Special Issue "Artemisinin: Against Malaria, Cancer and Viruses"
Deadline for manuscript submissions: closed (30 November 2017)
Prof. Dr. Svetlana B. Tsogoeva
Organic Chemistry Chair I and Interdisciplinary Center for Molecular Materials (ICMM), Friedrich-Alexander University of Erlangen-Nürnberg Nikolaus Fiebiger-Straße 10, 91054 Erlangen, Germany
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Interests: organocatalysis; domino reactions; one-pot processes; medicinal chemistry; design and synthesis of antiviral; anticancer and antimalarial agents
The natural 1,2,4 trioxane sesquiterpene artemisinin, isolated from the Chinese medicinal plant Artemisia annua L. (sweet wormwood) in 1972 by Youyou Tu (Nobel Prize, 2015), has proven to be a versatile antimalarial. In order to improve the pharmacological properties of artemisinin, several semisynthetic derivatives were developed: dihydroartemisinin, artesunic acid, and artemether. All three artemisinin derivatives proved to be highly active against malaria parasites and different cancer cell lines and also against viruses. In addition to the high safety of artemisinin and its derivatives, a high therapeutic tolerance, effectivity and a unique mode of action can be mentioned as the advantages of these compounds. Although the mechanism of action of artemisinin is still not completely understood, it is generally accepted that the endoperoxide linkage within the 1,2,4 trioxane system is essential for its activities. Generation of reactive oxygen species (ROS) and carbon-centered radicals are widely accepted as key intermediates responsible for the antimalarial and anticancer activities of artemisinin and its derivatives. In case of malaria, a disruption of the cellular redox cycling, an inhibition of a calcium-ATPase (SERCA, pFATP6), as well as a depolarization of the mitochondrial potential is discussed further. The advantage of artemisinin and its semi-synthetic analogue artesunic acid as anticancer agents lies not only in their potency as toxic agents to cancer cells, but also in their low toxicity to normal cells.
Over the past decade, a great deal of attention has been paid to the synthesis of new artemisinin derivatives and of a wide variety of atemisinin-derived dimers and hybrids as lead compounds of interest. These new molecular structures demonstrate improved properties compared to their parent compounds (e.g., circumventing multidrug resistance and low bioavailability), making the dimerization/hybridisation concept highly compelling for development of efficient antimalarial, anticancer and antiviral drugs.
The present Special Issue intends to highlight the past and present role of artemisinin and different types of artemisinin-derived compounds for the development of new efficient therapeutics for the treatment of malaria, cancer, and viruses and will consider the future prospects of artemisinin for drug discovery.
Prof. Dr. Svetlana B. Tsogoeva
Manuscript Submission Information
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- medicinal chemistry
- artemisinin’s mode of action
- artemisinin-derived hybrids/dimers