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10.1080/14756366.2021.1886093

http://scihub22266oqcxt.onion/10.1080/14756366.2021.1886093
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suck abstract from ncbi


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pmid33641565      J+Enzyme+Inhib+Med+Chem 2021 ; 36 (1): 659-668
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  • Exposure of human intestinal epithelial cells and primary human hepatocytes to trypsin-like serine protease inhibitors with potential antiviral effect #MMPMID33641565
  • Paszti-Gere E; Pomothy J; Jerzsele A; Pilgram O; Steinmetzer T
  • J Enzyme Inhib Med Chem 2021[Dec]; 36 (1): 659-668 PMID33641565show ga
  • Human intestinal epithelial cell line-6 (HIEC-6) cells and primary human hepatocytes (PHHs) were treated with 3-amidinophenylalanine-derived inhibitors of trypsin-like serine proteases for 24 hours. It was proven that treatment with MI-1900 and MI-1907 was tolerated up to 50 muM in HIEC-6. These inhibitors did not cause elevations in extracellular H(2)O(2) levels and in the concentrations of interleukin (IL)-6 and IL-8 and did not alter occludin distribution in HIEC-6. It was also found that MI-1900 and MI-1907 up to 50 muM did not affect cell viability, IL-6 and IL-8 and occludin levels of PHH. Based on our findings, these inhibitors could be safely applicable at 50 muM in HIEC-6 and in PHH; however, redox status was disturbed in case of PHH. Moreover, it has recently been demonstrated that MI-1900 prevents the replication and spread of the new SARS-CoV-2 in infected Calu-3 cells, most-likely via an inhibition of the membrane-bound host protease TMPRSS2.
  • |Antiviral Agents/*pharmacology[MESH]
  • |Cell Line[MESH]
  • |Cell Survival/drug effects[MESH]
  • |Epithelial Cells/cytology/*drug effects/enzymology[MESH]
  • |Gene Expression Regulation/drug effects[MESH]
  • |Hepatocytes/cytology/*drug effects/enzymology[MESH]
  • |Humans[MESH]
  • |Hydrogen Peroxide/metabolism[MESH]
  • |Interleukin-6/genetics/metabolism[MESH]
  • |Interleukin-8/genetics/metabolism[MESH]
  • |Intestinal Mucosa/cytology/drug effects/enzymology[MESH]
  • |Occludin/genetics/metabolism[MESH]
  • |Oxidation-Reduction/drug effects[MESH]
  • |Phenylalanine/analogs & derivatives/*pharmacology[MESH]
  • |Primary Cell Culture[MESH]
  • |Protease Inhibitors/*pharmacology[MESH]


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