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Ousingsawat, Jiraporn ; Centeio, Raquel ; Schreiber, Rainer ; Kunzelmann, Karl

Niclosamide, but not ivermectin, inhibits anoctamin 1 and 6 and attenuates inflammation of the respiratory tract

Article

Ousingsawat, Jiraporn , Centeio, Raquel, Schreiber, Rainer and Kunzelmann, Karl (2023) Niclosamide, but not ivermectin, inhibits anoctamin 1 and 6 and attenuates inflammation of the respiratory tract. Pflügers Archiv - European Journal of Physiology 476, pp. 211-227.

DOI to cite this document: 10.5283/epub.55059


Abstract

Inflammatory airway diseases like cystic fibrosis, asthma and COVID-19 are characterized by high levels of pulmonary cytokines. Two well-established antiparasitic drugs, niclosamide and ivermectin, are intensively discussed for the treatment of viral inflammatory airway infections. Here, we examined these repurposed drugs with respect to their anti-inflammatory effects in airways in vivo and in ...

Inflammatory airway diseases like cystic fibrosis, asthma and COVID-19 are characterized by high levels of pulmonary cytokines. Two well-established antiparasitic drugs, niclosamide and ivermectin, are intensively discussed for the treatment of viral inflammatory airway infections. Here, we examined these repurposed drugs with respect to their anti-inflammatory effects in airways in vivo and in vitro. Niclosamide reduced mucus content, eosinophilic infiltration and cell death in asthmatic mouse lungs in vivo and inhibited release of interleukins in the two differentiated airway epithelial cell lines CFBE and BCi-NS1.1 in vitro. Cytokine release was also inhibited by the knockdown of the Ca2+-activated Cl− channel anoctamin 1 (ANO1, TMEM16A) and the phospholipid scramblase anoctamin 6 (ANO6, TMEM16F), which have previously been shown to affect intracellular Ca2+ levels near the plasma membrane and to facilitate exocytosis. At concentrations around 200 nM, niclosamide inhibited inflammation, lowered intracellular Ca2+, acidified cytosolic pH and blocked activation of ANO1 and ANO6. It is suggested that niclosamide brings about its anti-inflammatory effects at least in part by inhibiting ANO1 and ANO6, and by lowering intracellular Ca2+ levels. In contrast to niclosamide, 1 µM ivermectin did not exert any of the effects described for niclosamide. The present data suggest niclosamide as an effective anti-inflammatory treatment in CF, asthma, and COVID-19, in addition to its previously reported antiviral effects. It has an advantageous concentration–response relationship and is known to be well tolerated.



Involved Institutions


Details

Item typeArticle
Journal or Publication TitlePflügers Archiv - European Journal of Physiology
PublisherSpringer
Open Access TypeDEAL (Springer)
Volume476
Page Rangepp. 211-227
Date18 November 2023
Date of publication22 Nov 2023 08:58
InstitutionsBiology, Preclinical Medicine > Institut für Physiologie > Prof. Dr. Karl Kunzelmann
Identification Number
ValueType
10.1007/s00424-023-02878-wDOI
KeywordsAnoctamin 1 · Anoctamin 6 · Inflammation · Asthma · Cystic fibrosis · COVID-19
Dewey Decimal Classification500 Science > 500 Natural sciences & mathematics
500 Science > 570 Life sciences
StatusPublished
RefereedYes, this version has been refereed
Created at the University of RegensburgYes
URN of the UB Regensburgurn:nbn:de:bvb:355-epub-550596
Item ID55059

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