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Biological activity and stability of aeruginosamides from cyanobacteria.

Ceg?owska, Marta; Kwiecie?, Patrycja; Szubert, Karolina; Brzuzan, Pawe?; Florczyk, Maciej; Edwards, Christine; Kosakowska, Alicja; Mazur-Marzec, Hanna

Authors

Marta Ceg?owska

Patrycja Kwiecie?

Karolina Szubert

Pawe? Brzuzan

Maciej Florczyk

Alicja Kosakowska

Hanna Mazur-Marzec



Abstract

Aeruginosamides (AEGs) are classified as cyanobactins, ribosomally synthesized peptides with post-translational modifications. They have been identified in cyanobacteria of genera Microcystis, Oscillatoria, and Limnoraphis. In this work, the new data on the in vitro activities of three AEG variants, AEG A, AEG625 and AEG657, and their interactions with metabolic enzymes are reported. Two aeruginosamides, AEG625 and AEG657, decreased the viability of human breast cancer cell line T47D, but neither of the peptides was active against human liver cancer cell line Huh7. AEGs also did not change the expression of MIR92b-3p, but for AEG625, the induction of oxidative stress was observed. In the presence of a liver S9 fraction containing microsomal and cytosolic enzymes, AEG625 and AEG657 showed high stability. In the same assays, quick removal of AEG A was recorded. The peptides had mild activity against three cytochrome P450 enzymes, CYP2C9, CYP2D6 and CYP3A4, but only at the highest concentration used in the study (60 ┬ÁM). The properties of AEGs, i.e., cytotoxic activity and in vitro interactions with important metabolic enzymes, form a good basis for further studies on their pharmacological potential.

Citation

CEGLOWSKA, M., KWIECIE?, P., SZUBERT, K., BRZUZAN, P., FLORCZYK, M., EDWARDS, C., KOSAKOWSKA, A. and MAZUR-MARZEC, H. 2022. Biological activity and stability of aeruginosamides from cyanobacteria. Marine drugs [online], 20(2): pharmaceutical potential of marine microorganisms, article 93. Available from: https://doi.org/10.3390/md20020093

Journal Article Type Article
Acceptance Date Jan 19, 2022
Online Publication Date Jan 21, 2022
Publication Date Feb 28, 2022
Deposit Date Jan 24, 2022
Publicly Available Date Jan 24, 2022
Journal Marine Drugs
Electronic ISSN 1660-3397
Publisher MDPI
Peer Reviewed Peer Reviewed
Volume 20
Issue 2
Article Number 93
DOI https://doi.org/10.3390/md20020093
Keywords Cyanopeptides; Aeruginosamides; Cytotoxicity; MiRNA; Cytochrome P450 enzymes; Metabolic stability
Public URL https://rgu-repository.worktribe.com/output/1575515
Additional Information This accompanying file contains supplementary material of 3 figures and can be found on page 14.

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