Niclosamide Is Active In Vitro against Mycetoma Pathogens
Redox-active drugs are the mainstay of parasite chemotherapy. To assess their repurposing potential for eumycetoma, we have tested a set of nitroheterocycles and peroxides in vitro against two isolates of <i>Madurella mycetomatis</i>, the main causative agent of eumycetoma in Sudan. All...
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| Format: | Article |
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MDPI AG
2021-06-01
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| Series: | Molecules |
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| Online Access: | https://www.mdpi.com/1420-3049/26/13/4005 |
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| author | Abdelhalim B. Mahmoud Shereen Abd Algaffar Wendy van de Sande Sami Khalid Marcel Kaiser Pascal Mäser |
| author_facet | Abdelhalim B. Mahmoud Shereen Abd Algaffar Wendy van de Sande Sami Khalid Marcel Kaiser Pascal Mäser |
| author_sort | Abdelhalim B. Mahmoud |
| collection | DOAJ |
| description | Redox-active drugs are the mainstay of parasite chemotherapy. To assess their repurposing potential for eumycetoma, we have tested a set of nitroheterocycles and peroxides in vitro against two isolates of <i>Madurella mycetomatis</i>, the main causative agent of eumycetoma in Sudan. All the tested compounds were inactive except for niclosamide, which had minimal inhibitory concentrations of around 1 µg/mL. Further tests with niclosamide and niclosamide ethanolamine demonstrated in vitro activity not only against <i>M. mycetomatis</i> but also against <i>Actinomadura</i> spp., causative agents of actinomycetoma, with minimal inhibitory concentrations below 1 µg/mL. The experimental compound MMV665807, a related salicylanilide without a nitro group, was as active as niclosamide, indicating that the antimycetomal action of niclosamide is independent of its redox chemistry (which is in agreement with the complete lack of activity in all other nitroheterocyclic drugs tested). Based on these results, we propose to further evaluate the salicylanilides, niclosamidein particular, as drug repurposing candidates for mycetoma. |
| first_indexed | 2024-03-10T09:54:41Z |
| format | Article |
| id | doaj.art-576251f60a804373b8fcade515219842 |
| institution | Directory Open Access Journal |
| issn | 1420-3049 |
| language | English |
| last_indexed | 2024-03-10T09:54:41Z |
| publishDate | 2021-06-01 |
| publisher | MDPI AG |
| record_format | Article |
| series | Molecules |
| spelling | doaj.art-576251f60a804373b8fcade5152198422023-11-22T02:25:14ZengMDPI AGMolecules1420-30492021-06-012613400510.3390/molecules26134005Niclosamide Is Active In Vitro against Mycetoma PathogensAbdelhalim B. Mahmoud0Shereen Abd Algaffar1Wendy van de Sande2Sami Khalid3Marcel Kaiser4Pascal Mäser5Department of Medical Parasitology and Infection Biology, Swiss Tropical and Public Health Institute, 4051 Basel, SwitzerlandFaculty of Pharmacy, University of Khartoum, Khartoum 11111, SudanErasmus Medical Center, Department of Medical Microbiology and Infectious Diseases, 3000 Rotterdam, The NetherlandsFaculty of Pharmacy, University of Science and Technology, Omdurman 14411, SudanDepartment of Medical Parasitology and Infection Biology, Swiss Tropical and Public Health Institute, 4051 Basel, SwitzerlandDepartment of Medical Parasitology and Infection Biology, Swiss Tropical and Public Health Institute, 4051 Basel, SwitzerlandRedox-active drugs are the mainstay of parasite chemotherapy. To assess their repurposing potential for eumycetoma, we have tested a set of nitroheterocycles and peroxides in vitro against two isolates of <i>Madurella mycetomatis</i>, the main causative agent of eumycetoma in Sudan. All the tested compounds were inactive except for niclosamide, which had minimal inhibitory concentrations of around 1 µg/mL. Further tests with niclosamide and niclosamide ethanolamine demonstrated in vitro activity not only against <i>M. mycetomatis</i> but also against <i>Actinomadura</i> spp., causative agents of actinomycetoma, with minimal inhibitory concentrations below 1 µg/mL. The experimental compound MMV665807, a related salicylanilide without a nitro group, was as active as niclosamide, indicating that the antimycetomal action of niclosamide is independent of its redox chemistry (which is in agreement with the complete lack of activity in all other nitroheterocyclic drugs tested). Based on these results, we propose to further evaluate the salicylanilides, niclosamidein particular, as drug repurposing candidates for mycetoma.https://www.mdpi.com/1420-3049/26/13/4005mycetoma<i>Madurella mycetomatis</i><i>Actinomadura</i>drug repurposingnitroimidazolesalicylanilide |
| spellingShingle | Abdelhalim B. Mahmoud Shereen Abd Algaffar Wendy van de Sande Sami Khalid Marcel Kaiser Pascal Mäser Niclosamide Is Active In Vitro against Mycetoma Pathogens Molecules mycetoma <i>Madurella mycetomatis</i> <i>Actinomadura</i> drug repurposing nitroimidazole salicylanilide |
| title | Niclosamide Is Active In Vitro against Mycetoma Pathogens |
| title_full | Niclosamide Is Active In Vitro against Mycetoma Pathogens |
| title_fullStr | Niclosamide Is Active In Vitro against Mycetoma Pathogens |
| title_full_unstemmed | Niclosamide Is Active In Vitro against Mycetoma Pathogens |
| title_short | Niclosamide Is Active In Vitro against Mycetoma Pathogens |
| title_sort | niclosamide is active in vitro against mycetoma pathogens |
| topic | mycetoma <i>Madurella mycetomatis</i> <i>Actinomadura</i> drug repurposing nitroimidazole salicylanilide |
| url | https://www.mdpi.com/1420-3049/26/13/4005 |
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