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Isolation and assessment of the in vitro anti-tumor activity of smenothiazole A and B, chlorinated thiazole-containing peptide/polyketides from the Caribbean sponge, Smenospongia aurea.

Esposito G, Teta R, Miceli R, Ceccarelli LS, Della Sala G, Camerlingo R, Irollo E, Mangoni A, Pirozzi G, Costantino V - Mar Drugs (2015)

Bottom Line: The study of the secondary metabolites contained in the organic extract of Caribbean sponge Smenospongia aurea led to the isolation of smenothiazole A (3) and B (4), hybrid peptide/polyketide compounds.Assays performed using four solid tumor cell lines showed that smenothiazoles exert a potent cytotoxic activity at nanomolar levels, with selectivity over ovarian cancer cells and a pro-apoptotic mechanism.

View Article: PubMed Central - PubMed

Affiliation: The NeaNat Group, Dipartimento di Farmacia, Università degli Studi di Napoli Federico II, Via D. Montesano 49, 80131 Napoli, Italy. germana.esposito@unina.it.

ABSTRACT
The study of the secondary metabolites contained in the organic extract of Caribbean sponge Smenospongia aurea led to the isolation of smenothiazole A (3) and B (4), hybrid peptide/polyketide compounds. Assays performed using four solid tumor cell lines showed that smenothiazoles exert a potent cytotoxic activity at nanomolar levels, with selectivity over ovarian cancer cells and a pro-apoptotic mechanism.

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Cell-cycle analysis by flow cytometry of A2780 ovarian carcinoma cells after 48 h of treatment with smenothiazoles.
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marinedrugs-13-00444-f007: Cell-cycle analysis by flow cytometry of A2780 ovarian carcinoma cells after 48 h of treatment with smenothiazoles.

Mentions: The most significant activity was observed on the A2780 ovarian carcinoma line. Both compounds were clearly able to induce apoptosis on this line at 70 and 100 nM. In order to evaluate whether these compounds can affect the phases of the cell cycle, untreated and treated A2780 cells were stained with propidium iodide. Analysis of the cell cycle showed that both compounds are able to reduce the number of cells in the S phase at 50 and 70 nM (Figure 7), leading to a block in the G0G1 phase.


Isolation and assessment of the in vitro anti-tumor activity of smenothiazole A and B, chlorinated thiazole-containing peptide/polyketides from the Caribbean sponge, Smenospongia aurea.

Esposito G, Teta R, Miceli R, Ceccarelli LS, Della Sala G, Camerlingo R, Irollo E, Mangoni A, Pirozzi G, Costantino V - Mar Drugs (2015)

Cell-cycle analysis by flow cytometry of A2780 ovarian carcinoma cells after 48 h of treatment with smenothiazoles.
© Copyright Policy
Related In: Results  -  Collection

License
Show All Figures
getmorefigures.php?uid=PMC4306946&req=5

marinedrugs-13-00444-f007: Cell-cycle analysis by flow cytometry of A2780 ovarian carcinoma cells after 48 h of treatment with smenothiazoles.
Mentions: The most significant activity was observed on the A2780 ovarian carcinoma line. Both compounds were clearly able to induce apoptosis on this line at 70 and 100 nM. In order to evaluate whether these compounds can affect the phases of the cell cycle, untreated and treated A2780 cells were stained with propidium iodide. Analysis of the cell cycle showed that both compounds are able to reduce the number of cells in the S phase at 50 and 70 nM (Figure 7), leading to a block in the G0G1 phase.

Bottom Line: The study of the secondary metabolites contained in the organic extract of Caribbean sponge Smenospongia aurea led to the isolation of smenothiazole A (3) and B (4), hybrid peptide/polyketide compounds.Assays performed using four solid tumor cell lines showed that smenothiazoles exert a potent cytotoxic activity at nanomolar levels, with selectivity over ovarian cancer cells and a pro-apoptotic mechanism.

View Article: PubMed Central - PubMed

Affiliation: The NeaNat Group, Dipartimento di Farmacia, Università degli Studi di Napoli Federico II, Via D. Montesano 49, 80131 Napoli, Italy. germana.esposito@unina.it.

ABSTRACT
The study of the secondary metabolites contained in the organic extract of Caribbean sponge Smenospongia aurea led to the isolation of smenothiazole A (3) and B (4), hybrid peptide/polyketide compounds. Assays performed using four solid tumor cell lines showed that smenothiazoles exert a potent cytotoxic activity at nanomolar levels, with selectivity over ovarian cancer cells and a pro-apoptotic mechanism.

Show MeSH
Related in: MedlinePlus