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

Roel M, Rubiolo JA, Ternon E, Thomas OP, Vieytes MR, Botana LM - Mar Drugs (2015)

Bottom Line: 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.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 Article: PubMed Central - PubMed

Affiliation: Departamento de Farmacología, Facultad de Veterinaria, Universidad de Santiago de Compostela (USC), Campus Lugo, 27002 Lugo, Spain. maria.roel@usc.es.

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.

No MeSH data available.


Related in: MedlinePlus

(A) Structure of crambescin C1 (CC1) and crambescin A1 (CA1); (B) Proliferation of HepG2 cells after CC1 treatment for 24 and 48 h; (C) Proliferation of HepG2 cells after CA1 treatment for 24 h and 48 h. In both cases cellular growth was determined by the 3-(4,5-dimethylthiazol-2-l)-2,5-diphenyltetrazolium bromide (MTT) method. * Significant differences respect to controls, p < 0.05, n = 3.
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marinedrugs-13-04633-f001: (A) Structure of crambescin C1 (CC1) and crambescin A1 (CA1); (B) Proliferation of HepG2 cells after CC1 treatment for 24 and 48 h; (C) Proliferation of HepG2 cells after CA1 treatment for 24 h and 48 h. In both cases cellular growth was determined by the 3-(4,5-dimethylthiazol-2-l)-2,5-diphenyltetrazolium bromide (MTT) method. * Significant differences respect to controls, p < 0.05, n = 3.

Mentions: In order to establish the appropriate concentrations to perform transcriptome analysis, we initially assayed the effects of CC1 and CA1 (Figure 1A) on HepG2 cells growth and viability.


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

Roel M, Rubiolo JA, Ternon E, Thomas OP, Vieytes MR, Botana LM - Mar Drugs (2015)

(A) Structure of crambescin C1 (CC1) and crambescin A1 (CA1); (B) Proliferation of HepG2 cells after CC1 treatment for 24 and 48 h; (C) Proliferation of HepG2 cells after CA1 treatment for 24 h and 48 h. In both cases cellular growth was determined by the 3-(4,5-dimethylthiazol-2-l)-2,5-diphenyltetrazolium bromide (MTT) method. * Significant differences respect to controls, p < 0.05, n = 3.
© Copyright Policy
Related In: Results  -  Collection

License
Show All Figures
getmorefigures.php?uid=PMC4556997&req=5

marinedrugs-13-04633-f001: (A) Structure of crambescin C1 (CC1) and crambescin A1 (CA1); (B) Proliferation of HepG2 cells after CC1 treatment for 24 and 48 h; (C) Proliferation of HepG2 cells after CA1 treatment for 24 h and 48 h. In both cases cellular growth was determined by the 3-(4,5-dimethylthiazol-2-l)-2,5-diphenyltetrazolium bromide (MTT) method. * Significant differences respect to controls, p < 0.05, n = 3.
Mentions: In order to establish the appropriate concentrations to perform transcriptome analysis, we initially assayed the effects of CC1 and CA1 (Figure 1A) on HepG2 cells growth and viability.

Bottom Line: 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.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 Article: PubMed Central - PubMed

Affiliation: Departamento de Farmacología, Facultad de Veterinaria, Universidad de Santiago de Compostela (USC), Campus Lugo, 27002 Lugo, Spain. maria.roel@usc.es.

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.

No MeSH data available.


Related in: MedlinePlus