Cytotoxic and peptidase inhibitory activities of selected non-hepatotoxic cyclic peptides from cyanobacteria

Biological Chemistry
Anja BubikTamara T Lah

Abstract

Toxic cyanobacterial blooms are a rich source of metabolites having a variety of biological activities. Two main groups of cyclic peptides, depsipeptides and ureido linkage-containing peptides, reportedly inhibit serine peptidases. We characterised their inhibitory properties against selected peptidases and investigated their influence on cell viability. The depsipeptide planktopeptin BL1125 is a strong linear competitive tight-binding inhibitor of leukocyte (K(i)=2.9 nm) and pancreatic (K(i)=7.2 nm) elastase and also of chymotrypsin (K(i)=6.1 nm). Anabaenopeptins B and F show no inhibition against chymotrypsin, but inhibit both elastases. The tested cyclic peptides do not inhibit trypsin, urokinase, kallikrein 1 or cysteine peptidases. All three tested cyanopeptides show no short-term cytotoxicity in concentrations of up to 10 mum, but impair the metabolic activity of normal human astrocytes after prolonged exposure (48-96 h), whereas glioblastoma cells, tumour cells of the same type, are resistant. Strong inhibition and relative selectivity of the tested cyanopeptides suggests that they are potential candidates for application in inflammatory diseases and possibly some types of cancers.

References

Jan 19, 1989·Biochimica Et Biophysica Acta·J G BiethJ L Dimicoli
Jun 1, 1973·Analytical Biochemistry·C Schwabe
Jul 17, 1973·Biochemical and Biophysical Research Communications·J Bieth, C G Wermuth
Jan 1, 1997·Natural Toxins·B Sedmak, G Kosi
Apr 12, 2002·Current Medicinal Chemistry·C E BallardB Wang
Oct 30, 2003·Chemistry & Biology·Ute MaternGeorg E Schulz
Aug 12, 2004·Chemical & Pharmaceutical Bulletin·Ken-Ichi Harada
Mar 21, 2007·The Journal of Biological Chemistry·Tara M StanneAdrian K Clarke

❮ Previous
Next ❯

Citations

Dec 16, 2011·Journal of Medicinal Chemistry·Pradeep CherukuCarole A Bewley
Jan 25, 2013·Marine Drugs·Hanna Mazur-MarzecJussi Meriluoto
Mar 15, 2011·Toxicology in Vitro : an International Journal Published in Association with BIBRA·Viviana R LopesVitor Vasconcelos
Dec 23, 2020·International Journal of Molecular Sciences·Dimitris PappasEmmanuel Panteris
Feb 13, 2019·The Journal of Organic Chemistry·Lukas Junk, Uli Kazmaier
Aug 27, 2021·Toxins·Patrick Romano MonteiroAgenor Valadares Santos

❮ Previous
Next ❯

Related Concepts

Related Feeds

Cancer Metabolism

In order for cancer cells to maintain rapid, uncontrolled cell proliferation, they must acquire a source of energy. Cancer cells acquire metabolic energy from their surrounding environment and utilize the host cell nutrients to do so. Here is the latest research on cancer metabolism.

Astrocytes

Astrocytes are glial cells that support the blood-brain barrier, facilitate neurotransmission, provide nutrients to neurons, and help repair damaged nervous tissues. Here is the latest research.