Inhibition of in vitro Ebola infection by anti-parasitic quinoline derivatives
| العنوان: | Inhibition of in vitro Ebola infection by anti-parasitic quinoline derivatives |
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| المؤلفون: | Beth Binnington, Shawn Goyal, Philippe M. Loiseau, Laurent Ferrié, Stephen D S McCarthy, Donald R. Branch, Bruno Figadère, Didier Desmaële |
| المساهمون: | Institut Galien Paris-Saclay (IGPS), Université Paris-Saclay-Centre National de la Recherche Scientifique (CNRS), Institut de Chimie du CNRS (INC)-Université Paris-Saclay-Centre National de la Recherche Scientifique (CNRS), Department of Laboratory Medicine and Pathobiology (LMP), University of Toronto, Centre for Innovation, Canadian Blood Services, Biomolécules : Conception, Isolement, Synthèse (BioCIS), Institut de Chimie du CNRS (INC)-Université Paris-Saclay-Centre National de la Recherche Scientifique (CNRS)-CY Cergy Paris Université (CY) |
| المصدر: | F1000Research F1000Research, Faculty of 1000, 2020, 9, pp.268. ⟨10.12688/f1000research.22352.1⟩ F1000Research, Faculty of 1000, 2020, 9, ⟨10.12688/f1000research.22352.1⟩ |
| بيانات النشر: | HAL CCSD, 2020. |
| سنة النشر: | 2020 |
| مصطلحات موضوعية: | 0301 basic medicine, viruses, 030106 microbiology, Amodiaquine, [CHIM.THER]Chemical Sciences/Medicinal Chemistry, medicine.disease_cause, Virus Replication, Antiviral Agents, General Biochemistry, Genetics and Molecular Biology, Efficacy, 03 medical and health sciences, chemistry.chemical_compound, Ebola virus, Chloroquine, [SDV.MHEP.MI]Life Sciences [q-bio]/Human health and pathology/Infectious diseases, medicine, [CHIM]Chemical Sciences, MTT assay, General Pharmacology, Toxicology and Pharmaceutics, ComputingMilieux_MISCELLANEOUS, General Immunology and Microbiology, business.industry, [CHIM.ORGA]Chemical Sciences/Organic chemistry, Brief Report, Quinoline, General Medicine, Articles, Ebolavirus, Virology, In vitro, 3. Good health, antiparasitic drugs, 030104 developmental biology, chemistry, Toxicity, [SDV.MP.VIR]Life Sciences [q-bio]/Microbiology and Parasitology/Virology, [SDV.SP.PHARMA]Life Sciences [q-bio]/Pharmaceutical sciences/Pharmacology, Quinolines, antiviral activity, business, medicine.drug |
| الوصف: | There continues to be no approved drugs for the treatment of Ebola virus disease (EVD). Despite a number of candidate drugs showing limited efficacy in vitro and/or in non-human primate studies, EVD continues to plaque certain areas of Africa without any efficacious treatments yet available. Recently, we have been exploring the potential for anti-malarial drugs to inhibit an in vitro model of Ebola Zaire replication using a transcription-competent virus-like particle (trVLP) assay. We examined the efficacy of chloroquine, amodiaquine and 36 novel anti-parasite quinoline derivatives at inhibiting Ebola virus replication. Drug efficacy was tested by trVLP assay and toxicity by MTT assay. Both chloroquine and amodiaquine were effective for inhibition of Ebola virus replication without significant toxicity. The half-maximal inhibitory concentration (IC50) of chloroquine and amodiaquine to inhibit Ebola virus replication were IC50, Chl = 3.95 µM and IC50, Amo = 1.45 µM, respectively. Additionally, three novel quinoline derivatives were identified as having inhibitory activity and low toxicity for Ebola trVLP replication, with 2NH2Q being the most promising derivative, with an IC50 of 4.66 µM. Quinoline compounds offer many advantages for disease treatment in tropical climates as they are cheap to produce, easy to synthesize and chemically stable. In this report, we have demonstrated the potential of anti-parasite quinolines for further investigation for use in EVD. |
| اللغة: | English |
| تدمد: | 2046-1402 |
| الوصول الحر: | https://explore.openaire.eu/search/publication?articleId=doi_dedup___::a2f3e7f04035db5022d32525b58c0388Test https://hal.archives-ouvertes.fr/hal-03005910Test |
| حقوق: | OPEN |
| رقم الانضمام: | edsair.doi.dedup.....a2f3e7f04035db5022d32525b58c0388 |
| قاعدة البيانات: | OpenAIRE |
| تدمد: | 20461402 |
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