+86-28-82633987
Product name: Arteether
Synonym name: Artemotil; Dihydroartemisinin ethyl ether; Dihydroqinghaosu ethyl ether
Catalogue No.: BP4357
Cas No.: 75887-54-6
Formula: C17H28O5
Mol Weight: 312.406
Botanical Source:
Type of Compound:
Purity: 95%~99%
Analysis Method: HPLC-DAD or/and HPLC-ELSD
Identification Method: Mass, NMR
Packing: Brown vial or HDPE plastic bottle
Storage: Store in a well closed container, protected from air and light. Put into refrigerate or freeze for long term storage.
Whenever possible, you should prepare and use solutions on the same day. However, if you need to make up stock solutions in advance, we recommend that you store the solution as aliquots in tightly sealed vials at -20℃. Generally, these will be useable for up to two weeks.
The product could be supplied from milligrams to grams
Inquire for bulk scale.
For Reference Standard and R&D, Not for Human Use Directly.
Storage conditions：Short-term storage at 2~8℃, long-term storage at -20 ~ -80℃
46.1500
3.2931
3.2928
.0119
4.6779
10.9664
High
68.5303
5.7144
No
No
Yes
No
Yes
No
1.5
Yes
No
No
No
Arteether, as a semi-synthetic derivative of artemisinin, has attracted attention since the late 20th century for its outstanding antimalarial activity. Malaria, as a parasitic disease threatening public health worldwide, especially prevalent in tropical and subtropical regions, severely impacts the lives and health of hundreds of millions of people. The discovery and application of artemisinin and its derivatives have greatly advanced malaria treatment and become a milestone in the development of antimalarial drugs. Arteether, with its excellent efficacy and low toxicity, has become one of the important clinical antimalarial drugs.
This paper will systematically review the chemical structure and physicochemical properties of artemisia ether, plant origin and extraction methods, pharmacological activity and mechanism of action, druggability evaluation and pharmacokinetic characteristics, combined with its clinical application status and future development trends, aiming to provide researchers in the field of natural product pharmacology with comprehensive and in-depth academic reference.
The chemical name of arteate ether is arteotether, CAS number 75887-54-6, molecular formula C16H26O5, and molecular weight 312.4060. Its structure is based on the lactone framework of artemisinin, belonging to the sesquiterpene lactone compound, and characteristically contains a peroxybridal ring structure, which is the key structural basis for its antimalarial activity.
In terms of physicochemical properties, Artemisia ether has a LogP value of 3.2931, indicating moderate lipid solubility, which is beneficial for cell membrane penetration and distribution in vivo. Its topological pole surface area (TPSA) is 46.15 Ų, indicating moderate polarity and good drug permeability. The low water solubility (0.0119 mg/mL) suggests limited solubility in the aqueous phase, but this can be partially overcome through formulation technology. Arteotether has a high blood-brain barrier penetration ability, which offers potential advantages in treating cerebral malaria. Additionally, arteotether does not exhibit hERG channel inhibitory activity, reducing the risk of cardiotoxicity. The Ames test result was 1.5, indicating a low genotoxicity risk.
The parent compound of artemisia ether, artemisinin, is mainly derived from the traditional Chinese medicinal plant Artemisia annua L. The discovery of artemisinin and its derivatives benefited from systematic isolation and identification of the active components in Artemisia annusa. Artemisinin naturally contains relatively low content, typically between 0.01% and 1.5%, and optimizing extraction processes is crucial for industrial production.
Traditional extraction methods include solvent extraction, liquid-liquid extraction, and chromatographic separation. Modern processes often use supercritical fluid extraction and high-performance liquid chromatography technologies to improve purity and yield. Artesoneether, as a semi-synthetic derivative of artemisinin, is usually obtained through chemical modification of artemisinin. The specific synthetic route includes the reduction of artemisinin to produce artemether, followed by the preparation of artemether through an esterification reaction with glycolic acid esterification. This process offers high conversion efficiency and product stability, making it suitable for large-scale production.
The main pharmacological activity of artemiste ether is concentrated in its antimalarial effects. It demonstrates strong lethal activity against Plasmodium falciparum and other malaria parasite strains, especially showing significant inhibitory effects on artemisinin-sensitive and some drug-resistant strains. In vitro experiments and animal model studies have shown that artemoether can rapidly reduce the parasite load in the blood, shorten the duration of malaria attacks, and alleviate clinical symptoms.
Additionally, arteether demonstrates good synergy in antimalarial combination therapy and is often used in combination with other antimalarial drugs such as chloroquine, quinine, or chloroquine phosphate to delay the development of resistance. Research on its anti-inflammatory and immunomodulatory effects has gradually advanced, suggesting that arteether may exert comprehensive therapeutic effects through multiple targets and pathways.
The antimalarial mechanism of artemietether mainly relies on its peroxybridge ring structure interacting with iron ions inside the malaria parasite cells, generating free radicals and reactive oxygen species (ROS), which cause oxidative damage to parasite proteins and membrane lipids, ultimately leading to parasite death.
Specific molecular targets include:
In summary, artemisia ether significantly enhances antimalarial efficacy and reduces resistance risk through multi-target and multi-mechanism synergistic effects.
The druggability parameters of artemietether indicate that it has good potential for drug development. The molecular weight of 312.4060 conforms to the Lipinski rule, and the LogP value of 3.2931 is suitable for cell membrane penetration. TPSA 46.15 Ų ensures good bioavailability. Although water solubility is relatively low, it can be effectively improved through modern formulation technologies such as liposomes and nanoparticles.
Pharmacokinetic studies show that artemietether is rapidly absorbed orally or intramuscularly, with a short plasma peak concentration duration and a moderate biological half-life, making it suitable for rapid control of malaria attacks. Its high blood-brain barrier permeability gives it an advantage in treating cerebral malaria. Arteotin ether is mainly metabolized by the liver, with safe metabolites, and excretion mainly via bile and urine.
In safety evaluation, artemisinate ether showed no hERG channel inhibition and had a low risk of cardiotoxicity. Ames trial results showed a low genotoxicity risk, and long-term toxicology studies support its clinical safety.
As an antimalarial drug, artemiether has demonstrated good efficacy and safety in clinical applications in multiple countries, especially in treating complex and drug-resistant malaria. Its rapid parasite elimination ability effectively reduces malaria recurrence and mortality, making it one of the artemisinin drugs recommended by the World Health Organization.
Future research directions include:
With the continuous rise in global malaria prevention and control demands, the clinical value and market potential of artemietether will keep growing, driving the deep integration of natural product pharmacology with modern drug development.
Artesotether, as a semi-synthetic derivative of artemisinin, has become an important drug in the antimalarial field due to its unique chemical structure and excellent pharmacological activity. Its multi-target mechanism of action, good druggability, and safety provide a powerful tool for malaria treatment. In the future, combined with modern drug design and formulation technologies, artemisinoether is expected to play a greater role in malaria and related fields. Ongoing basic and clinical research will further advance the breadth and depth of its application, helping global malaria prevention and control reach new heights.
Shenshuai
Wenjing
Hedandan
