TITLE:
Screening of Protease Inhibitory Activity in Aqueous Extracts of Marine Invertebrates from Cuban Coast
AUTHORS:
Lidice González, Rafael E. Sánchez, Laritza Rojas, Isel Pascual, Rossana García-Fernández, María A. Chávez, Christian Betzel
KEYWORDS:
Target Proteases, Marine Organisms, Protease Inhibitors, Screening
JOURNAL NAME:
American Journal of Analytical Chemistry,
Vol.7 No.4,
April
6,
2016
ABSTRACT: Protease inhibitors
have been isolated from many variable sources; however, the need to identify
and characterize new molecules has increased with the discovery of new
therapeutic targets and the lack of specificity of already identified compounds
with inhibitory activity. The goal of this work was to search for inhibitory
activity against four proteolytic enzymes already recognized as therapeutic
targets: human neutrophil elastase, dipeptidyl peptidase IV, subtilisin from Bacillus licheniformis and cathepsin K
in selected marine invertebrates from the Caribbean Sea. A systematic screening
was carried out with selected aqueous extracts belonging to 20 species from
seven different phyla: Annelida, Bryozoa, Chordata, Cnidaria, Equinodermata,
Mollusca and Porifera, all collected at the coast of Havana (Cuba). All
extracts showing initial inhibitory activity were characterized in terms of IC50 values and specific inhibitory activity (SIA). Model enzymes were used in the
case of human neutrophil elastase (porcine pancreatic elastase) and cathepsin K
(papain) for the screening and all positive results were confirmed by testing
toward the therapeutic targets. Ten extracts were identified showing inhibitory
activity against human neutrophil elastase, for which the most promising values
were obtained for Nerita peloronta.
Only one extract, Bunodosoma granulifera,
showed inhibitory activity against dipeptidyl peptidase IV with rather poor
values of IC50 and SIA. Seven extracts showed inhibitory activity
against B. licheniformis subtilisin
with very good IC50 and SIA values for Lissodendorix isodyctialis, Cenchritis
muricatus, and N. peloronta.
Finally, eight extracts were positive for cathepsin K with almost similar
parameters values among them. All these results confirmed the richness and
potential of the marine invertebrate’s fauna and indicated new promising
sources for the identification of natural compounds with potential application
in therapeutics.