Scientists at have actually established a groundbreaking autofluorescent compound by combining artemisinin and coumarin, 2 plant-derived substances. This development enables for exact imaging in live cells and has actually proven reliable versus drug-resistant malaria pathogens, especially plasmodium falciparum. The advancement of these autofluorescent hybrids, which can be observed without altering their efficiency, represents a substantial action forward in combating drug-resistant malaria.
This autofluorescence is particularly useful as it can be used for imaging in live cells and reveals how the medication works in an accurate time series.
Artemisinin is a highly-effective and common ingredient for the manufacture of malaria medication got from a plant called sweet wormwood (Artemisia annua L.). Coumarin is a secondary plant substance found in different plants.
In the development of drugs versus malaria, active compounds are labeled with fluorescent substances in order to determine how they act against malaria pathogens in accurate sequential order using imaging methods. This fluorescent labeling has already been utilized with artemisinin.
Combining compounds to accomplish autofluorescence
A considerable downside of labeling with fluorescent substances is the reality that they alter how the medication works. For example, this indicates that in particular situations cells infected with malaria soak up a drug like artemisinin in a different way after fluorescent marking than previously.
The solubility of the drug can also alter. This was avoided by the development of autofluorescent hybrids, which are substances made of 2 or more fundamental substances that are naturally fluorescent and whose mode of action can be precisely observed utilizing imaging strategies.
Active agent with unique abilities
The group led by Prof. Tsogoeva at the Chair of Organic Chemistry chose to combine artemisinin with bioactive coumarins because coumarin derivatives likewise possess anti-malaria properties. They can also be easily chemically changed so that they end up being very fluorescent.
The scientists found that it was not just possible to observe the mode of action of this very first autofluorescent artemisinin-coumarin hybrid in living red blood cells contaminated with P. falciparum.
In combination with Prof. Barbara Kappes (Department of Chemical and Biological Engineering, FAU) and Dr. Diogo R. M. Moreira (Instituto Gonçalo Moniz, Fiocruz Bahia, Brazil), they likewise discovered that the active agent was highly effective versus P. falciparum strains in vitro (in a test tube) that are resistant to chloroquin and other malaria drugs. Above all, nevertheless, the brand-new compound also proved extremely effective against the malaria pathogens in vivo in mouse designs.
With the production of the first autofluorescent artemisinin-coumarin hybrid, the FAU researchers hope that they have laid the structure for the development of more autofluorescent agents for treating malaria and have actually made significant process in getting rid of multi-drug resistance in the treatment of malaria.
Referral: “Autofluorescent antimalarials by hybridization of artemisinin and coumarin: in vitro/in vivo studies and live-cell imaging” by Lars Herrmann, Maria Leidenberger, Adrielle Sacramento de Morais, Christina Mai, Aysun Çapci, Mariana da Cruz Borges Silva, Fabian Plass, Axel Kahnt, Diogo R. M. Moreira, Barbara Kappes and Svetlana B. Tsogoeva, 24 October 2023, Chemical Science.DOI: 10.1039/ D3SC03661H.
Scientists at have developed a groundbreaking autofluorescent substance by integrating artemisinin and coumarin, 2 plant-derived compounds. This development permits precise imaging in live cells and has actually shown efficient against drug-resistant malaria pathogens, especially plasmodium falciparum. The development of these autofluorescent hybrids, which can be observed without changing their efficiency, represents a considerable advance in combating drug-resistant malaria.
A research group at FAU has developed drugs for treating malaria.
Malaria remains one of the most dangerous infectious illness globally. The introduction of drug-resistant malaria parasites requires the continual advancement of new medications.
A team of researchers at Friedrich-Alexander-Universität Erlangen-Nürnberg (FAU) led by Prof. Dr. Svetlana B. Tsogoeva has actually now integrated the anti-malaria drug artemisinin with coumarin, which, like artemisinin, is likewise found in plants, and developed an auto-fluorescent compound from both bioactive substances.
This autofluorescence is particularly advantageous as it can be used for imaging in live cells and reveals how the medication operates in an accurate time series. The working group also found that the autofluorescent artemisinin-coumarin hybrids have the ability to destroy a certain drug-resistant malaria pathogen called plasmodium palcifarum. They have published their findings in the journal Chemical Science.