Artemisinin Mechanism of Action
The Artemisinin mechanism of action is discussed below:
- Active form: Artemisinin acts as a prodrug, and the actual active form of the compound is dihydroartemisinin.
- Activation: It reacts with iron ions, primarily heme group which is released during the breakdown of hemoglobin by the parasite.
- Forms of free radicals: Upon activation, it generates free radicals or reactive oxygen species (ROS) through the cleavage of endoperoxide bridge.
- Clearance of the parasite: Free radicals thus generated damage parasitic proteins and cell membranes which leads to oxidative stress followed by rapid removal of the parasite from the bloodstream.
- Inhibition of Calcium ATPase: Artemisinin inhibits calcium ATPase of the pathogen, PfATP6, which plays a crucial role in calcium homeostasis and cellular signaling
- Broad spectrum activity: Artemisinin targets multiple stages in the lifecycle of the malarial parasite including asexual blood stages and also the dormant forms in the liver (hypnozoites).
- ACTs enhance efficacy and reduce drug resistance by the pathogen.
- While artemisinin’s endoperoxide is most active in intra-erythrocytic stages, some clinical observations have shown its efficacy across all stages of the parasite.
Uses of Artemisinin – Structure and Mode of Action
Artemisinin is a bioactive compound obtained from the leaves of a sweet wormwood plant known as Artemisia annua. It is a sesquiterpene endoperoxidase. Understanding Artemisinin uses and Artemisinin structure is crucial for appreciating its role in medicine.
In this article, we will cover Artemisinin mechanism of action, derivatives, and biological sources along with Artemisinin Combination Therapy in detail.
Table of Content
- What is Artemisinin?
- Chemical Nature of Artemisinin
- Structure of Artemisinin
- Derivatives of Artemisinin
- Isolation and Extraction of Artemisinin
- (a) Extraction
- (b) Isolation & purification
- Uses of Artemisinin
- Artemisinin Mechanism of Action
- Challenges and Concerns Related to Artemisinin
- Artemisinin Combination Therapy (ACT)