title: Crambescin C1 Exerts a Cytoprotective Effect on HepG2 Cells through Metallothionein Induction.
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.
authors.affiliation: Departamento de Farmacología, Facultad de Veterinaria, Universidad de Santiago de Compostela (USC), Campus Lugo, 27002 Lugo, Spain. maria.roel@usc.es.
authors.forename: María
authors.initials: M
authors.lastname: Roel
authors.affiliation: Departamento de Farmacología, Facultad de Veterinaria, Universidad de Santiago de Compostela (USC), Campus Lugo, 27002 Lugo, Spain. ja.rubiolo@usc.es.
authors.forename: Juan A
authors.initials: JA
authors.lastname: Rubiolo
authors.affiliation: Institut de Chimie de Nice, UMR 7272 Université Nice Sophia Antipolis, CNRS, Faculté des Sciences, Parc Valrose, 06108 Nice, France. eva.ternon@unice.fr.
authors.forename: Eva
authors.initials: E
authors.lastname: Ternon
authors.affiliation: Institut de Chimie de Nice, UMR 7272 Université Nice Sophia Antipolis, CNRS, Faculté des Sciences, Parc Valrose, 06108 Nice, France. olivier.thomas@unice.fr.|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. olivier.thomas@unice.fr.
authors.forename: Olivier P
authors.initials: OP
authors.lastname: Thomas
authors.affiliation: Departamento de Fisiología Animal, Facultad de Veterinaria, Universidad de Santiago de Compostela (USC), Campus Lugo, 27002 Lugo, Spain. mmercedes.rodriguez@usc.es.
authors.forename: Mercedes R
authors.initials: MR
authors.lastname: Vieytes
authors.affiliation: Departamento de Farmacología, Facultad de Veterinaria, Universidad de Santiago de Compostela (USC), Campus Lugo, 27002 Lugo, Spain. luis.botana@usc.es.
authors.forename: Luis M
authors.initials: LM
authors.lastname: Botana
mesh_terms: D000470:Alkaloids / Q000494:pharmacology; D000818:Animals; D001685:Biological Factors / Q000494:pharmacology*; D045744:Cell Line, Tumor; D049109:Cell Proliferation / Q000187:drug effects; D047132:Crambe Sponge / Q000378:metabolism; D019610:Cytoprotection / Q000187:drug effects*; D016193:G1 Phase / Q000187:drug effects; D056945:Hep G2 Cells; D006801:Humans; D008668:Metallothionein / Q000378:metabolism*; D011743:Pyrimidines / Q000494:pharmacology*; D016192:Resting Phase, Cell Cycle / Q000187:drug effects; D059467:Transcriptome / Q000187:drug effects
chemical_list: D000470:Alkaloids; D001685:Biological Factors; D011743:Pyrimidines; C086365:crambescin C1; D008668:Metallothionein
keywords: 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 o; CC1 protects them against oxidative injury by means of metallothionein induction even at low concentrations. Additionally; Crambe crambe; antioxidant effect; at high doses; cell cycle inhibition; crambescin-A1; crambescin-C1; crambescin-C1; crambescin-A1; metallothionein; Crambe crambe; sponge-derived compounds; transcriptome profiling; antioxidant effect; cell cycle inhibition The Mediterranean marine sponge Crambe crambe is the source of two families of guanidine alkaloids k; metallothionein; sponge-derived compounds; transcriptome profiling; 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