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The Cyanobacterial "Nutraceutical" Phycocyanobilin Inhibits Cysteine Protease Legumain.
Wilkinson, Isabel V L; Castro-Falcón, Gabriel; Roda-Serrat, Maria C; Purdy, Trevor N; Straetener, Jan; Brauny, Melanie M; Maier, Lisa; Brötz-Oesterhelt, Heike; Christensen, Lars P; Sieber, Stephan A; Hughes, Chambers C.
Afiliación
  • Wilkinson IVL; Center for Protein Assemblies (CPA), Department of Chemistry, Technical University of Munich, Ernst-Otto-Fischer-Str. 8, 85748, Garching, Germany.
  • Castro-Falcón G; Center for Marine Biotechnology and Biomedicine, Scripps Institution of Oceanography, University of California, San Diego, CA 92093, USA.
  • Roda-Serrat MC; Department of Green Technology, University of Southern Denmark, Campusvej 55, 5230, Odense M, Denmark.
  • Purdy TN; Center for Marine Biotechnology and Biomedicine, Scripps Institution of Oceanography, University of California, San Diego, CA 92093, USA.
  • Straetener J; Department of Microbial Bioactive Compounds, Interfaculty Institute of Microbiology and Infection Medicine, University of Tübingen, 72076, Tübingen, Germany.
  • Brauny MM; Cluster of Excellence EXC 2124, Controlling Microbes to Fight Infection, University of Tübingen, 72076, Tübingen, Germany.
  • Maier L; Microbiome-Host-Interaction Lab, Interfaculty Institute of Microbiology and Infection Medicine, University of Tübingen, 72076, Tübingen, Germany.
  • Brötz-Oesterhelt H; Cluster of Excellence EXC 2124, Controlling Microbes to Fight Infection, University of Tübingen, 72076, Tübingen, Germany.
  • Christensen LP; Microbiome-Host-Interaction Lab, Interfaculty Institute of Microbiology and Infection Medicine, University of Tübingen, 72076, Tübingen, Germany.
  • Sieber SA; Department of Microbial Bioactive Compounds, Interfaculty Institute of Microbiology and Infection Medicine, University of Tübingen, 72076, Tübingen, Germany.
  • Hughes CC; Cluster of Excellence EXC 2124, Controlling Microbes to Fight Infection, University of Tübingen, 72076, Tübingen, Germany.
Chembiochem ; 24(5): e202200455, 2023 03 01.
Article en En | MEDLINE | ID: mdl-36538283
The blue biliprotein phycocyanin, produced by photo-autotrophic cyanobacteria including spirulina (Arthrospira) and marketed as a natural food supplement or "nutraceutical," is reported to have anti-inflammatory, antioxidant, immunomodulatory, and anticancer activity. These diverse biological activities have been specifically attributed to the phycocyanin chromophore, phycocyanobilin (PCB). However, the mechanism of action of PCB and the molecular targets responsible for the beneficial properties of PCB are not well understood. We have developed a procedure to rapidly cleave the PCB pigment from phycocyanin by ethanolysis and then characterized it as an electrophilic natural product that interacts covalently with thiol nucleophiles but lacks any appreciable cytotoxicity or antibacterial activity against common pathogens and gut microbes. We then designed alkyne-bearing PCB probes for use in chemical proteomics target deconvolution studies. Target identification and validation revealed the cysteine protease legumain (also known as asparaginyl endopeptidase, AEP) to be a target of PCB. Inhibition of this target may account for PCB's diverse reported biological activities.
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Texto completo: 1 Colección: 01-internacional Base de datos: MEDLINE Asunto principal: Spirulina / Proteasas de Cisteína Idioma: En Revista: Chembiochem Asunto de la revista: BIOQUIMICA Año: 2023 Tipo del documento: Article País de afiliación: Alemania Pais de publicación: Alemania

Texto completo: 1 Colección: 01-internacional Base de datos: MEDLINE Asunto principal: Spirulina / Proteasas de Cisteína Idioma: En Revista: Chembiochem Asunto de la revista: BIOQUIMICA Año: 2023 Tipo del documento: Article País de afiliación: Alemania Pais de publicación: Alemania