Autofluorescent antimalarials by hybridization of artemisinin and coumarin: in vitro / in vivo studies and live-cell imaging.
Autor: | Herrmann L; Organic Chemistry Chair I and Interdisciplinary Center for Molecular Materials (ICMM), Friedrich-Alexander-Universität Erlangen-Nürnberg Nikolaus-Fiebiger-Straße 10 91054 Erlangen Germany svetlana.tsogoeva@fau.de., Leidenberger M; Institute of Medical Biotechnology, Friedrich-Alexander-Universität Erlangen-Nürnberg Paul-Gordon-Straße 3 91052 Erlangen Germany barbara.kappes@fau.de., Sacramento de Morais A; Instituto Gonçalo Moniz Fundação Oswaldo Cruz Salvador 40296-710 Brazil diogo.magalhaes@fiocruz.br., Mai C; Organic Chemistry Chair I and Interdisciplinary Center for Molecular Materials (ICMM), Friedrich-Alexander-Universität Erlangen-Nürnberg Nikolaus-Fiebiger-Straße 10 91054 Erlangen Germany svetlana.tsogoeva@fau.de., Çapci A; Organic Chemistry Chair I and Interdisciplinary Center for Molecular Materials (ICMM), Friedrich-Alexander-Universität Erlangen-Nürnberg Nikolaus-Fiebiger-Straße 10 91054 Erlangen Germany svetlana.tsogoeva@fau.de., da Cruz Borges Silva M; Instituto Gonçalo Moniz Fundação Oswaldo Cruz Salvador 40296-710 Brazil diogo.magalhaes@fiocruz.br., Plass F; Leibniz Institute of Surface Engineering (IOM) Permoserstrasse 15 04318 Leipzig Germany.; Physical Chemistry Chair I, Friedrich-Alexander-Universität Erlangen-Nürnberg Egerlandstrasse 3 91058 Erlangen Germany., Kahnt A; Leibniz Institute of Surface Engineering (IOM) Permoserstrasse 15 04318 Leipzig Germany.; Physical Chemistry Chair I, Friedrich-Alexander-Universität Erlangen-Nürnberg Egerlandstrasse 3 91058 Erlangen Germany., Moreira DRM; Instituto Gonçalo Moniz Fundação Oswaldo Cruz Salvador 40296-710 Brazil diogo.magalhaes@fiocruz.br., Kappes B; Institute of Medical Biotechnology, Friedrich-Alexander-Universität Erlangen-Nürnberg Paul-Gordon-Straße 3 91052 Erlangen Germany barbara.kappes@fau.de., Tsogoeva SB; Organic Chemistry Chair I and Interdisciplinary Center for Molecular Materials (ICMM), Friedrich-Alexander-Universität Erlangen-Nürnberg Nikolaus-Fiebiger-Straße 10 91054 Erlangen Germany svetlana.tsogoeva@fau.de. |
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Jazyk: | angličtina |
Zdroj: | Chemical science [Chem Sci] 2023 Oct 24; Vol. 14 (45), pp. 12941-12952. Date of Electronic Publication: 2023 Oct 24 (Print Publication: 2023). |
DOI: | 10.1039/d3sc03661h |
Abstrakt: | Malaria is one of our planet's most widespread and deadliest diseases, and there is an ever-consistent need for new and improved pharmaceuticals. Natural products have been an essential source of hit and lead compounds for drug discovery. Antimalarial drug artemisinin (ART), a highly effective natural product, is an enantiopure sesquiterpene lactone and occurs in Artemisia annua L. The development of improved antimalarial drugs, which are highly potent and at the same time inherently fluorescent is particularly favorable and highly desirable since they can be used for live-cell imaging, avoiding the requirement of the drug's linkage to an external fluorescent label. Herein, we present the first antimalarial autofluorescent artemisinin-coumarin hybrids with high fluorescence quantum yields of up to 0.94 and exhibiting excellent activity in vitro against CQ-resistant and multidrug-resistant P. falciparum strains (IC Competing Interests: There are no conflicts to declare. (This journal is © The Royal Society of Chemistry.) |
Databáze: | MEDLINE |
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