage, inhibiting cytochrome oxidase and disrupting nutrient supply. It inhibits TNF-induced proinflammatory cytokine production through the NF-κB and PI3 kinase/Akt pathways. |
| Pharmacokinetics | ART is widely distributed in the body, with high concentrations in the intestine, liver, and kidney. Primarily undergoes metabolic conversion; has a half-life (T1/2) of around 30 minutes after intravenous injection. |
| Dosage and Administration | Intravenous: 60 mg powder dissolved in sodium bicarbonate injection and diluted in glucose for infusion. Standard regimen involves 300 mg over four days for chloroquine-resistant malaria. Oral: Typical treatment involves a 3-5 day course, achieving low toxicity and high patient tolerance. |
| Side Effects and Precautions | Minimal side effects at therapeutic doses; high doses may cause temporary peripheral reticulocyte reduction. Not recommended for use within the first two months of pregnancy due to potential teratogenicity. |
InChI:InChI=1/C19H28O8/c1-10-4-5-13-11(2)15(16(22)23-9-7-14(20)21)24-17-19(13)12(10)6-8-18(3,25-17)26-27-19/h10-13,15,17H,4-9H2,1-3H3,(H,20,21)/t10-,11-,12+,13+,15-,17-,18-,19?/m1/s1
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A yeast strain with a defective mitosis regulating BUB3 gene showed increased Artesunate sensitivity and another strain with a defective proliferation-regulating CLN2 gene showed increased Artesunate resistance over the wild-type strain, wt644. None of the other DNA repair or DNA check-point deficient isogenic strains were different from the wild-type. These results and the known low toxicity of ART are clues that ART may be a promising novel candidate for cancer chemotherapy.
The endoperoxide moiety of artesunate generates ROS which helps during its mechanism of action. Other mechanisms include inducing apoptosis and cell cycle arrest and inhibiting tumour angiogenesis. There is a sequence of events that lead to the fatal damage of the parasite when exposed to artesunate. Iron-induced reduction inside the malaria parasite activates the endoperoxide linkage, which in turn triggers the release of several reactive intermediates.
