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Cyanopeptolins with trypsin and chymotrypsin inhibitory activity from the cyanobacterium nostoc edaphicum CCNP1411.

Mazur-Marzec, Hanna; Fidor, Anna; Cegłowska, Marta; Wieczerzak, Ewa; Kropidłowska, Magdalena; Goua, Marie; Macaskill, Jenny; Edwards, Christine

Authors

Hanna Mazur-Marzec

Anna Fidor

Marta Cegłowska

Ewa Wieczerzak

Magdalena Kropidłowska

Marie Goua

Jenny Macaskill



Abstract

Cyanopeptolins (CPs) are one of the most frequently occurring cyanobacterial peptides, many of which are inhibitors of serine proteases. Some CP variants are also acutely toxic to aquatic organisms, especially small crustaceans. In this study, thirteen CPs, including twelve new variants, were detected in the cyanobacterium Nostoc edaphicum CCNP1411 isolated from the Gulf of Gda{acute}nsk (southern Baltic Sea). Structural elucidation was performed by tandem mass spectrometry with verification by NMR for CP962 and CP985. Trypsin and chymotrypsin inhibition assays confirmed the significance of the residue adjacent to 3-amino-6-hydroxy-2-piperidone (Ahp) for the activity of the peptides. Arginine-containing CPs (CPs-Arg2) inhibited trypsin at low IC50 values (0.24-0.26 {aelig}M) and showed mild activity against chymotrypsin (IC50 3.1-3.8 {aelig}M), while tyrosine-containing CPs (CPs-Tyr2) were selectively and potently active against chymotrypsin (IC50 0.26 {aelig}M). No degradation of the peptides was observed during the enzyme assays. Neither of the CPs were active against thrombin, elastase or protein phosphatase 1. Two CPs (CP962 and CP985) had no cytotoxic effects on MCF-7 breast cancer cells. Strong and selective activity of the new cyanopeptolin variants makes them potential candidates for the development of drugs against metabolic disorders and other diseases.

Journal Article Type Article
Publication Date Jul 31, 2018
Journal Marine drugs
Electronic ISSN 1660-3397
Publisher MDPI
Peer Reviewed Peer Reviewed
Volume 16
Issue 7
Article Number 220
Institution Citation MAZUR-MARZEC, H., FIDOR, A., CEGLOWSKA, M., WIECZERZAK, E., KROPIDLOWSKA, M., GOUA, M., MACASKILL, J. and EDWARDS, C. 2018. Cyanopeptolins with trypsin and chymotrypsin inhibitory activity from the cyanobacterium nostoc edaphicum CCNP1411. Marine drugs [online], 16(7), article number 220. Available from: https://doi.org/10.3390/md16070220
DOI https://doi.org/10.3390/md16070220
Keywords Cyanobacteria; Nostoc; Cyanopeptolins; Protease inhibitors

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