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Mar. Drugs 2015, 13(8), 4633-4653; doi:10.3390/md13084633

Crambescin C1 Exerts a Cytoprotective Effect on HepG2 Cells through Metallothionein Induction

1
Departamento de Farmacología, Facultad de Veterinaria, Universidad de Santiago de Compostela (USC), Campus Lugo, 27002 Lugo, Spain
2
Institut de Chimie de Nice, UMR 7272 Université Nice Sophia Antipolis, CNRS, Faculté des Sciences, Parc Valrose, 06108 Nice, France
3
Institut Méditerranéen de Biodiversité et d'Ecologie Marine et Continentale, UMR 7263 CNRS, IRD, Aix Marseille Université, Avignon Université, Station Marine d'Endoume, Rue de la Batterie des Lions, 13007 Marseille, France
4
Departamento de Fisiología Animal, Facultad de Veterinaria, Universidad de Santiago de Compostela (USC), Campus Lugo, 27002 Lugo, Spain
*
Author to whom correspondence should be addressed.
Academic Editor: Paul Long
Received: 13 April 2015 / Revised: 19 June 2015 / Accepted: 19 June 2015 / Published: 27 July 2015
(This article belongs to the Special Issue Marine Secondary Metabolites)
View Full-Text   |   Download PDF [4961 KB, uploaded 29 July 2015]   |  

Abstract

The Mediterranean marine sponge Crambe crambe is the source of two families of guanidine alkaloids known as crambescins and crambescidins. Some of the biological effects of crambescidins have been previously reported while crambescins have undergone little study. Taking this into account, we performed comparative transcriptome analysis to examine the effect of crambescin-C1 (CC1) on human tumor hepatocarcinoma cells HepG2 followed by validation experiments to confirm its predicted biological activities. We report herein that, while crambescin-A1 has a minor effect on these cells, CC1 protects them against oxidative injury by means of metallothionein induction even at low concentrations. Additionally, at high doses, CC1 arrests the HepG2 cell cycle in G0/G1 and thus inhibits tumor cell proliferation. The findings presented here provide the first detailed approach regarding the different effects of crambescins on tumor cells and provide a basis for future studies on other possible cellular mechanisms related to these bioactivities. View Full-Text
Keywords: crambescin-C1; crambescin-A1; metallothionein; Crambe crambe; sponge-derived compounds; transcriptome profiling; antioxidant effect; cell cycle inhibition crambescin-C1; crambescin-A1; metallothionein; Crambe crambe; sponge-derived compounds; transcriptome profiling; antioxidant effect; cell cycle inhibition
This is an open access article distributed under the Creative Commons Attribution License which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited. (CC BY 4.0).

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MDPI and ACS Style

Roel, M.; Rubiolo, J.A.; Ternon, E.; Thomas, O.P.; Vieytes, M.R.; Botana, L.M. Crambescin C1 Exerts a Cytoprotective Effect on HepG2 Cells through Metallothionein Induction. Mar. Drugs 2015, 13, 4633-4653.

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