Is artemether and artemisinin derivative?
The artemisinin derivatives comprise the parent compound artemisinin, dihydroartemisinin (which is 5–10 times more potent) and the dihydroartemisinin derivatives artemether, artemotil (arteether) and artesunate.
What is artemether made from?
Artemether is a semisynthetic derivative of artemisinin, a naturally occurring sesquiterpene lactone obtained from the Chinese herb Artemisia annua (qing hao) [6].
What is the mechanism of action of artemisinin derivatives?
Artemisinin is believed to act via a two-step mechanism. Artemisinin is first activated by intraparasitic heme-iron which catalyzes the cleavage of this endoperoxide. A resulting free radical intermediate may then kill the parasite by alkylating and poisoning one or more essential malarial protein(s).
What is the difference between artesunate and artemisinin?
Artesunate is an artemisinin derivative. Artemisinin is extracted from the plant Artemisia annua. Artemisinin and its derivatives have been the most useful drug for malarial treatment in human history. The artesunate has an advantage of a hydrophilic group over other artemisinins which makes it a more potent drug.
Which of the following are artemisinin derivatives used in malaria?
For uncomplicated malaria in travellers, combination therapy based on artemisinin derivatives is one option, along with atovaquone + proguanil, quinine (less convenient) and mefloquine (frequent neuropsychological effects).
What is the difference between artemisinin and artesunate?
Is artemether derived from plants?
Artemisinin, from which the artemether component of Coartem®(artemether/lumefantrine, AL) is derived, is obtained from the plant sweet wormwood (Artemisia annua) which has been used for over 2,000 years as a Chinese herbal remedy.
What is the structure of artemether?
C16H26O5Artemether / Formula
How does artemisinin based combination therapies ACTs treat malaria?
Artemisinin-based combination therapies (ACTs) are the first-line therapy in almost all countries where malaria is endemic due to the high efficacy, tolerability, and ability of ACTs to reduce ongoing transmission of the parasite. ACTs are comprised of two components: an artemisinin derivative and a partner drug.
How is artemisinin manufactured?
Artemisinin is naturally produced in trichomes of leaves. At the same time, transgenic hairy roots are considered a good source to harvest artemisinin. However, the absence of trichomes in hairy roots suggests that artemisinin biosynthesis is not limited to trichomes.
What is chemical formula of artemisinin?
C15H22O5Artemisinin / Formula
Can artemisinin be synthesized?
Although total synthesis of artemisinin is difficult and costly, the semi-synthesis of artemisinin or any deriv. from microbially sourced artemisinic acid, its immediate precursor, could be a cost-effective, environmentally friendly, high-quality and reliable source of artemisinin.
What is the mechanism of action of artemether lumefantrine?
Lumefantrine binds to hemin produced during hemoglobin breakdown, preventing detoxification to crystalline malaria pigment (hemozoin). During the same process, the perOXide group in artemether binds to heme and releases toxic free-radicals.
How effective is artemisinin based combination therapies?
Artemisinin-based combination treatments (ACTs) are now generally accepted as the best treatments for uncomplicated falciparum malaria. They are rapidly and reliably effective.
Why is artemisinin synthesized?
Artemisinin is an endoperoxidized sesquiterpene from the Chinese medicinal plant Artemisia annua, used as an effective anti-malarial drug. Its biosynthesis pathway has been investigated for many years for scientific interest and for potential manufacturing applications to fulfill the market demand.
Where is artemisinin manufactured?
They contain derivatives of artemisinin, a molecule found in the plant sweet wormwood (Artemisia annua) that is grown mostly in China and Vietnam.
What are the active ingredients in artemisinin-based drugs?
The active pharmaceutical ingredients of the artemisinin-based drugs are ethers, such as artesunate or artemether, obtained via reduction of artemisinin into dihydroartemisinin (DHA) using sodium borohydride in methanol or ethanol as solvents, followed by etherification to the final APIs, see Fig. 1 [4], [5].
Is there a catalyst for etherification of dihydroartemisinin?
Derivatization of an important bio-pharmaceutical molecule artemisinin into its final API artemether was demonstrated as a sequence of two reactions under flow conditions for the first time. A highly effective catalyst for etherification of dihydroartemisinin, QuadraSil, was found.
How do you make artesunate from Artemisinin?
Artemisinin was extracted with dichloromethane and purified on the basis of variations in polarity and in the hydrophile/lipophile balance of solvents. Transformation into artesunate was a two-step process involving reduction to dihydroartemisinin using diisobutylaluminium hydride (DIBAL) followed by esterification using succinic anhydride.
Can artemether be derived from a bio-pharmaceutical molecule?
Derivatization of an important bio-pharmaceutical molecule artemisinin into its final API artemether was demonstrated as a sequence of two reactions under flow conditions for the first time. A highly effective catalyst for etherification of dihydroartemisinin, QuadraSil, was found. Close to quantitative yield of the product artemether was obtained.